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Role of lipid rafts in enterohemorrhagic Escherichia coli O157:H7 mediated hijacking of host cell signalling pathways to induce intestinal injury by Grace Shen-Tu, B.Sc. (Hon) A thesis submitted in conformity with the requirements for the degree of Doctor of Philosophy Institute of Medical Science, University of Toronto © Copyright by Grace Shen-Tu 2010

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Page 1: Role of lipid rafts in enterohemorrhagic Escherichia coli O157:H7 … · 2013. 11. 7. · alternative therapeutic approaches that will prevent the EHEC colonization without the release

Role of lipid rafts in enterohemorrhagic Escherichia coli O157:H7 mediated hijacking of host cell signalling

pathways to induce intestinal injury

by

Grace Shen-Tu, B.Sc. (Hon)

A thesis submitted in conformity with the requirements for the degree of Doctor of Philosophy

Institute of Medical Science, University of Toronto

© Copyright by Grace Shen-Tu 2010

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Role of lipid rafts in enterohemorragic Escherichia coli O157:H7 mediated hijacking of host cell signalling pathways to induce

intestinal injury

Grace Shen-Tu

Degree of Doctor of Philosophy

Graduate Department of Institute of Medical Science

University of Toronto

2010

Abstract

Enterohemorrhagic Escherichia coli O157:H7 (EHEC) is a human intestinal pathogen, which can

cause severe disease. EHEC O157:H7 is responsible for outbreaks of diarrhea and hemorrhagic

colitis. EHEC produces a potent cytotoxin known as Vero (Shiga-like) cytotoxin, which causes

diarrhea-associated hemolytic uremic syndrome (HUS), the most common cause of acute renal

failure in children. Current treatment remains predominantly supportive in nature because

antibiotics and non-steroidal anti-inflammatory drugs exacerbate the condition. Therefore,

alternative therapeutic approaches that will prevent the EHEC colonization without the release of

toxins need to be delineated. Understanding the pathobiology of disease is likely to yield novel

approaches to interrupt the infectious process.

My hypothesis was that pathogen-derived effectors associate with lipid rafts and, thereby,

promote the recruitment of host signal transduction proteins to lipid rafts in response to EHEC

O157:H7 infection. In this thesis, specific host signalling pathways hijacked by EHEC

O157:H7, through lipid raft signalling platforms, to elicit pathogenic effects are studied using

complementary approaches, including epithelial model cell lines and an animal model of

infection (Citrobacter rodentium challenge of mice).

A lack of osteopontin resulted in decreased attaching effacing lesions and reduced colonic

epithelial cell hyperplasia in response to C. rodentium infection. These findings suggest that C.

rodentium, mimicking EHEC O157:H7 infection, is capable of utilizing host cell components to

elicit its pathogenic effects.

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In vitro data showed that EHEC O157:H7 effector proteins manipulate cell signalling through

lipid rafts employed as platforms to recruit and activate host second messengers. PKC and PI3K

activation led to attaching and effacing lesions, disruption of tight junctions, and the initiation of

both innate and adaptive host immune responses. The results pointed towards a role for atypical

PKC in EHEC-induced attaching and effacing lesion formation.

The role of lipid rafts in EHEC O157:H7 pathogenesis was also studied using Citrobacter

rodentium-infected Niemann-pick type C (NPC) mice. Infection of NPC mice, which lack lipid

rafts, with C. rodentium resulted in delayed colonization and delayed onset of attaching-effacing

lesion formation, compared with infected wild type mice. C. rodentium-infected NPC mice also

demonstrated reduced colonic epithelial hyperplasia and decreased secretion of the pro-

inflammatory cytokine, interferon-γ.

Taken together, the findings presented in this thesis highlight the importance of host cell signal

transduction cascades in EHEC O157:H7 disease pathogenesis, and demonstrate a role for lipid

rafts and OPN in mediating host cell signaling responses to non-invasive enteric microbial

pathogens.

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Dedicated to my parents, Mr. Kuang Shen-Tu and Mrs. Chiung-Lin

Chen, and to my darling sister Ms. Nancy Ming Hsin Shen-Tu

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Acknowledgements

First and foremost, I would like to thank God for His guidance. I’m grateful to have my entire

family, mom, dad, and my sister, Nancy, supporting me through my many years of study. To my

long time friends, Jeff and Willa, I would like to express my gratitude for their friendship and

encouragement. To my fiancé, Peter, I would like you to know how much I cherish your love,

patience and understanding during the preparation of this thesis.

All the Sherman lab rats, past and present, at the Hospital for Sick Children have provided me

with support and encouragements throughout my graduate years. First of all, I would like to

thank Kathene for all her advice, in and outside the lab. Secondly, I would like to thank all my

friends in the lab who helped me during my journey: Jason and Narveen, for helping me get

started in the lab; Melanie, for being a great friend and giving me lots of technical help; Nathan,

for his helpful comments and being my skiing buddy; David and Juan, for their friendship and

support. Thirdly, I would like to thank Stella, Jamie, and Dana for their friendship.

The completion of this thesis would not have been possible without the help from both Eytan

Wine and Kevin Donato. Eytan has shared with me his vast scientific knowledge during our

research discussions, he worked tirelessly on our OPN project, and he is always willing to lend

an ear whenever I needed suggestions. To the other doctor, Kevin, who started and completed

this journey with me, I would like to thank you for your technical input over the years, for your

entertainment and friendship, and for your cool when I’m sweating over giving talks.

I owe my deepest gratitude to my supervisor, Dr. Philip Sherman. He has mentored me every

step of this journey: in my studies, student life, and now career life. I have matured immensely,

professionally and personally, under this nurturing and guiding environment provided by Phil.

His encouragement and support not only improved my skills in science, it also prepared me for

the career challenges ahead. I will continue to apply what I learned in my future endeavors, but I

have to admit, the baby egret doesn’t want to leave the comforts of this lab.

I would also like to thank my supervisory committee, Dr. Mingyao Liu and Dr. Christine Bear,

who provided critical analysis and guidance during these past five years. Lastly, I would like to

acknowledge the funding that I have received through master and doctoral awards provided by

the Canadian Institutes of Health Research (CIHR).

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Table of Contents

Title page….. ................................................................................................................................... i

Abstract….. ..................................................................................................................................... ii

Dedications .................................................................................................................................... iv

Acknowledgements ......................................................................................................................... v

Table of Contents ........................................................................................................................... vi

Dissemination of Work Arising from This Thesis ......................................................................... ix

List of Abbreviations ...................................................................................................................... x

List of Tables ............................................................................................................................... xvi

List of Figures ............................................................................................................................. xvii

Chapter 1. Introduction .................................................................................................................. 1

1.1 Bacterial infections of the gastrointestinal system, pathophysiology and disease .............. 2

1.1.1 Structure, Physiology, and Function of the GI Tract .............................................. 2

1.1.2 The Intestinal Barrier .............................................................................................. 4

1.1.3 Epithelial Cell Cytoskeleton ................................................................................... 6

1.1.4 Shiga-liketoxin (Verocytotoxin)-producing Escherichia coli O157:H7 ................. 7

1.1.5 Citrobacter rodentium as an AE enteropathogen in mice .................................... 16

1.2 Host Defense and Exploitation of Host Responses by Pathogens .................................... 21

1.2.1 Bacterial virulence factors .................................................................................... 21

1.2.2 Immune defense in microbial recognition ............................................................ 22

1.2.3 Inflammatory and Innate Responses to Bacteria .................................................. 25

1.2.4 Microbial Manipulation of the Host Epithelium ................................................... 27

1.3 Host cell mechanisms hijacked by bacteria during infection ............................................ 33

1.3.1 Osteopontin ........................................................................................................... 33

1.3.2 Detergent-resistant Microdomains ........................................................................ 35

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1.3.3 PI3K family: role in cell signalling and cytoskeletal rearrangements .................. 36

1.3.4 PKC: role in bacterial infection ............................................................................ 45

1.4 In vivo model of lipid raft during bacteria infection ......................................................... 50

1.4.1 Niemann-Pick Type C Disease ............................................................................. 50

1.5 Alternative preventative strategies .................................................................................... 53

1.5.1 Probiotics .............................................................................................................. 53

1.5.2 Probiotics in Disease Management ....................................................................... 53

1.5.3 Mechanism of Action ............................................................................................ 54

Chapter 2. Hypothesis and Objectives ......................................................................................... 56

Chapter 3. Osteopontin Mediates Citrobacter rodentium-Induced Colonic Epithelial Cell

Hyperplasia and Attaching-Effacing Lesions ............................................................ 59

3.1 Abstract .............................................................................................................................. 60

3.2 Introduction ....................................................................................................................... 61

3.3 Materials and Methods ...................................................................................................... 63

3.4 Results ............................................................................................................................... 71

3.5 Discussion ......................................................................................................................... 89

3.6 Acknowledgements ........................................................................................................... 94

Chapter 4. Detergent-Resistant Microdomains Mediate Activation of Host Cell Signalling in

Response to Attaching-Effacing Bacteria .................................................................. 95

4.1 Abstract ............................................................................................................................. 96

4.2 Introduction ....................................................................................................................... 97

4.3 Materials and Methods ...................................................................................................... 99

4.4 Results ............................................................................................................................. 106

4.5 Discussion ....................................................................................................................... 127

4.6 Acknowledgements ......................................................................................................... 133

Chapter 5. Recruitment of Protein Kinase C to Lipid Rafts in Response to

Enterohemorrhagic Escherichia coli O157:H7 is blocked by Lactobacillus

helveticus R0052 ...................................................................................................... 134

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5.1 Abstract ........................................................................................................................... 135

5.2 Introduction ..................................................................................................................... 136

5.3 Materials and Methods .................................................................................................... 138

5.4 Results ............................................................................................................................. 142

5.5 Discussion ....................................................................................................................... 165

Chapter 6. Discussion, Future Directions, and Significance ..................................................... 168

6.1 Discussion ....................................................................................................................... 169

6.2 Future Directions ............................................................................................................ 176

6.3 Significance ..................................................................................................................... 179

Chapter 7. References ................................................................................................................ 180

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Dissemination of Work Arising from This Thesis

Chapter 3 was published as:

*Eytan Wine, *Grace Shen-Tu, Mélanie G. Gareau, Harvey A. Goldberg, Christoph

Licht, Bo-Yee Ngan, Esben S. Sorensen, James Greenaway, Jaro Sodek, Ron Zohar,

Philip M. Sherman. Osteopontin mediates Citrobacter rodentium-induced colonic

epithelial cell hyperplasia and attaching-effacing lesions. American Journal of Pathology

September, 2010 (In Press).

Chapter 4 was published as:

Grace Shen-Tu, David B. Schauer, Nicola L. Jones, and Philip M. Sherman. Detergent-

resistant microdomains mediate activation of host cell signaling in response to attaching–

effacing bacteria. Laboratory Investigation 2010; 90: 266-281.

Chapter 5 is currently in progress:

Grace Shen-Tu, Ming-Yau Lu, and Philip M. Sherman. Recruitment of Protein Kinase C

to Lipid Rafts in Response to Enterohemorrhagic Esherichia coli O157:H7 infection is

blocked by Lactobacillus helveticus R0052.

Publication cited elsewhere in this thesis was taken from:

Kathene C. Johnson-Henry, Kevin A. Donato, Grace Shen-Tu, Mahsa Gordanpour, and

Philip M. Sherman. Lactobacillus rhamnosus Strain GG Prevents Enterohemorrhagic

Escherichia coli O157:H7-Induced Changes in Epithelial Barrier Function. Infection and

Immunity 2008; 76(4): 1340-1348.

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List of Abbreviations

Abbreviations Full Term

AE Attaching-effacing

Ab Antibody

ADP Adenosine diphosphate

AJC Apical junction complex

Akt Protein kinase B

AMP Adenosine monophosphate

AMPs Antimicrobial peptides

ANOVA Analysis of variance

aPKC Atypical protein kinase C

AQP Aquaporins

Arp 2/3 Actin-related proteins 2/3

ATP Adenosine triphosphate

BH Breakpoint-cluster-region homology

CD Cluster of differentiation

Cdc42 Cell division control protein 42 homolog

CDX 2/3 Caudal-related cdx 2/3 homeobox gene encoded nuclear transcription factor

CFTR Cystic fibrosis transmembrane conductance regulator

CFU Colony-forming units

CLC Chloride channels

CLCA Calcium activated chloride channels

cPKC Classical protein kinase C

CTS Type VI secretion system cluster

DAG Diacylglycerol

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DAI Disease acitivity index

DAPI 4’,6-diamidino-2-phenylindole

DMEM Dulbecco’s Modified Eagle Medium

DNA Deoxyribonucleic acid

DRM Detergent-resistant microdomains

DSS Dextran sulfate sodium

E. coli Escherichia coli

eae E. coli attaching and effacing gene

EHEC Enterohemorrhagic Esherichia coli

ELISA Enzyme-linked immunosorbent assay

EPEC Enteropathogenic Escherichia coli

Esp E. coli secreted protein

Eta-1 T-lymphocyte activation protein

F-actin Filamentous actin

FH Formin homology

FITC Fluorescein isothiocyanate

GAP GTPase activating protein

Gb3 Glycosphingolipid globotriaosylceramide

GI Gastrointestinal

GM1/2/3 Gangliosides

GSK3 Glycogen synthase kinase-3

GTP Guanosine triphosphate

HRP Horseradish peroxidase

HUS Haemolytic uremic syndrome

IBD Inflammatory bowel disease

IBS Irritable bowel syndrome

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IFN- Interferon-gamma

IgM/A Immunoglobulin M or A

IL Interleukin

Io liquid-ordered

IRS-1/2 Insulin receptor substrate 1/2

IS Insertion sequence

KC Keratinocyte chemoattractant

LB Luria Bertani

LDL Low density lipoprotein

LEE Locus of enterocyte effacement

LGG Lactobacillus GG

LifA Lymphocyte inhibitor factor A

LPS Lipopolysaccharide

Map Mitochondrial activated protein

MAPK Mitogen-activated protein kinase

MEM Minimum Essential Medium

MHC Major histocompatibility complex

MLC Myosin light chain

MLCK Myosin light chain kinase

MMP Matrix Metalloproteinase

mTOR mammalian target of rapamycin

MCD Methyl--cyclodextrin

NAIP Baculoviral IAP repeat-containing protein

NALP NACHT, LRR and PYD domains-containing protein

Nck Non-catalytic region of tyrosine kinase adaptor protein

NEC Necrotizing enterocolitis

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Neu5Gc N-glycolylneuraminic acid

NF-B Nuclear factor kappa-light-chain-enhancer of activated B cells

Nle Non-LEE encoded effector

NLR Nod-like receptor

NOD Nucleotide-binding oligomerization domain

NPC Niemann-pick type C

nPKC Novel protein kinase C

N-WASP Wiskott-Aldrich syndrome protein

OPN Osteopontin

Osp Outter surface protein

P70S6K

p70 ribosomal S6 kinase

PAMPs Pathogen-associated molecular patterns

PAR Proteinase-activated receptor

PBS Phosphate buffered saline

PCR Polymerase chain reaction

PH Pleckstrin homology

PI Post-infection

PI3K Phosphoinositide 3-kinase

PIP2 Phosphatidylinositol 4,5-bisphosphate

PIP3 Phosphatidylinositol 3,4,5-triphosphate

PKC Protein kinase C

PLC Phospholipase C

PRR Pattern-recognition receptor

PtdIns Phosphatidylinositol

PTK Protein tyrosine kinase

Rab Ras-related protein

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Rac Ras-related C3 botulinum toxin substrate

RAG Recombination-activating gene

Rho Ras homology gene family

RNA Ribonucleic acid

RND Resistance-nodulation-division

SBS Short bowel syndrome

SDS-PAGE Sodium dodecyl sulphate polyacrylamide gel electrophoresis

SH2/3 Src homology 2 or 3

SPI-6 Salmonella pathogenicity island 6

Src Sarcoma (proto-oncogenic tyrosine kinases)

STEC Shiga toxin-producing E. coli

Stx Shiga toxin

T1SS Type I secretion system

T2SS Type II secretion system

T5SS Type V secretion system

T6SS Type VI secretion system

TEM Transmission electron microscopy

Th or TH T helper

Tir Translocating intimin receptor

Tj Tight junction

TLRs Toll-like receptors

TNF- Tumor necrosis factor-alpha

TTP Thrombotic Thrombocytopenic purpura

TTSS Type III secretion system

VTEC Verocytotoxin-producing E. coli

WT Wild type

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ZO Zonula occludens

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List of Tables

Table 1.1 Classification of O157 and non-O157 STEC .......................................................... 11

Table 1.2 List of virulence factors secreted by EPEC, EHEC, and C. rodentium ................ 12

Table 3.1 Colonic Inflammation Histological Score ............................................................... 65

Table 3.2 Modified Disease Activity Index Score .................................................................... 69

Table 4.1 Baterial strains and treatments used in the in vitro studies ................................ 100

Table 6.1 PKC inhibitors used in vitro, in vivo, and in human studies ............................... 177

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List of Figures

Figure 1.1 Schematic diagram of EHEC O157:H7 signalling regulation of AE lesion

formation and barrier disruption. .......................................................................... 31

Figure 1.2 Schematic diagram of the PI3K family enzymes. ................................................. 38

Figure 1.3 Schematic diagram of class IA PI3K p85 regulatory subunit. ............................ 42

Figure 1.4 A: Schematic diagram of the structures of PKC isoforms. ................................. 47

Figure 3.1 OPN expression is increased in response to C. rodentium infection. ................... 73

Figure 3.2 Colonic epithelial cell hyperplasia and inflammation in response to C.

rodentium are associated with OPN. ...................................................................... 75

Figure 3.3 OPN mediates C. rodentium colonization. ............................................................. 77

Figure 3.4 Rectal OPN restores responses to C. rodentium infection in OPN-/-

mice. .......... 81

Figure 3.5 Formation of actin-dense attachment pedestals in mouse fibroblasts infected

by C. rodentium and EHEC O157:H7 is mediated by OPN. ................................ 83

Figure 3.6 Exogenous OPN does not restore adhesion pedestals in vitro. ............................. 85

Figure 3.7 Actin-dense pedestals are formed in C. rodentium-infected WT mice and

reduced in OPN-/-

mice. ........................................................................................... 87

Figure 4.1 Phosphoinositide 3-kinase (PI3K) is recruited to lipid rafts in response to

enterohaemorrhagic Escherichia coli O157:H7 infection, and newly

synthesized bacterial proteins are required for PI3K recruitment to lipid

rafts. ........................................................................................................................ 107

Figure 4.2 Activated phosphoinositide 3-kinase (PI3K) is recruitment to lipid rafts in

response to infection independent of the type III secretion system and Shiga-

like toxins 1 and 2. ................................................................................................. 109

Figure 4.3 Intact lipid microdomains are required for EHEC induced translocation of

phosphoinositide 3-kinase (PI3K) to lipid rafts, while secreted bacterial

factors are insufficient to induce this recruitment. ............................................. 112

Figure 4.4 Citrobacter rodentium colonization is delayed in the colonic mucosa of NPC -

/- mice. ...................................................................................................................... 115

Figure 4.5 Attaching-effacing lesions induced by Citrobacter rodentium infection are

delayed in NPC -/-

mice. ......................................................................................... 117

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Figure 4.6 Citrobacter rodentium-induced epithelial cell hyperplasia is reduced in NPC-/-

mice. ........................................................................................................................ 120

Figure 4.7 Colonocyte proliferation is reduced in NPC -/-

mice infected with Citrobacter

rodentium. ............................................................................................................... 122

Figure 4.8 Altered cytokine profiles in NPC -/-

mice infected with Citrobacter rodentium. 125

Figure 5.1 PKC is recruited to lipid rafts during EHEC O157:H7 infection. ................... 143

Figure 5.2 Newly synthesized bacterial proteins and intact lipid rafts are required for

PKC recruitment to lipid rafts in response to EHEC infection. ........................ 145

Figure 5.3 Western blots of protein kinase C from ultracentrifugation fractions of

whole cell extracts (Intestine 407 cells). ............................................................... 147

Figure 5.4 Recruitment of PKC is independent of the type III secretion system and the

production of Shiga toxins 1 and 2. ...................................................................... 149

Figure 5.5 Recruitment of PKC is dependent on intact lipid rafts on the plasma

membrane of host epithelial cells. ........................................................................ 153

Figure 5.6 EHEC-induced recruitment of PKC is not blocked by bisindolylmaleimide I. 155

Figure 5.7 PKC inhibitor Gö6983 prevents recruitment of atypical protein kinase C

(PKC) isoforms to lipid rafts in response to Escherichia coli O157:H7

infection. ................................................................................................................. 157

Figure 5.8 Atypical isoform of PKC is involved in the recruitment of PKC to lipid rafts

in response to EHEC O157:H7 infection. ............................................................ 159

Figure 5.9 An atypical isoform of PKC is involved in EHEC O157:H7-induced AE

lesion formation. .................................................................................................... 161

Figure 5.10 The recruitment of host signalling proteins is blocked by pretreating the

cells with probiotics. .............................................................................................. 163

Figure 6.1 Schematic diagram of suggested infectious process of EHEC O157:H7,

leading to AE lesion formation and barrier disruption. .................................... 174

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Chapter 1.

Introduction

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1.1 Bacterial infections of the gastrointestinal system,

pathophysiology and disease

The gastrointestinal (GI) tract has multiple roles, but its primary function is to convey nutrients

and water from the external environment into the mammalian body. This complex interface

starts from the oral cavity and extends caudally to the anus. The intestinal epithelium has the

largest mucosal surface area of the body, because it is required for digestive, absorptive,

excretory, and immunological functions (Mirpuri, Brazil et al. 2010).

Since the GI tract is continuously exposed to the outside environment, it has several protection

systems, including: low pH in the stomach, lining of the complete GI tract with a surface mucus

layer, a single cell layer of polarized epithelia, an enormous population of innate and adaptive

immune cells that lie beneath the epithelial surface in the submucosa, and the presence of

commensal microbes that colonize, to variable numbers and complexity, the lumen of the GI

tract (Tlaskalova-Hogenova et al. 2004; Zoetendal et al. 2008).

One of the key features of the GI tract is to regulate molecular trafficking between the intestinal

lumen and the submucosa, distinguishing between self and non-self; mounting immune

responses against pathogens while being tolerant of dietary antigens and beneficial bacteria

(Garrett, Gordon et al. 2010). Intestinal permeability is what regulates macromolecule

trafficking and its regulation is dependent on the integrity of intercellular tight junctions (tj)

(Turner 2009). In the past, tj were thought to be a fixed and unregulated barrier in the

paracellular space and its contribution to GI tract molecule trafficking was negligible. However,

it is now evident that tj are important, dynamic structures involved in GI development,

physiology, and function both in health and in a variety of disease states, including enteric

infections (Marchiando, Graham et al. 2010).

1.1.1 Structure, Physiology, and Function of the GI Tract

1.1.1.1 Structural components of the intestine

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Four different types of epithelial cells line the villi and crypts of the small intestine. The four

major epithelial cells include: absorptive enterocytes, goblet cells, enteroendocrine cells, and

Paneth cells. Enterocytes are polarized epithelial cells that are joined together via tj. They take

up and process luminal antigens through fluid-phase endocytosis. Enterocytes express class I

and II (in settings of inflammation) MHC molecules in order to present processed antigens to T-

cells (Snoeck, Goddeeris et al. 2005). Intestinal epithelial cells can be further divided according

to their proliferative activity, where cells in the crypt region have the highest activity while

surface epithelial cells are non-proliferative and more differentiated. Conventional thought is

that crypt cells are secretory in function, while enterocytes are absorptive. The intestinal villi are

lined by functional absorptive, goblet, and endocrine cells. The crypts contain stem cells, both

proliferative and poorly differentiated, as well as highly differentiated secretory Paneth cells.

The proliferative crypt cells differentiate into different cell types and either move upward toward

the villus (mainly cells with absorptive, mucus secretion, or hormone-producing functions) or

downward to the bottom of the crypt (Paneth cells) (Karam 1999). Recent studies point toward

the role of p38 mitogen-activated protein kinase (MAPKs) in interacting with CDX 2/3,

enhancing its transcription activity, and stimulating intestinal differentiation (Houde, Laprise et

al. 2001).

Goblet cells are found along the entire intestinal tract and their primary function is to secrete a

variety of mucins and trefoil peptides for lubrication and to protect the mucosa from irritation

(Artis and Grencis 2008).

The enteroendocrine cells are located deeper in gastric glands and in the lower portions of

intestinal crypts. These enteroendocrine cells are specialized to secrete a particular hormone that

influences either gastrointestinal secretion or motility (Mellitzer, Beucher et al. 2010).

Paneth cells are secretory epithelial cells located at the ends of intestinal crypts. The function of

these cells is secretion of antimicrobial cryptdins or defensins, and growth factors into the crypt

lumen (Vaishnava, Behrendt et al. 2008).

1.1.1.2 Water and electrolyte absorption

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One of the critical roles of the intestinal system is water and electrolyte absorption. Water

absorption is passive and, therefore, depends on rates of solute transport. In the basolateral

plasma membrane, there are sodium-potassium pumps that provide the energy for driving

transcellular and paracellular flows of fluid across the gut epithelium. There is also

transepithelial resistance, regulated mainly by intercellular tight junctions (Groschwitz and

Hogan 2009). Transcellular flow of water, on the other hand, is dependent mainly on sodium-

linked solute co-transporters in the apical microvillus membrane of small intestinal enterocytes.

Aquaporins (AQP), membrane proteins with high water selectivity, are also important in

transcellular fluid movement (Hansen, Holt et al. 2009). These protein channels are located in

apical and basolateral sides of the epithelial cell in both the small intestine and colon.

Intestinal absorption relies on sodium transport, whereas intestinal secretion is associated with

chloride transport through the cystic fibrosis transmembrane conductance regulator (CFTR)

present in the apical plasma membrane of gut epithelial cells. Unwarranted CFTR activity leads

to secretory diarrhea in response to bacterial-derived toxins, including choleragen of Vibrio

cholerae (Venkatasubramanian, Ao et al. 2010) and heat-labile enterotoxin of enterotoxigenic

Escherichia coli, ETEC (Crane, Choudhari et al. 2006).

Other chloride channels present in the intestine include the CLC family and the calcium activated

chloride channel (CLCA). The precise functional role of these chloride channels remains

unclear; however, it has been suggested that they play a role in neural (cholinergic) mediated ion

and water secretion in the colon (Catalan, Niemeyer et al. 2004; Basavappa, Vulapalli et al.

2005).

1.1.2 The Intestinal Barrier

1.1.2.1 Selectively permeable barrier

Barriers created by epithelial cells are essential to life. This is particularly true along the

gastrointestinal tract, where the epithelial barrier is responsible for nutrient and water transport

and, at the same time, the prevention of microbial contamination of the interstitial and systemic

tissues. The intercellular tight junction (tj) is the primary cellular determinant of epithelial

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barrier function (Groschwitz and Hogan 2009). The tj is responsible for both absorption and

secretory functions of the epithelia and is also a barrier between the apical and basolateral

compartments. Tj closely regulate the passive diffusion of ions and macromolecules through the

paracellular pathway and, thereby, control gradients created by the transcellular pathway

(Groschwitz and Hogan 2009). Other apical junction complex constituents, such as adherence

junctions and desmosomes, provide strong bonds essential for maintaining cellular proximity that

allows for tj formation (Marchiando, Graham et al. 2010).

Despite the presence of tj that seems to create an impermeable barrier, the electrical resistance of

the paracellular pathway varies by as much as one thousand-fold between different polarized

epithelia (Marchiando, Graham et al. 2010). The range of tight junction barrier function makes

water and nutrients absorption in the small intestine possible and the pore size through the

epithelium decreases in the distal intestine. Tj are complex and dynamic structures, which are

tightly regulated by a number of transmembrane, cytoskeletal, and regulatory proteins (Turner

2009).

Important transmembrane proteins in the tj include 24 members of the claudin family, which

regulate several aspects of tight junction permeability. Claudins are expressed in a tissue-

specific manner, and mutation or deletion of claudin family members can result in organ

dysfunction. The transmembrane tj protein, occludin, interacts directly with claudins and F-

actin, to regulate permeability (Groschwitz and Hogan 2009). Peripheral membrane proteins

zonula occludens 1, 2, and 3 (ZO-1, ZO-2, and ZO-3) contain three PDZ domains within their

amino-terminal portion. PDZ domains are involved in protein interactions and allow ZO-1, ZO-

2, and ZO-3, to bind to the carboxy terminal of claudins. This is critical because deletion or

mutation of the PDZ-binding motif prevents efficient claudins, occludin, and actin targeting to

the tight junction (Turner 2009).

1.1.2.2 Tight junction barrier regulation and effects on absorption

Even though the majority of claudin-1 is anchored at the tight junction in epithelial monolayers,

recent studies have shown a dynamic tight junction protein behavior (Groschwitz and Hogan

2009). Immunofluorescence imaging has shown that the majority of tight junction-associated

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ZO-1 and occludin are present in endocytosed vacuoles, via caveolae, that allows them to rapidly

move in and out of specific regions within the tight junction in a calcium-dependent manner

(Ivanov, Nusrat et al. 2004). Thus, although ZO-1 and occludin interact at the tight junction, this

interaction is constantly disassembling and reassembling (Shen, Weber et al. 2008).

The Ca2+

–calmodulin-dependent serine–threonine protein kinase myosin light chain kinase

(MLCK) is important in sodium–nutrient co-transport-induced tight junction regulation (Turner

2009). MLCK inhibition prevents MLC phosphorylation and disrupts epithelial barrier

regulation induced by Na+-glucose cotransport and blocks barrier regulation in intact intestinal

mucosa (Turner, Rill et al. 1997). Enteropathogenic Escherichia coli infection induces MLCK-

dependent MLC phosphorylation with increased tight junction permeability, indicating that

MLCK-dependent MLC phosphorylation is both a physiological and a pathophysiological

regulator of barrier function (Yuhan, Koutsouris et al. 1997). Moreover, enzymatic MLCK

activation is sufficient to trigger downstream signaling events essential for barrier regulation

(Shen, Black et al. 2006).

1.1.2.3 Epithelial barrier regulated by immune stimuli and

cytoskeleton

Cytokines, such as IFN-γ and TNF-alpha, also have the ability to regulate barrier function

(Bruewer, Luegering et al. 2003). Increased tight junction protein expression, removal of

proteins from the tj, junction protein degradation, kinase activation, and cytoskeletal

rearrangements all have been implicated in mediating cytokine-induced disruption of intestinal

barrier function. MLCK has a crucial role in TNF-alpha-induced epithelial barrier dysregulation,

both in vitro (Zolotarevsky, Hecht et al. 2002) and in vivo (Shen, Su et al. 2009). MLC

phosphorylation within the perijunctional actomyosin ring leads to increased myosin ATPase

activity, which is involved in tj regulation (Capaldo and Nusrat 2009). Both Rho family kinases

and AMP-activated protein kinase can directly phosphorylate MLC and inhibit MLC

phosphatase and, in turn, contribute to tj regulation (Utech, Ivanov et al. 2005; Capaldo and

Nusrat 2009).

1.1.3 Epithelial Cell Cytoskeleton

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Eukaryotic cells include three types of cytoskeletons: actin filaments, microtubules, and

intermediate filaments. These polymers are assembled from individual monomers in a reversible

fashion (Ku, Zhou et al. 1999). Knowledge of host cell actin filament architecture is needed in

order to learn the process of cell movement, host defenses, and bacterial and viral pathogenesis

(Burckhardt and Greber 2009; Guttman and Finlay 2009; Huang and Brumell 2009; Olson and

Nordheim 2010).

1.1.3.1 Actin regulation

Actin exists in two forms: monomeric and filamentous actin (F-actin), which is two helical

polymeric chains of actin monomers. Actin polymerization in vitro involves three steps: (1)

nucleation (formation of actin oligomers to form filaments later on); (2) elongation; and (3)

treadmilling (movement of monomers along the filament) (Le Clainche and Carlier 2008). Actin

nucleation is promoted by high actin-ATP concentration (Bean and Amann 2008), where the

nuclei persist longer for polymers to form. During elongation, ATP-dependent profilin and

thymosin activity promote polymerization, whereas depolymerization of ADP-actin at the

opposite end is promoted by cofilin (Le Clainche and Carlier 2008). These processes are strictly

regulated by other signalling cascades. For example, the Rho family of proteins, Rho, Rac, and

Cdc42, are activated, bind to, and induce conformational changes in the Wiskott-Aldrich

syndrome protein (N-WASP) family of proteins, exposing binding sites for the Arp2/3 complex

(Miki and Takenawa 2003). Binding of N-WASP protein to the Arp2/3 complex alters the

conformation of the complex and initiates actin filament elongation (Miki and Takenawa 2003).

Another example is formins, a group of multidomain proteins with formin homology (FH)

domains, which play a role in the regulation of cell shape and polarity (Schonichen and Geyer

2010). The formins, in the presence of profilin, nucleate the growth of actin assembly and

produce linear actin filaments. Formins at the peripheral membrane induce actin monomers to

add to growing filaments at the membrane-actin cytoskeleton interface resulting in directional

actin assembly for membrane protrusion (Chesarone, DuPage et al. 2010).

1.1.4 Shiga-liketoxin (Verocytotoxin)-producing Escherichia coli

O157:H7

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Haemolytic uraemic syndrome (HUS), the leading cause of acute renal failure in children, and

haemorrhagic colitis are some of the major clinical symptoms associated with

enterohaemorrhagic Escherichia coli, serotype O157:H7 (EHEC) infection (Karch 2001). EHEC

constitutes a subset of serotypes called Shiga toxin-producing E. coli (STEC), where bacterial-

derived toxins function as virulence factors during disease pathogenesis (Karmali, Petric et al.

1985).

1.1.4.1 Clinical presentations of E. coli O157:H7 infection

E. coli O157:H7 infection is a major health issue in North America, Europe, and other areas of

the world. E. coli O157:H7 infection leads to high hospitalization and case-fatality rates, wells

above more common infections caused by non-typhoidal Salmonellae and Campylobacters

(Slutsker, Ries et al. 1997).

Human infection by enterohemorrhagic Escherichia coli (EHEC) O157:H7 leads to a broad

clinical spectrum, ranging from asymptomatic colonization to death. The majority of infected

individuals initially experience non-bloody diarrhea, which resolves without further

complications (Tarr 1995). However, some patients will experience bloody diarrhea in the first 3

days of infection. Up to 10% of hemorrhagic colitis patients progress to develop either HUS or

thrombotic thrombocytopenic purpura (TTP) (Manning, Motiwala et al. 2008).

Currently, there is no effective treatment for EHEC infection and the use antibiotics may cause

more harm than good (Wong, Jelacic et al. 2000). Therefore, treatment is mainly supportive in

nature (Bavaro 2009). Further understanding of disease pathogenesis is required to be able to

develop novel intervention strategies to reduce the current burden of illness.

1.1.4.2 Bacterial Virulence: Evolution and Acquisition

It is wrong to assume E. coli is a homogenous species. In fact, the composition of the E. coli

genome is highly dynamic. For example, the fully sequenced genome of E. coli, strain K-12

showed that more than 200 lateral gene transfer events have occurred since it diverged from

Salmonella and 18% of contemporary genes were obtained through horizontal transfer from

other species.

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Virulence factors that separate various types of E. coli that cause enteric disease were acquired

through plasmids, bacteriophages, and genes from other bacteria (Lim, Yoon et al. 2010). The

evolution of EHEC O157:H7 likely began with an EPEC-like, serogroup O55 ancestor. From

this ancestor, EHEC O157:H7 has emerged through: (1) inheritance of the LEE pathogencity

island; (2) acquisition of a stx2-containing bacteriophage; and (3) acquisition of pO157 plasmid,

and (4) change of the rfb region somatic antigen from O55 to O157 (Donnenberg and Whittam

2001). Thereafter, evolution, diverged in 2 directions: the bacterial lineage lost motility, but

retained Stx2 to give rise to an O157:H- clone followed by acquisition of the stx1-containing

bacteriophage; and loss of the ability to ferment D-sorbitol and loss of beta-glucuronidase

(GUD) activity to give rise to the common O157:H7 clone that has now spread world-wide

(Donnenberg and Whittam 2001; Feng, Monday et al. 2007).

Seropathotype classification of various Shiga toxin (Stx)-producing E. coli

Although serotype O157:H7 has been implicated in most human disease outbreaks and in most

HUS cases, there are approximately 200 non-O157 STEC serotypes that are associated with

human illness (Karmali 2004). Canada had the first non-O157 serotype association with HUS,

and since then there have been increasing reports of non-O157 serogroups being implicated in

HUS in Latin America and Australia, and their frequency is also increasingly recognized in

European countries. Recent data indicate that as many as 20% of HUS cases in North America

are associated with non-O157 STEC (Karmali, Mascarenhas et al. 2003). STEC serotypes seem

to differ in pathogenic potential; therefore, the clinical and public health risks have been assessed

and the serotypes have been classified according to frequency of outbreaks and severity of

disease (Table 1.1) (Karmali, Mascarenhas et al. 2003).

1.1.4.3 LEE Pathogenicity Island: LEE-encoded and non-LEE

encoded bacterial virulence factors

Diarrheagenic enterohaemorrhagic Escherichia coli (EHEC), enteropathogenic E. coli (EPEC),

and Citrobacter rodentium are all non-invasive AE pathogens. They elicit their pathogenic

effects through secreted bacterial effector proteins/virulence factors and there is a diverse set of

virulence determinants that distinguish them according to phenotype and pathology (Tobe,

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Beatson et al. 2006). The locus of enterocyte effacement (LEE) is conserved in both EHEC

O157:H7 and EPEC and associated strongly with human disease (Deng, Puente et al. 2004).

The EHEC LEE is 45kb in size and has a 7.5kb prophage sequence that is not present in EPEC

(Yang, Kim et al. 2009). The LEE contains at least 41 different genes responsible for the

following major regions: (1) a type III secretion system (TTSS) that translocates molecules either

to the outside of the bacterium or directly into the host cell; (2) an adhesin, intimin, and its

translocated receptor, Tir (EspE), which is shuttled into the host cell membrane by the TTSS;

and (3) secreted proteins (Esp’s) (Table 1.2) that are important in manipulating host cell signal

transduction and attaching-effacing (A/E) lesion formation by cytoskeleton rearrangements

(Spears, Roe et al. 2006).

LEE-ecoded TTSS structural bacterial factors are: EspA, pilus protein of TTSS; EspB,

component of the translocation pore on the host cell surface; and EspD, interact with EspB for

form the translocation pore. Some of these bacterial secreted proteins include: EspF, which is

involved in the disruption of intercellular tight junctions; Map, involved in the disruption of tight

junctions and the formation of filopodium; EspH, playing a role in the disruption of cytoskeleton;

and EspG/G2, involved in disruption and modulation of the cytoskeleton (Deng, Puente et al.

2004; Tobe, Beatson et al. 2006); and EspFU/TccP, activates N-WASP, in a similar fashion as

Nck in EPEC infection, in AE lesion formation (Crepin, Girard et al. 2010).

Recently, more and more non-LEE encoded effectors have been identified (Table 1.2), and

determination of their function will advance the understanding of EHEC O157:H7 disease

pathogenesis. Some of the non-LEE-encoded virulence factors include: adhesins, responsible for

initial epithelial cell interactions by both EHEC and EPEC; NleH, homologous to the Shigella

effector OspG, which is a protein kinase that prevents ubiquitination and subsequent degradation

of phosphor-IθBα and downstream activation of the transcriptional factor NF-θB (Hemrajani,

Berger et al. 2010); OspG, a protein kinase that interferes with the NF-θB signaling; and OspD

and OspE, with currently unknown functions (Spears, Roe et al. 2006).

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Table 1.1 Classification of O157 and non-O157 STEC (Karmali, Mascarenhas et al. 2003)

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Table 1.2 List of virulence factors secreted by EPEC, EHEC, and C. rodentium (Spears,

Roe et al. 2006)

Effector protein Location in the genome Function(s)

EspA LEE pilus protein of E. coli TTSS, flagellar fillament

EspB LEEcomponent of translocation pore and modulate

host cell cytoskeleton

EspD LEEinteract with EspB to form translocation pore,

biogenesis of the EspA filaments

Tir/EspE LEE

extracellular domain binds intimin and

intracellular N and C termini tyrosin

phosphorylated, recruit cytoskeletal proteins, lead

EspG LEEformation of actin stress fibers and disrupt of

microtubule networks

EspF LEE

disrupt intestinal barrier function, permeabilize

mitochondrion membrane, modulate IF network,

remodel microvilli, induce mitochondrial death,

play direct role in EPEC-induced cell death

(apoptosis)

EspH LEE modulate the host actin cytoskeleton structure

Map LEE

induce host cell actin dynamics, disrupt tight-

junction barrier function, mimick GTP-active form

of Rho-family GTPases (Alto et al., 2006),

stimulate Cdc42-dependent filopodia formation

and disruption of mitochondrial membrane

potential

EspZ/SepZ LEEmay play a role in causing severe colonic

hyperplasia in mice.

EspJ CP-933Unot required for A/E lesion formation, plays a role

in host survival and pathogen transmission.

NleA/EspI CP-933P not required for A/E lesion formation.

NleB ~ F non-LEE

associated directly or indirectly with the

colonization and pathogenesis of EHEC, EPEC, or

C. rodentium .

NleG non-LEE role not determined

NleH non-LEE role in early C. rodentium infection process

EPEC/EHEC/C. rodentium

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Effector protein Location in the genome Function(s)

Type 1 fimbriae fim operon adherence to α-D-mannose-containing glycoproteins

Type IV pilus (Bfp) EAF plasmid initial adherence to epithelial cells

Orf3/EspG2 EspC PAI plays a similar role as EspG

Intimin LEE intimate attachment adhesion molecule

OmpA ompA mediates HeLa cell adherence

Escherichia coli

factor for adherence

(Eta)

efal (EHEC), toxB

(O157), lifA (EPEC)

adherence – intestinal colonization, posttranscription

regulation of TTSS

Flagellin fliC motility and adherence; H6 – EPEC, H7 – EHEC

Secreted serine

protease

espC (EPEC), espP

(EHEC)

epithelial/tight junction disruption, mucinase,

interference with complement cascade

Cif

(Cycle inhibiting

factor)

ι Prophage

induce recruitment of focal adhesion plaques,

assembly of stress fiers, inhibition of cell cycle G2/M

phase transition, and lead to accumulation of inactive

phophorylated Cdk1 (Marches et al., 2003)

Long polar fimbriae Ipf and IpA operonspossible involvement in follicle-associated

epithelium

Secreted protease

of C1 esterase

inhibitor (StcE)

non-LEE C1-INH protease

Shiga-like toxins

1/2non-LEE inhibits protein synthesis

Haemolysin non-LEEcytotoxic to red blood cells, leukocytes, and

fibroblasts

TccP/EspFU (Tir-

cytoskeleton

coupling protein)

CP-933U

associate indirectly with Tir, binds N-WASP, and

stimulates Nck-independent actin polymerization,

alter polarized epithelial barrier function (similar to

EspF function).

EPEC

EPEC/EHEC

EHEC

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1.1.4.4 Shiga-like toxins

Shiga toxin is the prototype of the Shiga toxin family, a group of structurally and functionally

related exotoxins. This family includes Shiga toxin derived from Shigella dysenteriae serotype 1

and the Shiga-like toxins produced by STEC (Johannes and Romer 2010).

In 1897, the Japanese microbiologist Professor Kiyochi Shiga characterized the bacterial origin

of dysentery as being caused by S. dysenteriae. Konowalchuk, in 1977, identified a group of E.

coli isolates that are able to kill Vero cells in culture by secreting a factor into the tissue culture

medium. These bacteria were named Verotoxin-producing E. coli (VTEC). By the early 1980s,

Alison O’Brien and her research group discovered that some E. coli produced a toxin very

similar to Shiga toxin and, therefore, named these microorganisms Shiga-like toxin-producing E.

coli (STEC) (Johannes and Romer 2010). Later, it became clear that VTEC and STEC are two

names describing the same organisms and toxins.

Shiga-like toxin 1 (Stx1) produced by E. coli is nearly identical to the Shiga toxin prototype,

since they only differ by a single amino acid in the catalytic A subunit of the toxin (Johannes and

Romer 2010). STEC produce both Stx1 and Stx2 variants. The two toxins signal through a

common receptor (CD77, also referred to as Gb3) and have the same intracellular mechanism of

action, but they only share 56% homology at the amino acid sequence level. Stx2-producing

STEC have been linked epidemiologically to more severe disease in infected humans and to

more neurological symptoms in challenged gnotobiotic piglets than strains producing only Stx1

(Schuller, Frankel et al. 2004).

Shiga toxin family members consist of a single enzymatically active A-subunit (molecular mass

of 32 kDa) and five identical B-subunits (pentamer with each B fragment weighing at 7.7 kDa)

allowing the toxin to bind to the target cell surface receptors. Such AB5 toxins have a strong

affinity for glycans terminating in the sialic acid N-glycolylneuraminic acid (Neu5Gc), a

monosaccharide that creates high-affinity receptors on human gut epithelia and kidney

vasculature (Byres, Paton et al. 2008).

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StxA possesses specific RNA N-glycosidase activity that cleaves a single adenine residue from

the 28S rRNA of the 60S ribosomal subunit, resulting in the inhibition of elongation factor-

dependent aminoacyl tRNA binding and chain elongation in host cell protein synthesis process

(Suh, Hovde et al. 1998).

StxB binds to the receptor glycosphingolipid globotriaosylceramide (Gb3; also known as CD77),

present on cell surface, leading to the internalization of the toxin (Lingwood 1996). Gb3 fatty

acid heterogeneity, hydroxylation, length of carbon chain, and degree of saturation each may

influence the lateral movement of the glycolipid receptor in the plasma membrane. The

conformation of the head group presented on the cell surface may also be affected. The

membrane environment, dissociation of the receptor from lipid rafts, and membrane cholesterol

content are all important in the recognition and intracellular trafficking of Stx’s (Ling, Boodhoo

et al. 1998; Soltyk, MacKenzie et al. 2002).

Shiga toxin is internalized into host cells via endocytosis. The toxin is associated with clathrin-

dependent endocytosis; however, Shiga toxin is still taken up efficiently when clathrin-dependent

endocytosis is inhibited (Johannes and Romer 2010). This finding shows that the clathrin

pathway is not essential for the initial steps of toxin entry. Toxin-induced plasma membrane

invagination is dependent on the host cellular machinery involving dynamin, actin, and plasma

membrane cholesterol. Shiga toxin promotes membrane reordering and establishes membrane

environments that form detergent-insoluble complexes (Nakajima, Kiyokawa et al. 2001).

Toxin-induced lipid partition drives nanocompartmentalization at the cytoplasmic level to induce

the recruitment of an intracellular sorting machinery and toxin translocation (Mahfoud, Manis et

al. 2009).

1.1.4.5 Transmission of STEC

Cattle are the major reservoir of EHEC O157:H7, but they are not affected by this

microorganism. Many other farm animals such as sheep, goats, pigs, and turkeys can also shed

EHEC O157:H7 in their feces (Williams, McGregor et al. 2008). The most common route of

transmission for EHEC to humans is via ingestion of contaminated foods and water (Lim, Yoon

et al. 2010). In addition, it can also spread from person to person and from animal to person

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(Donnenberg and Whittam 2001). For example, STEC infections have been noted in people

visiting petting zoos, dairy farms, and camp sites where cattle used to reside. There have also

been reports suggesting potential airborne transmission in buildings with animal exhibits (Varma,

Greene et al. 2003).

Contaminated food sources

Contaminated ground beef is the most common vehicle for EHEC O157:H7 outbreaks. In the

process of grinding beef, pathogens contaminating the surface of the meat are transferred to the

interior; therefore, to ensure complete killing of the bacteria, ground beef should be cooked all

the way through (Welinder-Olsson and Kaijser 2005). Other contaminated food vehicles linked

to EHEC O157:H7 outbreaks including: unpasteurized milk, fresh produce, and drinking water.

Epidemiological studies suggest that these food sources were contaminated by bovine and feral

swine fecal materials (Donnenberg and Whittam 2001).

1.1.5 Citrobacter rodentium as an AE enteropathogen in mice

EPEC and EHEC do not readily colonize and cause disease in mice. Therefore, a related murine-

specific, non-invasive AE enteric pathogen is widely employed as a relevant animal model of

human disease (Mundy, MacDonald et al. 2005). Citrobacter rodentium belongs to the family of

bacterial pathogens, including EPEC and EHEC, that causes attaching-effacing (AE) lesions in

infected hosts. The histopathological features of these pathogens are intimate adherence to the

host intestinal epithelial cells and the effacement of brushborder microvilli. C. rodentium is

presently the only known murine AE pathogen (Bergstrom, Kissoon-Singh et al. 2010).

1.1.5.1 Ancestry and Phylogeny

Citrobacter rodentium, formerly Citrobacter freundii biotype 4280, is a highly infectious

pathogen that causes transmissible murine colonic hyperplasia (Deng, Li et al. 2001). In the

1960s and 1970s there were spontaneous infectious outbreaks in mouse colonies that occurred in

the United States and Japan. These infections were associated with the Gram-negative pathogen

Escherichia coli, Citrobacter freundii biotype 4280 now referred to as C. rodentium.

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The genome of C. rodentium ICC168 contains a 5.3 Mb circular chromosome and four plasmids,

pCROD1, pCROD2, pCROD3, and pCRP3, that are 54 to 3kb in size. The genome sequence of

C. rodentium identified key phylogenetic information of C. rodentium and revealed 1, 585 C.

rodentium-specific coding sequences (no orthologues in EPEC or EHEC), 10 prophage-like

regions, and 17 genomic islands, including the LEE region, which encodes the TTSS and

effector proteins (Petty, Bulgin et al. 2010).

The genome of C. rodentium genome has similarity with E. coli K-12 and other

Enterobacteriaceae (Petty, Bulgin et al. 2010). In a phylogenetic study, C. rodentium clusters

within the phylogenetic tree between other members of the Enterobacteriaceae; however, C.

rodentium is more distantly reltated to E. coli than E. coli is to Salmonella. Furthermore,

genomic evidence shows that sequenced species within the genus Citrobacter do not cluster and

that the genus is polyphyletic. From comparisons of the gene sets of C. rodentium, EPEC, and

EHEC, it is apparent that there is a large percentage (~32%) of the C. rodentium genome that is

unique (Petty, Bulgin et al. 2010).

On the other hand, there are a number of homologous genes present in C. rodentium, EPEC, and

EHEC that are not found in the K-12 reference strain (Ren, Beatson et al. 2005; Petty, Bulgin et

al. 2010). The majority of such genes are located on mobile genetic elements and contain many

key virulence determinants, such as the Locus of enterocyte effacement (LEE) and TTSS effector

proteins (Hoffmann, Hill et al. 2009; Tauschek, Yang et al. 2010). The virulence acquisition

mechanism of C. rodentium effectors is similar to that used by both EPEC and EHEC, which is

specialized transduction by lambdoid phages (Deng, Li et al. 2001; Petty, Bulgin et al. 2010).

Yet, even though cargo genes are found at analogous sites in the bacterial genomes, phage gene

comparisons show that they probably came from distinct phages. The acquisition of the LEE and

its associated effector proteins probably had a dramatic effect on the pathogenesis of C.

rodentium in the mouse. Although C. rodentium is genetically distinct from EPEC and EHEC

and does not infect the same host, the three bacteria share similar infection mechanisms and

virulence genes that are found on mobile genetic elements (Petty, Bulgin et al. 2010).

1.1.5.2 LEE and TTSS

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The locus of enterocyte effacement (LEE) pathogenicity island, including the associated type III

secretion system (TTSS), is conserved amongst EPEC, EHEC, and C. rodentium genomes.

However, there are some notable differences: while the LEE of EPEC and EHEC are in the SelC

tRNA locus, the C. rodentium LEE is inserted into a non-synonymous location flanked by

insertion sequence (IS) elements (Petty, Bulgin et al. 2010). In contrast to EPEC and EHEC, the

rorf1 and espG genes of C. rodentium are located at the opposite end of the LEE (Deng, Li et al.

2001).

There are 35 genes in C. rodentium that encode proteins with great sequence homology to known

TTSS effector proteins that are translocated by C. rodentium TTSS (Petty, Bulgin et al. 2010).

These effector proteins are encoded on the LEE, prophage remnants (CPRr13, CPRr17, and

CPRr33), and genomic islands. The prophage-like elements share similarity with the lambdoid

prophages identified in the genomes of EPEC and EHEC (Iguchi, Thomson et al. 2009). CRPr13

encodes effectors homologues to effectors encoded on EHEC prophage Sp6. CRPr17 encodes

effectors homologues to NleC, NleB, and NleG encoded on lambdoid prophages in EPEC and

EHEC (Petty, Bulgin et al. 2010).

In addition to effectors homologues to EPEC and EHEC, C. rodentium also encodes new TTSS

translocated proteins, including EspS, which has some similarity to OspB of Shigella dysenteria.

EspS is translocated in an EspA (molecular syringe filament)-dependent manner. C. rodentium

also encodes EspT, which enables the ability to subvert eukaryotic cytoskeleton by activating

small Rho GTPases (Bulgin, Arbeloa et al. 2009).

C. rodentium also encodes a type II secretion system (T2SS), type I secretion system (T1SS), and

type VI secretion system (T6SS). There are two T6SS gene clusters in the genome of C.

rodentium that are named type VI secretion system cluster 1 (CTS1) and 2 (CTS2). CTS1 is

nearly identical to the T6SS gene clusters contained in Enterobacter cancerogenus and has

similarity to SPI-6 components encoded in Salmonella enterica (Folkesson, Lofdahl et al. 2002).

CTS2, very similar to a putative T6SS in C. freundii, encodes all the components required for the

assembly of a functional T6SS; however, there is a bona fide frameshift in this cluster, which

means that it is unlikely that CTS2 can produce a functional T6SS (Schauer, Zabel et al. 1995;

Mougous, Cuff et al. 2006).

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There are 20 potential type V secretion systems (T5SS) encoded in the C. rodentium genome. 14

of them are identified as putative autotransporter adhesins that are related to those encoded in

EPEC (Benz and Schmidt 1989) and ETEC (Brennan, Li et al. 1988), which are involved in

virulence.

C. rodentium carries 19 fimbrial biogenesis operons, including the Kfc chaperone-usher fimbrial

operon and CFC type IV fimbriae, which produce factors involved in gastrointestinal

colonization (Mundy, Pickard et al. 2003). C. rodentium also encodes nonfimbrial adhesins,

such as LifA (Klapproth, Sasaki et al. 2005) and intimin (Schauer and Falkow 1993) that are

essential for gut colonization.

C. rodentium secretes several effector proteins (Esps) into tissue sulture medium in a similar

fashion as EPEC and EHEC (Deng, Puente et al. 2004). Some of these proteins translocate into

host cells. These translocated proteins include EspA, EspB, and EspD (Deng, Puente et al.

2004).

The C. rodentium LEE is slightly larger than EPEC and EHEC LEEs, 36kb vs. 34kb. CR LEE

shares all 41 open reading frames (ORFs) with EPEC and EHEC LEE (Deng, Li et al. 2001)

(Table 1.2). In spite of the differences, the intimin gene from EPEC can complement a C.

rodentium eae mutant and EHEC tir gene can complement a C. rodentium tir deletion mutant.

Therefore, there is still a striking similarity between C. rodentium LEE and that of the AE E. coli

pathogens, implying that the role of these genes in pathogenesis and disease is conserved (Deng,

Li et al. 2001; Deng, de Hoog et al. 2010).

1.1.5.3 C. rodentium pathogenesis and murine model of EHEC

infection

C. rodentium causes transmissible murine colonic hyperplasia and a reproducible distal colitis in

infected mice of a variety of genetic backgrounds (Mundy, MacDonald et al. 2005). The AE

lesions induced by C. rodentium infection at the epithelial cell surface are indistinguishable from

EPEC and EHEC infections. C. rodentium infection is characterized by crypt hyperplasia,

epithelial cell proliferation, mucosal thickening, and an uneven apical enterocyte surface

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(Higgins, Frankel et al. 1999). In infected mice, large numbers of bacteria colonize the distal

colon and adhere to epithelial surface (Johnson-Henry, Nadjafi et al. 2005). The onset of

hyperplasic response is first seen on day 4 post oral administration of C. rodentium, and the

mucosal thickening reach a maximum between on day 10 post infection (Gareau, Wine et al.

2010). An inflammatory response is also activated, but the precise mechanism and underlying

molecular events still need to be delineated. Research results showing the functional

conservation of virulence proteins encoded by LEE from various AE pathogens indicate the

relevance of using C. rodentium-mouse intestine interaction as a model for studying human

EPEC and EHEC infections. This murine infection model also allows for the study of immune

responses to EPEC and EHEC LEE-encoded proteins (Deng, Li et al. 2001).

1.1.5.4 C. rodentium provides murine infectious model of IBD

Oral introduction of C. rodentium to mice is associated with an inflammatory cell infiltrate in the

distal colon. C. rodentium infection elicits a mucosal T-cell infiltrate that is associated with

colonic epithelial cell hyperplasia. The mucosal inflammatory infiltrate consists predominately

CD4+ T-cells, with a Th1 phenotype (Kang, Otsuka et al. 2010) that is said to provide a murine

model of Crohn disease (Higgins, Frankel et al. 1999).

In mice infected with C. rodentium, bacteria transverse the epithelial barrier and are detected in

the colonic mucosa where interactions with host immune cells occur.C. rodentium have been

detected in mesenteric lymph nodes of orally infected mice (Skinn, Vergnolle et al. 2006) similar

to what occurs in inflammatory bowel disease (IBD) patients - enteric bacteria have been

isolated from the mesenteric lymph nodes of patients with Crohn disease (Caradonna, Amati et al.

2000).

The T-cell infiltration, cytokine production, and epithelial cell proliferation observed in C.

rodentium-infected mice are similar to changes seen in other mouse models of IBD: including

mice with IL-2, IL-10, T-cell receptor alpha (TcRα), or TcRβ gene deletions. In these models,

disease occurs as a result of immune dysregulation and it is mediated by CD4+ T-cells of a Th1

phenotype (Spahn, Ross et al. 2008).

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1.2 Host Defense and Exploitation of Host Responses by

Pathogens

Infectious diseases are a major cause of morbidity and mortality around the world and are an

immense challenge in the biomedical research field. Improving sanitary conditions and

developing vaccines or therapies are all important in combating infectious diseases. However,

improving intervention strategies requires further understanding of the host immune system and

more importantly, microbial pathogenesis and host-microbe interactions (Mirpuri, Brazil et al.

2010).

The intestinal tract has upwards of 100 trillion microbes, composed by an estimated 500 species

at any given point in time (Turnbaugh, Ley et al. 2007; Canny and McCormick 2008). The

effect of microbial colonization on host health depends on microbial adaptation (Casadevall and

Pirofski 2000). Some microbes exert beneficial, positive effects in host intestine. In other

scenarios, pathogenic bacteria colonization has detrimental effects on the host, leading to

diarrheal disease and infectious colitis. The severity of the outcome depends on the condition of

the host immune system; for example, some pathogens only affect immune compromised

individuals (Pamer 2007).

1.2.1 Bacterial virulence factors

Depending on the micro-environment where bacteria colonize, enteric pathogens express various

virulence factors that allow them to penetrate epithelial surface, attach to cell surfaces, invade

intracellular compartments, evade host defense mechanisms, and effectively infect neighboring

cells. One example of this is how Streptococcus pneumoniae relies on its capsule to prevent

antibody and complement deposition on its surface, thereby avoiding phagocyte clearance

(Finlay and McFadden 2006). In mammals, there are two types of defense: innate and adaptive

or acquired (Shames, Auweter et al. 2009) that respond to virulence factors of enteric pathogens;

these are each considered in more detail below.

1.2.1.1 Bacterial lipopolysaccharide

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Lipopolysaccharide (LPS) is an abundant outer membrane component, an active entity of

endotoxin, of Gram-negative bacteria. Its biological activity is associated with its ability to

trigger host innate immune system to initiate inflammatory response. LPS was first described as

a highly toxic component bound tightly to cells of Vibrio cholerae. LPS induces high fever,

septic shock and even death of experimental animals. Similar effects have also been observed in

humans (Bilbo, Wieseler et al. 2010). Chemically, LPS contains 3 covalently bound parts – an

O-antigenic polysaccharide, a core oligosaccharide, and glycolipids. The glycolipid structural

component, known as lipid A, contains full endotoxic activity (Raetz and Whitfield 2002).

The repetitive glycan polymer found in LPS is known as the O-antigen. Following synthesis of

O-antigens, they are ligated to the core oligosaccharide as the outermost domain of LPS. The

composition of the O-antigen varies from strain to strain of E. coli and other Gram negative

organisms. The presence or absence of O chains classifies the LPS as either smooth or rough,

respectively. The core oligosaccharide attaches directly to lipid A and commonly contains 3-

deoxy-D-mannooctulosonic Acid (KDO) (Raetz and Whitfield 2002).

Lipid A is an amphiphilic molecule with covalently-bound hydrophilic part and lipophilic long

chain fatty acyl groups. The biosynthesis of lipid A-core starts with the acylation of the sugar

nucleotide UDP-GlcNAc (N-Acetylglucosamine). The acetyl group is then removed to obtain an

acylated glcN residue. Two of these residues together form the lipid A subunit (Raetz and

Whitfield 2002). The number and length of acyl chains vary depending on the bacterium. For

instance, hex-acylated lipid A molecules are commonly found in the Enterobacteriaceae family

of Gram negative bacteria (van Mourik, Steeghs et al. 2010).

1.2.2 Immune defense in microbial recognition

1.2.2.1 Innate immune response to microbes

Innate immune recognition of gut pathogens is mediated by pattern-recognition receptors

(PRRs), which have recognition capabilities for conserved and invariant features of the

microorganisms (Tlaskalova-Hogenova, Stepankova et al. 2004; Diacovich and Gorvel 2010).

PRRs bind to a large number of molecules unique to microorganisms that have common

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structural regions. Targets of PRRs are known as pathogen-associated molecular patterns

(PAMPs) (Tlaskalova-Hogenova, Stepankova et al. 2004).

A well characterized class of PRRs is the family of Toll-like receptors (TLRs) (Tlaskalova-

Hogenova, Stepankova et al. 2004; Mirpuri, Brazil et al. 2010). TLRs are transmembrane

receptors that recognize viral nucleic acids and several bacterial products, such as

lipopolysaccharide (TLR4), flagellin (TLR5), and lipotechoic acid (TLR2) (Roy and Mocarski

2007). TLRs elicit both inflammatory and antimicrobial responses after activation by microbial

ligands. TLRs activate macrophages to produce pro-inflammatory cytokines such as TNF-alpha,

IL-1β, and IL-6, which initiate local and systemic inflammatory responses (Roy and Mocarski

2007). TLRs also directly induce macrophages to produce antimicrobial peptides (AMPs),

including cathelicidins and defensins (Guani-Guerra, Santos-Mendoza et al. 2010). Cathelicidin

exerts a direct chemoattractive action on monocytes, neutrophils, and CD4+

T lymphocytes and it

is also able to bind LPS to block the release of TNF-α. Defensins have chemoattractant

properties on different cell types such as monocytes, T lymphocytes, and dendritic cells plus

they also are able to induce the production of diverse chemokines and cytokines (Guani-Guerra,

Santos-Mendoza et al. 2010).

The expression of these inflammatory cytokines is associated with the presence of Shiga toxin

and LPS. However, the development of HUS requires not only the presence of Shiga toxin, but

also pro-inflammatory stimuli such as LPS and TNF-α (Psotka, Obata et al. 2009). This finding

is pointing towards the possibility of using LPS as potential antigens in the development of

vaccines, there is increasing evidence that serum antibodies to the surface LPS may confer

protective immunity to these Gram-negative enteric pathogens (Horne, Vallance et al. 2002).

Gram negative bacteria induce inflammatory responses in host via the interaction between LPS

and receptors on both epithelial cells and innate immune cells such as macrophages and dendritic

cells (Horne, Vallance et al. 2002). LPS-binding protein (LBP) binds monomers of LPS that is

in circulation and a complex with CD14 is formed. CD14, a glycosylphosphatidylinositol-

anchored cell surface molecule, then forms a complex with Toll-like receptor 4 (TLR4), which

activates intracellular signaling (Stahl, Svensson et al. 2006).

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Although TLR4 is both a surface receptor and a Golgi-localized protein, the recycling of TLR4

from cell surface back and forth to the Golgi is not necessary for the initiation of cellular

activation (Latz, Visintin et al. 2003). Following activation with LPS, both TLR4 and CD14 are

clustered into lipid rafts where the rafts provide a platform for signal transduction responses

ultimately leading to actin cytoskeletal rearrangements. This finding point to TLR4 function as a

bacterial antigen receptor, which partition into lipid microdomains upon ligand stimulation leads

to intracellular signal transduction events (Szabo, Dolganiuc et al. 2007).

In addition to transmembrane receptors on the cell surface, there are intracellular receptors,

including Nod-like receptors (NLRs), that are involved in bacterial recognition (Roy and

Mocarski 2007). NLRs contain a nucleotide-binding oligomerization domain (NOD) and a

leucine-rich-repeat domain (Kumar, Kawai et al. 2009). The three types of domains present at

the amino terminus of NLRs categorize them into 3 subfamilies: NOD, NALP, and the NAIP

subfamily. The NOD subfamily is involved in sensing bacterial peptidoglycans to induce the

production of pro-inflammatory cytokines and chemokines, which results in the recruitment of

neutrophils to the site of infection (Kumar, Kawai et al. 2009). The NALP subfamily is involved

in the activation of the inflammatory response and inflammasome activation mediated by the IL-

1 cytokine family. There are several types of inflammasomes activated by NAIPs (Arend,

Palmer et al. 2008). NALPs can also contribute to antimicrobial defense by inducing apoptosis

(programmed cell death) of infected host cells (Petrilli, Papin et al. 2007).

1.2.2.2 Adaptive immune system

Adaptive immune recognition is mediated by both T-cells and B-cells. These cells express on

their surface a diverse group of receptors assembled from variable and constant fragments

through recombination-activating gene (RAG)-protein-mediated somatic recombination

(Maynard and Weaver 2009). Microbial antigens are taken up by antigen-presenting cells and

delivered to either mesenteric lymph nodes or the spleen where they are recognized by

lymphocytes (Medzhitov 2007).

In intestinal epithelia, dendritic cells residing underneath the epithelial monolayer take up

pathogens by phagocytosis (Moll 2003). Bacterial proteins are then processed into antigenic

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peptides and presented at the cell surface by MHC class I and/or class II molecules. This results

in TH (helper)-cell activation, which leads to differential cytokine and chemokine production

(Moser and Murphy 2000). The produced cytokines and chemokines control the recruitment,

from the systemic circulation into the lamina propria, of neutrophils, eosinophils, and basophils

to mount a mucosal defense against pathogens (Stadnyk, Dollard et al. 2000).

For B-cells, which can be directly activated by bacterial LPS or flagellin, antibodies of the IgM

and IgA classes generated by plasma cells are released into the mucus layer to combat enteric

pathogens (Tlaskalova-Hogenova, Stepankova et al. 2004).

1.2.3 Inflammatory and Innate Responses to Bacteria

The interaction between bacteria, the gut epithelium, and host defense responses are very

important in determining the fate of bacterial infections and disease outcomes. It is clear from

the previous section that epithelial cells produce various inflammatory mediators in response to

pathogens in order to manage or eliminate the infection. Many times this translates to an

increase in fluid section and intestinal motility, which aids in clearance of the pathogen by

―flushing‖, or recruitment of innate and adaptive inflammatory mediators and cells, which also

contribute to pathogen clearance. The hosts often pay a price by developing disease symptoms,

and the pathogen can benefit from these responses by spreading to other hosts (Klapproth, Sasaki

et al. 2005). Normally, the intestinal epithelial layer induces a controlled and balanced

inflammatory response to eliminate pathogens and limit the destructive consequences of mucosal

inflammation to minimal. A number of defects in this homeostasic balance can lead to a wide

range of disorders. Many gastrointestinal bacterial pathogens have developed many strategies to

promote inflammation leading to extensive epithelial injury and necrosis of the mucosa, affecting

large areas of the colon (Santos, Zhang et al. 2002). Invasive enteric pathogens, such as Shigella

spp. or S. Typhimurium, is found to associate with exacerbated epithelial injury and this is

attenuated when infecting CD18-deficient calves, whose neutrophils are unable to extravasate,

with the pathogen (Nunes, Lawhon et al. 2010). This suggests that neutrophils are mainly

responsible for the collateral tissue damage accompanying the severe inflammation and lead to

intestinal fluid accumulation and diarrhea. Diarrhea and dehydration that follows can be life

threatening; therefore, this draws a clear picture of how the protection against bacterial

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translocation and dissemination provided by exudative inflammation can become a burden and

need to be tightly monitored in order to limit the damage inflicted on the host (Winter, Keestra et

al. 2010).

Another problem associated with bacteria-induced severe inflammation is how they use this

aggressive inflammatory response to breach cell-cell junction followed with significant changes

in the gut microbiota (Guttman, Li et al. 2006). EPEC, EHEC, and C. rodentium have evolved

various mechanisms to target and disrupt tight junctions by manipulating Pho GTPases and

MCLK-mediated signalling in infected host cells. By hijacking these pathways, the pathogens

can manipulate the host actin cytoskeleton and, ultimately, the junction structure as well as the

innate immune response (Guttman and Finlay 2009). This inflammatory response is associated

with changes in the intestinal microbiota, which includes an increase in abundance of bacteria in

the phylum Proteobacteria, specifically members of the Enterobacteriaceae family (Lupp,

Robertson et al. 2007). Severe inflammation enteric pathogens such as Campylobacter jejuni

and S. Typhimurium, is followed by an increase in the population of Enterobacteriaceae

(Stecher, Robbiani et al. 2007). Furthermore, the intestinal inflammation caused by C.

rodentium-infection results in the overgrowth of the pathogen in the intestinal lumen of mice

(Stecher, Robbiani et al. 2007).

The onset of intestinal inflammation induced by pathogens allow them to take advantage of

environmental changes that accompany this host response. First, the removal of luminal contents

by the flushing action of diarrhea provide pathogens the opportunity to colonize the mucus layer

and outgrow the microbiota. An example would be S. Typhimurium benefiting from

inflammation by outgrowing the intestinal microbiota in mice and the S. Typhimurium mutants

are unable to use motility and chemotaxis to outcompete other microbes (Stecher, Barthel et al.

2008). Secondly, recent studies suggest that pathogens capable of inducing severe inflammatory

response possess virulence mechanisms that make them resistant against antimicrobials, and this

process enhances their competitiveness in the lumen of an inflamed gut. For instance, S.

Typhimurium synthesizes and releases a glycosylated derivative of enterobactin, salmochelin,

which is no longer bound by lipocalin-2, an antimicrobial, in an inflamed intestine and allows the

pathogen to resist against this antimicrobial protein. This advantage for pathogen is not observed

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in the absence of intestinal inflammation or in lipocalin-2-deficient mice (Raffatellu, George et al.

2009).

Both the innate and adaptive immune systems play a role in IBD. Gut microbiota changes have

been seen in IBD patients and the chronic intestinal inflammation is accompanied by a

significant increase in Enterobacteriaceae and a reduced biodiversity of bacteria in the phylum

Firmicutes (Marteau 2009). In mice, the induction of inflammation by bacteria during infection,

by a chemical inducer such as dextran sulphate sodium (DSS), or a genetic deficiency such as the

interleukin-10-deficient mouse model, can alter the compositions of the intestinal microbiota and

cause a reduction in bacterial diversity. In Citrobacter rodentium-infected mice, acute intestinal

inflammation occurs followed by the weakening of intestinal barrier functions and thereby

triggering chronic disease. S. Typhimurium possesses bacterial factors that allow them to

maintain active in macrophages and promotes intracellular S. Typhimurium proliferation, leading

to an increase in immune response. Intestinal inflammation by S. Typhimurium is characterized

by the disruption of crypt organization in the ileum, caecum, and colon by epithelial erosion and

ulceration, by reduction of goblet cells, by infiltration with acute pro-inflammatory cells (Barthel,

Hapfelmeier et al. 2003). Both of these bacterial infections are specific examples illustrating that

in the context of a bacterium, immunocompetent hosts can become susceptible to increased

inflammation and exacerbated disease symptoms caused by bacterial factors (Nell, Suerbaum et

al. 2010).

1.2.4 Microbial Manipulation of the Host Epithelium

EHEC O157:H7 elicits its pathogenic effects by attacking intracellular signal transduction

pathways in host cells. These bacteria manipulate more than one intracellular pathway and

interfere at a number of points along each pathway to ensure their own survival. Further

characterization of how EHEC subverts host cell signaling pathways is key to better

understanding this infectious disease (Bhavsar, Guttman et al. 2007).

1.2.4.1 Attaching-effacing Lesions

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One of the most commonly described cellular targets of pathogenic bacteria is the host

cytoskeleton. Many microorganisms manipulate the host cytoskeleton to gain entry into the cells

and to move around in the infected cell. Bacterial pathogens usually manipulate and control the

polymerization of actin filaments by interfering with cellular regulators of the process, such as

small GTPases (Stender, Friebel et al. 2000).

Manipulation of host cell cytoskeleton by an extracellular pathogen—EHEC

EHEC has elaborate actin-recruiting processes. E. coli secreted proteins (EspE, EspB, EspD,

Map, EspF, EspFU, and EspT) are injected into the cytosol of infected host cells through a type

III secretion system encoded molecular syringe (Welinder-Olsson and Kaijser 2005). Among the

various translocated proteins encoded on the 35-kb pathogenicity island, called the locus of

enterocyte effacement (LEE), is the EspE protein, also known as translocating intimin receptor

(Tir). Tir, with the help of other secreted proteins (EspFU), acts as a receptor for the bacterial

outer membrane protein intimin (Garmendia, Phillips et al. 2004; Cheng, Skehan et al. 2008).

There are also other receptors besides Tir, although controversial, that have been suggested to

play a role in bacterial adhesion such as nucleolin and β1 integrin (Sinclair and O'Brien 2004).

The Tir-intimin interaction gives rise to intimate attachment of EPEC and EHEC to host cells

and leads to cytoskeletal rearrangements via different mechanisms.

In EPEC infection, Tir inserts itself into the host cell membrane and is tyrosine phosporylated in

the C-terminus by host kinases such as Ab1- and Tec-family kinases, which leads to the

recruitment of kinases through interactions with their SH2 and SH3 domains (Bommarius,

Maxwell et al. 2007). Phospho-Tir then mediates the recruitment of the host adaptor protein Nck

(non-catalytic region of tyrosine kinase), which activates downstream neural Wiskott-Aldrich

syndrome protein (N-WASP) leading to actin polymerization through Arp2/3 at the bacteria

attachment site (Frankel and Phillips 2008). α-actinin is also recruited during this process and

contributes to pedestal formation by cross-linking actin filaments (Caron, Crepin et al. 2006).

On the other hand, Tir from EHEC (EspE) does not get phosphorylated by host kinases, but

instead interacts with another bacterial effector, EspFU. The function of EspFU is very similar to

Nck leading to the recruitment of the host actin cytoskeleton elements such as N-WASP and

Arp2/3 complex to form dense pedestals, and the effacement of intestinal brush-border

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microvilli, collectively known as the attaching-effacing lesion (Donato, Zareie et al. 2008)

(Figure 1.1). Activity of EspE of C. rodentium also does not require tyrosine phosphorylation

by host kinases (Deng, Vallance et al. 2003). Our laboratory has shown previously that depletion

of cellular cholesterol, a major component in lipid rafts, inhibits EHEC O157:H7-induced A/E

lesions (Riff, Callahan et al. 2005).

1.2.4.2 Apical Junction Complexes

Tight junction disruption by enteric pathogens

As shown by a number of infection models affecting the integrity of the intestinal epithelial

barrier, Apical junction complexes (AJCs) are clearly one of main targets of bacterial virulence

(Laukoetter, Bruewer et al. 2006). AJCs can be compromised by either bacterial toxins or

bacterial effectors, by direct contact of the pathogen or indirect manipulation of the signalling

pathways in host junction regulation, such as the phosphorylation or dephosphorylation of

junction-associated proteins. Pathogens causes dysregulation of the AJCs to breakdown the

intestinal barrier thereby increase fluid secretion, diarrhoea, and enhance transmission.

The EPEC TTSS and effector protein EspF decreases transepithelial electrical resistance (TER)

and alters intestinal epithelial AJC structure (Dean and Kenny 2004; Viswanathan, Lukic et al.

2004). EPEC disrupt tight junction architecture by interfering with tight junction protein-protein

interactions and redistributing tight junction proteins (Muza-Moons, Schneeberger et al. 2004).

Recent results show that enteropathogenic E. coli causes diarrhea by disruption of tight junctions

and by redistributing occludin (Shifflett, Clayburgh et al. 2005) (Figure 1.1). Similarly, EHEC

infection leads to decrease in TER, however, this appears to occur through different mechanisms

that can be rescued by TGF-β.

Other bacteria such as S. Typhimurium, can also cause structural and functional alterations in tj

through its SPI-1-dependent type 3 secretion of effectors (SopB, SopE, SopE2, and SipA). C.

jejuni-mediates barrier disruption through phosphorylation of junction-related proteins such as

ERK, JNK, and p38 MAPK, moreover, it causes redistribution of lipid raft-associated

hyperphosphorylated occludin (Grassl and Finlay 2008). The mouse pathogen C. rodentium, can

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alter apical junctional protein distribution during its attachment to the epithelial cells (Guttman,

Li et al. 2006).

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Figure 1.1 Schematic diagram of EHEC O157:H7 signalling regulation of AE lesion

formation and barrier disruption. EHEC adheres to epithelial cells and secrete its effector

proteins (Esps) into the host cell through type III secretion system (TTSS). Among the secreted

proteins is Tir which binds to EHEC intimin thereby activating the asparagine-proline-tyrosine

(NPY) motif on Tir to initiate downstream signalling molecules including: TccP2/EspFU, N-

WASP, Arp2/3. This signalling cascade is involved in EHEC-induced AE lesion formation.

EHEC also secrets EspF and NleH which interferes with tight junction proteins/cytoskeleton

regulation leading to tight junction disruption.

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1.3 Host cell mechanisms hijacked by bacteria during infection

Microbial infections result in characteristic stereotypic pattern of host inflammatory responses

(Serhan, Brain et al. 2007). The intestinal tract, coming in contact with numerous microbial

pathogens can develop enterocolitis in an infected individual. Interestingly, non-invasive bacteria

are emerging as enteric pathogens also capable of eliciting host damage and inducing

inflammatory responses by hijacking signal transduction pathways in host epithelial cells

(Croxen and Finlay 2010).

In the field of EHEC O157:H7 infection research, many results now point to bacteria pirating

signalling pathways such as the cytochrome c (cyt c)-caspase 3 pathway, the MAP kinases-

nuclear transcription factor pathway, and the PI3K-PKC pathway to induce host programmed

cell death, the production and secretion of chemokine CXCL8 (IL-8), the induction of attaching-

effacing (AE) lesions, as well as barrier disruption by manipulating the host cell cytoskeleton

(Ceponis, Riff et al. 2005).

1.3.1 Osteopontin

Osteopontin is a phosphorylated glycoprotein that is expressed by a wide range of cell types

(Sodek, Batista Da Silva et al. 2006). Originally, OPN was characterized as a bone matrix

protein (Prince and Butler 1987), T-lymphocyte activation protein (Eta-1) (Patarca, Saavedra et

al. 1993), and cell transformation-associated protein (Craig, Nemir et al. 1988). However, further

research pointed to OPN also being a matricellular protein with diverse biological activities

signalling through multiple cell-surface receptors (Sodek, Batista Da Silva et al. 2006). Another

major role of OPN is its function as an inflammatory cytokine. Recent studies have reported that

OPN is up-regulated in a number of inflammatory diseases and is needed for developing both

cellular immunity and wound healing (Morimoto, Kon et al. 2010). The development of many

inflammatory diseases is attenuated in the absence of OPN and OPN expression is up-regulated

in most wound injured organs (Yumoto, Ishijima et al. 2002).

Structure

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OPN is part of SIBLING family proteins that is synthesized as a ~34kDa nascent protein (Cho

and Kim 2009). OPN then goes through extensive post-translational modifications, such as

phosphorylation, glycosylation, and sulphation prior to being secreted as a 44-75 kDa protein.

These post-translational modifications relate to the different functional activities of OPN

(Giachelli and Steitz 2000). Most of the known functional activities of OPN are associated with

its highly conserved structural motifs that bind mineral, CD44, and integrin receptors (Lee,

Wang et al. 2008).

CD44 has been identified as an OPN receptor in cytokine responses of macrophages (Ashkar,

Weber et al. 2000). Ligation of CD44 receptors and β3-integrin by OPN domains leads to

macrophage recruitment and the production of cytokines and activation of metalloproteinases

(Weber 2002). Recent literature also shows that OPN can bind to and recruit complement factor

H to the cell surface via its interaction with αλβ3 and CD44 receptors (Fedarko, Fohr et al.

2000). The interaction of OPN with factor H likely plays a role in controlling OPN pro-

inflammatory effects. An intracellular form of OPN (iOPN) that co-localizes with CD44 in

fibroblasts, macrophages, and osteoclasts appears to modulate cytoskeleton-related functions

(Zohar, Zhu et al. 2004).

Osteopontin and mucosal immunity

Multiple studies link OPN expression with epithelial barrier changes. OPN is an important

luminal regulator where epithelial cells secrete OPN, which is then involved in controlling

epithelial barrier permeability and secretary functions (Gassler, Autschbach et al. 2002; Acheson

and Luccioli 2004). OPN has a critical function in regulating barrier defense processes,

including the expression of MHC-II and TLRs (Acheson and Luccioli 2004; Iwasaki and

Medzhitov 2004). The presence of OPN may also be important for supporting cell apoptosis and

preventing cell necrosis, which can lead to massive inflammation and loss of epithelial barrier

integrity (Kruidenier, Kuiper et al. 2003).

OPN expression increases at sites of inflammation by epithelial, stromal, and immune cells;

therefore, it is involved in both innate and adaptive immune signalling pathways. OPN is

secreted by activated T-cells to recruit macrophages and stimulate Th1 cytokine release through

OPN interaction with αλβ3 receptor (Cantor and Shinohara 2009). Conversely, secretion of the

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anti-inflammatory cytokine IL-10 is suppressed by OPN signalling through the CD44 receptor

(Shinohara, Jansson et al. 2005). In the absence of OPN expression, the Th2 cytokine response

is critical, and OPN-null mice display an increased susceptibility to infectious challenge with

intracellular pathogens, compared to their wild type littermates (Ashkar, Weber et al. 2000).

1.3.2 Detergent-resistant Microdomains

Detergent-resistant microdomains (DRMs), also known as lipid rafts, are liquid-ordered (Io)

phase microdomains that exist in cell membranes. The liquid-ordered (Io) phase is a sterol-

dependent composition in which lipid acyl chains are tightly packed. In plasma membrane, Io-

phase domains form in sterol-rich cell membranes where they are dispersed in disordered

membrane domains. DRMs are enriched in cholesterol and sphingolipids. The main function of

cholesterol is to ensure the integrity of lipid rafts (Kline, O'Connor Butler et al. 2010).

Detergent insolubility of lipid rafts

The existence of rafts was first described from the observation that eukaryotic cell plasma

membranes are not fully solubilized by non-ionic detergents, such as Triton X-100, at low

temperature. Using this extraction method, Io phase can be isolated using sucrose gradient

ultacentrifugation (Brown and Rose 1992). The principle behind this extraction method is that

the close packing of lipids in Io phase prevents detergent incorporation into the lipid bilayer (Xu,

Bittman et al. 2001).

Raft structure and function

Much of the evidence of raft functioning in eukaryotic cells comes from looking at DRM-

association of key proteins and the effect of cholesterol modulators in disrupting function

(Dykstra, Cherukuri et al. 2003; Pike 2003). Lipid rafts have important roles in both signal

transduction (Pike 2009) and membrane trafficking (Kirkham and Parton 2005).

Recent studies have further confirmed the existence and function of lipid rafts through

microscopic observations of cell surface signaling molecules assembling into large complexes

(Pike 2009). For example, DRM-association of T and B-cell receptors increases during

signaling, and signaling in T-cells is sensitive to cholesterol depletion (Kabouridis 2006).

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Lipid rafts and bacterial pathogens

Another strong evidence for raft function comes from observing the behavior of pathogens

(Grassme, Gulbins et al. 1997). Some pathogens bind order-preferring proteins and lipids on

host cell surfaces, thereby hijacking a host signaling platform to elicit pathogenic effects of

infection (Riethmuller, Riehle et al. 2006; Shen-Tu, Schauer et al. 2010). Invading bacteria also

have raft-targeting bacterial factors, which use rafts for internalization into the host cell

(Kalischuk, Inglis et al. 2009). More studies point to a highly regulated raft formation

mechanism that occur only in response to stimulation, such as receptor clustering (Hashimoto-

Tane, Yokosuka et al. 2010).

One example of receptor clustering, also a method used to visualize rafts, is cholera toxin-

induced clustering of the DRM-enriched ganglioside, GM1 (Ingelmo-Torres, Gaus et al. 2009).

Recruitment of raftophilic proteins to rafts promotes their interaction and creates signaling

platforms to reduce interference by non-raft proteins (Brown 2006). Multiple factors involved in

actin regulation - such as PLCγ1, diacylglycerol, PIP2, and PIP3 are common raft constituents

that can be targeted by pathogens for host cell attachment and subsequent entry by invasive

organisms (Zaas, Duncan et al. 2005; Chichlowski and Hale 2008).

1.3.3 PI3K family: role in cell signalling and cytoskeletal

rearrangements

Phospholipids are known as precursors for second messengers in cell surface receptor coupled

signal transduction pathways. Phosphoinositide 3-kinases (PI3Ks) are a family of enzymes

(Figure 1.2) involved in numerous cellular functions such as cell growth, proliferation,

differentiation, motility, survival, and intracellular trafficking (Ulici, Hoenselaar et al. 2008).

PI3Ks are related to intracellular signal transducer enzymes capable of phosphorylating the 3rd

position hydroxyl group of the inositol ring of phosphatidylinositol (PtdIns) (Jones, Paneda et al.

2005). PI3Ks generate three different lipids by converting PtdIns, PtdIns(4)P, and PtdIns(4,5)P2

to PtdIns(3)P, PtdIns(3,4)P2, and PtdIns(3,4,5)P3 (Cantrell 2001; Kooijman, King et al. 2009).

PtdIns(3)P is constitutively present in cells; whereas PtdIns(3,4)P2 and PtdIns(3,4,5)P3 are nearly

absent in resting cells, but following stimulation the intracellular concentration rises dramatically

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indicating an important function as second messengers (Vanhaesebroeck, Leevers et al. 1997;

Kok, Geering et al. 2009).

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Figure 1.2 Schematic diagram of the PI3K family enzymes. These class-specific structural

regions include: the p85-binding domain (p85); Ras-binding domain (Ras); a proline-rich region

(P, only present in p110 and PI3K-II); a leucine-zipper-like domain (bZIP, found only in

p110, , and ); a G-protein subunit binding domain (); a putative PH domain (only in

PI3K); and a C2 domain found only in class II PI3Ks. Conserved regions throughout the PI3K

family members include: the PI-kinase region; the Wortmannin-binding site (Wm), and the ATP-

binding site (ATP).

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Class IA PI3Ks

The class IA PI3Ks refers to a group of proteins with heterodimers ~200 kDa in size, which

contain a 110-120 kDa catalytic subunit and a 50-85 kDa regulatory subunit (Inukai, Funaki et al.

2001; Hawkins, Anderson et al. 2006). The class IA PI3K catalytic subunits include p110α, -β, -

δ, and homologous molecules from several other species (Walker, Perisic et al. 1999). They

have several conserved regions, including the adaptor- and the Ras-binding sites, the PI-kinase

region, and the C-terminal kinase domain (Vanhaesebroeck, Guillermet-Guibert et al. 2010).

The regulatory subunit of class IA PI3K is composed of a Src homology 3 (SH3) domain, a

breakpoint-cluster-region homology (BH) flanked by two proline-rich regions, and two C-

terminal SH2 domains spaced by an iSH2 region (Wymann and Pirola 1998) (Figure 1.3). The

iSH2 region mediates tight biding of p85 to catalytic subunit. The p85 subunit self-associates via

a SH3 domain (Kapeller, Prasad et al. 1994) and proline-rich sequences to regulate PI3K

activity. Proline-rich regions 1 and 2 flank the BH domains and act as ligands for SH3 domains

of non-receptor protein tyrosine kinases (PTK) like v-Src, Lyn, and Fyn (Pleiman, Hertz et al.

1994). The N- and C-terminal SH2 domains of p85α recognize the canonical phosphotyrosine

motif PYXXM. The BH domain of p85 is highly homologous to the GAP (GTPase activating

protein) domain of the breakpoint-cluster-region (Bcr) gene product (Diekmann, Brill et al.

1991). It specifically interacts with the Rho family proteins Cdc42 and Rac1.

Class IB PI3Ks

The class IB PI3Ks is stimulated by G-protein βγ subunits. They do not interact with the SH2-

domain-containing adaptors. The catalytic subunit, p110γ, contains an amino terminal Ras-

binding site, a PIK domain, and a catalytic domain (Vanhaesebroeck, Guillermet-Guibert et al.

2010).

Class II PI3Ks

The class II PI3Ks has an in vitro specificity towards PtdIns and PtdIns 4-P. This class of PI3Ks

are 170-210 kDa in size with a C-terminal C2 homology domain. No adaptor molecules have

been identified to date, and the mode of activation is still unclear. Studies suggest, however, that

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this class of PI3Ks binds to lipids in a calcium-independent manner (Vanhaesebroeck,

Guillermet-Guibert et al. 2010).

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Figure 1.3 Schematic diagram of class IA PI3K p85 regulatory subunit. The modular

domains are: Src homology 3 domain (SH3); P1 and P2 proline-rich regions; the breakpoint-

cluster-region (Bcr) homology domain (BH); the N- and C-terminal SH2 domains (NSH2 and

CSH2); and the inter-SH2 region (iSH2).

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Class III PI3Ks

This class of enzymes is homologues of S. cerevisiae Vps34p (vacuolar protein sorting mutant).

They only phosphorylate PtdIns and activity depends on functional Vps15p protein, a 170 kDa

Ser/Thr kinase, which activates and recruits Vps34p to membranes. This class of PI3Ks is

responsible for recruiting phosphatidylinositol kinase to the late Golgi compartment

(Vanhaesebroeck, Guillermet-Guibert et al. 2010).

Upstream of class I PI3Ks

Class I PI3Ks are involved in signalling through receptors with intrinsic or associated Tyr kinase

activity and by receptors linked to heterotrimeric G proteins (Kok, Geering et al. 2009). The

mechanism of G-protein induced PI3K signalling is still unclear, but studies have shown that

signalling may take place in specialized platforms in the membrane variously referred to as either

cholesterol-enriched microdomains or lipid rafts. The association of Src kinases with lipid rafts

plays a crucial role in the activation of PI3K-Akt signalling (Arcaro, Aubert et al. 2007). An

adaptor-mediated translocation of PI3Ks to receptor Tyr kinases, similar to signalling via IRS-

1/2, likely aids positioning of the catalytic subunits close to membranes with their lipid

substrates (Rodriguez-Viciana, Warne et al. 1994).

Furthermore, class I PI3Ks interact with Ras proteins in a GTP-dependent manner. Co-

expression studies looking at interaction between p110α-p85α and various Ras mutant point to

Ras actively involved in the regulation of p110α-p85α in vivo. Data indicate that the interaction

of Ras with PI3K results in allosteric activation and induces PI3K recruitment to plasma

membrane (Hu, Klippel et al. 1995).

Downstream of PI3K

PI3K lipid products interact with proteins and modulate their localization and activity. One

major function for PI3Ks is in cytoskeleton reorganization through exchange factors that regulate

the small GTP-binding protein Rac, which modulates the affinity of integrins for the extracellular

matrix (Hawkins, Eguinoa et al. 1995). In addition, a number of protein Ser/Thr kinases have

been identified as downstream targets of PI3Ks (Andjelkovic, Jakubowicz et al. 1996;

Andjelkovic, Alessi et al. 1997). These include: Akt, p70 ribosomal S6 kinase (p70S6k

) (Chung,

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Grammer et al. 1994), and protein kinase C (PKC) (Le Good, Ziegler et al. 1998). Akt Ser/Thr

protein kinases are activated upon receptor-Tyr kinase stimulation. This activation process

involves phosphorylation and a PH-domain mediated lipid binding. PI3K induced Akt activation

plays a critical role in protection against cell apoptosis. Signalling proteins downstream of Akt

are glycogen synthase kinase-3 (GSK3) and mitogen-activated protein kinase (MAPK). P70S6k

is activated in response to mitogenic stimuli and plays an important role in the progression of

cells from the G1 to S phase of the cell cycle. Activation of p70S6k

is regulated by PI3K, mTOR,

and PKC-mediated Ser/Thr-directed phosphorylation (Chung, Grammer et al. 1994). Lipid

products of PI3K activate a broad panel of PKC family members and PKC-related kinases

(Toker and Cantley 1997). However, there is no consensus as to which member of the PKC

family is the selected target of these lipids.

1.3.4 PKC: role in bacterial infection

There are at least 15 PKC isoforms encoded by 9 genes, depending on classification criteria

(Ohno and Nishizuka 2002). Each PKC isoform is ubiquitously expressed in a single cell. The

isoforms are subdivided into three categories based on primary structure and biochemical

properties: classical or conventional PKC (cPKC) isoforms (PKCα, βI, βII, and γ); novel PKC

(nPKC) isoforms (PKCδ, ε, ε, and ζ); and atypical PKC (aPKC) isoforms (PKCη/ι, and δ)

(Larsson 2006) (Figure 1.4).

Classical PKC isoforms

The cPKCs share structural motifs C1 and C2. The C1 domains in cPKCs contain a cysteine-

rich repeat and constitute a binding site for diacylglycerol (DAG) and phorbol esters, such as

PMA. The C2 domains in cPKCs are calcium-dependent phospholipid binding domains. cPKC

isoforms can be activated by DAG and phorbol esters in the presence of Ca2+

(Shirai and Saito

2002).

Novel PKC isoforms

The nPKCs also contain C1 and C2 motifs. The nPKC-C1 domain works in a similar fashion as

cPKC-C1 domain binding to DAG and phorbol esters. However, the sequence C2 domain of

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nPKC isoforms is divergent from the cPKC-C2 domain. nPKC isoforms can be activated by

DAG or phorbol esters, but this activation is not dependent on Ca2+

(Schechtman and Mochly-

Rosen 2001).

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Figure 1.4 A: Schematic diagram of the structures of PKC isoforms. All isoforms consist

of a regulatory domain and a catalytic domain. The conserved region of the regulatory domain

in all three isotypes is the pseudosubstrate (PS). In both the classical and novel isoforms

regulatory domain contains the phorbol ester-binding region (C1a and C1b). Only the classical

isoforms regulatory domain has a calcium-binding region. All three isotypes contain a conserved

catalytic domain, which includes an ATP-binding site and a kinase domain. B: Summary of

activators of the various PKC isoforms.

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Atypical PKC isoforms

The aPKC isoforms share structural motifs C1 and octicosapeptide (OPR). The C1 sequence in

aPKC isoforms are not repeated like the C1 sequences in cPKC and nPKC isoforms. They also

lack the regions required for the interaction with DAG and phorbol esters; therefore, aPKC

isoforms cannot bind to nor are they activated by DAG and phorbol esters (Ohno and Nishizuka

2002).

Role of PKC in actin cytoskeleton regulation

The cell cytoskeleton is regulated by a number of components including phorbol esters, which

has for a long time been known to stimulate cellular migration and motility (Rigot, Lehmann et

al. 1998). This is associated with effects on the actin cytoskeleton. Since phorbol esters are

well-known activators of cPKC and nPKC isoforms, it is reasonable to consider that PKCs are

regulators of cellular cytoskeletal rearrangement processes (Larsson 2006).

PKCα has emerged as a general promoter of cell spreading and migration (Lin, Shen et al. 2010).

Both PKCα and PKCε associate with β1 integrin, which is important in mediating the binding of

the cell with the extracellular matrix (Thodeti, Albrechtsen et al. 2003). The PKCδ isoform is

involved in the RhoA pathway in the induction of stress fibers (Li, O'Connor et al. 2005). PKC

isoforms also phosphorylate N-WASP, which may be one mechanism of control of the F-actin

cytoskeleton (Leibfried, Fricke et al. 2008). PKCδ plays a role in protein phosphatase 2A

associated regulation of the epithelial tight junction complex, via Ca2+

-mediated tight junction

protein redistribution (Nunbhakdi-Craig, Machleidt et al. 2002).

Role of PKC in diarrheagenic E. coli pathogenesis

PKC is involved in pathogenic E. coli infection (Crane and Vezina 2005). EPEC infection of

T84 and HeLa cells increases membrane-bound PKC activity accompanied by a decrease in

cytosolic PKC activity. .PKCα increases its plasma membrane-association in response to EPEC

infection in vitro (Crane and Oh 1997). The atypical PKCδ isoform plays an important role in

the regulation of epithelial tight junctions (Tomson, Koutsouris et al. 2004). EPEC-activated

PKCδ also participates in the disruption of barrier function (Tomson, Koutsouris et al. 2004).

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EPEC activation of proximal signalling pathways, PKCδ and ERK, converges downstream to

stimulate pro-inflammatory responses, including NF-θB activation. The mechanism by which

EPEC activate PKC isoforms is still largely unknown; however, PKCδ is recruited to ceramide-

enriched microdomains where it is activated (Savkovic, Koutsouris et al. 2003). Since enteric

pathogens signal through lipid-ordered membrane signalling platforms (Bi and Altman 2001),

my hypothesis is that EHEC O157:H7 could activate host PKC pathways through lipid raft

microdomains.

Protein kinase C also plays an important role in vascular complications and tumorigenesis, which

involves the participation of osteopontin (OPN), a glycosylated phosphoprotein (Denhardt,

Giachelli et al. 2001). Specifically, OPN inhibits IL-1-stimulated increases in translocation of

PKC- from cytosol to membrane fraction, and increases in MMP-2 and MMP-9 activities (Xie,

Singh et al. 2003). Even the regulation of actin cytoskeleton requires both PKC and OPN (Kang,

Zhou et al. 2008; Falkenburger, Jensen et al. 2010). Thus, it is important to delineate the role of

OPN in EHEC pathogenesis.

1.4 In vivo model of lipid raft during bacteria infection

1.4.1 Niemann-Pick Type C Disease

Niemann-Pick type C disease is characterized by accumulation of unesterified cholesterol in

perinuclear vesicles (Vanier 2010). Cholesterol is a major factor in maintaining cell structure

and function (Lusa, Blom et al. 2001). It is an essential component of the cell membrane,

especially important in lipid organization. The various concentrations of cholesterol often times

regulate membrane fluidity; therefore, it is involved in cell structural integrity and functions in

various locations in the cell (Jaureguiberry, Tricerri et al. 2010). Cytoplasmic cholesterol is also

a source of bioactive molecule that forms steroid hormones, vitamin D, and bile acids (Schmidt,

Holmstrom et al. 2010) Therefore, cholesterol regulates diverse cellular metabolisms, cellular

homeostasis, and extracellular and intracellular molecular communication.

1.4.1.1 Clinical Presentation and Symptoms

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Niemann-Pick disease, type C (NPC) is a lysosomal lipid storage disease with autosomal

recessive inheritance. NPC is a subacute progressive neurodegenerative disorder where

cholesterol and sphingolipid accumulate in endosomes and lysosomes because of incorrect

cholesterol trafficking (Ikonen and Holtta-Vuori 2004). This defect is particularly pronounced in

the liver and spleen cells, but more detrimental in the brain (Sayre, Rimkunas et al. 2010).

Symptoms include progressive ataxia, dystonia, and dementia (Strauss, Goebel et al. 2010). This

lipid accumulation causes progressive neurodegeneration and hepatosplenomegaly, leading to

death during early childhood (Patterson, Vecchio et al. 2010). An animal model of Niemann-

Pick disease type C occurs in mice that harbour the NPC1 knockout (Davidson, Ali et al. 2009).

1.4.1.2 Pathophysiology

The majority (95%) of NPC disease stems from mutations of the NPC1 protein, and the

remainder due to NPC2 mutations (Ikonen and Holtta-Vuori 2004). NPC1 and NPC2 proteins

share no sequence similarity, but they both are involved in cholesterol homeostasis and likely

play a role in the same signalling pathway (Sleat, Wiseman et al. 2004). A defect of NPC1

protein has a striking impact on sterol homeostasis in all cells. Low density lipoprotein (LDL)-

derived and endogenously synthesized sterols are mislocalized (Abi-Mosleh, Infante et al. 2009).

The failure of cells to esterify exogenously added cholesterol as well as this accumulation of

unesterified cholesterol in endo/lysosomal compartment and the Golgi apparatus are all

manifestations of NPC (Walkley and Suzuki 2004).

Not only is free cholesterol accumulation a phenotype in NPC mutants, but several classes of

sphingolipids are also accumulated. In addition, it has been shown that gangliosides such as

GM1, GM2, and GM3 are transported by a NPC1-defined pathway in cellular models (Vanier

1999; Sugimoto, Ninomiya et al. 2001). NPC disease causes biochemical and physiological

disturbances including changes in cholesterol and sphingolipid/ganglioside accumulation,

membrane microdomains (lipid rafts) (Kosicek, Malnar et al. 2010), sphingomyelinase activity

(Devlin, Pipalia et al. 2010), caveolin and annexin II expression (Garver, Krishnan et al. 2002),

peroxisomal function, copper metabolism, apoptosis, and neurotrophin response (Sturley,

Patterson et al. 2004). However, which are primary defects that arise from loss of this gene and

which are secondary consequences? This question remains to be answered.

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Evolutionary Findings

Evolution provides important clues to understand the functional mechanism and pathophysiology

of NPC1. Different from NPC2, NPC1 shows high percentage conservation in yeast, worms,

insects, plants, and mammals (Higaki, Almanzar-Paramio et al. 2004). NPC1 is a eukaryotic

member of the resistance-nodulation-division (RND) family of prokaryotic permeases (Davies,

Chen et al. 2000). These proteins have been studied in numerous bacteria and use proton-motive

force to remove hydrophobic molecules from the cell. NPC1 expression in Escherichia coli

facilitates the transport of metabolites, such as acriflavine and oleic acid, across the bacterial

membrane (Passeggio and Liscum 2005). These data point to additional basic functions of the

protein that predates sterol transport; however, these functions remain to be elucidated in

humans.

Pathway that affects NPC1 phenotype

There has been a new insight identifying a link between NPC1 dysfunction and cholesterol

trafficking by manipulating small GTPases in the Rab gene family. Overexpression of a subset

of Rab proteins can affect NPC1 phenotype (Kaptzan, West et al. 2009). Overexpressing Rab7

and 9, which regulate vesicle trafficking between the cell surface and endosomal compartments

in the cell, results in complete reversal of cholesterol/sphingolipid accumulation (Narita,

Choudhury et al. 2005). Therefore, the NPC1 defect leading to accumulation of

cholesterol/sphingolipid in late endosomal compartments can be normalized by altering these

Rab regulated pathways.

Role of NPC1 in the intestine

Compared to wild type cells, in NPC1-/- cells cholesterol is more readily incorporated into

detergent-resistant membranes (DRMs) after hydrolysis from LDL-cholesterol ester (Ikonen and

Holtta-Vuori 2004). This indicates that cholesterol/sphingolipid accumulation results in excess

formation of rafts in late endosomal compartments, whereas they are depleted under normal

circumstances. There is also a recent identification of the mammalian NPC1 relative, NPC1-L1,

as an intestinal transporter of cholesterol (Altmann, Davis et al. 2004). This may hint towards a

function in microbial-host interactions in the gut.

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1.4.1.3 Model to study Detergent-Resistant Microdomains

(DRMs)

In normal mammalian cells, cholesterol associate with sphingolipids to form lateral domains –

lipid rafts. Rafts are present in cholesterol-sphingolipid-enriched membranes, such as the

membrane of early and recycling endosomes (van der Meer-Janssen, van Galen et al. 2010).

Since in NPC disorders, cholesterol and sphingolipids accumulate in lysosomes, this lysosomal

storage defect is a result of accumulation of rafts in late endosomes and lysosomes.

In addition, the transport of hydrolyzed LDL-derived cholesterol to the plasma membrane is

defective in cells that do not have a functional NPC1 protein (Lusa, Blom et al. 2001). This

reflects impaired membrane dynamics of the late endocytic organelles suggesting that in NPC1

deficient cells cholesterol-sphingolipid-containing rafts accumulate and form multilamellar

bodies, which leads to aberrant raft formation in lysosomes, preventing the formation of these

rafts in cell plasma membranes (Garver, Krishnan et al. 2002). NPC1-deficient mice are,

therefore, a suitable model for studying plasma membrane lipid raft disruption and its effects on

microbial-host interactions (Riff, Callahan et al. 2005).

1.5 Alternative preventative strategies

1.5.1 Probiotics

Probiotics are selective nonpathogenic live microorganisms that have beneficial effects on host

health, disease prevention, or disease treatment (Gareau, Sherman et al. 2010). Some of these

microorganisms include ones that are presently part of the gut microflora.

1.5.2 Probiotics in Disease Management

Results from the rising numbers of studies and clinical trials indicate potential applications of

probiotics for the prevention and/or treatment of many gastrointestinal disorders including: IBD,

antibiotic-associated diarrhea, IBS, neonatal necrotizing enterocolitis (NEC), enteropathy in HIV

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infection, gluten intolerance, gastroenteritis, H. pylori infection, and colon cancer (Michail

2009).

Management of IBD

The pathogenesis of IBD involves a primary or secondary alteration of the intestinal microbiota.

Therefore, much research has been pursuing clinical studies to manipulate the intestinal

microbiota via the use of probiotics. Many probiotics show potential for therapeutic usage in

ulcerative colitis patients via induction of remission, reduction of clinical DAI scores, and

preventing the onset of pouchitis. Selected probiotics (eg. VSL#3) mediate their beneficial

effects via increasing the number of mucosal regulatory T cells indicating a beneficial

immunoregulatory mechanism of action in patients with a surgically fashioned ileal pouch

(Pronio, Montesani et al. 2008).

However, the potential use of probiotics in Crohn’s disease as a prevention or treatment strategy

remains controversial. For example, in a meta-analysis of eight randomized placebo-controlled

clinical trials, the use of Lactobacillus johnsonii, LGG, E. coli Nissle 1917, or Saccbaromyces

boulardii did not show efficacy in maintaining remission. This may be due to the lack of

understanding of probiotics mechanism and the insufficient knowledge of the underlying

pathogenesis of Crohn’s disease.

1.5.3 Mechanism of Action

The recent biomedical literature now corroborates that probiotics can be used as a supportive

treatment for a wide spectrum of intestinal diseases (Sherman, Ossa et al. 2009). In IBD animal

models, a strain of Lactobacillus plantarum was able to stabilize the mucosal barrier in an

interleukin-10 gene knockout mouse model of colitis (Kennedy, Kirk et al. 2001; Schultz,

Veltkamp et al. 2002). Other bifidobacteria and lactobacilli decrease intestinal permeability,

enhance mucosal IgA responses (Chen, Louie et al. 2005), and increase the production of anti-

inflammatory cytokines (Lamine, Eutamene et al. 2004). The probiotic Escherichia coli, strain

Nissle 1917 (EcN) induces an overriding signalling effect leading to restoration of a disrupted

epithelial barrier via PKCδ signalling pathway and the redistribution of ZO-2 (Zyrek, Cichon et

al. 2007).

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Probiotics are also capable of increasing host innate and adaptive immune functions. For

instance, cell-free extracts from probiotics have also been reported to enhance the phagocytosis

of viable Salmonella (Higgins, Erf et al. 2007).

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Chapter 2.

Hypothesis and Objectives

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Enterohemorrhagic Escherichia coli O157:H7 maintain a type III secretion system (TTSS) that

functions in secreting virulence factors directly into the cytosolic space of host cells (Larzabal,

Mercado et al. 2010). Many of these virulence factors, either directly or indirectly, influence the

structure of actin filaments that maintain host cell morphology and promote binding of bacteria

to host cells. Specifically, EspA, B, D, and Tir regulate host actin morphology, allowing the

formation of actin-based pedestals that underlie bacterial attachment sites on the host plasma

membrane surface (Batchelor, Prasannan et al. 2000; Hamada, Hamaguchi et al. 2010).

Multiple host signalling pathways are hijacked by EHEC O157:H7 to induce these host

cytoskeleton changes. Some of the host proteins exploited by EHEC O157:H7 include: N-

WASP, Arp 2/3, Nck (Vingadassalom, Kazlauskas et al. 2009), PLC, PI3K (Johnson-Henry,

Wallace et al. 2001), and small GTPases (Bulgin, Raymond et al. 2010). Osteopontin (OPN) has

also been shown to mediate actin cytoskeleton rearrangement (Kang, Zhou et al. 2008), which

can also be manipulated by bacterial pathogens during the infection process. However, the

precise mechanisms how these signalling molecules are activated by the bacteria to induce its

pathogenic effects are still largely undefined .

Lipid rafts are prominent targets of bacterial pathogens. Several pathogens with functional TTSS

secrete effector proteins that are targeted to lipid rafts, and these pathogens adhere at GM1-

enriched lipid raft microdomains (French, Panina et al. 2009). Lipid rafts are important for

attachment of bacterial pathogens (Hayward, Hume et al. 2009), bacterial invasion (Lafont and

van der Goot 2005), activating bacterial TTSS (van der Goot, Tran van Nhieu et al. 2004), and

cell-surface binding by A-B toxins (ie. Shiga toxins) (Lencer and Saslowsky 2005). Disruption

of these host lipid rafts, with the use of agents like methyl-β-cyclodextrin (MCD), protects cells

from TTSS-induced cytotoxicity (French, Panina et al. 2009). Lipid raft disruption using MCD

also causes a decrease in adherence of bundle-forming pili (BFP)-deficient EPEC. Translocation

of the effector proteins is also blocked when lipid rafts are disrupted (Allen-Vercoe, Waddell et

al. 2006). Taken together, these findings indicate that lipid rafts play a role in the adherence and

virulence of pathogens.

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The goal of this thesis project was to identify host signaling proteins involved in the microbial-

host interaction. The overall hypothesis of this thesis project was that EHEC O157:H7 effectors

associate with lipid rafts and promote the translocation of host signal transduction proteins to

lipid rafts, which then leads to the formation of A/E lesions. . The overall objective of this PhD

thesis was to determine how E. coli O157:H7 utilize host signalling platforms during the

infectious process.

The specific aims of this thesis were to:

1. Investigate how osteopontin (OPN) is involved in EHEC-induced A/E lesion formation, and

determine its role in C. rodentium pathogenesis in a murine model of AE infection.

2. Determine the role of lipid rafts in the recruitment of host signal transduction proteins during

EHEC O157:H7 infection.

3. Identify the specific PKC isoform(s) recruited to lipid rafts in response to EHEC O157:H7

infection, and assess whether this recruitment process can be interrupted.

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Chapter 3.

Osteopontin Mediates Citrobacter rodentium-Induced Colonic Epithelial Cell Hyperplasia and Attaching-Effacing Lesions

*Eytan Wine, *Grace Shen-Tu, Melanie G. Gareau, Harvey A. Goldberg, Christoph Licht,

Bo-Yee Ngan, Esben S. Sorensen, James Greenaway, Jaro Sodek, Ron Zohar, and Philip M.

Sherman. Osteopontin Mediates Citrobacter rodentium-Induced Colonic Epithelial Cell

Hyperplasia and Attaching-Effacing Lesions. American Journal of Pathology (2010) 177(3), in

press (September).

* G.S-T. and E.W. contributed equally to this work.

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3.1 Abstract

Background: Although osteopontin (OPN) is upregulated in inflammatory bowel diseases

(IBD), its role in disease pathogenesis remains controversial. The objective of this study,

therefore, was to determine the role of OPN in host responses to a non-invasive bacterial

pathogen, Citrobacter rodentium, which serves as a murine infectious model of colitis.

Methods: OPN gene knockout and wild-type (WT) mice were infected orogastrically with either

C. rodentium or LB broth. Mouse-derived OPN+/+

and OPN-/-

fibroblasts were incubated with C.

rodentium and attaching-effacing lesions demonstrated using transmission electron microscopy

and immunofluorescence.

Results: Colonic expression of OPN was increased by C. rodentium infection of WT mice.

Furthermore, colonic epithelial cell hyperplasia, the hallmark of C. rodentium infection, was

reduced in OPN-/-

mice and spleen enlargement by infection was absent in OPN-/-

mice. Rectal

administration of OPN to OPN-/-

mice restored these effects. There was a 8-17-fold reduction in

bacterial colonization in OPN-/-

mice, compared to WT mice, which was accompanied by

reduced attaching-effacing lesions, both in infected OPN-/-

mice and OPN-/-

mouse fibroblasts.

Adhesion pedestals were restored in OPN-/-

cells complemented with human OPN.

Conclusions: Lack of OPN results in decreased pedestal formation, colonization, and colonic

epithelial cell hyperplasia responses to C. rodentium infection, indicating that OPN impacts on

disease pathogenesis through bacterial attachment and altered host immune responses.

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3.2 Introduction

Osteopontin (OPN) is a multifunctional glycophosphoprotein involved in a variety of cellular

functions, including stimulation of T helper(H)1 cytokines and adhesion through binding to

integrins and CD44 receptors on cell surfaces. This cytokine is highly expressed in chronic

inflammatory and autoimmune diseases,(Hashimoto, Sun et al. 2007) and is localized in and

around inflammatory cells.(Scatena, Liaw et al. 2007) OPN is believed to exacerbate

inflammation in a variety of settings, including infectious diseases.(Hashimoto, Sun et al. 2007)

It is involved in recruiting inflammatory cells to sites of injury, as indicated by a decrease in

macrophage infiltration in ischemic kidneys in OPN-deficient (OPN-/-

) mice.(Hashimoto, Sun et

al. 2007) OPN is also involved in controlling expression of inflammatory mediators, such as

down-regulation of the anti-inflammatory cytokine interleukin (IL)-10 and an increase in levels

of the TH1 cytokine interferon (IFN)γ.(Morimoto, Inobe et al. 2004)

Accumulating evidence indicates that defects in the dynamic balance between organisms in the

commensal intestinal microbiota and host innate defensive responses at the intestinal mucosal

surface results in the induction of inflammatory bowel diseases (IBD).(Neish 2009) An

association between luminal bacteria and IBD is further supported by animal models,(Xavier and

Podolsky 2007) including the use of Citrobacter rodentium infection. C. rodentium is the

causative agent of transmissible murine colonic epithelial cell hyperplasia that harbors a locus of

enterocyte effacement (LEE) pathogenicity island, similar to enterohemorrhagic Escherichia coli

(EHEC) O157:H7, and is capable of forming dense F-actin bacterial attachment pedestals,

known as attaching-effacing (A/E) lesions, in mouse colon.(Deng, Vallance et al. 2003) The

resulting TH1 response and accompanying pathological changes represent findings observed in

patients with IBD.(Eckmann 2006) As a result, C. rodentium serves as a relevant animal model

to study potential infectious mechanisms of IBD.(Borenshtein, McBee et al. 2008)

An association between OPN and IBD was recently assessed using dextran sodium sulphate

(DSS) to induce colitis in wild-type (WT) and OPN-/-

mice. However, the results arising were

contradictory. One study suggested that lack of OPN has a protective effect,(Zhong, Eckhardt et

al. 2006) whereas others reported a detrimental outcome during the acute phase(da Silva, Pollett

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et al. 2006; Heilmann, Hoffmann et al. 2008; da Silva, Ellen et al. 2009) and protection from

chronic exposure to DSS.(Heilmann, Hoffmann et al. 2008) This controversy prompted us to

study an association between OPN and gut inflammation, using C. rodentium as a model of

infectious colitis, to provide insight regarding the role of OPN in the pathogenesis of IBD.

Herein, we describe the attenuation of C. rodentium-induced colonic epithelial cell hyperplasia

and a reduction in bacterial colonization in OPN-/-

mice. In addition, we demonstrate dependence

of adhesion pedestal formation in response to C. rodentium on the presence of OPN. Taken

together, these findings contribute to an improved understanding of the role of OPN in response

to intestinal infection.

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3.3 Materials and Methods

Mice. OPN-/-

mice, kindly provided by Drs. Susan Rittling (Forsyth Institute, MA) and David

Denhardt (Rutgers University, NJ), back-crossed into a C57BL/6 background, were generated

and maintained, as described previously.(Rittling, Matsumoto et al. 1998) All OPN-/-

mice and

C57BL/6 control mice (6-8 weeks old) were maintained in a specific pathogen-free environment.

The mice were transferred to a containment facility at least 3 days prior to pathogen inoculation.

Animal care and interventions were approved by the Hospital for Sick Children Laboratory

Animal Services.

Bacterial infection of mice. C. rodentium, strain DBS100 (ATCC 51459, generously provided

by the late Dr. David Schauer, Massachusetts Institute of Technology, Cambridge, MA) was

stored in LB broth with 10% glycerol at -80C. Bacteria were grown from frozen stocks on LB

agar plates at 37C and then re-grown in LB broth overnight at 37C. The inoculum was

prepared to reach a final infection suspension containing 109 colony-forming units (CFU)/mL.

Mice were inoculated by orogastric gavage with 0.1 mL of the bacterial suspension. Sham

controls were challenged with an equal volume of sterile LB broth. In most cases, mice were

maintained until post-infection (PI) day 10. In some experiments animals were euthanized on PI

days 3, 6, and 15 for tissue analyses and to establish the time-course of OPN responses and

bacterial colonization to infection.

In a subset of experiments, OPN purified from bovine milk, was either added to the drinking

water, to reach a concentration of 20 κg/mL,(Schack, Lange et al. 2009) or inserted into the

rectum of WT and OPN-/-

mice without anesthesia once a day [2 κg in 100 κL phosphate

buffered saline (PBS)] through a flexible plastic cannula. In all cases, OPN supplementation was

started 24 h prior to infection and maintained throughout the 10 days of infection, until sacrifice.

PBS was rectally inserted to control mice (to control for potential confounding effects of daily

rectal insertion).

Large bowel histology and immunohistochemistry. Large bowel sections were fixed in 10%

buffered formalin and stained with hematoxylin and eosin. Intestinal inflammation was graded

on coded sections by a single pathologist (B-YN; Table 3.1). Mucosal thickness and epithelial

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cell hyperplasia were assessed using a Zeiss Axioplan microscope and digital photographs

(SenSys; Photometrics, Tucson, AZ). The average depth of 20 well-oriented colonic crypts

measured for each mouse (V for Windows; Digital Optics, Auckland, New Zealand).

For immunohistochemistry, formalin-fixed, paraffin-embedded tissues were mounted onto

positive-charged microscope slides and baked overnight at 60C. Rabbit anti-mouse polyclonal

cleaved caspase 3 antibody (Ab) (Cell Signaling Technology, Danvers, MA) and rabbit-

monoclonal Ab against Ki67 (Lab Vision, Fremont, CA) were used on an automated immune

stainer (Benchmark, Ventana Medical Systems, Tucson, AZ) at dilutions of 1:40 and 1:100,

respectively. Immunodetection was carried out using an LSAB system employing a 1:100

dilution of biotinylated anti-rabbit immunoglobulin (Ig)G (Vector Laboratories, Burlingame,

CA) with a commercial secondary detection system (Ventana iVIEW DAB). Tissue sections

were dewaxed, heat-induced epitope retrieved, peroxidase blocked, endogenous biotin blocked,

and counterstained with hematoxylin.

For OPN immunohistochemistry, colonic sections were de-paraffinized and heat-induced epitope

retrieval was performed with Tris-EDTA pH 9. Rabbit polyclonal anti-OPN Ab (reacts with

human and mouse OPN; dilution 1:750; Abcam Inc., Cambridge, MA) was incubated for 1 h,

followed by incubation with secondary Ab and treatment with HRP-conjugated streptavidin as

the labeling reagent. Color was developed with NovaRed solution and counterstained with

hematoxylin.

ELISA. Immediately after euthanization, blood samples were obtained by cardiac puncture.

Serum was collected upon centrifugation at 18,000g for 10 min. Distal colonic sections were

collected in 1 mL Complete protease inhibitor cocktail (Roche Diagnostics, Mannheim,

Germany) and then homogenized. Samples were stored at -80C until use. Osteopontin levels in

serum samples and colonic homogenates were assessed using a mouse osteopontin immunoassay

kit as per the manufacturer’s instructions (R&D Systems Inc., Minneapolis, MN).

Immunoblotting. Aliquots of colonic homogenates were analyzed for OPN and β-actin. Proteins

were separated by pre-casted 10% Tris-HCl (Bio-Rad, Hercules, CA) sodium dodecyl sulphate

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Table 3.1 Colonic Inflammation Histological Score*

Score

Criterion 0 1 2 3 4

Goblet cells — ↓ ↓↓ ↓↓↓ ↓↓↓

Mucosal thickening — ↑ ↑↑ ↑↑↑ ↑↑↑

Inflammatory cells — ↑ ↑↑ ↑↑↑ ↑↑↑

Submucosa cell infiltration — — ↑ ↑↑ ↑↑↑

Destruction of architecture — — — ↑ ↑↑

Ulcers (epithelial cell surface) 0% 0–25% 25%–50% 50%–75% 75%–100%

Crypt abscesses 0 1–3 4–6 7–9 >10

Eosinophil infiltration — ↑ ↑↑ ↑↑↑ ↑↑↑

*Scoring criteria modified from Van der Sluis, et al. 2006

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polyacrylamide gel electrophoresis (SDS-PAGE) with a protein ladder standard (Bio-Rad, broad

molecular range ladder). After electrophoresis, proteins were transferred onto nitrocellulose

membranes (Pall Corporation, Pensacola, FL) and incubated in Odyssey blocking buffer (LI-

COR Biosciences, Lincoln, NE) before probing with rabbit polyclonal anti-human OPN Ab (also

reacts with mouse OPN; Abcam; 1:1000) and primary mouse monoclonal IgG Ab against β-actin

(Sigma, Saint Louis, Missouri; 1:5000) overnight. After washing the membrane (PBS plus 0.1%

Tween), blots were incubated with Ab [IRDye 800 goat anti-rabbit IgG (Rockland

Immunochemicals, Gilbertsville, PA; 1:20,000) and Alexa Fluor 680 goat anti-mouse IgG

(Invitrogen, Carlsbad, CA)] and incubated for 1 h at room temperature on a shaker. The blots

were then washed and the membrane was scanned; bands were detected using the Odyssey

system (LI-COR Biosciences). The integrative intensities of the detected bands were obtained by

software (Odyssey Infrared Imaging

System, LI-COR Biosciences). Quantification of

osteopontin expression was obtained by normalizing the integrated intensity of the OPN band

with β-actin expression.

mRNA expression of OPN using qRT-PCR. Quantitative real-time PCR was used to quantify

expression of OPN in colons of WT animals infected with C. rodentium and sham controls.

Briefly, colonic tissues were snap-frozen in liquid nitrogen and stored at -80C until further use.

Total RNA was isolated by homogenization in TRIzol reagent (Invitrogen), phase separation

using chloroform extraction, and precipitation from the aqueous phase using isopropyl alcohol.

Washed RNA was re-dissolved in RNase-free water and stored at -80C. RNA was treated with

DNase1 (Invitrogen) according to the manufacturer’s instructions. cDNA was synthesized using

the iScript synthesis kit (Bio-Rad) and stored at -20C. PCR was performed using SYBR green

reagents (Bio-Rad) and validated primers for β-actin (Forward: 5’-

GGCTGTATTCCCCTCCATCG; Reverse: 5’-CCAGTTGGTAACAATGCCATGT) and for

OPN (Forward: 5’-AGCAAGAAACTCTTCCAAGCAA; Reverse: 5’-

GTGAGATTCGTCAGATTCATCCG; Invitrogen). Expression levels were normalized using β-

actin as the reference gene and expressed as ΔΔCT values.

Cytokine assay. Distal colons homogenates were used for mouse TH1/TH2/IL-17 cytokine

detection using MESO Scale Discovery cytokine assay kits (Gaithersburg, Maryland, USA).

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Samples were prepared according to manufacturer’s protocol and levels of IFNγ, IL-1β, IL-2, IL-

4, IL-5, IL-10, IL-12, IL-17, KC, and tumor necrosis factor (TNF)α were quantified using

electrochemiluminescence detection.

Weight, stool changes, and bacterial colonization. All mice were checked daily for the

development of signs of morbidity. A disease activity index (DAI) score (Table 3.2, modified

from(Van der Sluis, De Koning et al. 2006)) was obtained by documenting body weight, stool

color and consistency and general appearance every 3 days until euthanization by cervical

dislocation on PI day 10. Rectal swabs were collected on the same days and plated onto

MacConkey agar plates, and incubated aerobically overnight at 37C. C. rodentium colonies

were distinguished by their typical size and morphology.(LeBlanc, Yeretssian et al. 2008) C.

rodentium colonization was quantified on day 10 by homogenization of either fecal pellets or

distal colonic tissue in 1 mL PBS and plating of 10-fold serial dilutions onto MacConkey agar.

C. rodentium colonies were enumerated after overnight growth at 37C, and results expressed as

CFU/g feces or colonic tissue.

Detection of bacterial translocation. Blood samples were obtained by cardiac puncture, and the

spleen, liver, and mesentery (including lymph nodes) removed, weighed, and homogenized

(Pro200 homogenizer, PRO Scientific Inc., Oxford, CT). Under sterile conditions, aliquots (10

κL) of blood or organ homogenate were plated in 10-fold serial dilutions onto blood agar plates

and incubated aerobically for 24 h at 37C, after which the number of bacterial CFU was

calculated per mL of blood or per g of tissue.

Cells and bacterial infection. WT, OPN-/-

, and OPN-/-

mouse fibroblasts complemented with

human OPN(Zohar, Zhu et al. 2004) were employed as in vitro model systems and cultured in

DMEM with 10% fetal bovine serum, 100 κg/mL penicillin G, 50 κg/mL gentamicin, and 0.3

κg/mL fungizone (37C; 5% CO2). OPN-rescued cells were supplemented with Geneticin (all

reagents from Gibco Laboratories, Grand Island, NY). Cells were infected with either EHEC

O157:H7 (Hospital for Sick Children, Toronto, ON, Canada) or C. rodentium [multiplicity of

infection (MOI) 100:1; 37C; 5% CO2]. In some experiments bovine milk OPN (5

κg/mL)(Sorensen and Petersen 1993) or recombinant OPN(Hunter, Grohe et al. 2009) were

added to the medium 1 h prior to bacterial infection.

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Transmission electron microscopy (TEM). Mouse fibroblasts were grown on six-well plates

and infected with C. rodentium (MOI 100:1) for 4 h at 37°C. Cells or colonic tissue samples

were then washed and fixed in 4% paraformaldehyde + 1% glutaraldehyde in PBS, post-fixed in

1% osmium tetroxide, dehydrated in a graded series of acetone, and subsequently infiltrated and

embedded in Epon-Araldite epoxy resin. The processing steps from post fixation to

polymerization of resin blocks were carried out in a microwave oven (Pelco BioWave 34770,

Pelco International, Redding, CA), as recommended by the manufacturer. Ultrathin sections

were cut with a diamond knife (Reichert Ultracut E, Leica Inc, Wetzlar, Germany). Sections

were stained with uranyl acetate and lead citrate before being examined by TEM (JEM-1011,

JEOL USA Corp., Peabody, MA). Digital electron micrographs were acquired directly with a

1024 X 1024 pixels CCD camera system (AMT Corp., Denver, MA).

Immunofluorescence. Mouse fibroblasts were grown on glass 22X22 mm No.1.5 coverslips

(VWR LabShop, Vatabia, IL) in 6 well plates covered with 2 mL of antibiotic-free media. Cells

were infected with EHEC or C. rodentium at MOI of 100:1 for 4.5–6 hours. Slides were washed,

fixed (paraformaldehyde), permeabilized (Triton-X 100), blocked for 30 min with 0.1% BSA,

and incubated in FITC-conjugated polyclonal goat-anti-EHEC O175:H7 Ab (1:100; Fitzgerald,

Concord, MA) or rabbit-anti-C. rodentium Ab with Alexa Fluor 594 Phalloidin for 1 h. Goat

anti-rabbit Cy2 secondary Ab (1:100; 1 h; 20°C; Jackson Immunoresearch Inc., West Grove, PA)

was used to visualize C. rodentium. Slides were stained with DAPI for 5 min prior to 3 washes

with PBS and then mounted using SlowFade Antifade Kits (Molecular Probes, Eugene, OR) and

analyzed under alternating phase-contrast and fluorescence microscopy (Leitz Dialux 22; Leica

Canada, Inc., Toronto, ON, Canada).

Adhesion assay. Mouse fibroblasts were grown in antibiotic-free culture medium in 6 well

plates overnight. Cells were then infected with 108 bacteria (MOI 100:1) for 4.5 h in 5% CO2 at

37°C. After infection, non-adherent bacteria were removed by washing the monolayers three

times with PBS (pH 7.0). Triton X-100 (0.1%, diluted in PBS) was added to each well and left

on an orbital spinner for 15 min at room temperature. To quantify the number of bacteria

adherent to cells, Serial dilutions were performed on each sample by taking 10 κl from a series of

10-fold diluted samples plating onto blood agar plates and cultured overnight in 37°C. The

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Table 3.2 Modified Disease Activity Index Score*

Score Weight loss % Stool consistency Blood loss Appearance

0 None Normal Negative Normal

1 1-5% Loose Hunched

2 5-10% Diarrhea Gross Starey coat

3 10-15% Lethargic

4 >15%

*Scoring criteria modified from Van der Sluis, et al. 2006

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number of bacteria on each plate was then counted to calculate the original number of adherent

bacteria.

Statistics. Results are expressed as means±SEM. ANOVA and unpaired Student’s t test were

employed, as appropriate, with Tukey’s post-hoc test for normal distribution was ascertained,

and nonparametric Kruskal-Wallis test for non-normal distribution. Fisher’s exact test was used

for analysis of categorical data. Analyses were conducted using InStat3 (GraphPad, San Diego,

CA). P<0.05 was considered significant.

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3.4 Results

C. rodentium infection increases OPN expression in mouse colons.

WT C57BL/6 and OPN-/-

mice (N=31 & 28, respectively) were challenged orogastrically with C.

rodentium (108

CFU/0.1 mL), and 16-20 additional mice in each group were used as sham-

infected controls. Experiments were conducted on at least 4 separate occasions. To determine

whether OPN mediates epithelial responses to C. rodentium, the effect of bacterial infection on

OPN expression in the colon was assessed during the 10 day course of infection by

immunohistochemistry, protein ELISA and western blotting, and qPCR. As expected, colons

from OPN-/-

mice did not stain positive for OPN, whereas uninfected WT mice (sham) had low

basal levels of OPN, located mainly at the luminal surface (Figure 3.1A). Infection with C.

rodentium led to a time-dependent increase in OPN expression throughout the entire length of

the crypts that peaked at PI day 10, when inflammation is most prominent, and then decreased at

PI day 15 (Figure 3.1A). OPN protein levels in colons increased by ~3 fold during infection

(Figure 3.1, B and C) and a 10-fold increase in OPN mRNA expression in colonic homogenates

of infected WT mice after 10 days of infection (Figure 3.1D), as well as parallel increases in

OPN serum (Figure 3.1E) were also observed. These findings support the involvement of OPN

in epithelial cell responses to infection, as shown in inflamed colons of human subjects with

IBD.(Qu-Hong and Dvorak 1997; Sato, Nakai et al. 2005)

OPN is associated with inflammation and colonic epithelial cell hyperplasia in response to C.

rodentium infection.

Colonic epithelial cell hyperplasia, the hallmark of the host response to C. rodentium

infection,(Mundy, MacDonald et al. 2005) was demonstrated by a doubling in crypt length in 10

day-infected WT mice (290±6 vs. 144±4 µm in WT sham; Figure 3.2, A and B; p<0.001).

However, C. rodentium infection increased crypt length in OPN-/-

mice by only 21% (205±8 vs.

169±4 µm in sham-OPN-/-

mice; p<0.05), which was considerably shorter than in infected WT

mice (Figure 3.2, A and B; p<0.001). Similarly, there were significant differences in histology

scores, employed as a reproducible measure of mucosal injury, between WT and OPN-/-

infected

mouse colons (7.1±1.1 vs. 3.9±0.8, respectively; Figure 3.2, C and D; p<0.05). Cytokine levels,

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measured in mouse colon homogenates, showed increases in IFNγ, IL-1β, and TNFα levels with

infection of WT mice (p<0.05) but no increase in infected KO mice (p>0.05). IFNγ was higher in

infected WT mice than in infected OPN-/-

mice (Figure 3.2 E; p<0.05). There were no changes

in levels of IL-2, IL-4, IL-5, IL-10, IL-17, or CK in both groups (data not shown). The reduced

crypt epithelial cell hyperplasia in OPN-/-

mice in response to C. rodentium infection was due to

a reduction in cell proliferative responses and not an increase in apoptosis (Figure 3.2, F and

G).

C. rodentium colonization of mice is reduced in the absence of OPN.

OPN-/-

mice had significantly less C. rodentium CFU/g feces than infected WT mice

(1.2×106±3.4×10

5 vs. 2.1×10

7±5.6×10

6, respectively; Figure 3.3A; p<0.005) after 10 days of

infection, suggesting that OPN contributes to maintenance of C. rodentium colonization in the

colon. There was also a reduction in bacteria in colonic tissue homogenates of infected OPN-/-

mice (5.4×105±1.4×10

5), relative to infected WT mice (4.3×10

6±1×10

6 CFU/g colon; Figure

3.3B; p<0.005). A reduction in colonization of OPN-/-

mice, relative to WT mice, was also

observed on PI day 6 and bacterial clearance was apparent on PI day 15; findings which indicate

that reduced pathogen colonization was not due to changes in the time-course of infection in

OPN-/-

mice (Figure 3.3, C and D; p<0.01). These results suggest that OPN-/-

mice were

partially protected from C. rodentium infection due to a reduction in bacterial colonization in the

absence of OPN. Consistent with previous reports,(Mundy, MacDonald et al. 2005) bacterial

colonization of WT mice peaked at PI day 6 (Figure 3.3C).

Weight loss and disease activity in response to C. rodentium infection are not affected by OPN.

DAI (Table 3.2) scores for WT- and OPN-/-

-infected mice on days 4 and 10 were higher than in

sham mice (p<0.05; data not shown). Ten days after challenge, both sham groups gained

approximately 10% body weight, while weights of C. rodentium-infected WT and OPN-/-

mice

remained unchanged. However, there was no difference in DAI between WT and OPN-/-

mice

infected with C. rodentium. The lack of profound effect for OPN on systemic responses to

infection is likely due to relatively mild systemic disease in C57BL/6 mice infected with C.

rodentium, compared to other mouse strains.(Vallance, Deng et al. 2003; Borenshtein, Nambiar

et al. 2007)

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Figure 3.1 OPN expression is increased in response to C. rodentium infection. A: Colonic

immunohistochemistry showed that OPN was present at low levels in uninfected WT mice (top

left panel), mainly located in the cytoplasm of surface epithelial cells. A time-dependent increase

in OPN expression was observed throughout the crypts of C. rodentium-infected WT mice as the

infection progressed to 10 days, followed by a reduction in OPN by PI day 15. Scale bar: 100

m. B: ELISA of WT mouse colons demonstrated a 3-fold increase in OPN levels with infection

(N=4-8; t test: *p<0.005). C: Western blotting of colonic homogenates of WT mice showed a

similar increase in OPN protein level, normalized to β-actin, on PI day 6 (N=4-5; ANOVA:

*p<0.01) and on PI day 10 (t test: +p<0.05). D: Colonic mRNA levels of OPN, relative to β-

actin, showed increased OPN expression in infected colons on PI day 10 by qPCR (N=5-9;

ANOVA: *p<0.01). E: Serum OPN levels, as measured by ELISA, were increased on PI day 10

and normalized by PI day 15 (N=5-9; ANOVA: *p<0.05).

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Figure 3.2 Colonic epithelial cell hyperplasia and inflammation in response to C. rodentium

are associated with OPN. A: A decrease in the hyperplastic response after 10 days of C.

rodentium infection was observed in OPN-/-

infected mice (bottom right panel), relative to

infected WT mice (bottom left panel). Scale bar: 100 m. B: Quantification was performed by

measuring colonic crypt length in 20 well-oriented crypts per mouse (N=15-24; ANOVA:

*p<0.05; ** p<0.001). C: Overall histologic grading of colitis (PI day 10) indicated higher

scores in WT-infected relative to OPN-/-

-infected colons (t test: *p<0.05). D: Breakdown of the

histology score revealed increased severity in WT-infected mice (blue bars) relative to OPN-/-

-

infected mice (green bars) with respect to mucosal thickening and abscess formation (t test:

*p<0.05) but no significant change in goblet cell displacement and inflammatory cell infiltration,

which was mainly neutrophilic in nature (p=0.06 and 0.05, respectively). E: TNFα and IFNγ

were increased in colonic homogenates of infected WT mice (t test: *p<0.05) but not OPN-/-

mice. IFNγ was higher in infected WT mice than in OPN-/-

mice (t test: *p<0.05). F: Cleaved

caspase-3 staining demonstrates a small number of apoptotic epithelial cells in uninfected WT

and OPN-/-

mice (arrowheads in top left and right panels, respectively). Infection with C.

rodentium resulted in an increase in apoptosis in WT mice (arrowheads in bottom left panel), but

not in OPN-/-

mice (bottom right panel). G: In both uninfected WT and OPN-/-

mice (top panels)

Ki67 staining indicated that the proliferative zone was limited to the bottom third of colonic

crypts. Infection with C. rodentium caused an increase in proliferation, which extended to the

whole length of the crypt only in WT colons (bottom left panel), but not in OPN-/-

mice (bottom

right panel). Scale bar: 100 m.

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Figure 3.3 OPN mediates C. rodentium colonization. A and B: Colonization with C.

rodentium on PI day 10 was measured by homogenizing fecal pellets and colonic tissues and

then quantifying bacterial growth in serial dilutions. OPN-/-

mice infected with C. rodentium had

significantly less CFU/g feces (A) and colonic homogenates (B), compared with infected WT

mice (t test: *p<0.005). C and D: A time-course of infection, quantifying CFU in feces (C) and

colonic homogenates (D) of infected OPN-/-

mice relative to infected WT mice showed a similar

pattern of peak colonization on days 6&10 and a reduction in bacterial load on day 15 (*p<0.01).

In WT mice, fecal colonization was maximum at 6 days PI (ANOVA: p<0.001 PI day 6 relative

to all other time points; KO mice: p>0.05).

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Rectal OPN supplementation partially restores colonic epithelial cell hyperplasia in response

to C. rodentium infection in OPN-/-

mice.

To support our hypothesis that OPN is involved in colonic epithelial cell hyperplasia, bovine

milk OPN was administered daily by rectal insertion to OPN-/-

mice. OPN alone had no effect on

crypt length in sham-infected OPN-/-

mice (183±3 vs. 168±7 µm with rectal PBS). By contrast,

rectal OPN given daily to OPN-/-

mice 24h prior to, and throughout the 10 day C. rodentium

infection increased the colonic crypt length (256±12 versus 196±20 µm in infected OPN-/-

mice

that received PBS alone rectally; Figure 3.4A; p=0.01). Although rectal delivery of exogenous

OPN did not completely restore crypt length to levels observed in infected WT mice (Figure

3.2B), these results confirm a role for OPN in mediating epithelial cell responses to C. rodentium

infection. In contrast, oral administration of OPN to infected OPN-/-

mice(da Silva, Ellen et al.

2009) did not increase crypt length (data not shown), possibly due to intraluminal degradation of

exogenous protein.

Bacterial translocation in infected mice is dependent on OPN.

At PI day 10, there was a non-significant reduction in bacterial translocation to mesenteric

lymph nodes of infected OPN-/-

mice (18%), relative to WT-infected mice (44%; Fisher’s exact

test: p=0.09), while 50% of OPN-treated OPN-/-

mice had viable bacterial translocation to lymph

nodes (Figure 3.4B). Bacterial translocation to the liver was higher in WT-infected mice and

OPN-treated OPN-/-

mice than in OPN-/-

mice (p<0.0001 and p<0.01, respectively). Positive

spleen cultures were uncommon and bacteremia was found in 50% of OPN-treated mice, but

only 2 mice in each of the other infected groups (Figure 3.4B; p=0.05). It is possible that the

reduced bacterial translocation observed is a consequence of lower colonization seen in OPN-/-

mice. However, eventhough rectal OPN restored crypt hyperplasia responses to C. rodentium

infection, pathogen colonization was not increased in OPN-treated versus PBS-treated mice

(Figure 3.4, C and D; p>0.05).

Increases in spleen weight and splenocyte numbers in response to C. rodentium infection are

mediated by OPN.

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There was a 46% increase in the weight of spleens of infected WT mice on PI day 10 (133±11

versus 91±7 mg in uninfected-WT; p<0.005), likely due to accumulation of immune cells within

the spleen after infection.(Berntman, Rolf et al. 2005) This effect was absent in OPN-/-

mice

(93±7 vs. 82±6 mg in infected and uninfected mice, respectively; Figure 3.4E; N=11-28). Daily

rectal delivery of OPN to infected OPN-/-

mice restored spleen weights to levels similar to

infected WT mice (120±17 mg).

There was a parallel increase in the number of splenocytes in WT mice from 88±15×106 to

159±19×106

cells/spleen following C. rodentium infection (p<0.01). Such an increase was absent

in OPN-/-

mice (78±5×106 vs. 85±7×10

6 with infection; Figure 3.4F), whereas rectal treatment of

OPN to OPN-/-

mice increased the number of splenocytes to 122±19×106 (p<0.05). There was no

difference between uninfected WT and OPN-/-

mice in spleen weights or numbers of splenocytes.

These findings suggest that OPN mediates effects that lead to the accumulation of immune cells

in the spleen and subsequent splenic enlargement.

C. rodentium infection of mouse fibroblasts results in pedestal formation.

Intimate adherence of C. rodentium to WT mouse fibroblasts, but not cells from OPN-/-

mice,

was demonstrated by TEM, with the formation of dense F-actin attachment pedestals after 4 h of

infection (Figure 3.5A), which is a pathognomonic feature of bacterial-induced A/E

lesions.(Mundy, MacDonald et al. 2005) This is the first demonstration of C. rodentium-induced

adherence pedestals, compatible with A/E lesions, in mouse-derived cells.(Tobe and Sasakawa

2002)

OPN promotes C. rodentium and EHEC-induced pedestals.

C. rodentium-infected WT mouse fibroblasts exhibited adhesion pedestals, as demonstrated by

accumulation of dense F-actin-binding phalloidin at sites of bacterial attachment after 6 h of

infection. In contrast, pedestals were not observed in infected OPN-/-

cells, indicating that OPN

plays a role in bacterial-induced rearrangements of the host cell cytoskeleton. Furthermore, when

human-OPN knock-in mouse fibroblasts were infected with C. rodentium, F-actin pedestals were

observed (Figure 3.5B). Similar findings were also found after 4.5 h infection of the 3 cell types

with EHEC (Figure 3.5C). This observation indicates that OPN is involved in formation of

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Figure 3.4 Rectal OPN restores responses to C. rodentium infection in OPN-/-

mice. A:

Quantification of colonic crypt length of OPN-/-

mice receiving bovine milk OPN by daily rectal

administration indicated a partial recovery in the phenotype with longer colonic crypts (N=8-15;

ANOVA; *p=0.01; representative micrographs below chart). B: Eighteen percent of infected

OPN-/-

mice (white bars) had bacterial translocation to the MLN, relative to 44% of infected WT

mice (black bars; p=0.09); translocation was restored in OPN-/-

mice pre-treated with rectal OPN

(gray bars). Bacterial translocation to the liver was higher in WT and rectal OPN-treated mice

than in infected OPN-/-

mice (Fisher’s exact test: ***p<0.0001; **p<0.01), and bacteremia was

more common in mice treated with rectal OPN (*p<0.05). C and D: Fecal (C) and colonic (D)

evidence of C. rodentium colonization was not increased in OPN-/-

mice pretreated with rectal

OPN (p=0.09 and 0.5, respectively). E: An increase was observed in the weight of spleens from

C. rodentium-infected WT mice (white bars in panels E&F), relative to uninfected WT mice

(black bars; N=12&8; ANOVA: **p<0.001). While infection of OPN-/-

mice did not change the

size of the spleen, topical rectal OPN given to OPN-/-

mice infected with C. rodentium led to an

increase in spleen weights (gray bars; N=6; *p<0.05). F: The number of splenocytes in WT mice

doubled following C. rodentium infection (ANOVA: **p<0.01). There was no change in the

splenocyte counts in OPN-/-

mice in response to enteric infection, but the addition of daily rectal

OPN to OPN-/-

mice produced a response similar to levels seen in infected WT mice (*p<0.05).

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Figure 3.5 Formation of actin-dense attachment pedestals in mouse fibroblasts infected by

C. rodentium and EHEC O157:H7 is mediated by OPN. A: Transmission electron

photomicrographs of mouse fibroblasts infected for 4 h at 37ºC with C. rodentium demonstrate

adhesion pedestals. Scale bar: 500 nm. B: C. rodentium-infected (bacteria stained green) WT

mouse fibroblasts exhibited dense F-actin foci (stained with phalloidin, red), indicating

formation of adhesion pedestals (arrowheads in top panels and magnified inserts corresponding

with the outlined area). Pedestals were not present, however, in infected OPN-/-

cells (middle

panel and insert show adherent bacteria that are not accompanied by A/E lesions in the absence

of OPN). Furthermore, when human OPN knock-in mouse fibroblasts were infected with C.

rodentium, A/E-like lesions were again observed (bottom panel and inserts). C: EHEC-infected

cells were stained with FITC-conjugated anti-EHEC (green), phalloidin (red), and DAPI (blue).

Similar to C. rodentium, EHEC infection of WT fibroblasts induced adhesion pedestals

(arrowheads in top panels), which were absent in infected OPN-/-

cells (middle panels) and

restored in human-OPN complemented OPN-/-

fibroblasts (arrowheads in bottom panels).

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adhesion pedestals and that the role of OPN in response to C. rodentium infection can be

extended to another intestinal pathogen containing the LEE pathogenicity island, EHEC

O157:H7. There was also a 37% reduction in overall adhesion of C. rodentium to OPN-/-

cells in

vitro relative to WT fibroblasts (p<0.05).

OPN status had no discernible effect on overall cell structure in uninfected fibroblasts. When

OPN-/-

cells were pretreated with either bovine milk-derived OPN or recombinant OPN, added to

the medium, no pedestals were seen in response to EHEC infection (Figure 3.6). These findings

suggest that an intracellular form of OPN mediates formation of pedestals, since addition of

exogenous OPN to OPN-/-

cells did not recover the WT phenotype in vitro. However, rectal OPN

was able to recover the effect in OPN-/-

mice.

To determine whether OPN is also involved in the formation of adhesion pedestals in vivo,

colonic sections were examined 6 days after infection, at the time of maximum bacterial

colonization (Figure 3.3C and (Borenshtein, Nambiar et al. 2007)). While colons of WT mice

were carpeted by multiple intimately adherent bacteria (Figure 3.7A), bacteria were absent from

most colonic sections of OPN-/-

mice and present only in small numbers in other areas (Figure

3.7B). Rarely, larger numbers of bacteria were found, located mainly in areas of mucosal damage

and cell shedding (Figure 3.7B, right panel). Rectal administration of OPN restored A/E

lesions, as shown by TEM (Figure 3.7C). Taken together, these results show that the formation

of A/E lesions in response to bacterial infections is dependent on the presence of OPN.

Figure 3.6 Exogenous OPN does not restore adhesion pedestals in vitro. Presence or absence

of OPN had no effect on F-actin phalloidin staining (red) of uninfected fibroblasts (left panels).

Pretreatment of OPN-/-

cells with extracellular, bovine milk-derived (top panels) or recombinant

(bottom panels) OPN did not induce pedestals with infection, as demonstrated by multiple

adherent bacteria (blue- C. rodentium; green- EHEC) without phalloidin-positive adhesion

pedestals.

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Figure 3.7 Actin-dense pedestals are formed in C. rodentium-infected WT mice and

reduced in OPN-/-

mice. A: Multiple bacteria carpeted the surface of colons of WT mice with

A/E lesions after 6 days of infection with C. rodentium. B: In infected OPN-/-

mice, there were

no bacteria seen in most areas of the colon (left panel). In other areas, some adherent organisms

were seen (middle panel) while only in rare cases were multiple adherent bacteria observed in

infected OPN-/-

mice, especially on shedding epithelial cells (arrows in right panel). C: OPN-/-

mice treated with rectal OPN and infected with C. rodentium showed multiple A/E lesions.

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3.5 Discussion

Due to recent controversies regarding the role of OPN in murine models of IBD,(da Silva, Pollett

et al. 2006; Zhong, Eckhardt et al. 2006; Heilmann, Hoffmann et al. 2008; da Silva, Ellen et al.

2009) we evaluated the involvement of OPN in the development of intestinal changes in mice

challenged with the murine enteric pathogen, C. rodentium. In the absence of OPN, mice were

protected from bacterial colonization and the colonic epithelial hyperplastic cell response

induced by C. rodentium. This protection correlated with a reduction in F-actin condensation

directly below adherent C. rodentium in vitro and in vivo, indicating that the contribution of OPN

to mucosal responses to infection could be, either directly or indirectly, mediated through

bacterial attachment.

IBD, including Crohn disease and ulcerative colitis, are chronic debilitating intestinal disorders

characterized by mucosal inflammation.(Xavier and Podolsky 2007) Increased levels of OPN are

described in both the serum and intestinal mucosa of patients with IBD and correlate with

disease severity.(Masuda, Takahashi et al. 2003; Heilmann, Hoffmann et al. 2008) In these

patients, OPN is produced by gut epithelia, IgG-producing plasma cells, and

macrophages.(Gordon and MacDonald 2005; Agnholt, Kelsen et al. 2007) Increased OPN

expression in areas of active inflammation suggests that OPN is involved in stimulating cytokine

production that contributes to a TH1-predominant adaptive immune response, as is observed in

Crohn disease.(Sato, Nakai et al. 2005) Since OPN is also associated with a decrease in the

production of the anti-inflammatory cytokine IL-10 by T cells from patients with Crohn

disease,(Agnholt, Kelsen et al. 2007) OPN-mediated defects in immune-regulation may further

contribute to the development of inflammation.

Most models studying the involvement of OPN in inflammation support a pro-inflammatory role

for this key regulator, because disease is usually attenuated when OPN is absent. For example,

OPN is elevated in the synovium of patients with rheumatoid arthritis and over-expression of

OPN in synovial T cells amplifies inflammation.(Xu, Nie et al. 2005) OPN-/-

mice with

experimental autoimmune encephalomyelitis, as a TH1 model of multiple sclerosis, are protected

from disease,(Chabas, Baranzini et al. 2001) while administration of exogenous OPN causes

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relapse and paralysis.(Hur, Youssef et al. 2007) OPN is also involved in integrin adhesion,(Kon,

Ikesue et al. 2008) inflammatory cell chemotaxis(Zhu, Suzuki et al. 2004), and in enhanced

neutrophil function.(Koh, da Silva et al. 2007) Our findings support a role for OPN in mediating

immune responses to C. rodentium infection as demonstrated by a reduction in the increase of

IFNγ in OPN-/-

mice.

Recent attempts to define a role for OPN in intestinal inflammation, using a chemically-induced

model of colitis (DSS), have yielded conflicting results. While our group has shown that OPN-/-

mice are more susceptible to DSS colitis, through a reduction in TNFα and neutrophil

recruitment,(da Silva, Pollett et al. 2006; da Silva, Ellen et al. 2009) other investigators found an

opposite effect.(Zhong, Eckhardt et al. 2006) More recently, Heilmann et al.(Heilmann,

Hoffmann et al. 2008) found that OPN-/-

mice are more susceptible to acute challenge with DSS,

associated with reduced IL-22 and macrophage activity but increased serum TNFα, while

chronic DSS-induced colitis was reduced in these mice. This variability can be explained, at least

in part, by the use of different mouse strains, OPN gene modification strategies, varying DSS

doses, animal facility conditions, and treatment protocols. The reported discrepancies also

highlight the limitations of the DSS model of colitis in mice and its applicability to

IBD.(Kawada, Arihiro et al. 2007) DSS exerts cytotoxic effects leading to breakdown of the

mucosal barrier and exposure of the submucosal immune system to massive stimulation by

luminal bacteria.(Wirtz, Neufert et al. 2007) Resolution of inflammation in this model is mainly

dependent on an ability to repair the breach, which is initiated by inflammation.(Khalil, Weiler et

al. 2007) Since OPN is important in both neutrophil and fibroblast recruitment and in matrix

deposition, which are essential for effective tissue repair,(Sodek, Batista Da Silva et al. 2006) it

is not surprising that, in the absence of OPN, mice are more susceptible to acute DSS colitis.(da

Silva, Pollett et al. 2006; Heilmann, Hoffmann et al. 2008) Furthermore, as shown by increased

mortality from chemical-induced colitis of rats treated with anti-L-selectin antibodies, neutrophil

function has a protective effect in this setting.(Kuhl, Kakirman et al. 2007)

Increases in spleen weight and splenocyte numbers seen in infected WT mice likely represent

pooling of immune cells into the spleen in response to infection, as observed in mice infected

with Salmonella Typhimurium.(Berntman, Rolf et al. 2005) Contrary to hindlimb-unloading, a

chronic stress model where splenic atrophy is reduced in the absence of OPN,(Wang, Shi et al.

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2007) C. rodentium infection induced an increase in spleen mass and cellularity, which was

prevented in OPN-/-

mice. The opposite effects of OPN on the spleen in these two settings can be

explained by differences between the stress models. The former is a chronic immune suppression

model, as indicated by increased serum corticosterone levels in WT, but not OPN-/-

-stressed

mice,(Wang, Shi et al. 2007) whereas the latter is a model of an acute, immune-mediated

response to bacterial infection. In both cases, OPN serves as a central mediator of immune

function that contributes to disease phenotype.

Our results clearly demonstrate that OPN-/-

mice are protected from the effects of C. rodentium

infection, including colonic epithelial cell hyperplasia, histological changes, and bacterial

translocation. In addition, the absence of OPN impaired the ability of C. rodentium to colonize

the colons, which is likely why OPN-/-

mice are not as severely affected as WT-infected mice.

However, while exogenous intrarectal OPN was able to restore some features in OPN-/-

mice,

there was no detectible increase in colonization of these mice with C. rodentium. This

discrepancy could be explained by only partial recovery of the WT phenotype with OPN

administration to OPN-/-

mice (as shown for epithelial cell hyperplasia), a type II statistical error,

or limitations of culture-based bacterial recovery methods used in this study. Since epithelial cell

hyperplasia, pedestal formation, bacterial translocation to the liver, and splenic responses were

all increased with rectal OPN treatment, the findings support a role for OPN in mediating

responses to C. rodentium infection in this model.

OPN could either directly mediate bacterial attachment to host cells, as recently shown for

Gram-positive bacteria,(Schack, Stapulionis et al. 2009) or modify host responses to bacteria.

Alternatively, since adhesion and A/E lesion formation involve multiple complex host and

microbial factors, it is possible that other mediators downstream to OPN could also explain these

findings. For example, reduced inflammation in the absence of OPN could lead to a decrease in

the abundance of epithelial attachment sites that are required for initial bacterial

adhesion.(Higgins, Frankel et al. 1999) Since the highest increase in OPN was observed on PI

day 10, it is more likely that OPN mediates signaling events related to A/E lesion formation and

epithelial cell hyperplasia rather than being directly involved in bacterial attachment, which is

observed earlier in the course of infection, around PI day 6.(Mundy, MacDonald et al. 2005)

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Although C. rodentium is widely used to study enteric bacterial infections and intestinal

inflammatory models,(Eckmann 2006; Frankel and Phillips 2008) adhesion pedestals have not

been demonstrated in mouse cells in vitro(Tobe and Sasakawa 2002) or in human intestinal cells,

unless C. rodentium is genetically modified to express a human enteropathogen-derived bacterial

adhesion.(Tobe and Sasakawa 2002) To our knowledge, the intimately adherent bacteria C.

rodentium and the accompanying F-actin-dense pedestals demonstrated in our study using

immortalized mouse fibroblasts, are the first to show the formation of pedestals compatible with

A/E lesions in response to C. rodentium infection in mouse cells. Furthermore, we found that the

formation of bacterial-induced changes in the host cytoskeleton were absent in cells lacking

OPN, and were restored by reintroducing human OPN into the cells, but not by pre-treating cells

with extracellular OPN. These findings indicate that OPN plays an important role in bacterial-

induced attachment pedestal formation and suggest that an intracellular form of OPN mediates

this effect since adding OPN to the medium was not sufficient to restore pedestals. In contrast,

addition of topical OPN through rectal administration in OPN-/-

mice did restore effects of C.

rodentium infection, possibly because OPN may be differentially processed and internalized in

the in vivo setting. The ability of exogenous OPN to be absorbed and attenuate DSS-induced

colitis(da Silva, Ellen et al. 2009) supports a potential use for this compound in future research.

C. rodentium attachment to cells involves either LEE-dependent (involved in A/E lesion

formation) or LEE-independent mechanisms. Since OPN was involved in pedestal formation,

this likely provides the mechanism for reduced pathogen colonization and less severe colonic

involvement in OPN-/-

mice. A specific reduction in the formation of adhesion pedestals and in

overall adhesion in vitro supports a role for actin rearrangements in anchoring bacteria and

stabilizing colonization, as demonstrated by the failure of espFu-/-

EHEC to persist colonization

in rabbits due to reduction in A/E lesions.(Ritchie, Brady et al. 2008) Furthermore, the OPN

receptor CD44 is recruited to pedestals upon EHEC infection, although, in contrast to OPN, A/E

lesions are still formed in the absence of this host protein.(Goosney, DeVinney et al. 2001) These

findings suggest that CD44 is not functional in the formation of pedestals, whereas our results

indicate that OPN is. Further in vivo evidence supporting a role for OPN in the formation of

adherence pedestals is provided by a reduction in A/E lesions in OPN-/-

mice on PI day 6, which

is likely the cause of the reduced colonization. Alternatively, it is also possible that OPN has a

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more profound effect on the composition of the intestinal microbiota, although this was not

directly addressed in this paper. This possibility is supported by the recent description of reduced

C. rodentium colonization and reduced epithelial cell hyperplasia when mice are colonized with

a single commensal microbe.(Ivanov, Atarashi et al. 2009)

Defects in migration of cells in the absence of OPN, such as shown for neutrophil

recruitment(Koh, da Silva et al. 2007) and macrophage chemotaxis,(Zhu, Suzuki et al. 2004) are

mediated by impaired cytoskeletal responses, likely due to a reduction in association with the

CD44 receptor.(Sodek, Batista Da Silva et al. 2006; Collins, Ho et al. 2008) Furthermore, while

unchallenged OPN-null fibroblasts exhibit a normal cytoskeleton, stressed cells show defects in

rearrangements of the actin cytoskeleton and in the ability to form stress fibers and focal

adhesions.(Lenga, Koh et al. 2008) Similarly, our findings suggest a role for OPN in modulating

host responses to intestinal bacteria in infected epithelial cells, which then specifically impacts

on the development of mucosal injury and responses to enteric pathogens.

Taken together, these findings indicate that OPN is required and sufficient for the formation of

pedestals in response to bacterial infection, explaining why OPN-/-

mice are protected from the

colonic changes typically seen in response to this non-invasive, enteric bacterial infection. This

provides a rationale for future studies on the role of OPN in mediating bacterial attachment to gut

epithelia in humans with IBD.

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3.6 Acknowledgements

The authors thank Lei Liu, University of Alberta, for technical assistance; Michael Ho and Yew

Meng Heng, Department of Pediatric Laboratory Medicine, Hospital for Sick Children for their

expertise in microscopy techniques; and Kelvin So, Toronto General Hospital, for

immunostaining. OPN-/-

mice were originally provided by Drs. Susan R. Rittling, Forsyth

Institute, Boston, MA and David T. Denhardt, Rutgers University, Piscataway, NJ. This work

was supported by an operating grant from the Canadian Institutes of Health Research (CIHR;

PMS) and operating grants from Dairy Farmers of Canada and CIHR (HAG, JS, RZ) and the

Danish Dairy Research Foundation (ESS). EW was supported by a fellowship award from the

Canadian Association of Gastroenterology/CIHR/Astra Zeneca partnership. GS is the recipient

of a CIHR Canada Graduate Scholarship Doctoral Research Award. PMS is the recipient of a

Canada Research Chair in Gastrointestinal Disease.

E.W. and G.S-T. contributed equally to this work.

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Chapter 4.

Detergent-Resistant Microdomains Mediate Activation of Host Cell Signalling in Response to Attaching-Effacing Bacteria

Grace Shen-Tu, David B. Schauer, Nicola L. Jones, and Philip M. Sherman. Detergent-

resistant microdomains mediate activation of host cell signaling in response to attaching-

effacing bacteria. Laboratory Investigation (2010) 90, 266-281.

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4.1 Abstract

Background: Enterohemorrhagic Escherichia coli (EHEC) O157:H7 causes outbreaks of bloody

diarrhea and the hemolytic-uremic syndrome. EHEC intimately adheres to epithelial cells,

effaces microvilli and induces attaching-effacing (AE) lesions. Detergent-resistant

microdomains (lipid rafts) serve as membrane platforms for recruitment of signaling complexes

to mediate host responses to infection.

Objective: The aim of this study was to define the role of lipid rafts in activating signal

transduction pathways in response to AE bacterial pathogens.

Methods: Epithelial cell monolayers were infected with EHEC (MOI 100:1, 3h, 37oC) and lipid

rafts isolated by buoyant density ultracentrifugation. Phosphoinositide 3-kinase (PI3K)

localization to lipid rafts was confirmed using PI3K and anti-caveolin-1 antibodies. Mice with

cholesterol storage disease Niemann-Pick, type C were used as an in vivo model to confirm the

role of lipid rafts in mediating signaling response to AE organisms.

Results: In contrast to uninfected cells, PI3K was recruited to lipid rafts in response to EHEC

infection. Metabolically active bacteria and cells with intact cholesterol-rich microdomains were

necessary for the recruitment of second messengers to lipid rafts. Recruitment of PI3K to lipid

rafts was independent of the intimin (eaeA) gene, type III secretion system and production of

Shiga-like toxins. Colonization of NPC-/-

colonic mucosa by C. rodentium and AE lesion

formation were both delayed, compared with wild-type mice infected with the murine-specific

AE bacterial pathogen. C. rodentium-infected NPC-/-

mice had reduced colonic epithelial

hyperplasia (64κm ± 8.251 vs. 112κm ± 2.958; p<0.05) and decreased secretion of IFN-γ (17.6

pg/mL ± 17.6 vs. 71pg/mL ± 26.3 , p<0.001).

Conclusions: Lipid rafts mediate host cell signal transduction responses to AE bacterial

infections both in vitro and in vivo. These findings advance current understanding of microbial-

eukaryotic cell interactions in response to enteric pathogens that hijack signaling responses

mediated through lipid rafts.

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4.2 Introduction

Escherichia coli is a facultative gram-negative bacterium normally present in the commensal

colonic microflora. However, some E. coli strains possess specific virulence factors enabling

them to cause disease in mammalian hosts (Kaper, Nataro et al. 2004). Enterohemorrhagic

Escherichia coli (EHEC) O157:H7 is responsible for outbreaks of diarrhea, hemorrhagic colitis

and the hemolytic-uremic syndrome (HUS), which is the most common cause of acute renal

failure in children (Jandu, Shen et al. 2007). For instance, an E. coli O157:H7 outbreak in North

America was reported in the fall of 2006 initiated from the ingestion of contaminated, pre-

packaged spinach (Cooley, Carychao et al. 2007).

Several virulence factors are thought to mediate disease pathogenesis. EHEC produces a potent

cytotoxin known as Vero (Shiga-like) toxin (Rendon, Saldana et al. 2007). Verotoxin is an AB5

subunit toxin which binds to globotriaosylceramide (Gb3) localized in membrane lipid rafts of

host cells (Nutikka and Lingwood 2004), inactivates 28S ribosomal RNA to disrupt protein

synthesis and promotes apoptosis, leading to epithelial cell death (Gobert, Vareille et al. 2007).

EHEC O157:H7 infection is also characterized by intimate bacterial attachment to epithelial cells

mediated through a variety of adherence factors (Gyles 2007). E. coli secreted proteins, encoded

on a 35-kilobase pathogenicity island referred to as the locus of enterocyte effacement (LEE), are

injected into the cytosol of infected cells through a type III secretion system encoded molecular

syringe (Welinder-Olsson and Kaijser 2005). The translocating intimin receptor (Tir), also

known as EspE, acts as a receptor for the eae gene-encoded bacterial outer membrane protein,

intimin (Campellone, Robbins et al. 2004). Tir-intimin interactions give rise to intimate

attachment of EHEC O157:H7 to eukaryotic cells and the recruitment of host actin cytoskeleton

elements, which form dense adhesion pedestals and the effacement of intestinal brush-border

microvilli, collectively known as the attaching-effacing (AE) lesion (Kaper, Nataro et al. 2004).

Citrobacter rodentium is a naturally occuring mouse-specific non-invasive bacterial pathogen

that is genetically related to EHEC, because it also uses attaching-effacing lesion formation as a

mechanism of infection and colonization of the colon. Genes encoding the ability for both C.

rodentium and EHEC to induce A/E lesions are located on the LEE pathogenicity island. C.

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rodentium infection of mice causes colonic epithelial hyperplasia that resolves spontaneously by

post-infection day 28 (Mundy, MacDonald et al. 2005).

The effector protein Tir is inserted into cholesterol- and sphingolipid-enriched microdomains in

the eukaryotic cell plasma membrane bilayer, referred to as lipid rafts (Zobiack, Rescher et al.

2002; Allen-Vercoe, Waddell et al. 2006). Cholesterol is an important component of eukaryotic

cellular membranes, which is known to dynamically associate with sphingolipids to form

heterogeneous microdomains (lipid rafts) (Simons and Toomre 2000). These cholesterol-

enriched microdomains serve as platforms for the recruitment of cell signaling complexes to a

micro-environment where they are sheltered from non-raft enzymes that can interfere with

signaling processes (Brown and London 1998; Simons and Toomre 2000). Lipid rafts contribute

to a variety of functions in eukaryotic cells, including cell signaling, trafficking and protein

sorting (Fielding and Fielding 2004; Laude and Prior 2004).

The aim of the present study was to determine if AE bacterial infections promote the recruitment

of phosphoinositide 3-kinase to lipid rafts and determine the role of these microdomains in

disease pathogenesis.

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4.3 Materials and Methods

Tissue culture cell lines. HEp-2 human laryngeal epithelial cell line (CCL23; American Type

Culture Collection, Manassas, VA) and Intestine 407 embryonic intestinal cells (CCL-6; ATCC)

were employed as model systems in vitro. HEp-2 cells were cultured at 37oC in 5% CO2 in

minimal essential medium (MEM) supplemented with 10% fetal bovine serum, 1% sodium

bicarbonate, 1% Fungizone, and 1% penicillin-streptomycin. Intestine 407 cells were cultured in

MEM supplemented with 10% fetal bovine serum and 2% penicillin-streptomycin (all media and

supplemental reagents from Life Technologies, Grand Island, NY).

Bacterial strains and growth conditions. Bacterial strains employed in this study are shown in

Table 4.1. Enterohemorrhagic Escherichia coli O157:H7, strain CL56 and E. coli, strain CL15

(O113:H21) were stored in -80°C and re-grown on 5% sheep blood agar plates at 4oC. Colonies

were transferred from plates into Penassay broth and incubated at 37oC for 18 h and then 3 h re-

growth in antibiotic-free tissue culture medium at 37oC for mid-log phase. Heat-killed bacteria

were prepared by boiling mid-log phase bacteria at 100oC for 30 min. Formalin-fixed bacteria

were washed with PBS and treated with formaldehyde (12%) for 6 to 18 h at 4oC.

Prior to infection of tissue culture cells, bacteria were washed with PBS and resuspended in

antibiotic-free MEM medium. For chloramphenicol treatment, mid-log phase bacteria were

pelleted and resuspended in chloramphenicol (100ug/mL) for 6 to 18 h at 4oC (Ceponis, McKay

et al. 2003). Bacteria were added to epithelial cells grown in 10cm diameter tissue culture dishes

(Starstedt Inc., Montreal, Quebec, Canada), at a multiplicity of infection of 100 bacteria to 1

eukaryotic cell, for 1h at 37oC in antibiotic-free MEM. Uninfected cells were used as a negative

control. After 0.5, 1 and 3.5 h of infection, cells were washed with phosphate-buffered saline

(PBS) (pH7.0) to remove non-adherent bacteria.

Cultured supernatant and conditioned medium preparation. To collect bacterial culture

supernatants, 10mL of EHEC O157:H7 grown in Penassay broth was centrifuged at 3,000 rpm

for 15min and supernatant filtered, using a 0.45 κm filter, into a new tube for storage at -20 until

use. To collect conditioned medium, EHEC O157:H7 strain CL-56 grown overnight in 10mL

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Table 4.1 Baterial strains and treatments used in the in vitro studies

E. coli strains Treatment Description

EHEC O157:H7

boil at 100oC for 30 min non-viable bacteria with disrupted structure

chlorophenicol stop the bacterial protein synthesis

formaldehyde kill the bacteria but keeping the structure intact

CL15 (O113:H21) -- without the LEE pathogenicity island

86-24 -- Wildtype EHEC

CVD451 -- Type III secretion-deficient mutant of parental strain 86-24

85-289 -- Wildtype EHEC

85-170 -- Stx1 and Stx2 negative mutant of parental strain 85-289

The various strains of E. coli and related mutants were grown overnight on sheep blood agar

from frozen stocks in 37°C and subsequently grown in Penassay broth overnight. The overnight

growth in broth was used to infect model cell lines to delineate microbial-host cell interaction

through signaling cross-talk.

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Penassay broth (37°C) was used to infect monolayers of HEp-2 cells (MOI 100:1). After 1 hr,

medium was centrifuged (3,000 rpm, 15 min), 30mL of conditioned medium was pooled together

and concentrated using a 3 kilodalton Amicon Ultrafilter (Millipore). Unfiltered conditioned

medium was collected using centrifugation and 100κg/ml of chloramphenicol was added to halt

bacterial protein synthesis.

Citrobacter rodentium, strain DBS100 (ATCC 51459) was stored in Luria Bertani (LB) broth

with 50% glycerol at –80oC. Bacteria were grown from frozen stocks on LB agar plates at 37

oC

and stored at 4oC for no more than 2 wks. Bacteria were inoculated into 10 ml LB broth and

grown at 37oC overnight. Prior to infection of mice, overnight cultures were centrifuged at 3,000

rpm for 10 min. and resuspended in 2.5 ml of LB broth to obtain a concentration of 1010

bacteria/ml.

Whole-cell protein extraction. HEp-2 cells were infected either with Escherichia coli O157H7

or C. rodentium for 1, 3, and 6 hr. Cells were washed three times with ice-cold phosphate-

buffered saline (PBS, pH 7.0) and whole-cell protein extracts collected

for storage at –80°C, as

previously described (Jandu, Ceponis et al. 2006).

Depletion of cholesterol using methyl-β-cyclodextrin (MβCD). HEp-2 cells were treated with

MβCD (Sigma Chemical Co., St. Louis, MO) (1-10mM) to disrupt cholesterol-enriched

microdomains by chelating plasma membrane cholesterol (Kilsdonk, Yancey et al. 1995). Prior

to bacterial infection, epithelial cells were incubated with MβCD (10mM) in antibiotic-free

MEM for 1 h at 37oC. The medium was aspirated off cell monolayers and washed with PBS

prior to bacterial infection (Riff, Callahan et al. 2005).

Treatment with pharmacological inhibitors. Tissue culture cells were pre-incubated with

either the phosphoinositide-3 kinase inhibitor LY294002 (100κM, Sigma Chemical Co., St.

Louis, MO) or an equal concentration of the inactive analogue LY303511 for 1 h at 37oC

(Johnson-Henry, Wallace et al. 2001). After removal of the inhibitor, cells were rinsed with PBS

and infected with bacteria for 1 h at 37oC.

Isolation of detergent-resistant membranes. Infected epithelial cells were scraped and

pelleted in 4 ml of sterile PBS in 15 ml conical tubes. Cells were then lysed with 0.8mL TN

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buffer (25 mM tris-HCl pH 7.5, 150 mM NaCl, 1 mM DTT, 10% sucrose, 1% Triton X-100,

leupeptin, 2 κg/ml pepstatin A, 10 κg/ml aprotonin, 0.5 mM PMSF, 1 mM Na3VO4) for 30 min

on ice. The samples were then mixed with 1.7 ml of OptiprepTM

(Axis-Shield PoC AS, Oslo,

Norway) and transferred into SW41 centrifuge tubes (Beckman Instruments, Inc., Palo Alto,

CA). OptiprepTM

(60%) was diluted with TN buffer to produce 35% and 5% solutions (adapted

from: (Schraw, Li et al. 2002) and (Song, Li et al. 1996)), which were then layered on top of

samples and centrifuged at 160,000 x g for 20 h at 4oC. Eight 1.5 ml fractions were then

collected from the top to bottom of the gradient generated by ultracentrifugation (Macdonald and

Pike 2005).

Immunoblotting. Aliquots (10κl) of each fraction were analyzed for PI3K and caveolin-1.

Proteins were separated by pre-cast 10% Tris-HCl (Biorad) sodium dodecyl sulphate

polyacrylamide gel electrophoresis (SDS-PAGE) with a protein ladder standard (BioRad, broad

molecular range ladder) at 120V for 1 to 1.25h at room temperature. After electrophoresis,

proteins were transferred onto nitrocellulose membranes (Pall Corporation, Pensacola, FL) at

100V for 1.5 h at 4oC and incubated in Odyssey blocking buffer (LI-COR

Biosciences, Lincoln,

NE) for 0.5 to 1h at 20°C. Blocking buffer was then decanted off and membranes probed with

anti-caveolin-1, as a lipid raft marker protein (Santa Cruz Biotechnology Inc., CA; 1:1000), and

primary antibodies against PI3-kinase p85 (Upstate Biotechnology, Lake Placid, NY; 1:1000)

overnight at 4oC on a shaker. Whole cell extracts were probed with native- and phospho-Akt

antibody (Cell Signaling, Beverly, MA; 1:1,000 dilution). After washing the membrane four

times with PBS plus 0.1% Tween (5 min. per wash), IRDye 800 goat anti-rabbit immunoglobulin

G (IgG) secondary antibody (Rockland Immunochemicals, Gilbertsville, PA; 1:20,000) was

added and incubated for 1 h at room temperature on a shaker. The blots were then washed 4

times with PBS plus 0.1% Tween and once with PBS alone. The membrane was then scanned

using the Odyssey system (LI-COR Biosciences) with the 800nm channel. The integrative

intensity of the detected bands was obtained using software provided with the infrared imaging

system (LI-COR Biosciences). Western analysis was performed on collected whole cell lysates

probed with both Akt (Cell Signaling Inc. Denvor, MA; 1:1000 dilution).

Immunostaining. HEp-2 cells were grown to subconfluency and treated with MβCD (10mM ,

Sigma Chemical Co., St. Louis, MO) for 1 hr at 37°C. To add cholesterol back into cholesterol-

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depleted cells, 200 κg/mL of soluble cholesterol (Sigma) in antibiotic-free medium was added to

cells for 45 min at 37°C. Post depletion-repletion of cholesterol, cells were washed with PBS,

fixed in 3.7% paraformaldehyde and permeabilized with 0.1% Triton X-100. Lipid rafts were

visualized using Alexa Fluor 594 labeled cholera toxin subunit B (Invitrogen Co., Carlsbad, CA)

(Hatano, Kubo et al. 2007).

Animals. BALB/c mice (n=5 for 6 days uninfected and C. rodentium-infected; n=5 for 12 days

uninfected and C. rodentium-infected) and homozygous BALB/cNctr-npc1m1N/m1N

(Npc1-/-

) mice

(n=4 for 6 days uninfected and C. rodentium-infected; n=4 for 12 days uninfected and C.

rodentium-infected) with Niemann-Pick type C disease were obtained from Jackson Laboratory

(Bar Harbor, ME) at 4-5 weeks of age, before the onset of a progressive neurologic disorder

(Dennis, Kudo et al. 2008). Animals were housed in microisolate cages in a containment unit

and allowed free access to water and chow. All animal experiments were performed following

review and approval by Laboratory Animal Services, Hospital for Sick Children, Toronto,

Canada.

Infection of mice with C. rodentium. Mice were inoculated orogastrically with either 109 C.

rodentium, in 100 l LB broth, or sham infected with an equal volume of LB broth alone and

then followed for 6 to 12 days (Mundy, MacDonald et al. 2005). Mice were monitored for

bacterial shedding using rectal swabs streaked onto MacConkey lactose agar plates (Johnson-

Henry, Nadjafi et al. 2005).

Tissue Collection. At necropsy, spleens and colonic sections were harvested for further

experimental analyses. Spleens were placed into 4 ml of RPMI tissue culture medium and kept

on ice. Segments (~ 5 mm in length) of distal colon were place into Universal fixative (4%

paraformaldehyde, 1% glutaraldehyde in 0.1 M phosphate buffer) for further processing for

electron microscopy (Mogilner, Srugo et al. 2007). Segments from the remainder of the distal

colon were placed in 10% neutral-buffered formalin and processed for histological assessment.

In some experimental groups, mice were injected intraperitoneally with a 10 mg/ml 5-bromo- 2’-

deoxyuridine (BrdU; Sigma) solution in PBS at a concentration of 5 l/g 1 hour prior to

sacrifice. Mice injected with BrdU were not used to prepare splenocytes.

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Histology and Immunohistochemistry. Formalin-fixed tissues were embedded in paraffin,

sectioned at 5-7 microns, and mounted onto positively charged microscope slides for further

processing. For histology, slides were rinsed in distilled water and stained with Mayer’s

hematoxylin for 15 min. Excess stain was removed by rinsing in water and sections fixed by

rinsing 5 times in ammonial water. Slides were then rinsed in 95% ethanol and counter-stained

in eosin for 3 min.

To detect C. rodentium bound to intestinal mucosal surfaces using immunohistochemistry,

mounted tissue sections were baked overnight at 60oC, dewaxed in xylene and hydrated to

distilled water through decreasing concentrations of ethanol. The immunohistochemical

procedure was performed on an auto-immunostainer (NEXESTM

, Vetana Medical Systems,

Tuscon AZ). Rabbit polyclonal anti-Citrobacter rodentium diluted 1:400, and secondary

antibody staining with biotinylated anti-rabbit IgG (Vector Laboratiories, Burlingame, CA) at a

dilution of 1:100, was detected using a DAB (3-3’-diaminobenzidine) detection system (Ventana

Medical Systems, Tuscon AZ). Slides were then counterstained with hematoxylin to provide

nuclear detail.

To detect apoptotic cells, the TUNEL assay for in situ end-labeling was performed and adapted

to an automated immuno/in situ hybridization instrument (DiscoveryTM

, Ventana). Prior to

staining, colonic sections were deparaffinized, as above, and blocked for endogenous peroxidase

by Protease I (Ventana Medical Systems) digestion for 12 min. Slides were then incubated with

recombinant terminal deoxynucleotidyl transferase (GIBCO BRL, Life Technologies, Grand

Island, NY) and biotin 16-dUTP (Roche Diagnostics Corporation, Indianapolis, IN) to label the

nuclei of cells undergoing programmed cell death (Kubo, Li et al. 2008). Colorimetric

visualization, using avidin-HRP and DAB, was performed as described above.

To detect proliferating cells within colonic crypts, colonic sections from mice injected

intraperitoneally with BrdU prior to euthanasia were dewaxed and hydrated, as detailed above.

Slides were then treated with pepsin digestion, acidified in 4N HCl to denature DNA, and

blocked for endogenous peroxidase. Immunohistochemical staining with a mouse anti-BrdU

antibody (Dako, Carpinteria CA) was performed on an auto-immunostainer (DiscoveryTM

,

Ventana Medical Systems) at a dilution of 1:50 using the ARKTM

kit (Dako) to prevent mouse-

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on-mouse cross reactivity. Detection and visualization employed a peroxidase-conjugated

streptavidin secondary reagent (Dako) and the DAB chromogen substrate.

Histology and immunohistochemistry slides were viewed using a light field microscope (Leica

DM 4600B, Leica Microsystems Inc., Richmond Hill, ON, Canada). Photomicrographs were

captured with a digital camera (Leica DC 500) and analyzed using integrated software (Leica

IM500 Image Manager).

Transmission electron microscopy. Distal colonic segments fixed in Universal fixative for 24

hr were post-fixed in 2% aqueous osmium tetroxide for 1 hr at 20ºC. Dehydration was

performed in graded acetone, followed by embedding in epoxy resin. Osmium post-fixation,

dehydration and embedding were conducted in a Pelco Biowave microwave oven (Pelco

International, Redding, CA). One micrometer thick sections were stained with toluidine blue and

ultra-thin sections stained with uranyl acetate and lead citrate. Electron microscopy examination

was performed using a transmission electron microscope (JEM 1230, Joel USA Corp., Peabody,

MA).

Cytokine profiles of splenocytes. The production of IFN- and IL-10 from isolated splenocytes

was performed, as described previously (Jones, Day et al. 2002; Johnson-Henry, Nadjafi et al.

2005). Briefly, spleens were mashed through sterile filter screens in RPMI medium to obtain

single cell suspensions. Cells were incubated in red cell lysis buffer for 3 min and washed 3

times. The pellet was layered with 5 mL of lympholyte-M (Cedarlanes Laboratories Ltd.,

Hornby, ON, Canada) and spun at 1,000 rpm for 10 min. Isolated cells were washed 3 times and

resuspended in RPMI medium containing 10% fetal calf serum. Splenocytes were enumerated

and equal numbers of cells incubated with sterile C. rodentium whole-cell sonicate for 72 hr at

37oC. IFN- and IL-10 cytokine levels were then measured using commercially available

immunoassay kits (Medicorp Inc., Montreal, QC, Canada), according to the manufacturer’s

instructions.

Data analyses. Results are reported as means ± standard errors of the mean (SEM). To test for

significance between two groups, the two-tailed Student’s t test was employed, with p<0.05

considered as statistically significant. One-way analysis of variance (ANOVA) was used for

data derived from more than two study groups (Bewick, Cheek et al. 2004).

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4.4 Results

Phosphoinositide 3-kinase (PI3K) is recruited to lipid rafts in response to enterohemorrhagic

Escherichia coli infection

Following E. coli O157:H7 infection of HEp-2 cells, PI3K was recruited to the sucrose fraction

containing caveolin-1, which was employed as a lipid raft marker protein (Jandu, Ceponis et al.

2006) (Figure 4.1a). There was a significant increase in the amount of PI3K present in the

lower density fraction of EHEC-infected cells, indicating that E coli O157:H7 induced the

translocation of PI3K to lipid rafts. Protein recruitment to lipid rafts was not observed when

tissue culture cells were infected with heat-killed bacteria (Figure 4.1a), demonstrating that

recruitment of PI3K is triggered by exposure of epithelial cells to live organisms, and not

bacterial surface-derived structural constituents. The increase of PI3K recruitment to lipid rafts

in EHEC-infected cells was quantified by using densitometry to determine integrated intensity

values (Figure 4.1b; n=5, p<0.05) Chloramphenicol-treated bacteria also markedly reduced the

recruitment PI3K to lipid rafts (Figure 4.1c), indicating that activation of these signal

transduction cascades is caused by newly synthesized bacterial proteins (Cole, Shirey et al.

2007). EHEC O157:H7-infection of Intestine 407 cells also induced activation and translocation

of PI3K (Figure 4.1d).

PI3K recruitment to lipid rafts is independent of known EHEC virulence factors

Similar to observations in EHEC O157:H7-infected cells, an increase in PI3K level in caveolin-

1-enriched fraction 3 was observed in response to infection with the eae negative E. coli, strain

CL15 (VTEC O113:H21), indicating that recruitment to lipid rafts in response to EHEC infection

(Figure 4.1a) is independent of the attaching-effacing (eae) gene, because strain CL15 does not

contain the LEE pathogenicity island required to cause AE lesions (Shen, Mascarenhas et al.

2004). Infection of HEp-2 cells with E. coli, strain CVD451, a type III secretion-deficient

mutant (Ceponis, McKay et al. 2003), also resulted in increased recruitment of PI3K to lipid rafts

(Figure 4.2a). Similarly, infection with E. coli, strain 85-170, a Stx-1 and Stx-2 negative mutant

(Ceponis, McKay et al. 2003), also demonstrated the recruitment of host signaling molecules to

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Figure 4.1 Phosphoinositide 3-kinase (PI3K) is recruited to lipid rafts in response to

enterohaemorrhagic Escherichia coli O157:H7 infection, and newly synthesized bacterial

proteins are required for PI3K recruitment to lipid rafts. Western blots of phosphoinositide

3-kinase (PI3K) from ultracentrifugation fractions of whole cell (HEp-2) extracts. The presence

of PI3K in the caveolin-1-containing fraction indicates that it is recruited to lipid rafts in

response to bacterial infection. The presence of PI3K in fraction 3 of VTEC O113:H21 infected

cells indicate that recruitment is independent of eae gene. The lack of PI3K in fraction 3 of

uninfected and boiled EHEC-infected cells demonstrates that recruitment is induced by live

bacteria (a). Recruitment was quantified by using densitometry and expressed graphically (n=5,

p<0.05) (b). PI3K was not recruited in host cells infected with chloramphenicol-treated EHEC

O157:H7, indicating that metabolically active bacteria are required for recruitment of host

signaling proteins (c). EHEC-infected Intestine 407 cells also induced translocation of PI3K to

lipid rafts (d).

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Figure 4.2 Activated phosphoinositide 3-kinase (PI3K) is recruitment to lipid rafts in

response to infection independent of the type III secretion system and Shiga-like toxins 1

and 2. Western blots of phosphoinositide 3-kinase (PI3K) from ultracentrifugation fractions of

whole cell (HEp-2) extracts. PI3K recruitment in EHEC mutant (CVD 451 and 85-170)-infected

cells indicates that signaling is independent of type III secretion system and Shiga-like toxins 1

and 2 (a). Cells treated with the PI3K inhibitor LY294002 prior to EHEC O157:H7 infection

had reduced amounts of PI3K recruited to lipid rafts, compared to the amount of PI3K recruited

in cells treated with the inactive analogue, LY303511, prior to EHEC infection (b).

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lipid rafts (Figure 4.2a). Taken together, these findings indicate that recruitment of signal

transduction molecules to lipid rafts is independent of the bacterial type III secretion system and

the production of Shiga-like toxins 1 and 2.

Recruitment of PI3K to lipid rafts is blocked by a specific PI3K kinase inhibitor

Recruitment of PI3K in response to EHEC O157:H7 infection was reduced in cells pre-treated

with the PI3K inhibitor, LY294002 (100κM), by 40% (relative to EHEC-infected alone) but not

when an equal concentration of an inactive analogue (LY303511) was employed (integrated

intensity readings of the PI3K band in immunoblots, relative to caveolin-1, was 0.805 for

LY294002-treated cells, 1.229 for LY303511-treated epithilia and 1.332 for EHEC-infected

cells) (Figure 4.2b). DMSO alone, tested as a vehicle control, also did not result in a reduction

in PI3K recruitment to lipid rafts (data not shown). These findings support the hypothesis that

activated PI3K is recruited to lipid rafts in response to EHEC infection (Cantley 2002).

MβCD blocks PI3K recruitment to lipid rafts in response to EHEC infection

To confirm that EHEC O157:H7-induced translocation of host proteins to lipid rafts was

dependent on intact lipid raft microdomains, pre-treatment of cells with methyl-β-cyclodextrin

(MβCD;10mM) was used to deplete cholesterol and, thereby, disrupt lipid rafts (Riff, Callahan et

al. 2005). Cells subjected to MβCD pretreatment failed to recruit PI3K to lipid rafts in response

to EHEC O157:H7 (Figure 4.3b). To verify that MβCD induced disruption of lipid rafts,

cholera toxin B subunit staining was performed (Hatano, Kubo et al. 2007). HEp-2 cells treated

with MβCD lacked visible choleragen B subunit staining around the cells (Figure 4.3h),

compared with untreated cells (Figure 4.3f). When MβCD-treated cells were rescued with

soluble cholesterol, cholera toxin labeling again showed the presence of lipid rafts in the plasma

membrane (Figure 4.3j).

Culture supernatant and conditioned medium cannot induce the recruitment of PI3K to lipid

rafts

To determine whether bacterial secreted factors were able to elicit EHEC-induced recruitment of

PI3K to lipid microdomains, culture supernatants and conditioned media were collected. Cells

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Figure 4.3 Intact lipid microdomains are required for EHEC induced translocation of

phosphoinositide 3-kinase (PI3K) to lipid rafts, while secreted bacterial factors are

insufficient to induce this recruitment. Conditioned medium did not induce the recruitment of

PI3K to lipid microdomains on host cell membranes (a). Disruption of lipid rafts by depleting

cellular cholesterol using MβCD (10mM) leads to decreased recruitment of the host signaling

protein, PI3K, in response to EHEC O157:H7 infection. Culture supernatant alone was unable to

induce recruitment of PI3K (b). Phosphorylation of the PI3K downstream effector Akt was not

detected in response to EHEC and C. rodentium infections (c and d), suggesting an alternative

activated pathway. Lipid raft disruption following cholesterol depleting MβCD treatment was

visualized using Alexa fluor 594-labeled cholera toxin subunit B: untreated cells (e and f),

MβCD-treated cells (g and h) and MβCD-treated epithelia replenished with soluble cholesterol

(i and j).

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treated with culture supernatant and conditioned medium (either filtered or non-filtered) did not

result in the recruitment of PI3K to lipid rafts (Figure 4.3a&b).

EHEC does not activate the PI3K/Akt pathway during infection

To investigate downstream signals activated in response to EHEC-mediated PI3K recruitment to

lipid rafts, whole cell protein extracts were taken 5 min to 1 hour (Figure 4.3d), and at 3 and 6 hr

post infection (Figure 4.3c). The amount of phopho-Akt was determined by western blotting.

Although PI3K was recruited to detergent-insoluble microdomains in response to EHEC

infection, phosphorylation of Akt, which is common downstream effector (Cantley 2002), was

not detected.

Delayed colonization of NPC colonic mucosa by C. rodentium

To extend these findings to the in vivo setting, wild type BALB/c and NPC-/-

mice were

employed. BALB/c and NPC-/-

mice were infected orogastrically with the murine-specific AE

bacterium, C. rodentium (Borenshtein, McBee et al. 2008). In all mice, C. rodentium was

recovered by rectal swabbing starting at day 3 post orogastric challenge until the end of the

infection protocol, indicating that the organism was able to successfully colonize and infect both

wild type and NPC-/-

mice. Six days post challenge, there was a homogeneous bacterial

adherence pattern on the colonic mucosa in infected BALB/c mice (Figure 4.4b). By contrast,

there was minimal C. rodentium adherence detected on the colonic surface of NPC-/-

mice at 6

days post infection (Figure 4.4e). Furthermore, a more homogeneous pattern of bacterial

adhesion was detected in NPC-/-

mice at 12 days post infection (Figure 4.4f). At this time,

adherent bacteria were largely cleared from the mucosa in wild type, C. rodentium-infected mice.

C. rodentium-induced attaching-effacing lesions are delayed in NPC -/-

mice

Segments of the distal colon were assessed by transmission electron microscopy for the presence

of AE lesions, characteristic of adherent C. rodentium (Mundy, MacDonald et al. 2005). In

contrast with uninfected mice which displayed intact apical microvilli on columnar epithelia

(Figure 4.5a), wild type mice challenged with C. rodentium for 6 days had large numbers of

intimately adherent bacteria with typical actin-enriched adhesion pedestals (Figure 4.5b), but by

12 days post inoculation AE lesions were no longer observed (Figure 4.5c). In contrast, AE

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Figure 4.4 Citrobacter rodentium colonization is delayed in the colonic mucosa of NPC -/-

mice. Immunohistochemistry of colonic mucosa stained with antibody against C. rodentium.

Uninfected wild type BALB/c (a). Wild type BALB/c infected for 6 days show a thick band of

C. rodentium adherent along the apical aspect of the luminal mucosa (b). Wild type BALB/c

mice infected for 12 days, showed C. rodentium staining of luminal contents and few adherent

bacteria (c). Uninfected NPC-/-

mouse colon (d). C. rodentium-infected NPC-/-

colonic sections

obtained 6 days following infectious challenge, demonstrate a few patches of adherent bacteria

(e). NPC-/-

tissues obtained from colons 12 days post infection showed C. rodentium binding to

mucosal surfaces of colonocytes (f). Approximate original magnifications for each

photomicrograph, X 200.

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Figure 4.5 Attaching-effacing lesions induced by Citrobacter rodentium infection are

delayed in NPC -/-

mice. Transmission electron photomicrographs of distal colonic mucosa of:

uninfected BALB/c columnar epithelium with intact brush boarder (a). Higher magnification of

an attaching-effacing lesion-producing C. rodentium bacterium (cr) on a BALB/c colonocyte 6

days post inoculation (b). The attaching-effacing lesion displays characteristic effacement of

the brush boarder microvilli at the site of intimate bacterial adherence and an F-actin-enriched

pedestal underlying the adherent bacterium. BALB/c mice colonic tissue obtained 12 days post

infectious challenge was devoid of attaching-effacing lesions (c). Uninfected NPC mouse tissue

(d). NPC-/-

mouse colon collected 6 days post C. rodentium orogastric inoculation lacked

attaching-effacing lesions (e). Bound C. rodentium (cr) to an NPC-/-

colonocyte 12 days post

challenge form attaching-effacing lesions (f). Bars = 2 m.

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lesions were not detected in NPC-/-

mice at 6 days post infection (Figures 4.5d and 4.5e).

Intimate bacterial adherence and adhesion pedestal formation was evident in NPC-/-

mice only

after 12 days following C. rodentium infection (Figure 4.5f).

C. rodentium-infected NPC -/- mice display reduced colonic epithelial cell hyperplasia

Compared to uninfected mice (Figure 4.6a), histological sections obtained from wild-type mice

showed an increase in thickness of the colonic epithelium at both 6 days (Figure 4.6b) and 12

days (Figure 4.6c) post C. rodentium challenge. In contrast, NPC -/-

mice had a reduction in

hyperplasia of the colonic mucosa in response to C. rodentium infection at 12 days (Figure 4.6d-

g).

The reduction in mucosal thickness of C. rodentium-infected NPC -/-

mice compared with

BALB/c mice could be due to either increased cell death or reduced cellular proliferation.

Histological sections of C. rodentium-infected wild-type and NPC -/-

colonic tissue assessed by

TUNEL assay showed no differences in surface epithelial cell apoptosis (data not shown).

However, colonocyte proliferation, assessed via BrdU staining in infected wild-type mice,

showed an increase in both the number of mitotic cells and the size of the proliferation zone at

both 6 days (Figure 4.7b) and 12 days (Figure 4.7c) post infection compared with uninfected

mice (Figure 4.7a). Colonocyte proliferation was maximal at day 6 post infection in wild-type

mice. In contrast with wild type mice, C. rodentium infection of NPC-/-

mice resulted in only

moderate increases in epithelial cell mitosis at both 6 and 12 days post infectious challenge when

maximal bacterial colonization was present (Figures 4.7e and 4.7f, respectively). These

changes were quantified as increases in the zone of proliferation – the maximal height of BrdU-

labeled cells from base of well-oriented crypts. (Figure 4.7g).

NPC -/-

mice produce reduced levels of the pro-inflammatory cytokine IFN-in response to C.

rodentium infection

The epithelial hyperplasia and colonic mucosal inflammation in C. rodentium infection is

analogous to enteric immunopathologic conditions in patients such as chronic inflammatory

bowel disease (Mundy, MacDonald et al. 2005). Multiple pro-inflammatory cytokines are

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Figure 4.6 Citrobacter rodentium-induced epithelial cell hyperplasia is reduced in NPC-/-

mice. Photomicrographs of representative colonic sections showing increases in crypt length in

response to C. rodentium infection. Uninfected BALB/c (a), 6 day infected BALB/c (b), 12 day

infected BALB/c (c), Uninfected NPC-/-

(d), 6 day infected NPC-/-

(e), 12 day infected NPC-/-

(f).

Original magnification for all photomicrographs X200. Increases in crypt length over the

uninfected baseline values were quantified (g). A difference in the change in crypt length was

observed at 12 days post infection (64κm ± 8.251 vs. 112κm ± 2.958; *p<0.05), but not at 6 days

post infection. BALB/c = black bars, NPC-/-

= white bars.

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Figure 4.7 Colonocyte proliferation is reduced in NPC -/-

mice infected with Citrobacter

rodentium. Photomicrographs of colonic sections showing proliferating colonocytes through

incorporation of BrdU during mitosis. Uninfected BALB/c crypts show few BrdU positive

dividing colonocytes (a). Large numbers of BrdU positive colonocytes are observed in BALB/c

tissue sections 6 days (b) and 12 days (c) post infection. Uninfected NPC-/-

crypts showed few

proliferating cells (d), and NPC-/-

colonic sections both 6 days (e) and 12 days (f) post infection

had just a moderate increase in the number of BrdU positive cells. Approximate original

magnification for each photomicrograph, X 200. The size of the zone of proliferation was

quantified and expressed as the change in zone size over the uninfected baseline (g).

Proliferation was maximal in BALB/c mice at day 6 post infection (71pg/mL ± 26.3 vs. 17.6

pg/mL ± 17.6, * p < 0.001). No differences were seen between BALB/c and NPC-/-

mice at 12

days post infection. BALB/c = black bars, NPC-/-

= white bars.

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elicited in response to C. rodentium infection (Higgins, Frankel et al. 1999; Chen, Louie et al.

2005). Therefore, to assess the adaptive immune responses elicited, splenocytes were isolated

from uninfected and C. rodentium-challenged BALB/c and NPC-/-

mice. Isolated splenocytes

were stimulated in vitro with C. rodentium sonicate and then IFN- and IL-10 levels, measured

as representative of Th1 and Tregulatory cytokine responses, respectively (Johnson-Henry, Nadjafi

et al. 2005). As shown in Figure 4.8a, wild-type mice displayed a pro-inflammatory, Th1-

predominant cytokine response 12 days after C. rodentium exposure. By contrast, infected NPC-

/- mice had a reduced IFN- response. This response may be regulated by an increased Tregulatory

response, because higher levels of IL-10 were present in splenocytes derived from NPC-/-

mice at

both 6 and 12 days post infection, compared with wild-type mice challenged with C. rodentium

(Figure 4.8b).

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Figure 4.8 Altered cytokine profiles in NPC -/-

mice infected with Citrobacter rodentium.

Cytokine profiles of splenocytes isolated from uninfected and C. rodentium challenged BALB/c

(black bars) and NPC-/-

(white bars) mice incubated with C. rodentium sonicates. IFN-γ

secretion at day 12 post infection was reduced in NPC-/-

mice (p < 0.05) (a). Anti-inflammatory

cytokine IL-10 secretion was increased at both 6 (p < 0.001) and 12 days (p < 0.05) following C.

rodentium infection of NPC-/-

mice (b).

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4.5 Discussion

Multiple signaling molecules play a role in orchestrating host cell responses to EHEC infection

(Johnson-Henry, Wallace et al. 2001) leading to the development of mucosal inflammation

(Ismaili, Philpott et al. 1995), cytoskeleton rearrangements (Shaner, Sanger et al. 2005) and

disruption of intercellular tight junctions (Philpott, McKay et al. 1998). PI3K, a lipid kinase,

catalyzes the production of membrane-bound lipid second messengers following stimulation via

tyrosine kinases, cytokine receptors and integrin receptors (Pizarro-Cerda and Cossart 2006). In

response to pathogen infections, PI3K regulates cytoskeleton rearrangements following both

bacterial adhesion (Kierbel, Gassama-Diagne et al. 2007) and invasion (Kierbel, Gassama-

Diagne et al. 2005) of other bacterial pathogens. However, the mechanisms by which EHEC

modulates host signal transduction pathways are still largely unknown.

Akt, also known as PKB, is key regulator of host cell survival by inhibiting apoptosis, control of

the cell cycle and various pro-inflammatory responses, including the activation of the

transcription factor NFθB. Akt is activated downstream of PI3K (Wiles, Dhakal et al. 2008).

Many bacterial effector proteins trigger the Akt pathway to manipulate host cell function leading

to increase adherence and invasion and induce cytoskeletal rearrangements (Edwards and

Apicella 2006). However, in our studies phosphorylation of Akt was not detected in response to

EHEC infection, supporting previous findings that EHEC infection inhibits activation of the

Akt/NF-θB signaling cascade (Bosse, Ehinger et al. 2007). Recruitment of PI3K to lipid rafts

likely stimulates alternate signaling pathways, such as small GTP-binding proteins, leading to

pedestal formation in the apical cytoplasm beneath intimately adherent attaching-effacing

organisms (Takenouchi, Kiyokawa et al. 2004).

The characteristic attaching-effacing lesions seen in eukaryotic cells following non-invasive

EHEC O157:H7 infection involves the presence of intact specialized lipid microdomains (Riff,

Callahan et al. 2005). We show, for the first time, using antibody against two closely related

PI3K p85 subunits (α and β) (Tang, Lu et al. 2007), that EHEC hijacks epithelial cell membrane

lipid microdomains to recruit the second messenger PI3K. Such recruitment was not the result of

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external bacterial surface structures, because PI3K recruitment to lipid rafts was only observed

when cells were infected with live microorganism and not when employing heat-killed bacteria.

Recruitment of PI3K to lipid rafts was observed when epithelial cell monolayers were infected

with EHEC strain CVD-451, a type III secretion mutant; indicating that PI3K recruitment to lipid

rafts is mediated by a non-type III secretion system bacterial effector (Guttman, Li et al. 2006).

This recruitment may be induced by secreted bacterial effectors localized in the detergent-

resistant microdomains with the ability to recruit SH2/3 ligands, leading to pedestal formation.

This has been shown previously, for example, when using Tir derived from an enteropathogenic

E. coli strain (Sason, Milgrom et al. 2009).

Cells infected with chloramphenicol-treated bacteria to block prokaryotic protein synthesis

(Jandu, Ceponis et al. 2006) reduced the recruitment of PI3K to lipid rafts during the infectious

process. This finding indicates that new bacterial protein(s) secreted into the culture medium

triggers the recruitment of PI3K to cholesterol-enriched microdomains in the host cell plasma

membrane. However, secreted bacteria factors alone (using conditioned medium collected from

host-bacteria co-cultures) did not induce the recruitment of PI3K to lipid rafts. Therefore,

bacteria attachment to cell monolayer is required. Such contact-dependent effects have been

described previously (Philpott, McKay et al. 1998).

Although production of Shiga toxins is reported to promote bacterial colonization in the human

intestine (Robinson, Sinclair et al. 2006), the ability of EHEC O157:H7 to elaborate Shiga

toxins does not play a role in recruiting PI3K to lipid rafts (Proulx, Seidman et al. 2001). The

reduction in EHEC-induced PI3K recruitment to lipid rafts in the presence of a specific

pharmacological inhibitor against PI3K suggests an activated protein was recruited. Such

recruitment likely is the first step leading epithelial barrier disruption and reorganization of the

host cell cytoskeleton.

Previous studies have shown that the presence of cholesterol-enriched plasma membrane

microdomains in vitro are required for adherence and pedestal formation by attaching-effacing E.

coli (Riff, Callahan et al. 2005; Allen-Vercoe, Waddell et al. 2006). When lipid rafts are

disrupted with the cholesterol-sequestering reagent, methyl-β-cyclodextrin, EHEC no longer

induces the translocation of PI3K to lipid rafts. The presence of caveolin-1 in low density

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fraction even after MβCD treatment likely is due to an uneven distribution of caveolin-1 in

caveolae present on the basolateral aspect of the plasma membrane and in membranes

surrounding intracellular organelles (Absi, Burnham et al. 2007). An alternative explanation is

that cholesterol is more readily removed from non-microdomain regions than from liquid-

ordered phase where it is more tightly packed and less easily extracted by agents such as MβCD

(Marbeuf-Gueye, Stierle et al. 2007).

The interaction of microbial pathogens with host cell membrane cholesterol and lipid rafts has

become a major theme of interest in disease pathogenesis (Goluszko and Nowicki 2005; Lafont

and van der Goot 2005). Previous in vitro studies demonstrate that multiple bacteria, including

Salmonella (Catron, Sylvester et al. 2002), Shigella (Lafont, Tran Van Nhieu et al. 2002),

Brucella (Watarai, Makino et al. 2002) and E. coli (Kansau, Berger et al. 2004; Riff, Callahan et

al. 2005; Allen-Vercoe, Waddell et al. 2006), interact with these cholesterol-enriched

microdomains. However, the molecular mechanisms underlying these interactions are still

largely undefined. Direct interactions of bacterial proteins with host lipid rafts have been

described. For example, type III secretion system bacterial effectors from Salmonella PipB

(Knodler, Vallance et al. 2003) and EPEC Tir (Allen-Vercoe, Waddell et al. 2006) are targeted to

lipid rafts, whereas Salmonella SipB and Shigella IpaB are cholesterol-binding proteins

(Hayward, Cain et al. 2005).

We showed previously that depletion of cellular cholesterol decreases intimate attachment of AE

E. coli (Riff, Callahan et al. 2005). AE lesions were restored when cells are allowed to recover

cholesterol (Riff, Callahan et al. 2005). These findings were confirmed using primary fibroblasts

harboring a defect in the Niemann-Pick C 1 (NPC1) gene (Riff, Callahan et al. 2005). Niemann-

Pick type C disease is a cholesterol storage disorder resulting in neurodegeneration (Chang, Reid

et al. 2005). Mutations in npc1 and npc2 result in aberrant lipid transport (Liscum and Sturley

2004; Mukherjee and Maxfield 2004), which results in decreased lipid rafts and lipid raft-

associated markers on the plasma membrane of affected cells (Garver, Krishnan et al. 2002).

Taken together, these findings suggest that lipid rafts are required for AE lesion formation in

response to EHEC O157:H7 and C. rodentium infection in vitro. Utilizing a series of

pharmacological inhibitors, we previously identified that host enzymes, including phospholipase

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C-γ (PLC-γ) and phosphoinositide 3-kinase (PI3-Kinase), are involved in the signal transduction

cascades leading to cytoskeletal rearrangements (Johnson-Henry, Wallace et al. 2001).

In this study, we describe the importance of cholesterol during host-pathogen interactions of the

mouse pathogen C. rodentium in vivo. To our knowledge, this is the first in vivo study

confirming an interaction between host cholesterol-enriched microdomains and an attaching-

effacing non-invasive enteric bacterial pathogen. While C. rodentium infection of wild type

BALB/c mice resulted in AE lesion formation maximally at 6 days post infection, C. rodentium-

induced lesions in NPC-/-

mice were found later during the infection period, at 12 days. This

difference is likely due to the inability of C. rodentium to bind and colonize the NPC-/-

colonic

mucosa despite similar shedding patterns in BALB/c and NPC-/-

mice. Maximum colonization

occured on days 6 and 10 post-infection in wild type mice and was decreased by post-infection

day 15 with resolution of disease. Such recovery was not observed in NPC mice infected with C.

rodentium. The colonization data suggest there could be a secondary, alternative binding

mechanism for C. rodentium to attach to the colonic mucosa. Partitioning of PI3K into

cholesterol-rich microdomains is necessary, but not sufficient, to induce attaching-effacing

lesions.

Adherence of C. rodentium to colonocytes correlated with maximal responses in cellular

proliferation. The time dependent binding could delay C. rodentium pathogenesis in the NPC-/-

mouse resulting in a less severe colonic epithelial cell hyperplasia response, compared to

infection in wild type mice. Colonization and binding of C. rodentium to mucosal surfaces

requires multiple factors. Initial adhesion of the bacterium to host cells is believed to be

accomplished by the CFC (colonization factor Citrobacter) type IV pilus (Mundy, Pickard et al.

2003). After initial adherence, attaching-effacing pathogens secrete Tir directly into the host

plasma membrane. Tir mutants are unable to colonize wild type mice and do not cause disease

(Schauer and Falkow 1993). The LEE pathogenicity island locus encodes Tir, an effector protein

which has been isolated from lipid rafts (Allen-Vercoe, Waddell et al. 2006). Furthermore, the

type III secretion system that delivers Tir to the host cell is regulated by lipid rafts (van der Goot,

Tran van Nhieu et al. 2004), and utilizes these cholesterol-rich microdomains as targets for pore

formation (Hayward, Cain et al. 2005), thereby allowing for a direct link between the bacterium

and host cells. During the normal course of infection, C. rodentium colonizes the colon within

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the first 2 to 3 days post infection (Mundy, Pickard et al. 2003), and is recovered in fecal samples

for no more than a few weeks (Wiles, Clare et al. 2004). Non-colonizing mutants, by contrast,

are cleared within days of inoculation (Schauer and Falkow 1993). Preventing either the initial

attachment of C. rodentium to host cells or preventing Tir translocation both would serve to

inhibit the colonization that was observed in NPC-/-

-infected mice.

The observation that maximal mitotic responses (incorporation of BrdU) occurred during times

of maximal binding of bacteria to colonic surfaces confirms the belief that the hyperplastic

response is contact dependent. Thus, reduced adhesion of C. rodentium to NPC-/-

colonic

mucosa may similarly abrogate the epithelial cell hyperplasic response. Current evidence

indicates that the colonic hyperplasia is dependent on the non-LEE-encoded effector A (NleA,

also known to as EspI) (Gruenheid, Sekirov et al. 2004), since C. rodentium strains harboring

deletions in nleA do not result in colonic epithelial cell hyperplasia (Mundy, Petrovska et al.

2004).

Reductions in lipid-raft microdomains likely also impact on type III secretion. Thus, decreased

transfer of NleA in NPC-/-

mice could well play a role in reducing the proliferative responses in

colonocytes. On the other hand, C. rodentium infection also results in the production of serine

proteases, which activate the proteinase-activated receptor 2 (PAR2) (Hansen, Sherman et al.

2005). Infected mice treated with a serine proteinase inhibitor and PAR2-/-

mice both show

decreased hyperplastic changes in colonic mucosa. Whether PAR2 activation is deficient in

NPC-/-

cells is not known, but PAR2 signaling is mediated by G-proteins, which are known to

associate with lipid raft microdomains (Simons and Toomre 2000).

Another important factor impacting on the development of C. rodentium-induced colonic

epithelial cell hyperplasia is the host immune system (Artis, Potten et al. 1999). C. rodentium

elicits a distinct pro-inflammatory cytokine response characterized by high levels of Th1

cytokines, including IFN- and IL-12 (Higgins, Frankel et al. 1999). In this study, there was a

decrease in pro-inflammatory cytokine responses in NPC-/-

mice challenged with C. rodentium as

well as marked differences in secreted Tregulatory cytokine profile. IL-10 is an anti-inflammatory

cytokine, which acts to counter-balance pro-inflammatory signals (O'Garra, Vieira et al. 2004;

Powrie 2004). Other studies have noted varying effects, with increases in both Tregulatory and Th2

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cytokines in response to C. rodentium infection. Johnson-Henry et al. (Johnson-Henry, Nadjafi

et al. 2005) observed that mice pretreated with probiotics had elevated IL-10 secretion from

splenocytes and ameliorated C. rodentium disease pathogenesis. By contrast, helminth infection,

which elevate Th2 cytokine responses, prevent colitis in non-infectious animal models (Reardon,

Sanchez et al. 2001; McKay 2006), but results in an increased severity of disease in response to

C. rodentium infection (Chen, Louie et al. 2005). A major difference between these outcomes is

the ability of C. rodentium to bind to the mucosal surface.

Taken together, these complementary in vitro and in vivo studies of host epithelial cell responses

to non-invasive, attaching-effacing pathogens demonstrate the importance of cholesterol-

enriched microdomains as signal transduction platforms which mediate signaling between the

infecting organism and the cytosol of the host epithelial cell.

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4.6 Acknowledgements

This work was supported by operating grants from the Canadian Institute for Health Research

(CIHR). GS-T was the recipient of a CIHR Canada Graduate Scholarship – Master’s Award,

CIHR Frederick Banting and Charles Best Canada Graduate Scholarships - Doctoral Award and

research training funding support provided by the SickKids Foundation Graduate

Scholarships at the University of Toronto. The in vivo studies were conducted by Jason D.

Riff, who was supported through a studentship by the Ontario Student Opportunity Trust Fund -

Hospital for Sick Children Foundation Student Scholarship Program, and a University of

Toronto Fellowship. PMS is the recipient of a Canada Research Chair in Gastrointestinal

Disease.

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Chapter 5.

Recruitment of Protein Kinase C to Lipid Rafts in Response to Enterohemorrhagic Escherichia coli O157:H7 is blocked by Lactobacillus helveticus R0052

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5.1 Abstract

Background: Enterohemorrhagic Escherichia coli, serotype O157:H7 (EHEC) causes outbreaks

of diarrhea, hemorrhagic colitis, and the haemolytic uremic syndrome (HUS), which is the

leading cause of acute renal failure in children. EHEC intimately attaches to epithelial cells,

effaces microvilli, and recruits F-actin into pedestals forming attaching-effacing (A/E) lesions.

Recent studies demonstrate that lipid rafts serve as platforms for the recruitment of cell signaling

complexes that mediate host cell responses to infection.

Objective: The aim of this study was to determine if PKC is recruited to lipid rafts in response to

EHEC O157:H7 infection.

Methods: HEp-2 and Intestine 407 epithelial cell monolayers were infected with EHEC (MOI

100:1, 3h, 37oC) and cell proteins extracted in Triton X-100 at 4

oC, using buoyant-density

ultracentrifugation to isolate detergent-resistant microdomains. Immunoblot analyses for PKC

was then performed and localization in lipid rafts confirmed by using anti-caveolin-1 antibody.

Results: In contrast to uninfected cells, PKC was recruited to lipid rafts in response to EHEC

O157:H7 infection. Metabolically active bacteria and cells with intact cholesterol-rich

microdomains were necessary for the recruitment of PKC. Recruitment of PKC to lipid rafts was

independent of the intimin (eaeA) gene, type III secretion system, and the production of Shiga-

like toxins. Inhibition studies, using myristoylated PKCδ pseudosubstrate, showed that atypical

PKC isoforms were activated in response to EHEC infection. Pre-incubation with the viable

probiotic Lactobacillus helveticus, strain R0052 prevented PKC recruitment to detergent-

resistant microdomains in response to EHEC challenge.

Conclusions: Detergent-resistant microdomains mediate atypical PKC signal transduction

responses to E. coli O157:H7 infection. These findings contribute further to understanding the

complex array of microbial-eukaryotic cell interactions that occur in response to EHEC

O157:H7.

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5.2 Introduction

Escherichia coli is a facultative, gram-negative bacterium normally present in the commensal

colonic microflora (Kaper et al., 2004), but virulent strains can be an important cause of

outbreaks of foodborne illnesses (Karmali 2004). EHEC O157:H7 is responsible for outbreaks

of diarrhea, hemorrhagic colitis, and the haemolytic uremic syndrome (HUS), which is the most

common cause of acute renal failure in children (Jandu, Shen et al. 2007). Pathogenic E. coli

strains possess virulence factors enabling them to cause disease in a colonized host (Kaper,

Nataro et al. 2004). Humans often become infected by eating contaminated food sources,

through person-to person transmission, or through direct contact with asymptomatically

colonized domesticated farm animals, particularly cattle (Barlow and Mellor 2010).

The majority of cases of diarrhea-associated HUS are caused by EHEC O157:H7. Current

treatment remains predominantly supportive in nature (Tarr, Gordon et al. 2005), because

antibiotics and non-steroidal anti-inflammatory drugs may exacerbate the condition. Instead of

eliminating cytotoxin production, these treatments kill the microorganism and release pre-formed

Shiga-like (also referred to as Vero) toxins from the periplasmic space (Panos, Betsi et al. 2006).

Therefore, alternative therapeutic approaches that will prevent the EHEC colonization without

the release of cytotoxins need to be delineated. Understanding the pathobiology of disease is

likely to yield novel approaches, which can be used to interrupt the infectious process.

EHEC O157:H7 infection is also characterized by intimate bacterial attachment to epithelial cells

through a variety of adherence factors (Gyles 2007). Bacterial effector proteins, encoded on a

35-kilobase pathogenicity island, referred to as the locus of enterocyte effacement (LEE), are

injected into the cytosol of infected cells through a type III secretion system encoded molecular

syringe (Welinder-Olsson and Kaijser 2005). EspE , also known as translocating intimin

receptor (Tir), acts as a receptor for the eaeA gene-encoded bacterial outer membrane protein,

intimin (Campellone, Robbins et al. 2004). EspE-intimin interactions give rise to intimate

attachment of EHEC O157:H7 to eukaryotic cells, the recruitment of host actin to form dense

adhesion pedestals, and the effacement of intestinal brush-border microvilli, collectively known

as the attaching-effacing lesion (Kaper, Nataro et al. 2004).

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Recent studies indicate that the effector protein EspE is inserted into cholesterol- and

sphingolipid-enriched patches in the eukaryotic cell plasma membrane bilayer, variously referred

to as lipid rafts and detergent-resistant microdomains (Zobiack, Rescher et al. 2002; Allen-

Vercoe, Waddell et al. 2006). These are islands of liquid-ordered phase, which disperse laterally

in the two-dimensional liquid-disordered plasma membrane (van der Goot and Harder 2001;

Zaas, Duncan et al. 2005). Such cholesterol-enriched microdomains serve as platforms for the

recruitment of cell signaling complexes to a micro-environment where they are sheltered from

non-raft enzymes that can interfere with signal transduction processes (Brown and London 1998;

Simons and Toomre 2000).

Recent studies have shown that lipid rafts play an essential role in mediating signal transduction

responses in eukaryotic cells (Manes, Ana Lacalle et al. 2003). Therefore, the aims of the present

study were to elucidate the role of PKC in EHEC O157:H7-induced recruitment to lipid rafts and

AE lesion formation as well as the protective effect of Lactobacillus helveticus (R0052) and

rhamnosus (R0011) in preventing EHEC-induced recruitment of PKC to detergent resistant

microdomains.

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5.3 Materials and Methods

Tissue culture cell lines. HEp-2 human laryngeal epithelial cell line (CCL23; American Type

Culture Collection, Manassas, VA) and Intestine 407 embryonic intestinal cells were employed

as model systems. Epithelial cells were cultured at 37oC in 5% CO2 in minimal essential

medium (MEM) supplemented with 10% fetal bovine serum, 1% sodium bicarbonate, 1%

Fungizone, and 1% penicillin-streptomycin (all media and supplemental reagents from Life

Technologies, Grand Island, NY).

Bacterial strains and growth conditions. Bacterial strains employed in this study are shown in

Table 4.1. Enterohemorrhagic Escherichia coli O157:H7, strain CL56 and E. coli, strain CL15

(O113:H21) were stored on 5% sheep blood agar plates at 4oC. Colonies were transferred from

plates into Penassay broth and incubated at 37oC for 18 h and then 3 hour re-growth at 37

oC to

achieve mid-log phase. Boiled bacteria were prepared by incubating mid-log phase bacteria at

100oC for 30 min. Formalin-fixed bacteria were washed with PBS and treated with

formaldehyde (12%) for 6 h to 18 h at 4oC.

Prior to infection of tissue culture cells, bacteria were washed with PBS and resuspended in

antibiotic-free MEM medium. For chloramphenicol treatment, mid-log phase bacteria were

pelleted and resuspended in chloramphenicol (100ug/mL) for 6 to 18 hours at 4oC (Ceponis et.

al., 2003). Bacteria were added to epithelial cells grown in 10 cm diameter tissue culture dishes

(Starstedt Inc., Montreal, Quebec, Canada), at a multiplicity of infection of 100 bacteria to 1

eukaryotic cell, for 1h at 37oC in antibiotic-free MEM. Uninfected cells were used as a negative

control. Cells incubated with the phorbol 12-myristate 13-acetate (PMA) (100nM), a general

activator of protein kinase C (Grigat, Soruri et al. 2007), was used as a positive control. After

0.5, 1, and 3.5 hours of bacterial infection, cells were washed with phosphate-buffered saline

(pH7.0) to remove nonadherent bacteria and then processed for isolation of detergent-resistant

microdomains.

Lactobacillus helveticus R0052 and Lactobacillus rhamnosus R0011, provided by Institute

Rosell-Lallemand Inc. (Montreal, Quebec, Canada), were grown overnight in 5% sheep blood

agar plates for 16 to 18 hours. Approximately 100κl was transferred into de Mann, Rogosa and

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Sharpe (MRS) broth (Difco, Detroit, MI) and cultured aerobically at 37°C overnight. HEp-2

cells, in antibiotic-free MEM, were pretreated with 108 CFU of L. helveticus R0052, L.

rhamnosus R0011 for 3 hrs prior to EHEC infection.Depletion of cholesterol using methyl-β-

cyclodextrin (MβCD). HEp-2 cells were treated with MβCD (Sigma Chemical Co., St. Louis,

MO) (1-10 mM) to disrupt cholesterol-enriched microdomains by reduction in levels of

cholesterol in the plasma membrane (Kilsdonk et. al., 1995). Prior to bacterial infection,

epithelial cells were incubated with MβCD (10 mM) in antibiotic-free MEM for 1 h at 37oC.

The medium was aspirated off cell monolayers and washed with PBS prior to bacterial infection

(Riff, Callahan et al. 2005).

Immunofluorescence microscopy. Eukaryotic cells were seeded onto Lab-Tek four-well

chamber slides (Nalge Nunc, Inc., Naperville, IL) and allowed to adhere overnight at 37oC. The

tissue culture medium was changed to antibiotic-free medium prior to bacterial infection. Cells

were then infected with 109 E. coli in 50κl at a multiplicity of infection of 100:1 at 37

oC in 5%

CO2. After 3 to 4 h of infection, non-adherent bacteria were removed by washing the cells three

times in phosphate-buffered saline (PBS) at pH 7.4. Cells were then fixed in 100% cold

methanol for 10 min. at room temperature. Following 3 washes with PBS, fixed cells were

incubated with mouse monoclonal immunoglobulin G anti-α-actinin primary antibody (1:100

dilution) (Sigma) for 1 h at 37oC. After washing with PBS, monolayers were incubated with

fluorescein isothiocyanate-conjugated rabbit anti-mouse IgG secondary antibody at a 1-in-100

dilution (Jackson ImmunoResearch Laboratories, Inc., West Grove, Pa) for 1 h and kept from the

light. Slides were mounted using SlowFade Antifade Kits (Molecular Probes, Eugene, Oreg.)

and analyzed under alternating phase-contrast and fluorescence microscopy (Leitz Dialux 22;

Leica Canada, Inc., Toronto, Ontario, Canada).

Quantification of attaching-effacing lesions was performed by using immunofluorescence

microscopy: more than 100 cells in four random fields with at least 25 HEp-2

cells stained for -

actinin were quantified per well. Results are expressed as the average number of -actinin foci ±

standard error (SEM) per cell in four separate experiments.

Treatments with pharmacological inhibitors. Cells were pretreated for 3 h with the general

protein kinase C inhibitor bisindolylmaleimide I (10mM) (Calbiochem, La Jolla, CA), or

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isoform-specific Gö6983 (10 or 60nM) (Calbiochem, La Jolla, CA) (Sakwe, Rask et al. 2005).

The myristoylated PKCδ pseudosubstrate or PKCα pseudosubstrate (60κM) (Biosource,

Camarillo, CA) was used to prevent activation and translocation of PKCδ to the plasma

membrane (Xin, Gao et al. 2007). Foci of α-actinin formed on cells were quantitated, as a

measure of attaching-effacing lesions (Riff, Callahan et al. 2005), after 3 to 4 h of bacterial

infection. For analysis of PKC movement to detergent-resistant membranes, epithelial cells

pretreated with inhibitors and then infected with bacteria for 1 h at 37oC.

Isolation of detergent-resistant membranes. Infected epithelial cells were scraped and

pelleted in 4 ml of sterile PBS in 15 ml conical tubes. Cells were then lysed with 0.8mL TN

buffer (25 mM tris-HCl pH 7.5, 150 mM NaCl, 1 mM DTT, 10% sucrose, 1% Triton X-100,

leupeptin, 2 κg/ml pepstatin A, 10 κg/ml aprotonin, 0.5 mM PMSF, 1 mM Na3VO4) for 30

minutes on ice and samples, mixed with 1.7 ml of OptiprepTM

(Axis-Shield PoC AS, Oslo,

Norway), transferred into SW41 centrifuge tubes (catalogue #344059, Beckman Instruments,

Inc., Palo Alto, CA). OptiprepTM

(60%) was diluted with TN buffer to produce 35% and 5%

solutions (Shen-Tu, Schauer et al. 2010), which were then layered on top of samples and

centrifuged at 160,000 x g for 20 hrs at 4oC. Eight 1.5 ml fractions were then collected from the

top to bottom of the gradient generated by ultracentrifugation (Macdonald et al., 2005).

Immunoblotting. Aliquots (10κl) of each fraction were analyzed for PKC and caveolin-1.

Proteins were separated by pre-cast 10% Tris-HCl (Biorad) sodium dodecyl sulphate

polyacrylamide gel electrophoresis (SDS-PAGE) with a protein ladder standard (BioRad, broad

molecular range ladder) at 120 volts for 1 to 1.25hr at room temperature. After electrophoresis,

proteins were transferred onto nitrocellulose membranes (Pall Corporation, Pensacola, FL) at

100 volts for 1.5 hrs at 4oC and incubated in Odyssey blocking buffer (LI-COR

Biosciences,

Lincoln, NE) for 0.5 to 1hr at room temperature. Blocking buffer was then decanted off and the

membrane probed with anti-caveolin-1 (Santa Cruz Biotechnology Inc., CA; 1:1000) and

primary antibodies against PKC (Santa Cruz; 1:1000) overnight at 4oC on a shaker. After

washing the membrane four times (5 min. per wash) with PBS plus 0.1% Tween, IRDye 800

goat anti-rabbit immunoglobulin G (IgG) secondary antibody (Rockland Immunochemicals,

Gilbertsville, PA; 1:20,000) was added and incubated for 1 hour at room temperature on a

shaker. The blots were then washed with PBS plus 0.1% Tween for 4 times and with PBS alone

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once. The membrane was then scanned and bands detected using the Odyssey system (LI-COR

Biosciences) with the 800nm channel. The integrative intensity of detected bands was obtained

using software provided with the infrared imaging system (LI-COR Biosciences).

Mass spectrometry of protein kinase C isoforms recruited to lipid rafts. Coomassie brilliant

blue and silver staining was used to visualize protein bands on an Odyssey infrared imaging

system. Bands corresponding to PKC (85kDa) were then cut from the gel. Excised bands were

analysed by Liquid Chromatography/Mass Spectrometry/Mass Spectrometry (LC-MS/MS)

(Johnson-Henry, Wallace et al. 2001). Protein sequence data generated from the experimental

samples were analyzed by Sequest® software and searched against a eukaryotic database created

from the NCBI website (Moore, Young et al. 2002; Johnson-Henry, Hagen et al. 2007).

Data analyses. Results are reported as means ± standard errors of the mean (SEM). To test for

significance between two groups, the two-tailed Student’s t test was employed, with p<0.05

considered as statistically significant. One-way analysis of variance (ANOVA) was used for

data derived from more than two experimental conditions (Bewick, Cheek et al. 2004).

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5.4 Results

Protein kinase C (PKC) is recruited to detergent-resistant microdomains in response to

enterohemorrhagic Escherichia coli infection.

Following E. coli O157:H7 infection of HEp-2 cells, PKC was recruited to the sucrose fraction

containing caveolin-1 (Figure 5.1), which was used as a marker protein for detergent-resistant

microdomains (Shen-Tu, Schauer et al. 2010). PKC movement to detergent-resistant membranes

was not observed when tissue culture cells were infected with boiled bacteria, demonstrating that

recruitment of PKC was triggered by exposure of epithelial cells to live organisms.

Chloramphenicol-treated bacteria also did not induce the movement of PKC to detergent-

resistant microdomains (Figure 5.2), indicating that signalling is induced by newly synthesized

bacterial proteins. Translocation of PKC to detergent-resistant membranes was also observed

when Intestine 407 cells were infected with EHEC O157:H7 (Figure 5.3).

PKC recruitment to lipid rafts is independent of known EHEC virulence factors

An increase in PKC expression in caveolin-enriched fractions was observed in response to

infection with E. coli, strain CL15 (serotype O113:H21), indicating that PKC recruitment to

detergent-resistant microdomains is independent of the attaching and effacing (eae) gene,

because this strain is eaeA negative and does not cause attaching-effacing lesions (Shen et. al.,

2004). Infection of HEp-2 cells with EHEC strain CVD451, a type III secretion-deficient mutant

(Ceponis, McKay et al. 2003), also resulted in increased PKC in detergent-resistant membranes

(Figure 5.4). Similarly, E. coli 85-170, a Stx-1 and Stx-2 negative mutant (Ceponis, McKay et

al. 2003), also demonstrated PKC movement to detergent-resistant, caveolin-1-enriched fractions

(Figure 5.4). Taken together, these findings indicate that PKC movement to detergent-resistant

membranes in infected epithelia is independent of the EHEC type III secretion system and the

production of Shiga-like toxins 1 and 2.

MβCD blocks PKC recruitment to lipid rafts in response to EHEC infection.

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Figure 5.1 PKC is recruited to lipid rafts during EHEC O157:H7 infection. A: Western

blots of protein kinase C from ultracentrifugation fractions of whole cell extracts. The presence

of PKC in the caveolin-1-containing fraction indicates that it is recruited to lipid rafts in response

to bacterial infection. The presence of PKC in fraction 3 of VTEC O113:H21 infected HEp-2

cells indicates that recruitment is independent of the attaching and effacing (eae) gene. The lack

of PKC in fraction 3 of uninfected and boiled EHEC-infected cells demonstrates that live

bacteria are required for recruitment. B: Integrated intensity of PKC expression over caveolin-1

expression in the 3rd

fraction of EHEC-infected and uninfected cells (n=4; *p<0.05). [MOI

100:1; rabbit anti-PKC and rabbit anti-caveolin-1 primary antibody (1:1000); IRDye 800 goat

anti-rabbit secondary antibody (1:20000)]

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Figure 5.2 Newly synthesized bacterial proteins and intact lipid rafts are required for PKC

recruitment to lipid rafts in response to EHEC infection. Western blots of protein kinase C

from ultracentrifugation fractions of whole cell extracts. PKC is not recruited in host cells

infected with chloramphenicol treated EHEC O157:H7, indicating that metabolically active

bacteria are required for host signalling protein recruitment. Migration of lipid rafts to fraction 3

is indicated by the presence of caveolin-1. [MOI 100:1; rabbit anti-PKC and rabbit anti-

caveolin-1 primary antibody (1:1000); IRDye 800 goat anti-rabbit secondary antibody (1:20000)]

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Figure 5.3 Western blots of protein kinase C from ultracentrifugation fractions of whole

cell extracts (Intestine 407 cells). The presence of PKC in the caveolin-1-containing fraction

indicates that it is recruited to lipid rafts in response to bacterial infection. [MOI 100:1; rabbit

anti-PKC and rabbit anti-caveolin-1 primary antibody (1:1000); IRDye 800 goat anti-rabbit

secondary antibody (1:20000)]

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Figure 5.4 Recruitment of PKC is independent of the type III secretion system and the

production of Shiga toxins 1 and 2. The recruitment of PKC to lipid rafts was observed in both

type III secretion mutant, CVD 451, infected and Shiga toxins-negative mutant, 85-170, infected

cells. This suggests that EHEC-induced recruitment of host signalling proteins is independent of

the EHEC type III secretion system and production of shiga toxins. [MOI 100:1; rabbit anti-

PKC and rabbit anti-caveolin-1 primary antibody (1:1000); IRDye 800 goat anti-rabbit

secondary antibody (1:20000)]

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To confirm that EHEC O157:H7-induced translocation of PKC was dependent on an intact lipid

raft microdomain, methyl-β-cyclodextrin (10mM) was employed to pre-treat cells and deplete

cholesterol from the plasma membrane and, thereby, disrupt lipid rafts (Riff, Callahan et al.

2005). Cells subjected to MβCD pretreatment did not result in PKC in caveolin-enriched

microdomains in response to EHEC O157:H7 challenge (Figure 5.5), indicating that intact lipid

rafts likely play a role in epithelial cell PKC signal transduction responses to EHEC infection.

Recruitment of PKC to lipid rafts and AE lesion formation in response to EHEC infection is

blocked by specific inhibitors.

Treatment with the phorbol ester PMA (100nM), which results in the activation of conventional

PKC isoforms (Dries, Gallegos et al. 2007), did not induce translocation of PKC to caveolin-1-

enriched membrane fractions (data not shown). Pre-treatment of epithelial cells with the pan-

PKC inhibitor bisindolylmaleimide I (10mM) for 3 hrs prior to EHEC O157:H7 infection also

did not result in a reduction in PKC movement to detergent-resistant microdomains following

EHEC infection (Figure 5.6). Similarly, cells pre-treated with a low dose of the PKC inhibitor

Gö6983 (10nM) did not block translocation of PKC to lipid rafts in response to EHEC O157:H7

infection. By contrast, epithelial cells pre-treated with a higher dose of PKC inhibitor Gö6983

(60nM) resulted in a reduction in PKC levels in detergent-resistant microdomains (Figure 5.7),

suggesting that an atypical PKC isoform was recruited to lipid rafts in response to EHEC

O157:H7 infection (Cuschieri, Umanskiy et al. 2004). Myristoylated PKC-zeta pseudosubstrate

pre-treated epithelial cells also exhibited a decrease in the amount of PKC recruited to caveolin-

1-enriched membrane fractions in response to EHEC O157:H7 infection (Figure 4.8), indicating

the PKCδ isoform is activated in EHEC-infected epithelial cells. PKCδ is also involved in

EHEC-induced AE lesion formation. In contrast to the observed AE lesions on EHEC-infected

cells pretreated with PKCα pseudosubstrate, infected cells pretreated with PKCδ pseudosubstrate

did not exhibit AE lesions (Figure 4.9).

Recruitment of second messengers to detergent-resistant membranes is inhibited by

pretreatment with Lactobacillus helveticus R0052

Pre-treatment of epithelial cells with Lactobacillus helveticus R0052 3 hr prior to EHEC

O157:H7 infection resulted in a reduction in levels of both PKC and PI3K in detergent resistant

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membranes in response to EHEC O157:H7 infection (Figure 5.10A). Immunoblotting results

were quantified by densitometry and showed a significant reduction in levels of both PKC and

PI3K present in caveolin-1-enriched membrane fractions when epithelial cells were pre-

incubated with L. helveticus R0052 prior to EHEC infection (Figure 5.10B). This effect was

specific, because a similar effects was not observed in epithelial cells pretreated with

Lactobacillus rhamnosus, strain R0011 (Figure 5.10C)

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Figure 5.5 Recruitment of PKC is dependent on intact lipid rafts on the plasma membrane

of host epithelial cells. When lipid rafts are disrupted by depleting cholesterol using MβCD,

there is a decrease in PKC recruitment, indicating that functional lipid rafts are required for

recruitment. [MOI 100:1; rabbit anti-PKC and rabbit anti-caveolin-1 primary antibody (1:1000);

IRDye 800 goat anti-rabbit secondary antibody (1:20000)]

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Figure 5.6 EHEC-induced recruitment of PKC is not blocked by bisindolylmaleimide I.

HEp-2 cells pretreated with bisindolylmaleimide I did not block the recruitment of PKC to lipid

rafts in response to EHEC O157:H7 infection, indicating that the classical and novel isoforms of

PKC are not the ones involved in the infection process. [MOI 100:1; rabbit anti-PKC and rabbit

anti-caveolin-1 primary antibody (1:1000); IRDye 800 goat anti-rabbit secondary antibody

(1:20000)]

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Figure 5.7 PKC inhibitor Gö6983 prevents recruitment of protein kinase C (PKC) to lipid

rafts in response to Escherichia coli O157:H7 infection. Representative western blots of

protein kinase C in ultracentrifugation fractions of whole cell extracts. Migration of lipid rafts to

fraction 3 is indicated by the presence of caveolin-1. PKC recruitment to rafts in both EHEC-

infected and infected cells treated with the PKC inhibitor Gö6983 (at 10 nM) suggests that

neither the classical nor the novel isoforms of PKC are involved in PKC recruitment to lipid rafts

in response to infection. By contrast, a reduction of recruited PKC in infected epithelium treated

with a higher concentration (60 nM) of the same inhibitor indicates that atypical PKC isoforms

are likely involved in EHEC O157:H7 induced protein recruitment. [n=3; MOI 100:1; rabbit

anti-PKC and rabbit anti-caveolin-1 primary antibody (1:1000); IRDye 800 goat anti-rabbit

secondary antibody (1:20000)]

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Figure 5.8 Atypical isoform of PKC is involved in the recruitment of PKC to lipid rafts in

response to EHEC O157:H7 infection. A: Western blots of protein kinase C (PKC) from

ultracentrifugation fractions of whole cell extracts. Cells treated with 60κM of PKC-zeta

inhibitor resulted in a significant decrease in the amount of PKC translocation to lipid rafts in

response to EHEC infection. B: Significant reduction in the amount of PKCδ recruited to lipid

rafts is shown by densitometry of PKC present in lipid raft-containing fraction 3 in cells treated

with 60κM of PKC-zeta pseudosubstrate prior to EHEC O157:H7 infection (MOI 100:1; 1h,

n=4; *P<0.05).

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Figure 5.9 An atypical isoform of PKC is involved in EHEC O157:H7-induced AE lesion

formation. When cells were treated with PKCα pseudosubstrate (60µM) prior to infection,

EHEC-induced actin cytoskeletal rearrangement was still present. However, cells treated with

60κM of PKC-δ pseudosubstrate resulted in amelioration of EHEC-induced attaching-effacing

lesions.

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Figure 5.10 The recruitment of host signalling proteins is blocked by pretreating the cells

with probiotics. Translocation of host signalling molecules PKC in response to EHEC infection

was inhibited when cells were pre-treated with the probiotic A: L. helveticus R0052 (*p<0.05),

but not B: L. rhamnosus strain R0011. These findings indicate that strain R0052 possesses a

factor, absent in strain R0011, that is able to attenuate the infectious process. C: One of the

distinguishing factor, S-layer protein, has been ruled out as the factor inhibiting EHEC-induced

recruitment of host proteins to lipid rafts. [MOI 100:1; rabbit anti-PKC and rabbit anti-caveolin-

1 primary antibody (1:1000); IRDye 800 goat anti-rabbit secondary antibody (1:20000)]

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5.5 Discussion

We have shown, for the first time, that EHEC hijacks epithelial cell membrane lipid

microdomains to recruit and activate second messengers PKC in order to cause intestinal damage

and elicit further pathogenic effects. Such recruitment is not the result of non-bacterially related

external factors, because this phenomenon was only observed when cells were infected with live

microorganisms and not heat-killed bacteria. This recruitment still occurred when epithelial

monolayers were infected with EHEC strain CVD-451, a type III secretion mutant; indicating

that PKC recruitment to lipid rafts is mediated by a non-type III secretion system bacterial

effector. It is known that both EHEC O157:H7 and enteropathogenic Escherichia coli O127:H6

are capable of disrupting intestinal barrier function and cause inflammation in the gut by

manipulating key signaling cascades inside host cells (Guttman, Li et al. 2006).

Previous studies have shown that the presence of cholesterol enriched host plasma membrane

microdomains are required for adherence and pedestal formation by these attaching and effacing

Escherichia coli (Riff, Callahan et al. 2005; Allen-Vercoe, Waddell et al. 2006). When lipid

rafts are disrupted with the cholesterol-sequestering reagent, methyl-β-cyclodextrin, EHEC no

longer induced the translocation of PKC to lipid rafts. This finding provides evidence that

EHEC O157:H7 induces rearrangements in the host cytoskeleton and the formation of adhesion

pedestals by activating PLC-gamma and PI3K pathways via functionally intact lipid raft

signaling complexes.

Cells infected with chloramphenicol treated bacteria to block prokaryotic protein synthesis

(Jandu, Ceponis et al. 2006) did not initiate the recruitment of PKC to lipid rafts during the

infectious process. This finding indicates that new bacterial protein(s) secreted into the culture

medium triggers the recruitment and activation of both PKC to cholesterol-enriched

microdomains in the host cell plasma membrane.

Although production of Shiga toxins is reported to promote bacterial colonization in human

intestine (Robinson, Sinclair et al. 2006), the ability of EHEC O157:H7 to elaborate Shiga-like

toxins did not play a role in recruiting PKC to lipid rafts (Proulx, Seidman et al. 2001).

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Phospholipase Cγ also plays a role in microbial-host interactions following pathogenic E. coli

infection, triggering an increase in intracellular calcium (Kenny and Finlay 1997). This pathway

mediates EHEC-induced attaching-effacing lesions (Johnson-Henry, Wallace et al. 2001). The

downstream second messenger, protein kinase C (PKC), was found in lipid rafts one hour post

EHEC infection. This finding shows that PKC also plays key role in the regulation of

cytoskeleton dynamics in response to infection, leading to the formation of attaching-effacing

lesion formation and the disruption of inter-cellular tight junctions (Tomson, Koutsouris et al.

2004).

Protein kinase C has been implicated in the regulation of diverse cellular events (Dempsey,

Newton et al. 2000). Due to its complex functions in the cell, complementary experimental

approaches have been developed to investigate the biology of PKC. Traditionally, both

antibodies and inhibitors have been used to study the expression, as well as the activity, of PKC

in cells in the presence of specific stimuli (Mochly-Rosen, Henrich et al. 1990; Disatnik, Buraggi

et al. 1994). Protein kinase C comprises a complex family of serine/threonine protein kinases

involved in the regulation of multiple cellular responses (Dempsey, Newton et al. 2000). There

are three PKC subfamilies and approximately 12 isoforms currently identified, which are

activated and translocated through differential mechanisms (Steinberg 2004).

The possibility of atypical PKC, instead of classical PKC, involvement in EHEC O157:H7

infectious process was first suggested when the positive control phorbol 12-myristate 13-acetate

(PMA), as a surrogate of DAG (Foey and Brennan 2004), did not activate and translocate PKC

from the cytosol to lipid rafts. Similarly, pre-treating cells with a classical PKC inhibitor

(Cuschieri, Umanskiy et al. 2004), bisindolylmaleimide I, prior to infection did not result in the

inhibition of EHEC-induced translocation of PKC to lipid rafts. Cells pretreated with the lower

dosage of the concentration dependent PKC inhibitor Gö6983 also verified this result.

Furthermore, the higher dosage of Gö6983 significantly reduced the amount of PKC recruited to

lipid rafts in response to EHEC O157:H7 infection, indicating that EHEC was activating PKCδ

through lipid rafts. Finally, a highly specific myristolated PKCδ pseudosubstrate confirmed that

PKCδ was the PKC isoform responding to EHEC challenge of epithelial cells.

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The atypical isoform of PKC, including PKC, are key regulators of critical intracellular

siganlling pathways induced by extracellular stimuli (Hirai and Chida 2003). Recent studies

show that PKCδ controls colonic epithelial cell proliferation (Umar, Sellin et al. 2000), regulates

tight junctions (Tomson, Koutsouris et al. 2004), and mediates the activation of host immune

responses to bacterial infection (Savkovic, Koutsouris et al. 2003). Further studies in appropriate

animal models (Duran, Rodriguez et al. 2004) now have to be conducted to confirm the specific

roles of PKCδ in the pathobiology of EHEC-induced disease.

The adhesion of enteric pathogens to intestinal epithelial cells can also be blocked as an

alternative way to interrupt the infectious process (Collado, Meriluoto et al. 2007). Side effects

and resistance to antibiotics has prompted studies investigating whether beneficial organisms,

referred to as probiotics (29), can act as a barrier to infection by preventing colonization of

enteric pathogens (Sherman, Ossa et al. 2009). Probiotics, including Lactobacillus helveticus,

strain R0052 prevent E. coli O157:H7-mediated pathogenesis in vitro (Sherman, Johnson-Henry

et al. 2005) and the pathobiology of Citrobacter rodentium infection in a murine model of

infection in vivo.

There is an increasing literature indicating that probiotics can be used as treatment for a spectrum

of intestinal diseases. For instance, in animal models of inflammatory bowel disease,

Lactobacillus plantarum stabilizes the mucosal barrier and prevents gut inflammation in the

interleukin-10 gene knockout mouse model of colitis (Kennedy, Kirk et al. 2001; Schultz,

Veltkamp et al. 2002). Other bifidobacteria and lactobacilli decrease intestinal

permeability(Johnson-Henry, Donato et al. 2008), enhance mucosal IgA responses (Chen, Louie

et al. 2005), and increase levels of anti-inflammatory cytokines (Lamine, Eutamene et al. 2004).

Evidence also suggests that mixtures of probiotics can reduce relapse rates in the setting of

pouchitis in humans (Guslandi, Mezzi et al. 2000; Guslandi, Giollo et al. 2003; Rolfe, Fortun et

al. 2006)In this study, epithelial cell monolayers pre-incubated with probiotics inhibited EHEC

from hijacking host membrane rafts and manipulating PKC signalling pathways.

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Chapter 6.

Discussion, Future Directions, and Significance

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6.1 Discussion

Enterhemorrhagic Escherichia coli (EHEC) is one of the most important food-borne pathogens

and its clinical outcomes pose a huge health care burden on society (Manning, Motiwala et al.

2008). EHEC O157:H7 is the most prevalent EHEC serotype in North America contributing to

>75,000 human infections, approximately 5,000 deaths, and an average of 17 outbreaks a year.

Some of the major outbreaks over the years include: the 1993 outbreak in western North

America due to ingestion of undercooked ground hamburger purchased at a fast food chain

(CDC 1993), the large 1996 outbreak in Japan related to contaminated radish sprouts, which had

low rates of HUS (Michino, Araki et al. 1999), and the 2006 outbreak related to contaminated

spinach in North America, which had high rates of hospitalization and HUS (CDC 2006). New

routes of infection, such as direct contact with animals in petting zoos and the ability of EHEC to

survive in a variety of food items has become the major sources of new disease outbreaks and are

contributing to the widespread occurrences of outbreaks of the infection (Lim, Yoon et al. 2010).

The treatment of EHEC O157:H7 infection is largely supportive (Panos, Betsi et al. 2006).

Dehydration that is associated with infection is treated with oral or intravenous rehydration to

reduce the stress of volume depletion on kidneys. Anti-diarrheal medications are avoided

because decrease intestinal motility may delay clearance of the pathogen, increase toxin

absorption, and increase the risk or severity of HUS (Wong, Jelacic et al. 2000). Most common

preventative strategies include avoiding eating undercooked ground beef and avoiding the

consumption of unpasteurized milk and unchlorinatied water.

Several studies have shown that antibiotics are not efficacious as treatment for EHEC infections

(Kimmitt, Harwood et al. 2000). Mechanisms that have been postulated to explain the

ineffectiveness: antibiotics may eliminate competing intestinal microflora leading to overgrowth

and colonization of EHEC O157:H7; antibiotics can cause lysis of the bacteria followed by the

release of toxins that then can be absorbed systemically; or antibiotics might induce the

expression of toxin encoding genes. Clinical studies have shown that the use of antibiotics is

associated with longer duration of bloody diarrhea in patients, increases the risk of developing

HUS, and enhances acquisition of a secondary person-to-person EHEC O157:H7 infection with

an increased mortality rate (Carter, Borczyk et al. 1987).

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It is unclear why the severity of EHEC outbreaks, illness, and frequency varies dramatically in

various outbreaks, but this point out the need for better EHEC detection ability, swiftness of

diagnosis, and enhanced treatment regimens. In order to see improvements in all these aspects of

management, a better understanding of the disease and underlying infection mechanisms are

needed.

Host cell responses against EHEC O157:H7 infection are diverse and intricate (Bhavsar,

Guttman et al. 2007). There are multiple signalling molecules involved in orchestrating host

responses including: the development of mucosal injury, cytoskeleton rearrangements, and the

disruption of tight junction integrity. Attaching and effacing Escherichia coli infection of

intestinal epithelial cells induces an inflammatory response in which NF-θB is activated and

induces upregulation of the chemokine CXCL-8 (previously referred to as intereukin-8)

expression (Gobert, Vareille et al. 2007).

An association between osteopontin (OPN) and chronic inflammatory bowel diseases (IBD) was

recently assessed using dextran sodium sulphate (DSS) to induce colitis in both wild-type and

OPN knock-out mice, but the results presented in published studies are conflicting (da Silva,

Pollett et al. 2006; Heilmann, Hoffmann et al. 2008; da Silva, Ellen et al. 2009). Our interest

was defining association between OPN and gut inflammation, using Citrobacter rodentium as a

murine model of infectious colitis. In the absence of OPN, there was a decrease in bacterial

colonization and colonic epithelial cell hyperplasia. This protective effect was associated with a

reduction in actin dense foci directly underneath the adherent C. rodentium both in vitro and in

vivo. These findings indicate that OPN may be either directly or indirectly involved in mediating

bacterial attachment to host intestinal epithelial cells.

Most previous studies looking at the function of OPN suggest that OPN plays a key role in

inflammatory regulation, because disease is attenuated when OPN is absent and OPN is involved

in integrin adhesion (Kon, Ikesue et al. 2008), inflammatory cell chemotaxis (Zhu, Suzuki et al.

2004), and in enhanced neutrophil function (Koh, da Silva et al. 2007). Our findings highlight

the immune regulatory role of OPN in response to C. rodentium infection, because there was a

reduction in the increase of IFN in OPN-/- mice. This demonstrates that OPN serves as a

crucial mediator of innate immune function. There was partial restoration of the WT phenotype

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with exogenous, intrarectal administration of OPN, but this also suggests the possibility that

intracellular OPN may play a role in C. rodentium-induced disease pathogenesis. These evidence

also indicate that C. rodentium can also hijack host cell inflammatory responses against the

pathogen to elicit host damage (Croxen and Finlay 2010). Host immune mechanism involving

OPN is being hijacked by C. rodentium to induce disease and injury to the intestine. Ways in

which microbial pathogens hijack host machinery to elicit disease and the host molecules used

by EHEC and C. rodentium are still largely unclear. This project has shown that host membrane

rafts provide a means for EHEC and C. rodentium to usurp host signalling molecules for

inducing host injury.

An increase in IP3 response is observed in EHEC O157:H7-infected epithelial cells (Frankel,

Phillips et al. 1998). Infection of HEp-2 cells with EHEC O157:H7, strain CL56 triggers

hydrolysis of phosphatidylinositol 4,5-bisphosphate into IP3 and diacylglycerol (DAG) (Dytoc,

Fedorko et al. 1994; Foubister, Rosenshine et al. 1994). This increase in IP3 causes an increase

in flux of intracellular Ca2+

(Ismaili, Philpott et al. 1995) which, together with the elevated

concentration of DAG, activates protein kinase C. Phosphoinositide mediated signal

transduction pathways play a crucial role in actin remodeling and plasma membrane dynamics

(Di Paolo, Lenci et al. 2006). Several intracellular pathogens interfere with phosphoinositide

signalling cascades to invade into host eukaryotic cells. Induction of A/E lesion formation by

EHEC is associated with changes in the host cell signal transduction machinery.

Our laboratory has shown previously that depletion of cellular cholesterol, using methyl-β-

cyclodextrin inhibits EHEC O157:H7-induced A/E lesions. The pathogenic effects of EHEC are

restored when epithelial cells grown in tissue culture are allowed to recover cholesterol (Riff,

Callahan et al. 2005). These findings suggest that lipid rafts are required for bacterial adherence

and A/E lesion formation. Using a series of pharmacological inhibitors of cell-signalling, our

laboratory also previously identified that enzymes, including phospholipase C-γ (PLC-γ) and

phosphoinositide 3-kinase (PI3K), could be involved in the signal transduction cascades leading

to cytoskeletal rearrangements in response to EHEC O157:H7 infection (Johnson-Henry,

Wallace et al. 2001).

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Herein, we now provide additional experimental evidence that EHEC O157:H7 infection induces

the recruitment of host signalling molecules, including PI3K and PKC, to lipid rafts leading to

AE lesion formation. Such recruitment is dependent on the integrity of host cell plasma

membrane rafts. Sequestering cholesterol and, thereby, disrupting the structure of lipid rafts

decreases the ability of EHEC O157:H7 to efficiently activate host signalling pathways involving

both PI3K and PKC to elicit its pathogenic effects.

Live and metabolically active bacteria are necessary for the mobilization of PKC and PI3K to

lipid rafts. Translocation of PKC and PI3K to lipid rafts is independent of the eaeA (intimin)

gene, type III secretion system, and production of Shiga-like toxins. Bacterial factors secreted

into culture supernatants and conditioned medium did not induce the translocation of host

signalling proteins to lipid rafts. This result suggests either a structural feature or bacteria

surface membrane protein that is eliciting the recruitment of host proteins to lipid rafts in

response to EHEC infection. . Interestingly, EHEC O157:H7 did not activate Akt, the common

downstream molecule from PI3K. This suggests that the mobilization of PI3K to lipid rafts

likely is associated with activation of alternative signal transduction pathways, such as small

GTPases (Zeidan, Paylor et al. 2007), to induce pedestal formation underneath intimately

adherent bacteria.

The mobilization of PKC to lipid rafts in response to EHEC O157:H7 infection was inhibited by

specific PKC isoform inhibitors. By using concentration-dependent PKC isoform-specific

inhibitors and myristoylated PKC pseudosubstrate, PKC was found to be the activated in

response to EHEC infection. This suggests that atypical PKC could play a role in the

pathogenesis of EHEC O157:H7infection - similar to its role in the pathogenesis of other

pathogenic bacteria, such as Helicobacter pylori (Tan, Tompkins et al. 2009), Staphylococcus

aureus (Ohnemus, Kohrmeyer et al. 2008), Mycobacterium tuberculosis (Yang, Lee et al. 2007),

and non-typhoidal Salmonellae (Procyk, Rippo et al. 1999).

EHEC O157:H7 does not colonize the gut or cause disease in mice, unless the animals are pre-

treated with broad-spectrum antibiotics (Wadolkowski, Burris et al. 1990). Therefore, C.

rodentium is widely used as an animal model to study the infection mechanisms of virulence of

non-invasive A/E organisms (Vallance, Deng et al. 2003).

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NPC-/- mice serve as an animal model to delineate the role of lipid rafts in an in vivo setting.

The lack of lipid rafts in a gene knockout mouse results in colonization delay and adherence of

C. rodentium to the colonic mucosa (12 vs. 6 days in NPC-/- and wild type mice, respectively)

and the delayed appearance of C. rodentium-induced AE lesions. These findings indicate that

lipid rafts play a role in both the adhesion of non-invasive, pathogenic bacteria to intestinal

epithelial cells as well as initiating signalling cascades in host cells to induce AE lesion

formation.

NPC-/- mice also showed a reduction in colonic epithelial cell hyperplasia in response to C.

rodentium infection, compared to wild-type-infected mice. This reduction was a result of a

decrease in mitotic cells and a decrease in the size of the proliferation zone in NPC-/- mice in

comparison to wild-type mice. A decrease in proinflammatory cytokine response in infected

NPC-/- mice was also observed; specifically, levels of IFN- and IL-12.

OPN could directly mediate bacterial adherence and actin cytoskeleton rearrangement leading to

AE lesions. OPN could also act in conjunction with its receptor CD44 to mediate the

pathogenesis of EHEC O157:H7 and C. rodentium infections. Alternatively, OPN could mediate

AE lesion formation and tight junction disruption via its association with EHEC-activated host

signalling pathways, involving lipid raft microdomains and signalling molecules such as PLC,

PI3K, and isoforms of PKC (Figure 6.1).

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Figure 6.1 Schematic diagram of suggested infectious process of EHEC O157:H7, leading

to AE lesion formation and barrier disruption. EHEC O157:H7 attach and intimately adhere

to host cell surface in close proximity to lipid raft microdomains where the TTSS is activated and

various bacterial virulence factors are secreted. These secreted virulence factors act to induce

the translocation of host signalling proteins to lipid rafts thereby activating downstream

signalling cascades involving PI3K, PKC, and OPN, leading to cytoskeletal rearrangements,

attaching-effacing lesions, and tight junction disruption.

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6.2 Future Directions

Host cell factors likely play a crucial role in recruiting PKC and PI3K to lipid rafts in response to

EHEC O157:H7 infection. For instance, PKC is one of the major signalling proteins that leads to

NF-θB activation in response to bacterial infections (Savkovic, Koutsouris et al. 2003).

Therefore, cyclohexamide (10κg/ml; Sigma) could be used to halt eukaryotic de novo protein

synthesis and, thereby, determine if new host cell protein synthesis is involved in the observed

recruitment of PKC and PI3K in response to EHEC O157:H7 infection (Sanfilippo, Chirimuuta

et al. 2004). Moreover, PKC might serve as a downstream target of PI3K signalling in response

to EHEC infection. A co-immunoprecipitation experiment would be able to determine if PI3K

and PKC physically act in conjunction following EHEC infection in the formation of AE lesions

and tight junction disruption.

The contribution of various PKC isozymes to the pathogenesis of Escherichia coli O157:H7

infection still remains unclear. Recent studies, using in vitro models, indicate that PKC likely

plays crucial role in EHEC-induced signalling responses, which leading to A/E lesions formation

(Johnson-Henry, Wallace et al. 2001), disruption of barrier function (Ceponis, Riff et al. 2005),

and activation of pro-inflammatory cytokines (Savkovic, Koutsouris et al. 2003).

Transgenic mouse models have been used to detect the functional activities of individual PKC

isozymes (Dorn, Souroujon et al. 1999; Reyland, Anderson et al. 1999; Fields, Murray et al.

2003) For instance, PKCε is suggested to play a role in myocardial infarction and in heart failure

(Koyanagi, Noguchi et al. 2007). Atypical PKCδ controls colonic epithelial cell proliferation

(Umar, Sellin et al. 2000). To corroborate my in vitro findings of the involvement of protein

kinase C in EHEC O157:H7 infection, an animal model of infection can now be used. There are

several PKC knockout mice available commercially (ie. PKCα, , and ) and PKCδ knockout

mice have been described (Martin, Duran et al. 2002). Such mice should now be used to further

delineate the role of PKC-mediated signalling in response to C. rodentium infection.

To complement studies using gene knockout mice, relatively specific pharmacological inhibitors

can be orally administered to wild-type, C. rodentium-infected mice (Table 6.1)

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Table 6.1 PKC inhibitors used in vitro, in vivo, as well as in human studies

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(Birchall, Bishop et al. 1994; Wakasaki, Koya et al. 1997; Koya, Haneda et al. 2000; Hambleton,

Hahn et al. 2006; Mendez-Samperio, Alba et al. 2007). Previous studies by Birchall et al. (1994)

showed that an orally administered, selective inhibitor of PKC was effective in preventing T-cell

activation in rats leading to chronic inflammatory responses in vivo. Studies by Chmura et al.

(2000) showed that mice with tumour cells injected into their hind limbs followed by treatment

with a selective PKC inhibitor, chelerythrine chloride (Sigma Chemical Corp., St. Louis, MO),

resulted in tumour regression. Future studies could employ chelerythrine chloride in the C.

rodentium infection model to determine the function of PKC in the pathogenesis of attaching-

effacing bacterial infection in vivo.

Short interfering RNA (siRNA) can also be used to knock down atypical PKCs in mice prior to

infection (Parkinson, Le Good et al. 2004). In recent years, numerous studies have been

conducted to find more efficient ways to deliver siRNAs to target organs; however, silencing

genes are still limited by the stability of siRNAs molecules in vivo and limited efficiency of their

up-take by target cells and tissues (Dillon, Sandy et al. 2005). However, more recent evidence

provides for an efficient method of siRNA delivery in mice (Baregamian, Rychahou et al. 2007).

These siRNA pretreated mice could then be subjected to C. rodentium infection, as described in

this thesis.

Even though our recent findings indicate that OPN plays a role in EHEC and C. rodentium-

induced AE lesion formation and in vivo colonic epithelial cell hyperplasia, its precise

mechanism of action remains unknown. Further biochemical analysis is required to determine if

OPN is directly involved in EHEC-induced host signalling cascades leading to its pathogenic

effects and whether lipid rafts are required for the activation and recruitment of OPN to AE

lesions. The presence of CD44, the receptor for OPN, in host cell membrane lipid microdomains

during EHEC infection should be analyzed and downstream targets should also be deduced using

complementary co-immunoprecipitation and immunostaining experimental techniques.

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6.3 Significance

Defining the function of lipid-rich membrane microdomains, which mediates signal transduction

pathways such as PLC, PI3K, PKC, and OPN is required to better define host responses to

EHEC O157:H7 infection. . Such knowledge could lead, ultimately, to the development of novel

strategies to interrupt the infectious process and reduce the complications of human disease

(D'Adamo 2009). By investigating the role of cholesterol-rich lipid rafts and host signalling

molecules, in the pathogenesis of C. rodentium in a murine model of AE infection, can further

contribute to current understanding of host-microbe interactions.

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Chapter 7.

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