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    ANTITUMOUR - VINCA

    BYS.PRIYADHARSHINI.

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    Common names:Periwinkle, pin-wheel flower.Botanical synonyms: Catharanthusroseus,

    Lochnera rosea.

    Tamil name is Nithiya kalyani.

    Perennial herb.

    Everblooming with flowers commonly rose-purple or white.

    Seen to grow even in cracks of concrete

    paves.

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    Antimitotic Agents: One Possible TreatmentAnti-tumor agents that inhibit the function of microtubules

    through the binding of their subunits or through directcessation of their growth.

    Microtubules(MTs):Protein polymers formed by a-Tubulin and b-tubulin

    heterodimers that play an important role in critical cell

    functions such as movement, phagocytosis and axonal

    transport. They also play a key role in the formation of the

    mitotic spindle apparatus and cytokinesis at the end of

    mitosis.

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    In normal cells, microtubules are formed when a cell starts

    dividing during mitosis. Once the cell stops dividing,microtubules are broken down or destroyed.

    Anti-Cancer Plant Alkaloids:Tubulin-Binding Agents

    Vinca Alkaloids: The cellular mechanism of action of vincaalkaloids is the prevention of microtubule assembly, causingcells to arrest in the late G2 phase by preventing formation of

    mitotic filaments for nuclear and cell division.

    Vinblastine,vincristin, vindesine and vinorelbine are allalkaloids derived from the periwinkle plant (Vinca rosea).

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    Vinca Alkaloids (Second Antimitotic Group):

    The Vincas work through their ability to bind to the B-

    tubulin subunit of microtubules, blocking their ability to

    polymerize with the a-tubulin subunit to form complete

    microtubules.

    This causes the cell cycle to arrest in metaphase

    because, in absence of an intact mitotic spindle,

    duplicated chromosomes cannot align along the division

    plate. The ultimate fate of such cells is to undergoapoptosis.

    The Vinca alkaloids are all derived from the

    Madagascan periwinkle plant, Vinca rosea.

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    Scientists first observed its anticancer properties in

    a lab in 1962 with the observation of regression oflymphocytic leukemia in rats.

    Indication:

    Vinblastine-used in combination with Bleomycin andCisplatin for metastatic testicular tumors.

    Vincristine - used in combination with prednisone to

    induce remission in childhood leukemia.

    Vinorelbine -used to treat non-small-cell lung cancer

    and breast cancer.

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    Vinblastine:Vinblastine [Velban] was the first of the Vincas to be usedin the treatment of cancer.

    Useful in the treatment of: bladder and testicular cancers,Kaposis sarcoma, neuroblastoma and Hodgkins disease.

    Side effects include: leukopenia, GI disturbances,cellulitis, phlebitis.

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    STRUCTURE OF VINBLASTINE

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    Vincristine:

    Vincristine [Oncovin]

    Useful in the treatment of: pediatric leukemias and lymphomas,

    non-Hodgkins lymphoma, neuroblastoma and rhabdomyosarcoma.

    Better tolerated by children than adults.

    Side effects: myelosuppression, hyponatremia, numbness/tingling ofextremities, loss of deep tendon reflexes, and loss of motor function.

    Intrathecal administration results in fatal central neurotoxicity.

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    STRUCTURE OF VINCRISTINE

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    Vinorelbine:

    Vinorelbine [Navelbine]

    Used in the treatment of: lung carcinoma, breast cancer.

    Side effects include: granulocytopenia, thrombocytopenia,

    myelosuppression, and less neurotoxicity than all of the

    other Vincas.

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    STRUCTURE OF VINORELBINE

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    Vindesine:Vindesine [Eldisine]

    Useful in the treatment of: breast and lung cancer,leukemia.

    Side effects: immunodeficiency, anemia, myalgia,

    fatigue, mouth ulcers, GI upset.

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    STRUCTURE OF VINDESINE

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