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    Isolation of a new vinca alkaloid from the leaves of Ervatamia microphylla as an inhibitor of ras functions.
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    Abstract:
    A new vinca alkaloid was isolated from a chroloform extract of Ervatamia microphylla leaves as a potent inhibitor of ras functions. The structure of the new alkaloid was elucidated by spectroscopic analysis to be a dimer of aspidosperma-class indoles. The new inhibitor, named III-121C, induced normal morphology in K-ras(ts)-NRK cells at around 0.3 microgram/ml. It also inhibited DNA, RNA, and protein synthesis weakly at 0.3 microgram/ml. It inhibited the growth of K-ras(ts)-NRK cells with IC50s of 0.29, and 0.20 microgram/ml at 33 degrees C and 39 degrees C, respectively. III-121C is the first vinca alkaloid that inhibits ras functions.
    Keywords:
    Vinca
    Vinca alkaloid
    Microgram
    Apocynaceae
    A new indole alkaloid, 11-hydroxypolyneuridine, was isolated from Vinca major subsp. major L. and the known indole alkaloids vallesiachotamine and isovallesiachotamine from Vinca minor L. This is the first report on the alkaloids of both Vinca species growing in Turkey; vallesiachotamine and isovallesiachotamine were isolated from a Vinca species for the first time. V. minor may be considered as a new source for these two alkaloids due to their occurrence in high amount in the aerial parts of the plant. The alkaloid extracts of the two Vinca species were found to have high lipid peroxidation inhibitory and DPPH radical scavenging activities. Anticholinesterase activity of the extracts was also very strong.
    Vinca
    Indole alkaloid
    Apocynaceae
    Vinca alkaloid
    Catharanthus roseus
    Citations (12)
    Vinca minor L. (Apocynaceae) is a medicinal plant that has long been used to treat cerebral and memory disorders in European folk medicine. Furthermore, it contains more than 50 alkaloids, some of them having bisindole structure such as the antineoplastic alkaloids present in Catharanthus roseus (L.) G. Don (Apocynaceae). In this study, the plant's alkaloid extract was divided into three fractions and the cytotoxic effects on cell proliferation of HT-29, Caco-2, T47D, and NIH/3T3 cell lines were examined. All alkaloid fractions showed a dose-dependent cytotoxic effect on the cell lines. IC50 values confirmed that the growth and proliferation of NIH/3T3 cells were less affected in comparison to other cell lines.
    Apocynaceae
    Vinca
    Catharanthus roseus
    Vinca alkaloid
    Citations (24)
    Vinca alkaloids are a set of drugs obtained from the periwinkle plant. They are naturally extracted from the plant Catharanthus roseus, and have hypoglycemic and cytotoxic effects. These are used to treat diabetes, high blood pressure and are also used as disinfectants. The vinca alkaloids are important as they can fight against cancer. The four major vinca alkaloids having medicinal properties are: Vinblastine (VBL), vinorelbine (VRL), vincristine (VCR) and vindesine (VDS). Vinflunine is a new synthetic vinca alkaloid, which has been approved in Europe for the treatment of second-line transitional cell carcinoma of the urothelium. Vinca alkaloids are the second-most-used class of cancer drugs.
    Vinca
    Catharanthus roseus
    Vinca alkaloid
    Vindesine
    Vinorelbine
    Colchicine
    Apocynaceae
    Vindoline
    Citations (10)
    Specific monoclonal antibodies(mAbs) against bis-indole alkaloids related to vinblastine were established to develop a simple and specific immunoassay system for the quantitation of Vinca alkaloids. Vinca alkaloids were extracted from tissue cultured cells of periwinkle plant (Vinca rosea L.). Spleen cells from Balb/c mice immunized with vinblastine-bovine serum albumin(VBL-BSA) conjugate as immunogen were fused with myeloma cells(Sp2/0-Ag.14) in the presence of polyethylene glycol. In the preliminary experiments, 32 clones which highly reacted with VBL-BSA conjugate were selected by ELISA(Enzyme-linked immunosorbent assay). These clones were further analyzed by inhibition assay of ELISA. The results obtained with two typical monoclonal antibodies, KN-1 and KN-2, were described. KN-1 exhibited considerable reactivities with soluble dimeric bis-indole alkaloids, whereas no cross reacted with monomeric bis-indole alkaloids. However KN-2 showed cross reactivity with mono- and di-meric bis-indole alkaloids. Furthermore, KN-1 was applied to the immunoassay system for determining the VBL amounts of in vitro cultured cell extracts. This assay system could detect dimeric vinca alkaloid as low as 0.05 nM.
    Vinca
    Immunogen
    Vinca alkaloid
    Conjugate
    Bovine serum albumin
    Apocynaceae
    Citations (0)
    A new vinca alkaloid was isolated from a chroloform extract of Ervatamia microphylla leaves as a potent inhibitor of ras functions. The structure of the new alkaloid was elucidated by spectroscopic analysis to be a dimer of aspidosperma-class indoles. The new inhibitor, named III-121C, induced normal morphology in K-ras(ts)-NRK cells at around 0.3 microgram/ml. It also inhibited DNA, RNA, and protein synthesis weakly at 0.3 microgram/ml. It inhibited the growth of K-ras(ts)-NRK cells with IC50s of 0.29, and 0.20 microgram/ml at 33 degrees C and 39 degrees C, respectively. III-121C is the first vinca alkaloid that inhibits ras functions.
    Vinca
    Vinca alkaloid
    Microgram
    Apocynaceae
    Citations (52)