P-5 Taxodium属およびMaytenus属植物より単離した微小管重合阻害活性を有する新規ジテルペン、トリテルペンの構造と活性(ポスター発表の部)

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Antimitotic agents that inhibit the microtuhule formation and the mitotic arrest of eucaryotic cells, such as paclitaxel and vinblastine, are important components of current anticancer therapy. Paclitaxel is potent polymerization of purified tubulin, causing stabilization and bundling of microtuhules. The antimitotic agents have potential applications in drug development. Recently much effort has been directed to the isolation and synthesis of new antimitotic drugs that target the tubulin/microtubule system and display efficacy against drug-refractory carcinomas. During our search for bioactive compounds targeting the tubulin/microtubules from medicinal plants, we found that the extract from the fruits of Taxodium distichum and bark of Maytenus chuchuhuasca remarkably inhibit the polymerization of tubulin. Further investigation on the extract of T distichum that target tubulin resulted in the isolation of two new abietane-type diterpencs, taxodistines A and B. The structures and relative stereochemistry were elucidated on the basis of 2D NMR data. On the other hands, four known quinoid triterpenes, tingenone, 22β-hydroxytingenone, pristimerin, and celasterol have been isolated from the extract of M. chuchuhuasca which inhibit the polymerization of tubulin. Celasterol with a carboxylic acid and a diosphenol functions potently inhibited the polymerization of tubulin in a concentration-dependent manner. Taxodistine B also showed inhibition of polymerization of tubulin.
天然有機化合物討論会の論文
2007-08-24

P-5 Taxodium属およびMaytenus属植物より単離した微小管重合阻害活性を有する新規ジテルペン、トリテルペンの構造と活性(ポスター発表の部)

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