12 有糸分裂阻害物質リゾキシンおよび関連化合物の構造と作用

概要

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Rhizoxin (1a) is a novel 16 membered anti-fungal and anti-tumor macrolide isolated from Rhizopus chinensis, the pathogen of the rice seedling blight. The fungus produced also the homologues, 1b-3b, 4 and 5. Biosynthesis of rhizoxin was studied and incorporation of 1 mole serine, 12 moles acetate and 6 methionin methyls was established by feeding experiment using ^<13>C labeled precursors. Rhizoxin inhibited the mitosis the tumor cells in a manner similar to that of vincristine and showed similar chemoterapeutic effect to those of vicristine. The mode of action of rhizoxin was investigated. In vitro polymerization of microtubule proteins purified from prcine brains was completely inhibited at a 10×10^<-6>M concentration of rhizoxin. Activity of rhizoxin against tubulin polymerization was compared with those other antitubulin drugs such as colchcine, vinblastine and ansamitocin P-3. The homologues of rhizoxin, 1b-3b, also inhibited grouth of rice seedling roots and of P. oryzae similarly. Anti-tubulin activities of these compounds were also the same extent as rhizoxin.
天然有機化合物討論会の論文
1986-09-09