34 変異株によるChartreusin関連新規抗生物質の創製(口頭発表の部)

概要

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In the screening of microbial metabolites active against tumors, we found that Streptomyces chartreusis D329 produced chartreusin(1). Though 1 itself was not utilized clinically, elsamicin A(2) (one of natural products) showed high therapeutic activities against murine tumor and was expected to be useful based on its antitumor activities. Therefore, we tried to mutate the Streptomyces with N-methyl-N'-nitro-N-nitrosoguanidine in order to produce the novel antibiotics related to 1. From analyses of about 3500 strains, we found a mutant strain (D329-185 strain, FERM BP-3269) which produced demethylchartreusin (3) and D329C compound (4). As a result of further analysis of the other products in the fermentation broth of the mutant strain, novel chrymutasin A (5), B (6) and C (7) were isolated. The structure of 4 was determined from spectral studies in comparison with 1. The structures of 5, 6 and 7 were determined from spectral studies, incorporation studies of ^<13>C-labeled-acetates and the synthesis of derivative. Compound 5 showed the strongest cytotoxicities among 4, 5, 6 and 7, and hence antitumor activities of 5 in vivo were assayed. Compound 5 showed that the T/C value was 173% against Meth A murine fibrosarcoma (ip-ip).
天然有機化合物討論会の論文
1993-09-10