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加利利链霉菌合成蒽环类抗生素。II. 通过微生物糖基化获得的新型蒽环类抗生素的结构及生物活性。

Biosynthesis of anthracycline antibiotics by Streptomyces galilaeus. II. Structure of new anthracycline antibiotics obtained by microbial glycosidation and biological activity.

作者信息

Matsuzawa Y, Yoshimoto A, Oki T, Naganawa H, Takeuchi T, Umezawa H

出版信息

J Antibiot (Tokyo). 1980 Nov;33(11):1341-7. doi: 10.7164/antibiotics.33.1341.

Abstract

New anthracycline antibiotics derived from epsilon-, gamma- and beta-rhodomycinones and epsilon-isorhodomycinone by the microbial glycosidation using an aclacinomycin-negative mutant, the strain KE303, of Streptomyces galilaeus MA144-M1 were studied to elucidate their structures and biological activities. These antibiotics were the products in which the anthracyclinones added as precursors were linked at C-7 or C-10 position with the same trisaccharide moiety (cinerulosyl-2-deoxyfucosyl-rhodosaminyl group) as in the parental antibiotic aclacinomycin A. In addition to antimicrobial activity, they exhibited the growth inhibition of cultured L1210 leukemia cells and the marked inhibition against DNA and RNA synthesis.

摘要

利用加利利链霉菌MA144-M1的阿克拉霉素阴性突变株KE303,通过微生物糖基化作用,从ε-、γ-和β-红霉酮以及ε-异红霉酮衍生得到新型蒽环类抗生素,并对其结构和生物活性进行了研究。这些抗生素是以前体形式添加的蒽环酮在C-7或C-10位与和母体抗生素阿克拉霉素A中相同的三糖部分(灰糖基-2-脱氧岩藻糖基-鼠李糖胺基)相连的产物。除了抗菌活性外,它们还表现出对培养的L1210白血病细胞的生长抑制作用以及对DNA和RNA合成的显著抑制作用。

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