A-94964，一种由链霉菌属菌株SANK 60404产生的新型细菌转位酶I抑制剂。I. 分类学、分离及生物活性。

A-94964, a novel inhibitor of bacterial translocase I, produced by Streptomyces sp. SANK 60404. I. Taxonomy, isolation and biological activity.

作者信息

Murakami Ryo, Fujita Yoko, Kizuka Masaaki, Kagawa Tomoka, Muramatsu Yasunori, Miyakoshi Shunichi, Takatsu Toshio, Inukai Masatoshi

机构信息

Exploratory Research Laboratories II, Daiichi-Sankyo Co., Ltd., 1-16-13 Kitakasai, Edogawa-ku, Tokyo 134-8630, Japan.

出版信息

J Antibiot (Tokyo). 2008 Sep;61(9):537-44. doi: 10.1038/ja.2008.71.

DOI:10.1038/ja.2008.71

PMID:19160520

Abstract

Bacterial phospho-N-acetylmuramyl-pentapeptide translocase (translocase I: EC 2.7.8.13) is a key enzyme in peptidoglycan biosynthesis, and a known target of antibiotics. Here we report a novel nucleoside inhibitor against translocase I, A-94964, isolated from the culture broth of the strain Streptomyces sp. SANK 60404. A-94964 inhibited bacterial translocase I with IC50 value of 1.1 microg/ml, and showed antimicrobial activities against Staphylococcus aureus and Enterococcus faecalis with MIC of 100 and 50 microg/ml, respectively. A-94964 did not show cytotoxicity against mammalian cell lines.

摘要

细菌磷酸 - N - 乙酰胞壁酰 - 五肽转位酶（转位酶I：EC 2.7.8.13）是肽聚糖生物合成中的关键酶，也是已知的抗生素作用靶点。在此，我们报道了一种从链霉菌属菌株SANK 60404的培养液中分离得到的新型核苷类转位酶I抑制剂A - 94964。A - 94964抑制细菌转位酶I的IC50值为1.1微克/毫升，对金黄色葡萄球菌和粪肠球菌的抗菌活性的MIC分别为100和50微克/毫升。A - 94964对哺乳动物细胞系未表现出细胞毒性。