科斯他汀，一种来自小单孢菌属TP-A0468的具有抗肿瘤活性的喹诺环素类抗生素。

Kosinostatin, a quinocycline antibiotic with antitumor activity from Micromonospora sp. TP-A0468.

作者信息

Furumai Tamotsu, Igarashi Yasuhiro, Higuchi Hiroko, Saito Noriko, Oki Toshikazu

机构信息

Biotechnology Research Center, Toyama Prefectural University, Kosugi, Japan.

出版信息

J Antibiot (Tokyo). 2002 Feb;55(2):128-33. doi: 10.7164/antibiotics.55.128.

DOI:10.7164/antibiotics.55.128

PMID:12002993

Abstract

Kosinostatin, a quinocycline antibiotic was isolated from the culture broth of an actinomycete strain TP-A0468 along with isoquinocycline B. The producing strain was isolated from the seawater sample collected in Toyama Bay and identified as Micromonospora sp. based on the taxonomic study. Kosinostatin was obtained from the culture fluid by solvent extraction and ODS column chromatography. Kosinostatin inhibited the growth of Gram-positive bacteria strongly (MIC=0.039 microg/ml) and Gram-negative bacteria and yeasts moderately (MIC= 1.56 approximately 12.5 microg/ml). It showed cytotoxicity against various cancer cell lines with the IC50 of 0.02 approximately 0.6 microm and inhibited human DNA topoisomerase Ila with the IC50 of 3 approximately 10 microM.

摘要

嗜盐菌素是一种喹诺环素类抗生素，与异喹诺环素B一起从放线菌菌株TP - A0468的培养液中分离得到。该产生菌是从富山湾采集的海水样本中分离出来的，经分类学研究鉴定为小单孢菌属。嗜盐菌素通过溶剂萃取和ODS柱色谱法从培养液中获得。嗜盐菌素对革兰氏阳性菌有强烈的抑制作用（MIC = 0.039微克/毫升），对革兰氏阴性菌和酵母菌有中等程度的抑制作用（MIC = 1.56至12.5微克/毫升左右）。它对多种癌细胞系具有细胞毒性，IC50为0.02至0.6微摩尔，对人DNA拓扑异构酶IIa的抑制作用IC50为3至10微摩尔。