海洋链霉菌M518产的新星形孢菌素衍生物的生物活性  

Bioactivity of a new staurosporine derivative from a marine Streptomyces sp. strain M518

作　　者：吴少杰[1,2] 李富超[1] 秦松[1] 赵方庆[1,2] 侯艳华[1,1] Serge Fotso Heinz H.Fiebig Hartmurt Laatsch 

机构地区：[1]中国科学院海洋研究所,青岛266071 [2]中国科学院研究生院,北京100049 [3]Department of Organic and Biomolecular Chemistry, University of G（o）ttingen,Tammannstrasse 2, D-37077 G（o）ttingen, Germany [4]Oncotest GmbH, Am Flughafen 12-14, D-79108 Freiburg, Germany

出　　处：《高技术通讯》2007年第8期874-879,共6页Chinese High Technology Letters

基　　金：863计划（2003AA624020）、青岛市科技计划（05-2-JC-56）和江苏省海洋生物技术重点建设实验室开放课题（2005HS002）资助项目.

摘　　要：从海洋放线菌M518中分离到1个新结构化合物N-甲酰胺基-星形孢菌素（N-carboxamido-staurosporine） （1c）,以及两个同类型已知化合物星形孢菌素（staurosporine）（1a）和N-甲酰基-星形孢菌素（N-formyl-staurosporine）（1b）.为了解新化合物的生物活性,对37株人类肿瘤细胞和9种受试微生物细胞株进行了抑制活性筛选,发现化合物1c具有强烈的抗肿瘤活性,对37株肿瘤细胞的平均抑制浓度IC50,IC70和IC90分别为0.016、0.171和2.352μg·mL-1.其活性强于专利化合物1b.通过测定发现,分离到的三种孢菌素类化合物都具有较好的抗微藻活性.菌株M518经16S rRNA系统进化学分析,属于链霉菌属（Streptomyces sp.）.A new staurosporine derivative, N-carboxamido-staurosporine （lc）, was isolated from a marine actinomycetes strain M518, together with the known compounds N-formyl-staurosporine （1b） and staurosporine （1a）. Anticancer activities against 37 human cancer cell lines of 1b and 1c and antimicrobial activities against 9 microorganisms of 1a, 1b and 1c were tested. The results showed that 1c exhibited stronger anticancer bioactivity than lb. The average IC50, IC70 and IC90 of lc against 37 cell lines were 0.016,0.171 and 2.352μg·mL^-1 respectively. Compounds la, lb and lc also exhibited good inhibitory activity against microalgae. Phylogenetic analysis based on 16S rRNA gene indicated that strain M518 belongs to Streptomyces genus.

关 键 词：星形孢菌素 生物活性 海洋链霉菌 16SrRNA 

分 类 号：TQ457.021[化学工程—农药化工]