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Divergolides T-W with Apoptosis-Inducing Activity from the Mangrove-Derived Actinomycete Streptomyces sp. KFD18

文献类型： 外文期刊

作者： Zhou, Li-Man 1 ; Kong, Fan-Dong 2 ; Xie, Qing-Yi 2 ; Ma, Qing-Yun 2 ; Hu, Zhong 3 ; Zhao, You-Xing 2 ; Luo, Du-Qiang 1 ;

作者机构： 1.Hebei Univ, Minist Educ, Coll Life Sci, Key Lab Med Chem & Mol Diag, Baoding 071002, Peoples R China

2.Chinese Acad Trop Agr Sci, Inst Trop Biosci & Biotechnol, Hainan Key Lab Res & Dev Nat Prod Li Folk Med, Haikou 571101, Hainan, Peoples R China

3.Shantou Univ, Dept Biol, Guangdong Prov Key Lab Marine Biotechnol, Shantou 515063, Peoples R China

关键词： mangrove-derived actinomycete; ansamycins; divergolides; apoptosis-inducing activity

期刊名称：MARINE DRUGS （ 影响因子：5.118； 五年影响因子：5.951 ）

ISSN： 1660-3397

年卷期： 2019 年 17 卷 4 期

页码：

收录情况： SCI

摘要： Four new ansamycins, named divergolides T-W (1-4), along with two known analogs were isolated from the fermentation broth of the mangrove-derived actinomycete Streptomyces sp. KFD18. The structures of the compounds, including the absolute configurations of their stereogenic carbons, were determined by spectroscopic data and single-crystal X-ray diffraction analysis. Compounds 1-4 showed cytotoxic activity against the human gastric cancer cell line SGC-7901, the human leukemic cell line K562, the HeLa cell line, and the human lung carcinoma cell line A549, with 1 being the most active while compounds 5 and 6 were inactive against all the tested cell lines. Compounds 1 and 3 showed very potent and specific cytotoxic activities (IC50 2.8 and 4.7 mu M, respectively) against the SGC-7901 cells. Further, the apoptosis-inducing effect of 1 and 3 against SGC-7901 cells was demonstrated by two kinds of staining methods for the first time.

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