Divergolides T–W with Apoptosis-Inducing Activity from the Mangrove-Derived Actinomycete <i>Streptomyces</i> sp. KFD18
Li-Man Zhou,
Fan-Dong Kong,
Qing-Yi Xie,
Qing-Yun Ma,
Zhong Hu,
You-Xing Zhao,
Du-Qiang Luo
Affiliations
Li-Man Zhou
College of Life Science, Key Laboratory of Medicinal Chemistry and Molecular Diagnosis of Ministry of Education, Hebei University, Baoding 071002, China
Fan-Dong Kong
Hainan Key Laboratory for Research and Development of Natural Product from Li Folk Medicine, Institute of Tropical Bioscience and Biotechnology, Chinese Academy of Tropical Agricultural Sciences, Haikou 571101, China
Qing-Yi Xie
Hainan Key Laboratory for Research and Development of Natural Product from Li Folk Medicine, Institute of Tropical Bioscience and Biotechnology, Chinese Academy of Tropical Agricultural Sciences, Haikou 571101, China
Qing-Yun Ma
Hainan Key Laboratory for Research and Development of Natural Product from Li Folk Medicine, Institute of Tropical Bioscience and Biotechnology, Chinese Academy of Tropical Agricultural Sciences, Haikou 571101, China
Zhong Hu
Guangdong Provincial Key Laboratory of Marine Biotechnology, Department of Biology, Shantou University, Shantou 515063, China
You-Xing Zhao
Hainan Key Laboratory for Research and Development of Natural Product from Li Folk Medicine, Institute of Tropical Bioscience and Biotechnology, Chinese Academy of Tropical Agricultural Sciences, Haikou 571101, China
Du-Qiang Luo
College of Life Science, Key Laboratory of Medicinal Chemistry and Molecular Diagnosis of Ministry of Education, Hebei University, Baoding 071002, China
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 µM, 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.
