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

1
College of Life Science, Key Laboratory of Medicinal Chemistry and Molecular Diagnosis of Ministry of Education, Hebei University, Baoding 071002, China
2
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
3
Guangdong Provincial Key Laboratory of Marine Biotechnology, Department of Biology, Shantou University, Shantou 515063, China
*
Authors to whom correspondence should be addressed.
These authors contributed equally to this paper.
Mar. Drugs 2019, 17(4), 219; https://doi.org/10.3390/md17040219
Received: 19 March 2019 / Revised: 5 April 2019 / Accepted: 8 April 2019 / Published: 11 April 2019
(This article belongs to the Collection Marine Compounds and Cancer)
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Abstract

Four new ansamycins, named divergolides T–W (14), 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 14 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. View Full-Text
Keywords: mangrove-derived actinomycete; ansamycins; divergolides; apoptosis-inducing activity mangrove-derived actinomycete; ansamycins; divergolides; apoptosis-inducing activity
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Zhou, L.-M.; Kong, F.-D.; Xie, Q.-Y.; Ma, Q.-Y.; Hu, Z.; Zhao, Y.-X.; Luo, D.-Q. Divergolides T–W with Apoptosis-Inducing Activity from the Mangrove-Derived Actinomycete Streptomyces sp. KFD18. Mar. Drugs 2019, 17, 219.

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