Divergolides T–W with Apoptosis-Inducing Activity from the Mangrove-Derived Actinomycete <i>Streptomyces</i> sp. KFD18
Four new ansamycins, named divergolides T–W (<b>1</b>–<b>4</b>), along with two known analogs were isolated from the fermentation broth of the mangrove-derived actinomycete <i>Streptomyces</i> sp. KFD18. The structures of the compounds, includi...
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MDPI AG
2019-04-01
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author | Li-Man Zhou Fan-Dong Kong Qing-Yi Xie Qing-Yun Ma Zhong Hu You-Xing Zhao Du-Qiang Luo |
author_facet | Li-Man Zhou Fan-Dong Kong Qing-Yi Xie Qing-Yun Ma Zhong Hu You-Xing Zhao Du-Qiang Luo |
author_sort | Li-Man Zhou |
collection | DOAJ |
description | Four new ansamycins, named divergolides T–W (<b>1</b>–<b>4</b>), along with two known analogs were isolated from the fermentation broth of the mangrove-derived actinomycete <i>Streptomyces</i> 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 <b>1</b>–<b>4</b> 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 <b>1</b> being the most active while compounds <b>5</b> and <b>6</b> were inactive against all the tested cell lines. Compounds <b>1</b> and <b>3</b> showed very potent and specific cytotoxic activities (IC<sub>50</sub> 2.8 and 4.7 µM, respectively) against the SGC-7901 cells. Further, the apoptosis-inducing effect of <b>1</b> and <b>3</b> against SGC-7901 cells was demonstrated by two kinds of staining methods for the first time. |
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spelling | doaj.art-eeb404d1dac940af81b96516c328c84c2022-12-22T03:10:37ZengMDPI AGMarine Drugs1660-33972019-04-0117421910.3390/md17040219md17040219Divergolides T–W with Apoptosis-Inducing Activity from the Mangrove-Derived Actinomycete <i>Streptomyces</i> sp. KFD18Li-Man Zhou0Fan-Dong Kong1Qing-Yi Xie2Qing-Yun Ma3Zhong Hu4You-Xing Zhao5Du-Qiang Luo6College of Life Science, Key Laboratory of Medicinal Chemistry and Molecular Diagnosis of Ministry of Education, Hebei University, Baoding 071002, ChinaHainan 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, ChinaHainan 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, ChinaHainan 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, ChinaGuangdong Provincial Key Laboratory of Marine Biotechnology, Department of Biology, Shantou University, Shantou 515063, ChinaHainan 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, ChinaCollege of Life Science, Key Laboratory of Medicinal Chemistry and Molecular Diagnosis of Ministry of Education, Hebei University, Baoding 071002, ChinaFour new ansamycins, named divergolides T–W (<b>1</b>–<b>4</b>), along with two known analogs were isolated from the fermentation broth of the mangrove-derived actinomycete <i>Streptomyces</i> 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 <b>1</b>–<b>4</b> 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 <b>1</b> being the most active while compounds <b>5</b> and <b>6</b> were inactive against all the tested cell lines. Compounds <b>1</b> and <b>3</b> showed very potent and specific cytotoxic activities (IC<sub>50</sub> 2.8 and 4.7 µM, respectively) against the SGC-7901 cells. Further, the apoptosis-inducing effect of <b>1</b> and <b>3</b> against SGC-7901 cells was demonstrated by two kinds of staining methods for the first time.https://www.mdpi.com/1660-3397/17/4/219mangrove-derived actinomyceteansamycinsdivergolidesapoptosis-inducing activity |
spellingShingle | Li-Man Zhou Fan-Dong Kong Qing-Yi Xie Qing-Yun Ma Zhong Hu You-Xing Zhao Du-Qiang Luo Divergolides T–W with Apoptosis-Inducing Activity from the Mangrove-Derived Actinomycete <i>Streptomyces</i> sp. KFD18 Marine Drugs mangrove-derived actinomycete ansamycins divergolides apoptosis-inducing activity |
title | Divergolides T–W with Apoptosis-Inducing Activity from the Mangrove-Derived Actinomycete <i>Streptomyces</i> sp. KFD18 |
title_full | Divergolides T–W with Apoptosis-Inducing Activity from the Mangrove-Derived Actinomycete <i>Streptomyces</i> sp. KFD18 |
title_fullStr | Divergolides T–W with Apoptosis-Inducing Activity from the Mangrove-Derived Actinomycete <i>Streptomyces</i> sp. KFD18 |
title_full_unstemmed | Divergolides T–W with Apoptosis-Inducing Activity from the Mangrove-Derived Actinomycete <i>Streptomyces</i> sp. KFD18 |
title_short | Divergolides T–W with Apoptosis-Inducing Activity from the Mangrove-Derived Actinomycete <i>Streptomyces</i> sp. KFD18 |
title_sort | divergolides t w with apoptosis inducing activity from the mangrove derived actinomycete i streptomyces i sp kfd18 |
topic | mangrove-derived actinomycete ansamycins divergolides apoptosis-inducing activity |
url | https://www.mdpi.com/1660-3397/17/4/219 |
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