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Bioactive metabolites from marine-derived Streptomyces sp. A68 and its Rifampicin resistant mutant strain R-M1

Author:
Qin, Le-Le, Zhou, Biao, Ding, Wanjing, Ma, Zhongjun
Source:
Phytochemistry letters 2018 v.23 pp. 46-51
ISSN:
1874-3900
Subject:
Streptomyces, X-ray diffraction, bisphenol A, cell lines, cytotoxicity, enzyme inhibition, fermentation, inhibitory concentration 50, metabolites, mutants, protein kinase C, rifampicin, spectral analysis, stereochemistry
Abstract:
Three new indolocabazole analogues (1-3), one eudesmane-type derivative (4), one bisphenol A propyl ether analogue (5), were purified from the fermentation of the marine- derived Streptomyces sp. A68 and its Rifampicin-resistant mutant strain R-M1. The structures were established through the interpretation of spectroscopic data combined with literature data review. The absolute stereochemistry of 1 was further confirmed by X-ray crystallography analysis. Bioactivity test showed that compounds 1-3 had evident cytotoxic activity towards PC-3 cell lines. Furthermore, 1-3 and 5 also exhibited potent kinase inhibitory activity against PKCα, ROCK II and BTK with IC50 of values ranging from 0.17 to 3.24μM.
Agid:
5915525