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Bioorg Med Chem. 2011 Nov 15;19(22):6570-5. doi: 10.1016/j.bmc.2011.05.044. Epub 2011 May 30.

Bendigoles D-F, bioactive sterols from the marine sponge-derived Actinomadura sp. SBMs009.

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  • 1Department of Microbial Natural Products, Helmholtz Institute for Pharmaceutical Research Saarland (HIPS) and Saarland University, Saarbrücken, Germany.

Abstract

Marine derived actinomycetes have become an important source of bioactive natural products. Here we report the structure and bioactivity of the bendigoles D-F (1-3), 3-keto sterols isolated from the new marine sponge derived bacterium, Actinomadura sp. SBMs009. The isolation of these compounds was guided by a novel high-content screen for NF-κB and glucocorticoid receptor (GR) activity, and cytotoxicity assays. The structures of 1-3 were determined by detailed analysis of NMR, MS, and single crystal X-ray diffraction data. Interestingly, 1 displayed cytotoxicity against the L929 (mouse fibroblast) cell line with an IC(50) approximated to 30 μM and was the most active inhibitor of GR-translocation, while 3 was the most effective inhibitor of NF-κB nuclear translocation with an IC(50) of 71 μM.

Copyright © 2011 Elsevier Ltd. All rights reserved.

PMID:
21684166
[PubMed - indexed for MEDLINE]
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