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  • Title: Bendigoles D-F, bioactive sterols from the marine sponge-derived Actinomadura sp. SBMs009.
    Author: Simmons L, Kaufmann K, Garcia R, Schwär G, Huch V, Müller R.
    Journal: Bioorg Med Chem; 2011 Nov 15; 19(22):6570-5. PubMed ID: 21684166.
    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.
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