Microsporins A and B: new histone deacetylase inhibitors from the marine-derived fungus Microsporum cf. gypseum and the solid-phase synthesis of microsporin A |
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| Authors: | Wenxin Gu Paul R Jensen Richard B Silverman |
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| Institution: | a Department of Chemistry, Department of Biochemistry, Molecular Biology, and Cell Biology, Center for Drug Discovery and Chemical Biology, Northwestern University, Evanston, IL 60208-3113, USA
b Center for Marine Biotechnology and Biomedicine, Scripps Institution of Oceanography, University of California, San Diego, La Jolla, CA 92093-0204, USA |
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| Abstract: | Two new cyclic peptides, microsporins A and B (7 and 8), were isolated from culture extracts of the marine-derived fungus Microsporum cf. gypseum obtained from a sample of the bryozoan Bugula sp. collected in the U.S. Virgin Islands. The structures of the new compounds were determined by extensive interpretation of 2D NMR data and by chemical methods. Microsporins A and B are potent inhibitors of histone deacetylase and demonstrate cytotoxic activity against human colon adenocarcinoma (HCT-116), as well as against the National Cancer Institute 60 cancer cell panel. The total synthesis of microsporin A on solid-phase is also reported. |
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| Keywords: | Microsporum gypseum Marine fungus Cyclic tetrapeptide Histone deacetylase Aoda Cytotoxins Solid-phase synthesis |
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