Bisabosquals, novel squalene synthase inhibitors. I. Taxonomy, fermentation, isolation and biological activities |
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Authors: | Minagawa K Kouzuki S Nomura K Yamaguchi T Kawamura Y Matsushima K Tani H Ishii K Tanimoto T Kamigauchi T |
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Institution: | Shionogi Research Laboratories, Shionogi & Co., Ltd., Osaka, Japan. kazuyuki.minagawa@shionogi.co.jp |
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Abstract: | In the course of screening for yeast squalene synthase inhibitors, bisabosqual A was isolated from the culture broth of Stachybotrys sp. RF-7260. The related compounds bisabosquals B, C and D were also isolated from Stachybotrys ruwenzoriensis RF-6853. Bisabosquals inhibited squalene synthases. IC50 values of bisabosqual A against the microsomal squalene synthases from Saccharomyces cerevisiae, Candida albicans, HepG2 cell and rat liver were 0.43, 0.25, 0.95 and 2.5 microg/ml, respectively. Bisabosqual C exhibited inhibitory activities similar to bisabosqual A. Bisabosqual A showed broad spectrum antifungal activity in vitro. |
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