Bisabosquals, Novel Squalene Synthase Inhibitors I. Taxonomy, Fermentation, Isolation and Biological Activities

KAZUYUKI MINAGAWA; SHUICHI KOUZUKI; KAZUHIDE NOMURA; TAKAHIRO YAMAGUCHI; YOSHIMI KAWAMURA; KEISUKE MATSUSHIMA; HIROYOSHI TANI; KIKUO ISHII; TATSUO TANIMOTO; TOSHIYUKI KAMIGAUCHI

doi:10.7164/antibiotics.54.890

Bisabosquals, Novel Squalene Synthase Inhibitors

I. Taxonomy, Fermentation, Isolation and Biological Activities

KAZUYUKI MINAGAWA, SHUICHI KOUZUKI, KAZUHIDE NOMURA, TAKAHIRO YAMAGUCHI, YOSHIMI KAWAMURA, KEISUKE MATSUSHIMA, HIROYOSHI TANI, KIKUO ISHII, TATSUO TANIMOTO, TOSHIYUKI KAMIGAUCHI

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ジャーナルフリー

2001 年 54 巻 11 号 p. 890-895

DOI https://doi.org/10.7164/antibiotics.54.890

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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 2.5μg/ml, respectively. Bisabosqual C exhibited inhibitory activities similar to bisabosqual A. Bisabosqual A showed broad spectrum antifungal activity in vitro.

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