Journal of Antibiotics 2005-01-01

Fungal phenalenones inhibit HIV-1 integrase.

Kazuro Shiomi, Ryosuke Matsui, Miki Isozaki, Harumi Chiba, Takahiro Sugai, Yuichi Yamaguchi, Rokuro Masuma, Hiroshi Tomoda, Tomoko Chiba, Hua Yan, Yoshihiro Kitamura, Wataru Sugiura, Satoshi Omura, Haruo Tanaka

文献索引：J. Antibiot. 58(1) , 65-8, (2005)

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摘要

A phenalenone compound, atrovenetinone methyl acetal, was isolated from a culture broth of Penicillium sp. FKI-1463 as an HIV-1 integrase inhibitor, and it showed anti-HIV activity in vitro. HIV-1 integrase inhibition and anti-HIV activity of two other natural phenalenones were also studied. Among the tested compounds, funalenone inhibited HIV-1 integrase with an IC50 value of 10 microM and showed the best selectivity (anti-HIV, IC50=1.7 microM; cytotoxicity, IC50=87 microM).