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

Index: J. Antibiot. 58(1) , 65-8, (2005)

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Abstract

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).