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Fungal phenalenones inhibit HIV-1 integrase
Authors:Shiomi Kazuro  Matsui Ryosuke  Isozaki Miki  Chiba Harumi  Sugai Takahiro  Yamaguchi Yuichi  Masuma Rokuro  Tomoda Hiroshi  Chiba Tomoko  Yan Hua  Kitamura Yoshihiro  Sugiura Wataru  Omura Satoshi  Tanaka Haruo
Affiliation:School of Pharmaceutical Sciences, Kitasato University, Minato-ku, Tokyo 108-8641, Japan.
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).
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