Fungal phenalenones inhibit HIV-1 integrase |
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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 |
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Affiliation: | School of Pharmaceutical Sciences, Kitasato University, Minato-ku, Tokyo 108-8641, Japan. |
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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). |
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