Fungal Phenalenones Inhibit HIV-1 Integrase

被引:0
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作者
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 Ōmura
Haruo Tanaka
机构
[1] School of Pharmaceutical Sciences Kitasato University,
[2] The Kitasato Institute,undefined
[3] Kitasato Institute for Life Sciences,undefined
[4] Kitasato University,undefined
[5] AIDS Research Center,undefined
[6] National Institute of Infectious Diseases,undefined
[7] Advanced Clinical Research Center,undefined
[8] Institute of Medical Science,undefined
[9] The University of Tokyo,undefined
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关键词
enzyme inhibitor; HIV interase; AIDS; phenalenone;
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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 µM and showed the best selectivity (anti-HIV, IC50=1.7 µM; cytotoxicity, IC50=87 µM).
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页码:65 / 68
页数:3
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