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标题：Inhibitory Activity of Flavonoids and Tannins against HIV-1 Protease
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作者：Hong-Xi XU ; Min WAN ; Hui DONG 等
期刊名称：Biological and Pharmaceutical Bulletin
印刷版ISSN：0918-6158
电子版ISSN：1347-5215
出版年度：2000
卷号：23
期号：9
页码：1072-1076
DOI：10.1248/bpb.23.1072
出版社：The Pharmaceutical Society of Japan
摘要：Twenty-nine flavonoids and six hydrolyzable tannins were studied for their inhibitory activity against human immunodeficiency virus (HIV)-1 protease using fluorescence and HPLC assays. Among the flavonoids, flavones, flavanones, flavonols, catechols and chalcones, the flavonols were the most active category while flavanones and catechols displayed low activity. Quercetin was the most potent inhibitor of the target enzyme with an IC₅₀ value of 58.8 μM, while butein and luteolin showed moderate activity. Of the hydrolyzable tannins tested, three ellagitannins which contain a hexahydroxydiphenoyl (HHDP) unit linked to the O-3 and O-6 positions of the sugar, were found to strongly inhibit HIV-1 protease. The IC₅₀ values of corilagin and repandusinic acid on HIV-1 protease were 20.7 and 12.5 μM, respectively.
关键词：flavonoid;hydrolyzable tannin;HIV-1 protease;fluorescence assay;HPLC assay