Inhibition of HIV-1 Integrase by Galloyl Glucoses from Terminalia chebula and Flavonol Glycoside Gallates from Euphorbia pekinensis
Mi‐Jeong Ahn(Seoul National University), Chul Young Kim(Seoul National University), Ji Suk Lee(Seoul National University), Tae Gyun Kim(Ministry of Food and Drug Safety), Seung Hee Kim(National Institute of Food and Drug Safety Evaluation), Chong-Kyo Lee(Korea Research Institute of Chemical Technology), Bo-Bin Lee(Chung-Ang University), Cha‐Gyun Shin(Chung-Ang University), Hoon Huh(Seoul National University), Jinwoong Kim(Seoul National University)
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Abstract
The bioassay-directed isolation of Terminalia chebula fruits afforded four human immunodeficiency virus type 1 (HIV-1) integrase inhibitors, gallic acid ( 1) and three galloyl glucoses ( 2 - 4). In addition, four flavonol glycoside gallates ( 5 - 8) from Euphorbia pekinensis containing the galloyl moiety also showed the inhibitory activity at a level comparable to those of 2 - 4. By comparison with the activities of the compounds not bearing this moiety, it is proposed that the galloyl moiety plays a major role for inhibition against the 3'-processing of HIV-1 integrase of these compounds.
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