1,2,3,6-Tetragalloylglucose (TEgG) is a competitive inhibitor of UDP-glucuronyltransferase UGT1A1 , targeting the competitive substrate binding site of UGT1A1. 1,2,3,6-Tetragalloylglucose inhibits UGT1A1-mediated β-estradiol 3-glucuronidation and SN-38 glucuronidation with IC 50 of 6.01 μM and 4.31 μM, respectively, and binds to UGT1A1 with K i of 3.55 μM. 1,2,3,6-Tetragalloylglucose also induces tumor cell apoptosis , inhibit cell proliferation, activates caspase-3 and induces DNA fragmentation in HL-60 cells. 1,2,3,6-Tetragalloylglucose also inhibits HIV integrase and reverse transcriptase , and inhibits HCV protease .
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