Licochalcone A displays potent and broad-spectrum inhibition on human UDP-glucuronosyltransferases

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  Licochalcone A (LCA), a major bioactive compound isolated from the roots of Glycyrrhiza glabra, displays multiple bioactivities, such as anti-parasitic, anti-inflammatory and anti-cancer.The aim of the present study is to evaluate the inhibitory effects of LCA on human UDP-glucuronosyltransferases (UGTs).The human recombinant UGT isoforms were used as enzyme source, and a nonspecific substrate 4-methylumbelliferone (4-MU) was ultilized as probe sbustrate.Our results demonstrated that LCA displayed strong inhibitory effects towards UGT1A1, 1A3, 1A4, 1A6, 1A7, 1A9 and 2B7 (0.09μmol/L ≤ IC50 ≤ 6.12 μmol/L), and moderate inhibitory effects towards UGT1A8, 1A10, 2B4, 2B15 and 2B17 (IC50 =20.16, 18.01, 24.22, 12.95 and 31.92 μ mol/L, respectively).
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