title: Inhibitory effects of wogonin on catalytic activity of cytochrome P450 enzyme in human liver microsomes.
abstract: Wogonin, derived from the root of Scutellaria baicalensis, is a popular herb for its anticancer, anti-inflammatory, neuroprotective and anti-convulsant effects. The purpose of this study was to investigate the effect of wogonin on human hepatic cytochrome P450s (CYP450s) in vitro. Isoform-specific substrate probes of CYP1A2, 2C9, 2C19, 2D6, 2E1 and 3A4 were incubated in human liver microsomes with or without wogonin. IC(50) and K (i) values were estimated and the types of inhibition were determined. Wogonin was a potent, competitive inhibitor of CYP1A2 (K (i) = 0.24 μM), and a weak inhibitor of CYP2C19 (IC(50) = 101.10 μM), but was not able to inhibit CYP2C9, CYP2D6, CYP2E1 and CYP3A4 (IC(50) > 200 μM). Wogonin could inhibit the activity of CYP1A2 and CYP2C19 with varying potency, while it is a strong inhibitor of CYP1A2. These findings suggested that it was necessary to study the potential pharmacokinetic drug interaction in vivo.
authors.affiliation: School of Pharmacy, China Pharmaceutical University, Nanjing, Jiangsu, People's Republic of China.
authors.forename: Tingting
authors.initials: T
authors.lastname: Li
authors.forename: Ning
authors.initials: N
authors.lastname: Li
authors.forename: Qinglong
authors.initials: Q
authors.lastname: Guo
authors.forename: Hui
authors.initials: H
authors.lastname: Ji
authors.forename: Di
authors.initials: D
authors.lastname: Zhao
authors.forename: Shan
authors.initials: S
authors.lastname: Xie
authors.forename: Xiaonan
authors.initials: X
authors.lastname: Li
authors.forename: Zhixia
authors.initials: Z
authors.lastname: Qiu
authors.forename: Deen
authors.initials: D
authors.lastname: Han
authors.forename: Xijing
authors.initials: X
authors.lastname: Chen
authors.forename: Qidong
authors.initials: Q
authors.lastname: You
mesh_terms: D001189:Aryl Hydrocarbon Hydroxylases / Q000037:antagonists & inhibitors; D055162:Biocatalysis; D065609:Cytochrome P-450 CYP1A2 Inhibitors; D065731:Cytochrome P-450 CYP2C19; D065607:Cytochrome P-450 Enzyme Inhibitors; D003577:Cytochrome P-450 Enzyme System / Q000378:metabolism; D004347:Drug Interactions; D004791:Enzyme Inhibitors / Q000494:pharmacology*; D044950:Flavanones / Q000494:pharmacology*; D006801:Humans; D008862:Microsomes, Liver / Q000187:drug effects / Q000201:enzymology*
chemical_list: D065609:Cytochrome P-450 CYP1A2 Inhibitors; D065607:Cytochrome P-450 Enzyme Inhibitors; D004791:Enzyme Inhibitors; D044950:Flavanones; D003577:Cytochrome P-450 Enzyme System; D001189:Aryl Hydrocarbon Hydroxylases; C045793:CYP2C19 protein, human; D065731:Cytochrome P-450 CYP2C19; C085514:wogonin