汉黄芩素对人肝微粒体细胞色素P450酶催化活性的抑制作用。
Inhibitory effects of wogonin on catalytic activity of cytochrome P450 enzyme in human liver microsomes.
作者信息
Li Tingting, Li Ning, Guo Qinglong, Ji Hui, Zhao Di, Xie Shan, Li Xiaonan, Qiu Zhixia, Han Deen, Chen Xijing, You Qidong
机构信息
School of Pharmacy, China Pharmaceutical University, Nanjing, Jiangsu, People's Republic of China.
出版信息
Eur J Drug Metab Pharmacokinet. 2011 Dec;36(4):249-56. doi: 10.1007/s13318-011-0050-0. Epub 2011 Jun 29.
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.
汉黄芩素源自黄芩的根部，因其具有抗癌、抗炎、神经保护和抗惊厥作用而成为一种常用草药。本研究的目的是在体外研究汉黄芩素对人肝细胞色素P450（CYP450）的影响。将CYP1A2、2C9、2C19、2D6、2E1和3A4的同工酶特异性底物探针与人肝微粒体一起孵育，其中一部分含有汉黄芩素，一部分不含。估算IC(50)和K (i)值并确定抑制类型。汉黄芩素是CYP1A2的强效竞争性抑制剂（K (i) = 0.24 μM），是CYP2C19的弱抑制剂（IC(50) = 101.10 μM），但不能抑制CYP2C9、CYP2D6、CYP2E1和CYP3A4（IC(50) > 200 μM）。汉黄芩素能够以不同效力抑制CYP1A2和CYP2C19的活性，而它是CYP1A2的强抑制剂。这些发现表明有必要在体内研究潜在的药代动力学药物相互作用。
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