Inhibitory effects of wogonin on catalytic activity of cytochrome P450 enzyme in human liver microsomes
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- 作者：Tingting Li (1)
Ning Li (1)
Qinglong Guo (2)
Hui Ji (1)
Di Zhao (1)
Shan Xie (1)
Xiaonan Li (1)
Zhixia Qiu (1)
Deen Han (1)
Xijing Chen (1) (3)
Qidong You (2) - 关键词：Cytochrome P450 ; Drug–drug interaction ; Wogonin ; Enzyme inhibition
- 刊名：European Journal of Drug Metabolism and Pharmacokinetics
- 出版年：2011
- 出版时间：December 2011
- 年：2011
- 卷：36
- 期：4
- 页码：249-256
- 全文大小：334KB
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Ning Li (1)
Qinglong Guo (2)
Hui Ji (1)
Di Zhao (1)
Shan Xie (1)
Xiaonan Li (1)
Zhixia Qiu (1)
Deen Han (1)
Xijing Chen (1) (3)
Qidong You (2)
1. School of Pharmacy, China Pharmaceutical University, Nanjing, Jiangsu, People’s Republic of China
2. Jiangsu Key Laboratory of Carcinogenesis and Intervention, China Pharmaceutical University, Nanging, 210009, Jiangsu, People’s Republic of China
3. Center of Drug Metabolism and Pharmacokinetics, China Pharmaceutical University, Nanging, 210009, Jiangsu, People’s Republic of China
文摘
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. IC50 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 (IC50?=?101.10?μM), but was not able to inhibit CYP2C9, CYP2D6, CYP2E1 and CYP3A4 (IC50?>?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.