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题名: Inhibition of human cytochrome P450 enzymes by licochalcone A, a naturally occurring constituent of licorice
作者: He, Wei1, 2;  Wu, Jing-Jing3;  Ning, Jing3, 4;  Hou, Jie4;  Xin, Hong1, 2;  He, Yu-Qi3;  Ge, Guang-Bo3;  Xu, Wei1
关键词: Licochalcone A (LCA) ;  Human liver microsomes (HLMs) ;  Cytochrome P450 enzymes (CYPs) ;  Inhibition ;  Herb-drug interactions (HDIs)
刊名: TOXICOLOGY IN VITRO
发表日期: 2015-10-01
DOI: 10.1016/j.tiv.2015.06.014
卷: 29, 期:7, 页:1569-1576
收录类别: SCI
文章类型: Article
WOS标题词: Science & Technology ;  Life Sciences & Biomedicine
类目[WOS]: Toxicology
研究领域[WOS]: Toxicology
英文摘要: Licochalcone A (LCA) is a major bioactive compound in traditional Chinese herbal liquorice that possesses multiple pharmacological activities. However, the effects of the potential herb-drug interactions (HDIs) between LCA and therapeutic drugs on the inhibition of human cytochrome P450 (CYP) enzymes remain unclear. In the present study, the inhibitory effects of LCA on seven major human CYP isoforms, including CYP1A2, 2D6, 2E1, 2C19, 2C8, 2C9 and 3A4, were investigated in human liver microsomes (HLMs). The results demonstrated that LCA significantly inhibited the activities of CYP1A2, 2C19, 2C8, 2C9 and 3A4 and exhibited weak inhibitory effects on CYP2E1 and CYP2D6. Dixon and Lineweaver-Burk plots revealed that the inhibition types of LCA against CYP1A2, 2C9, 2C19 and 2C8 were best fit as mixed-type inhibitions, while LCA was a competitive inhibitor towards CYP3A4. The inhibition kinetic parameters (K-i) were calculated to be 1.02 mu M, 0.17 mu M, 3.89 mu M, 0.89 mu M, and 2.29 mu M, for CYP1A2, 2C9, 2C19, 2C8, and 3A4, respectively. Furthermore, the areas under the plasma concentration-time curves (AUCs) of several drugs that are primarily metabolized by CYPs were estimated to increase by 2-398% in the presence of LCA, which suggested that LCA exhibited high HDI potentials via CYP inhibition. These data are significant for the clinical applications of LCA-containing herbs. (C) 2015 Elsevier Ltd. All rights reserved.
关键词[WOS]: DRUG-DRUG INTERACTIONS ;  HUMAN LIVER-MICROSOMES ;  HUMULUS-LUPULUS ;  P450 1A1 ;  METABOLISM ;  FLAVONOIDS ;  CYP3A4 ;  CLEARANCE ;  SUBSTRATE ;  IDENTIFICATION
语种: 英语
WOS记录号: WOS:000361263500029
Citation statistics: 
内容类型: 期刊论文
URI标识: http://cas-ir.dicp.ac.cn/handle/321008/146545
Appears in Collections:中国科学院大连化学物理研究所_期刊论文

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作者单位: 1.Harbin Med Univ, Affiliated Hosp 1, Harbin 150001, Peoples R China
2.Harbin Med Univ, Harbin 150081, Peoples R China
3.Chinese Acad Sci, Dalian Inst Chem Phys, Lab Pharmaceut Resource Discovery, Dalian 116023, Peoples R China
4.Dalian Med Univ, Dalian 116044, Peoples R China

Recommended Citation:
He, Wei,Wu, Jing-Jing,Ning, Jing,et al. Inhibition of human cytochrome P450 enzymes by licochalcone A, a naturally occurring constituent of licorice[J]. TOXICOLOGY IN VITRO,2015,29(7):1569-1576.
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