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中国临床药理学与治疗学 ›› 2011, Vol. 16 ›› Issue (4): 474-480.

• 综述与讲座 • 上一篇    

细胞色素P450酶与维生素A的代谢

王萍, 刘晓东   

  1. 中国药科大学药物代谢动力学重点实验室,南京 210009,江苏
  • 收稿日期:2011-03-08 修回日期:2011-03-22 发布日期:2011-06-22
  • 通讯作者: 刘晓东,男,教授,博士生导师,从事中药药物代谢动力学、药物相互作用以及创新药物的药代动力学、P-糖蛋白与血脑屏障研究。Tel: 13951867732   E-mail: xdliu@cpu.edu.cn
  • 作者简介:王萍,女,在读硕士,主要从事药物Ⅰ相代谢酶和药物相互作用研究。Tel: 13851804624 E-mail: ping0442312@gmail.com

Cytochrome P450s and the metabolism of vitamin A

WANG Ping, LIU Xiao-dong   

  1. Key Lab of Drug Metabolism & Pharmacokinetics, China Pharmaceutical University, Nanjing 210009, Jiangsu, China
  • Received:2011-03-08 Revised:2011-03-22 Published:2011-06-22

摘要: 维生素A是人体必不可少的一种脂溶性维生素,在体内可以代谢为生物活性更高的视黄醛和视黄酸。细胞色素P450酶是重要的药物Ⅰ相代谢酶,在人体内有广泛的分布。它不仅参与了外源性物质的代谢,在内源性物质的代谢中也有重要的作用。CYP450酶在维生素A的代谢中扮演了重要的角色。人体内参与维生素A代谢的CYP450酶主要是CYP1,CYP2C, CYP2E, CYP3A和CYP26家族。同时其代谢物视黄酸可以与核受体 (维生素A酸受体,视黄醇类X受体) 相结合,诱导CYP450酶的表达和活性。本文通过对近几年来维生素A代谢的研究进展做一综述,阐述了CYP1、CYP2C、CYP2E、CYP3A和CYP26家族在维生素A代谢中的作用以及视黄酸诱导CYP450酶的分子机制。

关键词: 细胞色素 P450, 视黄醇, 视黄醛, 视黄酸, 维生素A

Abstract: Vitamin A, as a kind of fat-soluble vitamin, could be metabolized to retinal and retinoic acid, which exhibited higher bioactivities. Cytochrome P450s (CYP450s) participated in not only the metabolism of xenobiotics but also metabolism of endogenous chemicals, such as vitamin A. It was reported that CYP1, CYP2C, CYP2E, CYP3A and CYP26 families were the CYP450s that mainly mediated metabolism of vitamin A. However, expression and activities of CYP450s could also be regulated by retinoic acid binding to nuclear receptors (RARs, RXRs). Besides CYP450s, transcription of several lipid transporters gene was also under the regulation of retinoic acid. Here, we reviewed the relative importance of CYP450s on vitamin A metabolism and molecule mechanism that how retinoic acid modulated the expression and activities of CYP450s and lipid transporters, in order to provide some new ideas and new targets for the study of disease caused by the lipid metabolic disorder.

Key words: Cytochrome P450, Retinol, Retinal, Retinoic acid, Vitamin A

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