Inhibition of cytochrome P450 by furanocoumarins in grapefruit juice and herbal medicines

作     者：Lian-qing GUO1, Yasushi YAMAZOE2Department of Clinical Pharmacology, Jinling Hospital, Nanjing 210002, China 2Division of Drug Metabolism and MolecularToxicology, Graduate School of Pharmaceutical Sciences, Tohoku University, Sendai 980-8578, Japan 

作者机构：Department of Clinical Pharmacology Jinling Hospital Nanjing 210002 Division of Drug Metabolism and Molecular Toxicology Graduate School of Pharmaceutical Sciences Tohoku University Sendai 980-8578 日本 

出 版 物：《Acta Pharmacologica Sinica》 (中国药理学报(英文版))

年 卷 期：2004年第25卷第2期

页      面：3-10页

核心收录：

学科分类：1008[医学-中药学(可授医学、理学学位)] 1006[医学-中西医结合] 100602[医学-中西医结合临床] 10[医学] 

主　　题：psoralens grapefruit juice herbal medicine enzyme inhibitors cytochrome P-450 enzyme system drug interaction 

摘      要：Furanocoumarins (psoralens) exist in various plants and some of them are used to cure skin diseases. Thesechemicals draw attentions recently because of their abilities to arouse drug interaction through inhibition of cyto-chrome P450. Grapefruit juice is a well-known example for food-drug interaction. But in vitro and in vivo studieshave shown that the causative components are mainly furanocoumarin derivatives with geranyloxy side chains. Invitro experiments confirmed that furanocoumarins from grapefruit juice are both competitive and mechanism-based inhibitors of CYP3A4. Although the inhibition appeared to be stronger in the dimers than that in the monomers,all contribute comprehensively to the grapefruit juice-drug interaction. Further experiments with other furanocoumarinsand related citrus fruits or umbelliferous herbal medicines indicate that drug interaction might also occur with stuffsother than grapefruit juice, especially with traditional medicine.