期刊
DRUG TESTING AND ANALYSIS
卷 8, 期 3-4, 页码 307-310出版社
WILEY
DOI: 10.1002/dta.1863
关键词
CYP2D6; CYP3A4; enzyme inhibition; stimulants; dietary supplements
资金
- US Food and Drug Administration (FDA)
A number of dietary supplements used for weight loss and athletic performance enhancement have been recently shown to contain a variety of stimulants, for which there is a lack of pharmacological and toxicological information. One concern for these emerging compounds is their potential to inhibit metabolic enzymes in the liver such as cytochromes P450 (CYP), which can lead to unexpected interactions among dietary supplements, drugs, and other xenobiotics. In this study, inhibition of human recombinant CYP2D6 and CYP3A4 by 27 amine stimulants associated with dietary supplements and their analogs was evaluated by luminescence assays. The strongest CYP2D6 inhibitors were coclaurine (IC50=0.14 +/- 0.01M) and N-benzylphenethylamine (IC50=0.7 +/- 0.2M), followed by several other relatively strong inhibitors (IC50, 2-12M) including -methylphenethylamine, N,-dimethylphenethylamine (phenpromethamine), 1,3-dimethylamylamine (DMAA), N,-diethylphenethylamine, higenamine (norcoclaurine) and N,N-diethylphenethylamine. Only nine compounds inhibited CYP3A4 by 20-55% at 100M. Results of this study illustrate that several amine stimulants associated with dietary supplements inhibit CYP2D6 and CYP3A4 in vitro, and these compounds may participate in adverse drug-dietary supplement interactions in vivo. Copyright (c) 2015 John Wiley & Sons, Ltd.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据