法尼甾体X受体
核受体
化学
胆固醇
内科学
内分泌学
受体
甾醇
药理学
生物
生物化学
医学
转录因子
基因
作者
Nancy L. Urizar,Amy B. Liverman,D'Nette T. Dodds,Frank Valentin Silva,Peter Ordentlich,Yingzhuo Yan,Frank J. Gonzalez,Richard A. Heyman,David J. Mangelsdorf,David D. Moore
出处
期刊:Science
[American Association for the Advancement of Science (AAAS)]
日期:2002-05-31
卷期号:296 (5573): 1703-1706
被引量:520
标识
DOI:10.1126/science.1072891
摘要
Extracts of the resin of the guggul tree ( Commiphora mukul ) lower LDL (low-density lipoprotein) cholesterol levels in humans. The plant sterol guggulsterone [4,17(20)-pregnadiene-3,16-dione] is the active agent in this extract. We show that guggulsterone is a highly efficacious antagonist of the farnesoid X receptor (FXR), a nuclear hormone receptor that is activated by bile acids. Guggulsterone treatment decreases hepatic cholesterol in wild-type mice fed a high-cholesterol diet but is not effective in FXR-null mice. Thus, we propose that inhibition of FXR activation is the basis for the cholesterol-lowering activity of guggulsterone. Other natural products with specific biologic effects may modulate the activity of FXR or other relatively promiscuous nuclear hormone receptors.
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