Journal
PHYTOTHERAPY RESEARCH
Volume 24, Issue 3, Pages 369-373Publisher
WILEY
DOI: 10.1002/ptr.2948
Keywords
oleanolic acid; bile acids; FXR
Categories
Funding
- National Natural Science Foundation of China [30672463]
- National Basic Research Program of China (973-Program) [2006CB50390]
- Knowledge Innovation Program of the Chinese Academy of Sciences [KSCX2-YW-R-085]
Ask authors/readers for more resources
Oleanolic acid (OA) is an ingredient found in some Traditional Chinese Medicine remedies for treating liver ailments. Bile acid biosynthesis and catabolism are in part controlled in the liver by transcription factor farnesoid X receptor (FXR). It was hypothesized that OA may act through FXR to mediate some of its beneficial health effects. In this study, it was found that OA bound to the ligand binding domain (LBD) of FXR and blocked its ability to interact with coactivator SRC-3. OA also dose-dependently suppressed the activity of FXR-LBD induced by its endogenous ligand chenodoxycholic acid (CDCA). Consistently, OA partially blocked the ability of CDCA to induce a FXR target gene bile salt export protein (BSEP). On the other hand, OA did not affect the expression of another FXR target gene organic solute transporter (OST-beta). Intriguingly, OA modestly enhanced the expression of a third FXR target gene short heterodimer partner (SHP). This evidence collectively suggested that OA acts as a gene selective modulator of FXR. Copyright (C) 2009 John Wiley & Sons, Ltd.
Authors
I am an author on this paper
Click your name to claim this paper and add it to your profile.
Reviews
Recommended
No Data Available