期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 21, 期 19, 页码 5876-5880出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2011.07.095
关键词
Ursolic acid; PPAR-alpha; Agonist; Lipid metabolism; Hepatocyte
资金
- Korean Forest Service [S120909L130110]
- Ministry for Food, Agriculture, Forestry and Fisheries, Republic of Korea [F20926409H220000110]
- Korea Institute of Marine Science & Technology Promotion (KIMST) [F20926409H220000110] Funding Source: Korea Institute of Science & Technology Information (KISTI), National Science & Technology Information Service (NTIS)
In this study, we confirmed that ursolic acid, a plant triterpenoid, activates peroxisome proliferator-activated receptor (PPAR)-alpha in vitro. Surface plasmon resonance and time-resolved fluorescence resonance energy transfer analyses do not show direct binding of ursolic acid to the ligand-binding domain of PPAR-alpha; however, ursolic acid enhances the binding of PPAR-alpha to the peroxisome proliferator response element in PPAR-alpha-responsive genes, alters the expression of key genes in lipid metabolism, significantly reducing intracellular triglyceride and cholesterol concentrations in hepatocytes. Thus, ursolic acid is a PPAR-alpha agonist that regulates the expression of lipid metabolism genes, but it is not a direct ligand of PPAR-alpha. (C) 2011 Elsevier Ltd. All rights reserved.
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