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Ursolic acid is a PPAR-alpha agonist that regulates hepatic lipid metabolism

Authors
Jia, YaoyaoBhuiyan, Muhammad Javidul HaqueJun, Hee-jinLee, Ji HaeHoang, Minh HienLee, Hak-JuKim, NahyunLee, DonghoHwang, Kwang YeonHwang, Bang YeonChoi, Dal-WoongLee, Sung-Joon
Issue Date
1-Oct-2011
Publisher
PERGAMON-ELSEVIER SCIENCE LTD
Keywords
Ursolic acid; PPAR-alpha; Agonist; Lipid metabolism; Hepatocyte
Citation
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, v.21, no.19, pp.5876 - 5880
Indexed
SCIE
SCOPUS
Journal Title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume
21
Number
19
Start Page
5876
End Page
5880
URI
https://scholar.korea.ac.kr/handle/2021.sw.korea/111397
DOI
10.1016/j.bmcl.2011.07.095
ISSN
0960-894X
Abstract
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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