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

Yaoyao Jia, Muhammad Javidul Haque Bhuiyan, Hee Jin Jun, Ji Hae Lee, Minh Hien Hoang, Hak Ju Lee, Nahyun Kim, Dongho Lee, Kwang Yeon Hwang, Bang Yeon Hwang, Dal Woong Choi, Sung Joon Lee

Research output: Contribution to journalArticlepeer-review

67 Citations (Scopus)

Abstract

In this study, we confirmed that ursolic acid, a plant triterpenoid, activates peroxisome proliferator-activated receptor (PPAR)-α 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-α; however, ursolic acid enhances the binding of PPAR-α to the peroxisome proliferator response element in PPAR-α-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-α agonist that regulates the expression of lipid metabolism genes, but it is not a direct ligand of PPAR-α.

Original languageEnglish
Pages (from-to)5876-5880
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Volume21
Issue number19
DOIs
Publication statusPublished - 2011 Oct 1

Keywords

  • Agonist
  • Hepatocyte
  • Lipid metabolism
  • PPAR-α
  • Ursolic acid

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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