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, DalWoong Choi, Sung-Joon Lee

Research output: Contribution to journalArticle

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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

Fingerprint

Peroxisome Proliferator-Activated Receptors
Lipid Metabolism
Liver
Genes
Peroxisome Proliferators
Ligands
Fluorescence Resonance Energy Transfer
Surface Plasmon Resonance
Surface plasmon resonance
Response Elements
ursolic acid
Hepatocytes
Triglycerides
Cholesterol
Gene Expression

Keywords

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

ASJC Scopus subject areas

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

Cite this

Ursolic acid is a PPAR-α agonist that regulates hepatic lipid metabolism. / Jia, Yaoyao; Bhuiyan, Muhammad Javidul Haque; Jun, Hee Jin; Lee, Ji Hae; Hoang, Minh Hien; Lee, Hak Ju; Kim, Nahyun; Lee, Dongho; Hwang, Kwang Yeon; Hwang, Bang Yeon; Choi, DalWoong; Lee, Sung-Joon.

In: Bioorganic and Medicinal Chemistry Letters, Vol. 21, No. 19, 01.10.2011, p. 5876-5880.

Research output: Contribution to journalArticle

Jia, Yaoyao ; Bhuiyan, Muhammad Javidul Haque ; Jun, Hee Jin ; Lee, Ji Hae ; Hoang, Minh Hien ; Lee, Hak Ju ; Kim, Nahyun ; Lee, Dongho ; Hwang, Kwang Yeon ; Hwang, Bang Yeon ; Choi, DalWoong ; Lee, Sung-Joon. / Ursolic acid is a PPAR-α agonist that regulates hepatic lipid metabolism. In: Bioorganic and Medicinal Chemistry Letters. 2011 ; Vol. 21, No. 19. pp. 5876-5880.
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AU - Bhuiyan, Muhammad Javidul Haque

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AU - Hoang, Minh Hien

AU - Lee, Hak Ju

AU - Kim, Nahyun

AU - Lee, Dongho

AU - Hwang, Kwang Yeon

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AU - Choi, DalWoong

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