title: Ursolic acid is a PPAR-α agonist that regulates hepatic lipid metabolism.
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.
authors.affiliation: Department of Biotechnology, Graduate School of Biotechnology, Korea University, Seoul 136-713, Republic of Korea.
authors.forename: Yaoyao
authors.initials: Y
authors.lastname: Jia
authors.forename: Muhammad Javidul Haque
authors.initials: MJ
authors.lastname: Bhuiyan
authors.forename: Hee-Jin
authors.initials: HJ
authors.lastname: Jun
authors.forename: Ji Hae
authors.initials: JH
authors.lastname: Lee
authors.forename: Minh Hien
authors.initials: MH
authors.lastname: Hoang
authors.forename: Hak-Ju
authors.initials: HJ
authors.lastname: Lee
authors.forename: Nahyun
authors.initials: N
authors.lastname: Kim
authors.forename: Dongho
authors.initials: D
authors.lastname: Lee
authors.forename: Kwang Yeon
authors.initials: KY
authors.lastname: Hwang
authors.forename: Bang Yeon
authors.initials: BY
authors.lastname: Hwang
authors.forename: Dal-Woong
authors.initials: DW
authors.lastname: Choi
authors.forename: Sung-Joon
authors.initials: SJ
authors.lastname: Lee
mesh_terms: D002784:Cholesterol / Q000032:analysis; D004305:Dose-Response Relationship, Drug; D055808:Drug Discovery; D004353:Drug Evaluation, Preclinical; D005227:Fatty Acids / Q000378:metabolism; D017930:Genes, Reporter; D056945:Hep G2 Cells; D022781:Hepatocytes / Q000378:metabolism; D006801:Humans; D015228:Hypertriglyceridemia / Q000188:drug therapy / Q000503:physiopathology*; D000960:Hypolipidemic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D050356:Lipid Metabolism; D008099:Liver / Q000378:metabolism*; D008156:Luciferases / Q000032:analysis; D058990:Molecular Targeted Therapy; D047493:PPAR alpha / Q000819:agonists* / Q000235:genetics; D020025:Peroxisome Proliferators / Q000378:metabolism; D008517:Phytotherapy; D011485:Protein Binding; D014280:Triglycerides / Q000032:analysis; D014315:Triterpenes / Q000737:chemistry / Q000494:pharmacology*; D000097245:Ursolic Acid
chemical_list: D002784:Cholesterol; D005227:Fatty Acids; D000960:Hypolipidemic Agents; D008156:Luciferases; D047493:PPAR alpha; D020025:Peroxisome Proliferators; D014280:Triglycerides; D014315:Triterpenes; D000097245:Ursolic Acid