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

  • Bioorg Med Chem Lett. 2011 Oct 1;21(19):5876-80. doi: 10.1016/j.bmcl.2011.07.095.
Yaoyao Jia  1 ,  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
Affiliations
  • 1. Department of Biotechnology, Graduate School of Biotechnology, Korea University, Seoul 136-713, Republic of Korea.
PMID: 21855333 DOI: 10.1016/j.bmcl.2011.07.095
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.