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Bioorg Med Chem Lett. 2011 Oct 1;21(19):5876-80. doi: 10.1016/j.bmcl.2011.07.095. Epub 2011 Aug 3.

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

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Department of Biotechnology, Graduate School of Biotechnology, Korea University, Seoul 136-713, Republic of Korea.


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.

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