Catalposide is a natural agonistic ligand of peroxisome proliferator-activated receptor-α

Ji Hae Lee, Hee jin Jun, Minh Hien Hoang, Yaoyao Jia, Xiang Hua Han, Dong Ho Lee, Hak Ju Lee, Bang Yeon Hwang, Sung Joon Lee

Research output: Contribution to journalArticle

9 Citations (Scopus)

Abstract

Peroxisome proliferator-activated receptor-alpha (PPARα) is a nuclear receptor that regulates the expression of genes related to cellular lipid uptake and oxidation. Thus, PPARα agonists may be important in the treatment of hypertriglyceridemia and hepatic steatosis. In this study, we demonstrated that catalposide is a novel natural PPARα agonist, identified from reporter gene assay-based activity screening with approximately 900 natural plant and seaweed extracts. Results of time-resolved fluorescence resonance energy transfer analyses suggested that the compound interacted directly with the ligand-binding domain of PPARα. Cultured hepatocytes stimulated with catalposide exhibited significantly reduced cellular triglyceride concentrations, by 21%, while cellular uptake of fatty acids was increased, by 70% (. P<0.05). Quantitative PCR analysis revealed that the increase in cellular fatty acid uptake was due to upregulation of fatty acid transporter protein-4 (+19% vs. the control) in cells stimulated with catalposide. Additionally, expression of genes related to fatty acid oxidation and high-density lipoprotein metabolism were upregulated, while that of genes related to fatty acid synthesis were suppressed. In conclusion, catalposide is hypolipidemic by activation of PPARα via a ligand-mediated mechanism that modulates the expression of in lipid metabolism genes in hepatocytes.

Original languageEnglish
Pages (from-to)568-572
Number of pages5
JournalBiochemical and biophysical research communications
Volume422
Issue number4
DOIs
Publication statusPublished - 2012 Jun 15

Keywords

  • Catalposide
  • Hepatocyte
  • Lipid metabolism
  • Peroxisome proliferator receptor

ASJC Scopus subject areas

  • Biophysics
  • Biochemistry
  • Molecular Biology
  • Cell Biology

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