Trans-Caryophyllene is a natural agonistic ligand for peroxisome proliferator-activated receptor-α

Chunyan Wu, Yaoyao Jia, Ji Hae Lee, Hee Jin Jun, Hae Seung Lee, Kwang Yeon Hwang, Sung Joon Lee

Research output: Contribution to journalArticlepeer-review

34 Citations (Scopus)


Intake of dietary aroma compounds may regulate cellular lipid metabolism. We demonstrated that trans-caryophyllene, a flavor compound in plant foods and teas, activates peroxisome proliferator-activated receptor (PPAR)-α through direct interaction with the ligand-binding domain of PPAR-α. The agonistic activity of trans-caryophyllene was investigated by the luciferase reporter assay, surface plasmon resonance, and time-resolved fluorescence resonance energy transfer assay. Following the stimulation of cells with trans-caryophyllene, intracellular triglyceride concentrations were significantly reduced by 17%, and hepatic fatty acid uptake was significantly increased by 31%. The rate of fatty acid oxidation was also significantly increased. The expressions of PPAR-α and its target genes and proteins in fatty acid uptake and oxidation were significantly up-regulated as well. In HepG2 cells transfected with small interfering RNA of PPAR-α, the effects of trans-caryophyllene on PPAR-α responsive gene expressions, intracellular triglyceride, fatty acid uptake and oxidation were disappeared. These results indicate that the aroma compound, trans-caryophyllene, is PPAR-α agonist thus regulates cellular lipid metabolism in PPAR-α dependent manners.

Original languageEnglish
Pages (from-to)3168-3174
Number of pages7
JournalBioorganic and Medicinal Chemistry Letters
Issue number14
Publication statusPublished - 2014 Jul 15


  • Hepatocyte
  • Lipid metabolism
  • PPAR-α
  • trans-Caryophyllene

ASJC Scopus subject areas

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


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