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 journalArticle

16 Citations (Scopus)

Abstract

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
Volume24
Issue number14
DOIs
Publication statusPublished - 2014 Jul 15

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Peroxisome Proliferator-Activated Receptors
Ligands
Fatty Acids
Lipid Metabolism
Oxidation
Assays
Triglycerides
Flavor compounds
Edible Plants
Fluorescence Resonance Energy Transfer
Surface Plasmon Resonance
Hep G2 Cells
Surface plasmon resonance
Tea
caryophyllene
Luciferases
Gene expression
Small Interfering RNA
Gene Expression
Liver

ASJC Scopus subject areas

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

Cite this

Trans-Caryophyllene is a natural agonistic ligand for peroxisome proliferator-activated receptor-α. / Wu, Chunyan; Jia, Yaoyao; Lee, Ji Hae; Jun, Hee Jin; Lee, Hae Seung; Hwang, Kwang Yeon; Lee, Sung-Joon.

In: Bioorganic and Medicinal Chemistry Letters, Vol. 24, No. 14, 15.07.2014, p. 3168-3174.

Research output: Contribution to journalArticle

Wu, Chunyan ; Jia, Yaoyao ; Lee, Ji Hae ; Jun, Hee Jin ; Lee, Hae Seung ; Hwang, Kwang Yeon ; Lee, Sung-Joon. / Trans-Caryophyllene is a natural agonistic ligand for peroxisome proliferator-activated receptor-α. In: Bioorganic and Medicinal Chemistry Letters. 2014 ; Vol. 24, No. 14. pp. 3168-3174.
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