trans-Caryophyllene is a natural agonistic ligand for peroxisome proliferator-activated receptor-alpha
- Authors
- Wu, Chunyan; Jia, Yaoyao; Lee, Ji Hae; Jun, Hee-jin; Lee, Hae-Seung; Hwang, Kwang-Yeon; Lee, Sung-Joon
- Issue Date
- 15-7월-2014
- Publisher
- PERGAMON-ELSEVIER SCIENCE LTD
- Keywords
- trans-Caryophyllene; PPAR-alpha; Hepatocyte; Lipid metabolism
- Citation
- BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, v.24, no.14, pp.3168 - 3174
- Indexed
- SCIE
SCOPUS
- Journal Title
- BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
- Volume
- 24
- Number
- 14
- Start Page
- 3168
- End Page
- 3174
- URI
- https://scholar.korea.ac.kr/handle/2021.sw.korea/97964
- DOI
- 10.1016/j.bmcl.2014.04.112
- ISSN
- 0960-894X
- 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)-alpha through direct interaction with the ligand-binding domain of PPAR-alpha. 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-alpha 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-alpha the effects of trans-caryophyllene on PPAR-alpha responsive gene expressions, intracellular triglyceride, fatty acid uptake and oxidation were disappeared. These results indicate that the aroma compound, trans-caryophyllene, is PPAR-alpha agonist thus regulates cellular lipid metabolism in PPAR-alpha dependent manners. (C) 2014 Elsevier Ltd. All rights reserved.
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