Induction of ABCA1 and ABCG1 expression by the liver X receptor modulator cineole in macrophages

Hee Jin Jun, Minh Hien Hoang, Siok Koon Yeo, Yaoyao Jia, Sung-Joon Lee

Research output: Contribution to journalArticle

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Abstract

We investigated the effect of cineole on the expression of genes related to reverse cholesterol transport and hepatic fatty acid metabolism. Cineole, a small aroma compound in teas and herbs, significantly stimulated the transactivation of liver X receptor modulator (LXR)-α and LXR-β. The mRNA and protein expression of LXRs and their target genes, including ABCA1 and ABCG1, was significantly increased in macrophages stimulated with cineole. This led to the subsequent removal of cholesterol from the cells. Interestingly, cineole showed tissue-selective LXR induction: hepatocytes stimulated with cineole showed significantly reduced expression of LXR-α and LXR-α-responsive genes, including FAS and SCD-1 (P <0.05). Accordingly, hepatocytes treated with cineole displayed reduced cellular lipid accumulation compared with control cells, as assessed by Oil Red O lipid staining and cholesterol quantification. These results suggest that cineole is a selective LXR modulator that regulates the expression of key genes in reverse cholesterol transport in macrophages without inducing lipogenesis in hepatocytes. This selective LXR modulator may have practical implications for the development of hypocholesterolemic or anti-atherosclerotic agents and also suggests.

Original languageEnglish
Pages (from-to)579-583
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Volume23
Issue number2
DOIs
Publication statusPublished - 2013 Jan 15

Fingerprint

Macrophages
Liver
Modulators
Cholesterol
Hepatocytes
Genes
Lipids
Gene Expression
Lipogenesis
Tea
eucalyptol
Liver X Receptors
Transcriptional Activation
Fatty Acids
Metabolism
Staining and Labeling
Messenger RNA
Tissue
Proteins

Keywords

  • Cholesterol
  • Cineole
  • Hepatocytes
  • Liver X receptor
  • Macrophage

ASJC Scopus subject areas

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

Cite this

Induction of ABCA1 and ABCG1 expression by the liver X receptor modulator cineole in macrophages. / Jun, Hee Jin; Hoang, Minh Hien; Yeo, Siok Koon; Jia, Yaoyao; Lee, Sung-Joon.

In: Bioorganic and Medicinal Chemistry Letters, Vol. 23, No. 2, 15.01.2013, p. 579-583.

Research output: Contribution to journalArticle

Jun, Hee Jin ; Hoang, Minh Hien ; Yeo, Siok Koon ; Jia, Yaoyao ; Lee, Sung-Joon. / Induction of ABCA1 and ABCG1 expression by the liver X receptor modulator cineole in macrophages. In: Bioorganic and Medicinal Chemistry Letters. 2013 ; Vol. 23, No. 2. pp. 579-583.
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