Journal
BIOMEDICINE & PHARMACOTHERAPY
Volume 83, Issue -, Pages 257-264Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.biopha.2016.06.046
Keywords
Baicalin; Atherosclerosis; Cholesterol efflux; PPAR gamma; LXR alpha
Funding
- Zhejiang Provincial Medicine and Health Research Foundation [2016KYA186]
- Taizhou Science and Technology Plan [14SF03]
- Natural Science Foundation of Zhejiang Province [LY13H290003]
- Regional Centre for Disease of Zhejiang Province
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Background: Atherosclerosis (AS) is associated with severe cardiovascular disease. The antiinflammatory, anti-oxidation, and lipid regulating properties of baicalin suggest potential as an antiatherosclerotic agent. We therefore investigated whether baicalin can protect against the development of atherosclerosis in an AS rabbit model and explored the underling mechanisms in THP-1 macrophages. Methods and results: In vivo, treatment with baicalin markedly decreased atherosclerotic lesion sizes and lipid accumulation in AS rabbit carotid arteries. Western blotting revealed that the protein expression levels of both peroxisome proliferator-activated receptor gamma (PPAR gamma) and liver X receptor alpha (LXR alpha) were up-regulated in the baicalin group compared with the model group. In vitro, baicalin restricted oxidized-low density lipoprotein (ox-LDL)-induced intracellular lipid accumulation and foam cell formation in THP-1 macrophages. Molecular data showed that baicalin significantly increased the expression levels of PPAR gamma, LXR alpha, ATP binding cassette transporters (ABC) A1 and ABCG1. Cell transfection experiments (including PPAR gamma and LXR alpha siRNAs) suggested that the effects of baicalin are mediated by the PPAR gamma-LXR alpha signalling pathway, which stimulates the expression of ABCA1 and ABCG1. Conclusion: These results suggest that baicalin potentially exerts anti-atherosclerosis effects, possibly through the PPAR gamma-LXR alpha-ABCA1/ABCG1 pathway, by promoting efflux of cholesterol from macrophages and delaying the formation of foam cells. (C) 2016 Elsevier Masson SAS. All rights reserved.
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