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Chinese Journal of Clinical Pharmacology and Therapeutics ›› 2011, Vol. 16 ›› Issue (5): 492-495.

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Ezetimibe inhibiting intracellular lipid accumulation through caveolin-1 in rat vascular smooth muscle cells

TUO Qin-hui1, YUAN Hao-yu1, GUO Yan1, YU Wei-xia1 , LIAO Duan-fang2   

  1. 1Institute of Pharmacy and Pharmacology, University of South China, Hengyang 421001, Hunan, China;
    2Department of Pharmacology, Hunan University of Chinese Medicine, Changsha 410208,Hunan,China
  • Received:2011-01-12 Revised:2011-03-28 Published:2011-07-08

Abstract: AIM: To determine the effects of ezetimibe on intracellular lipid accumulation and related mechanism in rat vascular smooth muscle cells (VSMCs).METHODS: VSMCs taken from rat aorta were respectively treated with different concentration of ezetimibe(0, 3, 10, 30 μmol/L)for 24 hours or treated with 30 μmol/L of ezetimibe for different time (0, 6, 12, 24, 48 hours). The concentration of total cholesterol and free cholesterol were detected by high performance liquid chromatography. The expression of caveolin-1 were detected by western blotting.RESULTS: The contents of intracellular total cholesterol (TC) and free cholesterol (FC) were significantly decreased with a peak at 30 μmol/L for 24 h in lipid-loaded cells by ezetimibe in a dose- and time-dependent manner.The level of caveolin-1 protein was elevated 70% by ezetimibe.CONCLUSION: Ezetimibe inhibits cholesterol:methy-β-cyclodextrin (Chol:MβCD)-induced cholesterol accumulation in cultured VSMC through modulating caveolin-1 .

Key words: Ezetimibe, Vascular smooth muscle cells, Cholesterol, Caveolin-1

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