白藜芦醇对PPAR-γ激动作用的研究  

Agitation effect of resteratrol on PPAR-γ

作　　者：葛恒[1] 张俊峰[1] 王彬尧[1] 王长谦[1] 

机构地区：[1]上海第二医科大学附属仁济医院心内科,上海200001

出　　处：《中国药学杂志》2005年第12期905-908,共4页Chinese Pharmaceutical Journal

基　　金：国家自然科学基金项目(30070869)

摘　　要：目的探讨白藜芦醇是否为过氧化物酶体增殖剂激活受体γ(PPAR-γ)的激动剂。方法在自身不表达PPAR-γ蛋白的U937细胞中电穿孔共转染PPARγ表达质粒和其报告质粒,从而构建PPAR-γ激动剂筛选模型。同时在U937细胞内单独转染PPAR-γ报告质粒作为阴性对照。转染细胞中加入已知PPAR-γ的激动剂吡格列酮30μmol·L-1和15,30μmol·L-1的白藜芦醇,培养24h后裂解细胞,测定细胞内报告质粒所表达虫荧光素酶的活性,该活性大小即代表药物激动PPAR-γ的能力。结果共转染细胞中加入吡格列酮后显著激动了PPAR-γ,使虫荧光素酶活性增强了4.2倍(P<0.001),验证了筛选模型的有效性。而加入15和30μmol·L-1白藜芦醇后,虫荧光素酶活性也分别提高1.78(P=0.033)和2.47倍(P=0.01)且与剂量相关(P=0.04)。而单独转染报告质粒的U937细胞加入上述药物后,虫荧光素酶活性无显著差异。结论白藜芦醇能够剂量依赖的激动PPAR-γ。OBJECTIVE: To demonstrate whether resveratrol is an activator of PPAR-γ. METHODS: U937 cells, which doesn't express protein were cotransfected with PPAR-γ expression vector and PPAR-γ reporter vector by electroporation. Cells transfected with reporter vector were served as negative control. Transfected cells were cultured with known PPAR-a˜ activator pioglitazone 30 μmol&middotL-1 or resveratrol 15 and 30 μmol&middotL-1 for 24 h. Cells were lysated and assayed for reporter luciferase activity, which presented the drug capability to activate. RESULTS: 30 μmol pioglitazone strongly activated PPAR-γ, increased luciferase activity up to 4.2 fold, compared with DMSO treating control. Resveratrol 15 and 30 μmol&middotL-1 also significantly activated PPAR, the luciferase activity increased to 1.78 fold (P = 0.033) and 2.47 fold (P = 0.01) of control, respectively. The effect of resveratrol was dose-dependent (P = 0.04). CONCLUSION: Resveratrol could dose-dependently activate PPAR-γ.

关 键 词：白藜芦醇 过氧化物酶增殖刺激活受体γ 激动剂 动脉粥样硬化 炎症 

分 类 号：R965[医药卫生—药理学]