白藜芦醇的提取分离及其对内皮素-1的拮抗作用

ISOLATION OF RESVERATROL AND ITS ANTAGONISTIC EFFECTS ON ENDOTHELIN-1

目的 :研究草药红背丝绸化学成分的提取分离及其活性成分白藜芦醇对内皮素的拮抗作用。方法 :用不同剂量白藜芦醇拮抗 ET- 1引起的小鼠急性死亡、大鼠离体血管条收缩、整体大鼠升压作用、致平滑肌细胞增殖效应 ,以及白藜芦醇拮抗 [1 2 5 I]ET- 1与血管平滑肌成纤维细胞结合实验。结果 :白藜芦醇对 ET- 1致小鼠急性死亡有明显的保护作用 ;可明显地拮抗由 ET- 1引起的离体大鼠主动脉条的收缩作用 ;能够拮抗 ET- 1导致的大鼠血压的上升幅度 ;可明显抑制 ET- 1引起的家兔胸主动脉血管平滑肌细胞增殖 ;在一定程度可以拮抗 [1 2 5 I]ET- 1与血管平滑肌成纤维细胞的结合 ,说明白藜芦醇与 ET受体有一定的结合作用。结论 :白藜芦醇是一种新结构类型的非肽类ET-

OBJECTIVE:To extract and isolate the constituents of Cissus assamica (Laws.)Craib,a medicinal herb used to treat snake bite in Guangxi province,and evaluate the antagonistic effects of resveratrol on ET 1 biological response.METHODS:The acute death of mouse,vasoconstriction of isolated aortic ring,systolic blood pressure elevation and vascular muscle proliferation induced by ET 1 were antagonized by resveratrol.The experiment of resveratrol and [ 125 I]ET 1 binding with NIH 3T3 cells was employed.RESULTS:Resveratrol could protect mouse from acute death induced by ET 1.Resveratrol could relax ET 1 contracted isolated rat aortic rings. Resveratrol could blunt the elevation of blood pressure induced by ET 1.Resveratrol could transiently inhibit the VSMC proliferation induced by ET 1.Resveratrol showed competitive effect of [ 125 I]ET 1 binding with NIH 3T3 cells in a certain degree.CONCLUSION:All these results prompt that resveratrol is a new kind of non peptide endothelin antagonist.