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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- 1拮抗剂
Objective : To study the extraction and separation of chemical constituents of herbal red back silk and the antagonism of its active ingredient resveratrol on endothelin. METHODS: Different doses of resveratrol were used to antagonize the acute death of mice induced by ET-1, the contraction of isolated rat vascular strips, the increase of global rat pressure, the proliferation of smooth muscle cells, and the antagonism of resveratrol [1 2 5 I]ET-1 binding to vascular smooth muscle fibroblasts. RESULTS: Resveratrol had a protective effect on ET-1-induced acute death in mice; it could antagonize the contraction of isolated rat aortic strips induced by ET-1; it could antagonize the effects of ET-1. The increase of rat blood pressure can significantly inhibit the proliferation of vascular smooth muscle cells induced by ET-1 in rabbit thoracic aorta; to a certain extent, it can antagonize the binding of [125I]ET-1 and vascular smooth muscle fibroblasts, indicating that Retinol and ET receptors have a certain degree of binding. Conclusion : Resveratrol is a novel structural type of non-peptide ET-1 antagonist