目的:研究桂皮酸类化合物咖啡酸和阿魏酸对内皮素(endothelin1,ET1) 生物效应的拮抗作用。方法:体内ET1iv 致小鼠急性死亡、体外血管平滑肌细胞培养、主动脉条收缩试验和ET 受体结合试验。结果:咖啡酸和阿魏酸(ip) 能剂量依赖性地显著延长ET1 致小鼠急性死亡时间,在离体器官可观察到咖啡酸与阿魏酸能拮抗ET1的缩血管效应;放射性受体配体结合实验表明,咖啡酸和阿魏酸可竞争性地抑制ET1 与其受体的结合。结论:咖啡酸和阿魏酸为新的非肽类ET 拮抗剂 Objective: To study the antagonism of the biological effects of cinnamic acid caffeic acid and ferulic acid on endothelin-1 (ET-1). METHODS: In vivo ET1iv induced acute death in mice, in vitro culture of vascular smooth muscle cells, aortic strip contraction test, and ET receptor binding assay. RESULTS: Caffeic acid and ferulic acid (ip) significantly prolonged the time of acute death of mice induced by ET1 in a dose-dependent manner. Caffeic acid and ferulic acid were observed to antagonize the vasoconstrictive effect of ET1 in isolated organs. Radioactive receptor ligand binding experiments showed that caffeic acid and ferulic acid competitively inhibited the binding of ET-1 to its receptor. Conclusion: Caffeic acid and ferulic acid are new non-peptide ET antagonists