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本研究用咖啡酸、阿魏酸和CA-1201 对ET-1 生物效应的拮抗作用进行了探讨。结果表明:1.咖啡酸、阿魏酸和CA-1201 在0.1~100 m g/kg 剂量范围内,对ET-1 引起的小鼠死亡有明显的保护作用,该作用存在剂量依赖性;2.三种药物对 ET- 1 缩血管效应有明显的拮抗作用,咖啡酸和CA-1201拮抗效能相近,而阿魏酸的拮抗效能强于咖啡酸和CA-1201;3.三种药物均能拮抗ET-1 的升血压作用,与对照组相比,该作用有显著性意义;4.三种药物对 ET-1 致家兔血管平滑肌细胞增殖有明显的抑制作用,该作用具剂量依赖性。结论:咖啡酸、阿魏酸和 CA-1201 能有效地拮抗ET-1 的生物效应,是一类新的ET 拮抗剂
In this study, the antagonistic effects of caffeic acid, ferulic acid and CA-1201 on the biological effects of ET-1 were investigated. The result shows: 1. Caffeic acid, ferulic acid and CA-1201 had a protective effect on ET-1-induced mouse death in the dose range of 0.1 ~ 100 m g / kg, and the effect was dose-dependent.2. The three drugs showed obvious antagonism on the vasoconstrictive effect of ET-1. The antagonistic effects of caffeic acid and CA-1201 were similar, but the antagonistic potency of ferulic acid was stronger than that of caffeic acid and CA-1201.3. The three drugs can antagonize the ET-1 blood pressure, compared with the control group, the role of significant; 4. The three drugs significantly inhibited the proliferation of vascular smooth muscle cells induced by ET-1 in a dose-dependent manner. CONCLUSION: Caffeic acid, ferulic acid and CA-1201 can effectively antagonize the biological effects of ET-1 and are a new class of ET antagonists