咖啡酸、阿魏酸和CA-1201拮抗ET-1的生物效应

Antagonism effects of caffeic acid, ferulic acids and CA-1201 on ET-1 biological responses

目的：探讨咖啡酸、阿魏酸和ＣＡ－ １２０１ 对ＥＴ－ １ 生物效应的拮抗作用。方法：用不同剂量的咖啡酸、阿魏酸和ＣＡ－ １２０１ 拮抗ＥＴ－ １ 引起小鼠急性死亡、缩血管效应、升压效应及致平滑肌细胞增殖效应。结果：（１） 咖啡酸、阿魏酸和ＣＡ－ １２０１ 在０－１ ～１００ ｍｇｋｇ 剂量范围内，对ＥＴ－ １ 致小鼠死亡有明显的对抗作用，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，该作用有显著差异；（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

AIM:To evaluate the antagonistic effects of caffeic acid, ferulic acid and CA-1201 on endothelin-1 biological responses.METHODS:The acute death of mouse, vasoconstriction of isolated aortic ring, systolic blood pressure evaluation and vascular smooth muscle cells (VSMC) proliferation induced by ET-1 were antagonitized by caffeic acid, ferulic acid and CA-1201.RESULTS:(1)Caffeic acid, ferulic acid and CA-1201 of 0.1～10 mg/kg could protect mouse from acute death induced by ET-1 in a dose dependent manner;(2)These drugs against vasoconstriction induced by ET-1, in which the antagonism efficacy of caffeic acid and CA-1201 was similar and the efficacy of ferulic acid was better than both caffeic acid and CA-1201;(3)These drugs could blunted significantly blood pressure elevation by ET-1 comparing with control groups respectively;(4)These drugs could inhibit the VSMC proliferation induced by ET-1 in concentration-dependent manner.CONCLUSION:Caffeic acid, ferulic acid and CA-1201 can antagonize ET-1 biological effects, which may be a new kind of ET-1 antagonists.