咖啡酸和阿魏酸及其类似物对内皮素-1生物效应的拮抗作用

目的：对咖啡酸和阿魏酸以及两者化学衍生物肉桂酰胺类似物Ｎ３（５甲基异吓恶唑）基３，４二羟基肉桂酰胺（化合物１）和Ｎ４安替比林基４羟基３甲氧基肉桂酰胺（化合物２）拮抗内皮素１（ＥＴ１）的缩血管及致血管平滑肌细胞增殖效应进行了初步研究。方法：用这四种化合物对ＥＴ１缩血管及致血管平滑肌细胞增殖作用的拮抗效应拮抗进行了研究。结果：咖啡酸和阿魏酸及其衍生物对ＥＴ１缩血管及致血管平滑肌细胞增殖效应有明显的拮抗作用，该作用具剂量依赖性，经药效动力学分析，阿魏酸及其衍生物的拮抗活性显著大于咖啡酸及其衍生物；这四种化合物能剂量依赖性地抑制ＥＴ１致血管平滑肌细胞增殖作用。结论：咖啡酸和阿魏酸及其衍生物为一类新的ＥＴ拮抗剂。

Study on the antagonist effects of caffeic acid,ferulic acid and their analogs on ET-1 biological responses

OBJECTIVE: The antagonist effects on vasoconstriction aortic smooth muscle cells proliferation induced by endothelin1 were investigated on caffeic acidferulic acid and their analogs N35methylisoxazolyl3,4dihydroxy cinnamoylamide from caffeic acid and N4antipyryl4hydroxy3methoxycinnamoylamide. METHODS: The antagonist effects of these compounds on vasoconstriction and aortic smooth muscle cells proliferation induced by ET1 were studied. RESULTS: The results showed that these four compounds could inhibit vasoconstriction and aortic smooth muscle cells proliferation induced ET1 with dosedependent manner,having analyzed the pharmacodynamic parameters,the effects of ferulic acid and its analog were more potent than that of caffeic acid and its analog. CONCLUSIONS: Both caffeic acidferulic acid and their analogs can be a new kind of ET1 antagonists.