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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(ET1)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ET1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ET1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ET1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。
OBJECTIVE: To investigate the effects of caffeic acid, ferulic acid and their derivatives Cinnamate N3 (5methylisoxazolide) 3,4dihydroxycinnamide (Compound 1) and N4antipyrine Bilin base 4 hydroxy 3 methoxy cinnamide (compound 2) antagonistic endothelin 1 (ET 1) vasoconstriction and vascular smooth muscle cell proliferation was studied. Methods: Antagonistic antagonistic effect of these four compounds on the proliferation of ET 1 vasoconstrictor and vascular smooth muscle cells were studied. Results: Caffeic acid and ferulic acid and their derivatives on ET 1 vasoconstrictor and vascular smooth muscle cell proliferation was significantly antagonistic effect, the role of a dose-dependent, pharmacodynamics analysis, ferulic acid and its Derivatives antagonistic activity was significantly greater than caffeic acid and its derivatives; these four compounds can dose-dependent inhibition of ET 1 induced vascular smooth muscle cell proliferation. Conclusion: Caffeic acid and ferulic acid and their derivatives are a new class of ET antagonists.