摘要
对咖啡酸和阿魏酸的化学结构进行改造，得到两种肉桂酰胺类似物Ｎ３－（５－甲基异唑）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），并分别对其拮抗内皮素－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。结果发现，这四种化合物对ＥＴ－１ 的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。咖啡酸和阿魏酸及其衍生物为一类新的ＥＴ
The structures of caffeic acid and ferulic acid were modified , getting N 3 5 methylisoxazolyl 3,4 dihydroxy cinnamoylamide from caffeic acid and N 4 antipyryl 4 hydroxy 3 methoxycinnamoylamide from ferulic acid. The caffeic acid、ferulic acid and their analogs were investigated antagonist effects on vasoconstriction aortic smooth muscle cells proliferation induced by endothelin 1. The results showed that these four compounds could inhibit vasoconstriction and aortic smooth muscle cells proliferation induced ET 1 with dose dependent manner. Both caffeic acid 、ferulic acid and their analogs can be a new kind of ET 1 antagonists.
出处
《空军总医院学报》
1998年第3期130-132,共3页
Journal of General Hospital of Air Force,PLA
基金
国家自然科学基金资助项目!No.39670886
