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内皮素(endothelin,ET)是由内皮细胞合成的生物活性物质之一,具有强大的缩血管和促血管平滑肌细胞增殖作用,是一种内源性损伤因子,在许多心、脑、肺、肾和血管疾病的发病中都具有重要意义 本文就内皮素的结构、家族和在体内的分布与释放调节、生物效应以及内皮素受体与受体拮抗剂分别进行了阐述,内皮素拮抗剂的研究是药物开发的重要方向之一,目前已相继合成了BQ_(123)等多个品种 值得一提的是,我国学者就中药与中药方剂对ET的表达和影响进行了广泛的研究,已有多篇报道,认为有些中药与中药方剂具有抑制ET的表达与释放,降低血浆内皮素(SET)水平等作用 因此,从中药中筛选ET生物效应拮抗剂是有发展前景的,可为心血管等疾病的预防和治疗开辟另一条途径
Endothelin (ET), one of the bioactive substances synthesized by endothelial cells, has a powerful vasoconstrictor and vascular smooth muscle cell proliferation and is an endogenous damaging factor. It is found in many heart, brain, lung and kidney And vascular disease are of great significance.In this paper, the structure of endothelin, family and distribution and release regulation in the body, the biological effects and the endothelin receptor and receptor antagonist were described, the study of endothelin antagonists Is one of the important directions of drug development. At present, several varieties such as BQ_ (123) have been synthesized one after another. It is worth mentioning that Chinese scholars have done extensive research on the expression and influence of ET on traditional Chinese medicine and traditional Chinese medicine. Reported that some traditional Chinese medicine and traditional Chinese medicine prescription has the inhibition of ET expression and release and reduce plasma endothelin (SET) level and so the role of traditional Chinese medicine screening of biological effects of ET antagonists are promising, for cardiovascular diseases Prevention and treatment open up another avenue