摘要
用固相法在国际上首次合成了高纯度并具有生物活性的 ACEI 八肽,并对其生物活性进行了研究。研究结果表明;①ACEI 八肽对人血和脑组织及大鼠血和肺组织的血管紧张素转换酶(ACE)具有明显的抑制作用。②ACEI 八肽静脉快速注入(60μg/kg)可明显降低大鼠血压及降低血醛固酮浓度。侧脑室(icy)注射(6μg/kg)对血压没有影响。③少量 ACEI 八肽在不影响血管紧张素和醛固酮浓度的情况下能加强脑钠素(BNP)的降压效果。④BNP 或其片断具有抑制 ACE 活性的作用。结果对于肾素-血管紧张素系统特别是高血压病生理的深入研究具有重要意义。
We first reported in literature the syuthesize of high purity and biologically active ACEI oetapeptide with solid phase method.The resulta of the study on the relationship between depressive action on blood pressure of ACEI and brain natiuretic peptide(BNP)showed that: 1)ACEI octopeptide inhibited significantly ACE level of plasma and membrane fraction of lung tissue in rats.IC_(50) was 10μmol/L and 5 μmol/L respectively;2)although ACEI admin- istrated(60 μg/0.6 ml/kg)by iv rapidly could supress blood pressure and aldosterone con- centration of plasma in rats,icy injection of ACEI(6μg/0.6ml.kg^-)was found no effect on blood pressure;3)tiny amount of ACEI octapeptid with no influence on plasma AT-(?) and aldosterone concentration increased the hypotensive effect of BNP,and 4)BNP or its fragments was found inhibitive on human plasma ACE activity.We conclude that our result may play an important role in the studies of renin-angioleusin system and physio-pathology of hyperteusive diseases.
关键词
血管紧张素Ⅰ
转换酶
化学合成
angiotensin converting enzyme
angiotensin converting enzyme inhibitor octopeptide
brain natfiuretic peptide
blood pressure
