摘要
联合应用金属蛋白内肽酶抑制剂一Thiorphan与二羧基肽酶抑制剂一Captopril,显著延缓脑钠素(BNP)的血液清除和组织降解,增强其对正常血压和高血压大鼠的降压效应,提高BNP对大鼠主动脉狭窄引起的心衰和高血压的疗效。用脂质体作为药物载体联合运载酶抑制剂与BNP,可进一步增强BNP的作用。结果表明,应用酶抑制剂和(或)脂质体是增强和延长BNP生物学效应的有效措施。
The in vivo degradation of atrial natriuretic peptide and brain natriuretic peptide (BNP) is veryfast, and their too short biological effect is one of mainly limitations of their clinical application.This work found that by means of mixing endopeptidase inhibitor-thiorphan and dicarboxylic pep-tidase inhibitor-captopril. or by using lipid liposome as carrier of BNP and enzyme inhibitors, BNPretention in blood circulation after iv injection was significantly prolonged, BNP degradation in tissueswas slowed down, depressor effect of BNP on normotensive WKY rat and spontaneously hypertensiverat was prolonged and potentiated, and the therapeutic effect of BNP on rat heart failure and hyper-tension induced by abdominal aortic stenosis was markedly enhanced. Potentiated effect of BNP by lip-osome was obviously superior to that by enzyme inhibitor mixture. The results show that applicationof enzyme inhibitors or liposome is an effective approach to potentiate and to prolong the biologicaleffect of BNP.
出处
《北京医科大学学报》
CSCD
1992年第4期267-270,共4页
Journal of Peking University(Health Sciences)
