Soskel N T, Watanabe S, Hardie R, Shenvi A B, Punt J A, Kettner C
Am Rev Respir Dis. 1986 Apr;133(4):635-8. doi: 10.1164/arrd.1986.133.4.635.
The peptide boronic acid, MeOSuc-Ala-Ala-Pro-boroVal-pinacol (AAPbV), is an effective inhibitor of both pancreatic and leukocyte elastase. Initial work showed that AAPbV diminishes the effect of emphysema induced by pancreatic elastase. This initial work has been expanded to show that AAPbV provides a high degree of protection against elastase-induced increases in lung volume and mean linear intercept when given intratracheally at 200 mg/kg either 15 min before, simultaneous with, or 15 min after instilling elastase. Intraperitoneal administration, although less effective, is dose dependent and dependent on the time of treatment. We conclude that a reversible protease inhibitor can be used to prevent aberrant proteolysis in vivo.
肽硼酸MeOSuc-Ala-Ala-Pro-boroVal-频哪醇酯（AAPbV）是胰腺弹性蛋白酶和白细胞弹性蛋白酶的有效抑制剂。初步研究表明，AAPbV可减轻胰腺弹性蛋白酶诱导的肺气肿效应。这项初步研究已得到扩展，结果显示，在气管内注入弹性蛋白酶前15分钟、同时或之后15分钟给予200mg/kg的AAPbV，可高度保护肺部免受弹性蛋白酶诱导的肺容积增加和平均线性截距增加的影响。腹腔注射虽然效果较差，但具有剂量依赖性且取决于治疗时间。我们得出结论，一种可逆的蛋白酶抑制剂可用于预防体内异常蛋白水解。
