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[实验性心肌缺血中蛋白水解酶及其抑制剂的活性]

[Activity of proteolytic enzymes and their inhibitors in experimental myocardial ischemia].

作者信息

Karapetian R G, Oganesian S S, Akopian T N, Dzhanpoladian E G

出版信息

Vopr Med Khim. 1993 Jan-Feb;39(1):29-31.

PMID:8498066
Abstract

Proteolytic activity and activity of endogenous inhibitors of endopeptidases (using chymotrypsin and papain) were studied in the myocardium of rats with experimental ischemia during an acute phase (60 min) and within 5 days after ligation of the left descending coronary artery; effects of the beta-adrenoblocking agent propranolol and the calcium antagonist verapamil on these activities was also studied. During the acute phase of ischemia, the activity of acid proteases was increased by 30%, that of Ca(2+)-activated neutral proteases by 15-20%. At the same time, the activity of serine proteases inhibitors was decreased while the activity of thiol protease inhibitors was increased. Within 5 days of coronary artery occlusion, Lysosomal thiol-dependent endopeptidases were activated in the myocardium; a considerably higher activity of the inhibitors of serine- and cysteine-containing endopeptidases was detected. The cardioactive drugs propranolol and verapamil affected selectively both endopeptidase activity and their inhibitors.

摘要

在实验性缺血大鼠心肌的急性期(60分钟)以及左冠状动脉结扎后5天内,研究了蛋白水解活性和内肽酶内源性抑制剂的活性(使用胰凝乳蛋白酶和木瓜蛋白酶);还研究了β-肾上腺素能阻滞剂普萘洛尔和钙拮抗剂维拉帕米对这些活性的影响。在缺血急性期,酸性蛋白酶的活性增加了30%,钙激活中性蛋白酶的活性增加了15%-20%。同时,丝氨酸蛋白酶抑制剂的活性降低,而巯基蛋白酶抑制剂的活性增加。在冠状动脉闭塞5天内,心肌中的溶酶体巯基依赖性内肽酶被激活;检测到含丝氨酸和半胱氨酸的内肽酶抑制剂的活性明显更高。心脏活性药物普萘洛尔和维拉帕米对内肽酶活性及其抑制剂均有选择性影响。

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