Aĭsina R B, Kazanskaia N F, Andreenko G V, Liutova L V, Pén'ia K
Vopr Med Khim. 1985 Jul-Aug;31(4):30-4.
Plasmin, free of an activator, was obtained after activation of the highly purified human plasminogen by means of trypsin immobilized on Sepharose 4B and after removal of the enzyme from the system. Plasmin was acylated at the active centre using p-amidinophenyl ester of p'-anisic acid to produce the fibrinolytic agent causing a long-term effect. Inactive acyl plasmin was deacylated with the constant rate k3 = 3.10(-4) c-1 (r1/2 = 40 min) at pH 7.4 and 37 degrees. Preliminary studies of the anisoyl-plasmin effect on the system of fibrinolysis in rats showed that in the absence of fibrin clot the fibrinolytic activity was not increased immediately in the euglobulin fraction of blood but after 30 min in result of deacylation of the acyl-enzyme administered into circulation.
通过固定在琼脂糖4B上的胰蛋白酶激活高度纯化的人纤溶酶原并从系统中去除该酶后，获得了无激活剂的纤溶酶。使用对茴香酸的对脒基苯酯在活性中心对纤溶酶进行酰化，以产生具有长效作用的纤溶剂。在pH 7.4和37℃下，无活性的酰化纤溶酶以恒定速率k3 = 3.10(-4) c-1（半衰期r1/2 = 40分钟）进行脱酰化。对大鼠纤溶系统的茴香酰纤溶酶作用的初步研究表明，在没有纤维蛋白凝块的情况下，血液优球蛋白部分的纤溶活性不会立即增加，而是在循环中注入的酰基酶脱酰化30分钟后增加。
