刘秀文, 汤仲明, 梁心平, 马宪梅, 陈伟强. 重组葡激酶对兔实验性肺栓塞的溶栓作用J. 药学学报, 1998, 33(11): 801-806.
引用本文: 刘秀文, 汤仲明, 梁心平, 马宪梅, 陈伟强. 重组葡激酶对兔实验性肺栓塞的溶栓作用J. 药学学报, 1998, 33(11): 801-806.
Liu Xiuwen, Tang Zhongming, Liang Xinping, Ma Xianmei , Chen Weiqiang, . THROMBOLYSIS BY STAPHYLOKINASE IN RABBITS WITH EXPERIMENTAL PULMONARY EMBOLUSJ. Acta Pharmaceutica Sinica, 1998, 33(11): 801-806.
Citation: Liu Xiuwen, Tang Zhongming, Liang Xinping, Ma Xianmei , Chen Weiqiang, . THROMBOLYSIS BY STAPHYLOKINASE IN RABBITS WITH EXPERIMENTAL PULMONARY EMBOLUSJ. Acta Pharmaceutica Sinica, 1998, 33(11): 801-806.

重组葡激酶对兔实验性肺栓塞的溶栓作用

THROMBOLYSIS BY STAPHYLOKINASE IN RABBITS WITH EXPERIMENTAL PULMONARY EMBOLUS

  • 摘要: 目的旨在观察重组葡激酶(rSaK)对兔肺栓塞的溶栓作用。用体外制备125I-人纤维蛋白血块,颈静脉注入。0.5h内静滴2和0.5万AU·kg-1rSaK,与NS和2万U·kg-1链激酶(SK)比较。另设2.5h滴注组,速度与低剂量同而总剂量与高剂量同。结果表明,各组肺动脉内残留血栓分别为62%±11%,78%±7%,92%±7%,60%±13%和64%±16%,给药组与对照比较有显著差异。体外实验rSaK与血凝块作用0.5h和2.5h的溶解率相近。rSaK和SK的最大溶解速率分别为34和10kBq·min-1,Km值均为1.7kBq·ml-1。提示:rSaK的疗效取决于总剂量。

     

    Abstract: Thrombolysis effect of recombinant staphylokinase (rSaK) developed in China was evaluated in rabbits with experimental pulmonary embolus model. 125I-labeled human fibrin blood clot was prepared in vitro and was injected through jugular vein resulting in a pulmonary embolus. Twenty thousands AU·kg-1(rSaK-H) or 5000 AU·kg-1(rSaK-L) of rSaK was infused in 0.5 h at constant rate by a peristaltic 20000 U·kg-1. Another 20000 AU·kg-1 of rSaK was infused within 2.5 h(rSaK-2.5 h). The residual labeled blood clot in lungs were found to be 62%±11%(rSaK-H), 78%±7%(rSaK-L), 92%±7%(NS), 60%±13%(SK), and 64%±16%(rSaK-2.5 h).125Ilabeled degradation products in blood and urine were also statistically higher in thrombolytic agents treated group than those in NS controls. The results suggest that the thrombolytic effect of rSaK was determined by total dose and not determined by infusion time. Two of seven rabbits in the rSaK 2.5 h infusion group, the bleeding time was prolonged to more than 10 minutes while no prolongation was seen in rSaK high dose group. The clot lysis curves were very similar in 0.5 h or 2.5 h treatment of rSAK in vitro. Michaelis-Menten kinetics studies in vitro revealed that the Kms of rSaK and SK were almost the same, while a higher maximal velocity(34 kBq·min-1) was observed in rSaK than that in SK (10 kBq·min-1).

     

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