蚓激酶抗凝、纤溶的机制及其与组织型纤溶酶原激活剂的关系
蚓激酶|组织型纤溶酶原激活剂,关键词：
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关键词：蚓激酶；组织型纤溶酶原激活剂
摘要 目的 探讨蚓激酶抗凝、纤溶机制及其与组织型纤溶酶原激活剂(t-PA)的关系。 方法 给正常和高凝大鼠口服蚓激酶胶囊(2.5mg*ml-1 *100g-1 体重，3天)后测白陶土部分凝血活酶时间(KPTT)、凝血酶原时间(PT)、优球蛋白溶解时间(ELT)、纤溶酶原含量和体外血栓形成的变化，以及体内血浆及体外培养的内皮细胞上清液中t-PA、t-PA抑制物(PAI)活性的变化。 结果 正常和高凝大鼠口服蚓激酶后KPTT明显延长；ELT明显缩短。体外血栓形成仪测定显示血栓长度、重量均明显减小。纤溶酶原含量明显降低。正常大鼠、高凝大鼠血浆t-PA活性升高(均为P<0.05)，与纤溶酶原含量降低间呈明显负相关(r=-0.872，P<0.05)。在大鼠肺微血管内皮细胞培养中加入蚓激酶(50～200mg/L)后，上清液中t-PA活性明显升高(P<0.01)，呈量-效依赖关系；但PAI活性无明显变化。蚓激酶溶液中含有t-PA活性，其与药物浓度呈显著正相关(r=0.8585，P<0.05)。 结论 蚓激酶能部分抑制内凝血途径，激活纤溶，后者又与t-PA活性升高有关。
Anticoagulative andfibrinolytic effects of lumbrokinase and their relation to tissue plasminogen activator
Zhang Guoping, Jin Huiming,Zhang Ming, et al. Department of Pathophysiology, Shanghai Medical University, Shanghai200032
Abstract Objective To investigate theanticoagulative and fibrinolytic effects of lumbrokinase and their relation to tissueplasminogen activator (t-PA). Methods Normal and hypercoagulation rats were given orallumbrokinase (2.5 mg/ml per 100 g body weight) for 3 days. Then kaolin partialthromboplastin time (KPTT), prothrombin time (PT), euglobulin lysis time (ELT),plasminogen and thrombogenesis in vitro were assayed. Plasma t-PA and plasminogenactivator inhibitor (PAI) activity was detected not only in plasma but also in ratpulmonary microvascular endothelial cell (PMVEC) culture treated with lumbrokinase. Results KPTT of bothnormal and hypercoagulation rats were prolonged (P<0.05) after administration of lumbrokinase. ELT in both groups were markedly shorter than that in the controls. Thelength and weight of thrombus were reduced (P<0.01). The content of plasminogendecreased significantly. Plasma t-PA activity increased from 2.66±0.17 to 3.43±0.11 IU/ml in normal rats, and from 2.02±0.20 to 2.70±0.12 IU/ml in hypercoagulation rats (P<0.05).There was a negative correlation between t-PA and plasminogen. The t-PA activity in ratPMVEC culture media was significantly elevated after cultivation with lumbrokinase (50-200mg/L, P<0.01). The changes were dose-dependent. PAI activity showed no such changes.Lumbrokinase per se had certain t-PA activity, which was positively correlated with itsconcentration. Conclusions Lumbrokinase inhibits intrinsiccoagulation pathway and activates fibrinolysis via the increase of t-PA activity producedby microvascular endothelial cells.
Key Words Lumbrokinase Tissue plasminogenactivator
蚓激酶是从蚯蚓中提炼而得的一种多成份酶〔1〕 ......
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