Doutremepuich C, Deharo E, Guyot M, Lalanne M C, Walenga J, Fareed J
Laboratoire d'hématologie, Faculté de Pharmacie, Bordeaux, France.
Thromb Res. 1989 Jun 1;54(5):435-45. doi: 10.1016/0049-3848(89)90213-2.
Hirudin, a potent inhibitor of blood coagulation, differs in its antithrombotic activity according to the source of isolation. It was therefore of interest to study recombinant hirudin. Hirudin was obtained by a genetic process from E. coli. Its antithrombotic action was investigated in an experimental (rat) model of venous thrombosis and was compared to heparin whose results are known. Heparin (400 micrograms/kg) and hirudin (12.5, 25 and 50 micrograms/kg) present an antithrombotic effect and limit the extension of an existing thrombus (p less than 0.05). Higher heparin dosages increase the bleeding time mean value (p less than 0.05) whereas hirudin does not. So, recombinant hirudin presents the same antithrombotic action as heparin but with very inferior dosage. This activity seems not dose-dependent and is associated to weak hemorrhagic effects.
水蛭素是一种强效的血液凝固抑制剂，其抗血栓活性因分离来源而异。因此，研究重组水蛭素很有意义。水蛭素是通过基因工程方法从大肠杆菌中获得的。在静脉血栓形成的实验（大鼠）模型中研究了其抗血栓作用，并与已知结果的肝素进行了比较。肝素（400微克/千克）和水蛭素（12.5、25和50微克/千克）均具有抗血栓作用，并能限制现有血栓的扩展（p<0.05）。较高剂量的肝素会增加平均出血时间（p<0.05），而水蛭素则不会。因此，重组水蛭素与肝素具有相同的抗血栓作用，但剂量要低得多。这种活性似乎不依赖剂量，且出血效应较弱。
