Brinkhous K M, Sandberg H, Garris J B, Mattsson C, Palm M, Griggs T, Read M S
Proc Natl Acad Sci U S A. 1985 Dec;82(24):8752-6. doi: 10.1073/pnas.82.24.8752.
The procoagulant protein F.VIII:C is noncovalently bound to von Willebrand factor (vWF) to give the factor VIII macromolecular complex. New highly purified preparations of isolated human F.VIII:C, devoid of vWF and about 500,000-fold purified, were administered to hemophilia A and von Willebrand disease (vWD) dogs to determine their hemostatic effectiveness and survival in the circulation. Two preparations of F.VIII:C were used: peak 1, with active components of Mr 185,000-280,000, and peak 2, with a single component of Mr 170,000. In hemophilic dogs, with no plasma F.VIII:C but normal vWF, both preparations immediately elevated plasma F.VIII:C to expected levels, promptly stopped induced and spontaneous hemorrhages, and gave sustained plasma levels of F.VIII:C. The isolated F.VIII:C immediately complexed with endogenous vWF in hemophilic plasma and was eliminated exponentially, with a half-life (t1/2) of about 9 hr. Survival of peak 2 F.VIII:C was longer than that of peak 1 material. In contrast, F.VIII:C complexed to vWF in a therapeutic concentrate administered to hemophilic dogs was eliminated biexponentially with first-phase t1/2 of 3.2 hr and second-phase t1/2 of 9 hr. In vWD dogs with no vWF and reduced F.VIII:C levels, the isolated F.VIII:C produced supernormal levels of F.VIII:C without effect on induced bleeding. It was rapidly eliminated from plasma with a t1/2 of about 1 hr, as was the complexed F.VIII:C in the concentrate. These data indicate that isolated F.VIII:C promptly complexes with vWF and in this form is highly effective in controlling hemophilic hemorrhages with good survival in plasma. Without endogenous vWF with which to complex, the F.VIII:C is promptly eliminated.
促凝血蛋白F.VIII:C与血管性血友病因子(vWF)非共价结合,形成VIII因子大分子复合物。将新的高度纯化的、不含vWF且纯度约为50万倍的人F.VIII:C分离制剂给予甲型血友病和血管性血友病(vWD)犬,以确定其止血效果和在循环中的存活情况。使用了两种F.VIII:C制剂:峰1,活性成分的分子量为185,000 - 280,000;峰2,单一成分的分子量为170,000。在没有血浆F.VIII:C但vWF正常的血友病犬中,两种制剂均能立即将血浆F.VIII:C提高到预期水平,迅速停止诱导性和自发性出血,并使血浆F.VIII:C水平持续维持。分离的F.VIII:C立即与血友病血浆中的内源性vWF结合,并呈指数级消除,半衰期(t1/2)约为9小时。峰2的F.VIII:C存活时间比峰1的物质长。相比之下,给予血友病犬的治疗性浓缩物中与vWF结合的F.VIII:C呈双指数消除,第一相t1/2为3.2小时,第二相t1/2为9小时。在没有vWF且F.VIII:C水平降低的vWD犬中,分离的F.VIII:C产生超正常水平的F.VIII:C,但对诱导性出血无影响。它从血浆中迅速消除,t1/2约为1小时,浓缩物中结合的F.VIII:C也是如此。这些数据表明,分离的F.VIII:C能迅速与vWF结合,以这种形式在控制血友病性出血方面非常有效,且在血浆中具有良好的存活能力。如果没有内源性vWF与之结合,F.VIII:C会迅速被消除。