Onishi M, Miyashita Y, Motomura T, Yamashita S, Sakamoto N, Akashi M
R&D Department, Terumo Corp., Kanagawa, Japan.
J Biomater Sci Polym Ed. 1998;9(9):973-84. doi: 10.1163/156856298x00280.
We studied anticoagulant and antiprotease activities of the poly(glucosyloxyethyl methacrylate) sulfate [poly(GEMA)-sulfate] in plasma and purified enzyme systems in order to evaluate the anticoagulant behavior of a heparin-like sulfated glucoside-bearing polymer. As a result, we found that poly(GEMA)-sulfate can inhibit some coagulation proteases, although its antiprotease behavior differed from those of heparin and dextran sulfate. Poly(GEMA)-sulfate could not enhance antithrombin activity; therefore, we did not observe any significant inhibition of Factor Xa via antithrombin. However, we found that poly(GEMA)-sulfate was able to inhibit thrombin through the activation of heparin cofactor II. In addition, poly(GEMA)-sulfate was able to inhibit Tenase. In our previous research. we found that the anticoagulant activity of poly(GEMA)-sulfate is due primarily to the formation of an insoluble complex with fibrinogen. This paper showed that the antiprotease activities of poly(GEMA)-sulfate contribute to some extent to its anticoagulant activity.
我们研究了聚（甲基丙烯酸葡糖氧基乙酯）硫酸盐[聚（GEMA）-硫酸盐]在血浆和纯化酶系统中的抗凝和抗蛋白酶活性，以评估一种类似肝素的含硫酸化葡糖苷聚合物的抗凝行为。结果，我们发现聚（GEMA）-硫酸盐可以抑制一些凝血蛋白酶，尽管其抗蛋白酶行为与肝素和硫酸葡聚糖不同。聚（GEMA）-硫酸盐不能增强抗凝血酶活性；因此，我们未观察到通过抗凝血酶对因子Xa的任何显著抑制作用。然而，我们发现聚（GEMA）-硫酸盐能够通过激活肝素辅因子II来抑制凝血酶。此外，聚（GEMA）-硫酸盐能够抑制凝血酶原酶复合物。在我们之前的研究中，我们发现聚（GEMA）-硫酸盐的抗凝活性主要归因于与纤维蛋白原形成不溶性复合物。本文表明，聚（GEMA）-硫酸盐的抗蛋白酶活性在一定程度上有助于其抗凝活性。
