Krupinski K, Breddin H K, Casu B
Department of Haematology, Medical School, Biaøystok, Poland.
Haemostasis. 1990;20(2):81-92. doi: 10.1159/000216112.
Pig mucosal heparin (GAG 98), in which the binding site for antithrombin had been inactivated by periodate oxidation (GAG 262), a supersulfated low-molecular-weight heparin (GAG 869), a low-molecular-weight heparin (Fragmin), and sodium pentosanpolysulfate have been investigated on their anticoagulant effects in vitro and ex vivo and in an animal thrombosis model in which rat mesenteric venules are damaged by defined laser energy. GAG 262 and pentosanpolysulfate had a markedly reduced anticoagulant effect compared to heparin, Fragmin, and the supersulfated low-molecular-weight heparin fragment. Similarily, the doses necessary to inhibit thrombus formation in the laser model were much higher for GAG 262 and for pentosanpolysulfate compared to heparin and the low-molecular-weight heparin Fragmin, but much lower for the supersulfated heparin fragment. The antithrombotic effect of the low-molecular-weight heparin Fragmin and the supersulfated heparin fragment after subcutaneous injection lasted much longer than the ex vivo detectable anticoagulant effect. Although some correlation between the antithrombotic and the anticoagulant effect in the laser model is evident, there seems to be no direct correlation between amount and duration of factor IIa or factor Xa inhibition and extent and duration of the inhibition of thrombus formation.
猪黏膜肝素（GAG 98），其抗凝血酶结合位点已通过高碘酸盐氧化使其失活（GAG 262），一种超硫酸化低分子量肝素（GAG 869），一种低分子量肝素（法安明），以及戊聚糖多硫酸钠，已在体外、离体以及在大鼠肠系膜小静脉被特定激光能量损伤的动物血栓形成模型中研究了它们的抗凝作用。与肝素、法安明和超硫酸化低分子量肝素片段相比，GAG 262和戊聚糖多硫酸钠的抗凝作用明显降低。同样，在激光模型中抑制血栓形成所需的剂量，GAG 262和戊聚糖多硫酸钠比肝素和低分子量肝素法安明高得多，但超硫酸化肝素片段则低得多。皮下注射后，低分子量肝素法安明和超硫酸化肝素片段的抗血栓作用持续时间比离体可检测到的抗凝作用长得多。虽然在激光模型中抗血栓作用与抗凝作用之间存在一些相关性，但因子IIa或因子Xa抑制的量和持续时间与血栓形成抑制的程度和持续时间之间似乎没有直接相关性。
