Desnoyers P, Bara L, Samama M
Laboratoire Central d'Hématologie, Hôtel-Dieu, Paris, France.
Pathol Biol (Paris). 1989 Jun;37(6):759-67.
Although the specific anticoagulant activity of dermatan sulphate is seventy times less than that of standard heparin, its venous antithrombotic activity, tested on a great number of experimental models, appears at gravimetric doses which are only seven fold higher. This antithrombotic activity is not correlated with the factor Xa inhibition, but is associated with thrombin generation inhibition and potentiation of heparin cofactor II. Meanwhile, others factors, still non entirely identified, i.e. like the release of endogenous tissue plasminogen activators, must probably be involved in the antithrombotic activity of dermatan sulphate. In contrast to heparin, dermatan sulphate possesses hemorrhagic properties only at doses which are forty times higher than the antithrombotic dose. These hemorrhagic properties seem associated with an inhibition of collagen induced platelet aggregation. Finally, the pharmacokinetic profile of dermatan sulphate after intravenous injection in the rabbit, is different from that of standard heparin, and close to that of low molecular weight heparins.
尽管硫酸皮肤素的特定抗凝血活性比标准肝素低70倍,但其在大量实验模型上测试的静脉抗血栓活性,在重量剂量仅高7倍时就会出现。这种抗血栓活性与Xa因子抑制无关,而是与凝血酶生成抑制和肝素辅因子II的增强有关。与此同时,其他尚未完全确定的因素,如内源性组织纤溶酶原激活剂的释放,可能也参与了硫酸皮肤素的抗血栓活性。与肝素不同,硫酸皮肤素仅在比抗血栓剂量高40倍的剂量下才具有出血特性。这些出血特性似乎与胶原诱导的血小板聚集抑制有关。最后,硫酸皮肤素静脉注射给兔子后的药代动力学特征与标准肝素不同,与低分子量肝素相近。