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目的研究半合成-β1,4-葡聚糖硫酸钠(Na-MCS)的抗凝血效果和作用机制。方法采用凝固分析法、以肝素为阳性对照进行抗凝血效果的评价,再通过发色底物法对凝血因子进行抑制分析,揭示Na-MCS的抗凝血作用机制。结果0.6μg.mL-1Na-MCS即可显著延长APTT和TT,但在更高浓度下对PT影响仍不大,使正常人血浆的APTT延长1倍的Na-MCS剂量为0.7μg.mL-1,低于活性为150 u.mg-1的肝素。结论在一定浓度范围内,Na-MCS的抗凝血活性与肝素相当,Na-MCS通过抗凝血酶AT-III的调节作用来抑制凝血因子IIa和Xa的活性,从而产生抗凝血作用。
Objective To study the anticoagulant effect and mechanism of semisynthetic-β1,4-dextran sulfate sodium (Na-MCS). Methods The coagulation analysis method was used to evaluate the anticoagulant effect of heparin as positive control. The inhibitory analysis of coagulation factors by chromogenic substrate method revealed the anticoagulant mechanism of Na-MCS. Results 0.6μg.mL-1Na-MCS can significantly prolong the APTT and TT, but at a higher concentration of PT is still not large, so that the normal plasma APTT double the amount of Na-MCS 0.7μg.mL- 1, lower than the activity of 150 u.mg-1 of heparin. CONCLUSION: Na-MCS exhibits anticoagulant activity comparable to that of heparin at a range of concentrations. Na-MCS inhibits the activity of coagulation factors IIa and Xa by the action of antithrombin AT-III, resulting in anticoagulant effects.