王兆梅, 李琳, 李冰, 郭祀远. 半合成β-1,4-葡聚糖硫酸钠的抗凝血特性J. 药学学报, 2006, 41(4): 323-327.
引用本文: 王兆梅, 李琳, 李冰, 郭祀远. 半合成β-1,4-葡聚糖硫酸钠的抗凝血特性J. 药学学报, 2006, 41(4): 323-327.
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WANG Zhao-mei, LI Lin, LI Bing, GUO Si-yuan. Anticoagulant property of a semi-synthesized sodium β-1,4-glucan sulfateJ. Acta Pharmaceutica Sinica, 2006, 41(4): 323-327.
Citation: WANG Zhao-mei, LI Lin, LI Bing, GUO Si-yuan. Anticoagulant property of a semi-synthesized sodium β-1,4-glucan sulfateJ. Acta Pharmaceutica Sinica, 2006, 41(4): 323-327.
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半合成β-1,4-葡聚糖硫酸钠的抗凝血特性

Anticoagulant property of a semi-synthesized sodium β-1,4-glucan sulfate

    摘要
  • 摘要: 目的研究半合成β-1,4-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0.6 μg·mL-1 Na-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0.7 μg·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。

     

    Abstract: AimTo investigate the anticoagulant efficacy and mechanism of a semi-synthesized sodium β-1,4-glucan sulfate (Na-MCS). MethodsAnticoagulant activity was evaluated by means of coagulation assays in comparison with heparin. The anticoagulant mechanism of Na-MCS was disclosed by inhibitory analysis of the activities of coagulation factors using chromogenic substrates. Results0.6 μg·mL-1 Na-MCS could significantly prolong APTT and TT, but has less effect on PT at an even higher concentration. The dosage of Na-MCS required to double APTT of normal human plasma was 0.7 μg·mL-1, lower than that of heparin with the activity of 150 u·mg-1. ConclusionNa-MCS represented a potent anticoagulation activity in vitro, which matched the efficacy of heparin in a certain range of concentrations. Na-MCS exhibited anticoagulant activity due to inhibition of the coagulation factors IIa and Xa by the mediation of anti-thrombin AT-III.

     

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