祝贺, 吕友晶, 韩现伟, 刘世龙, 郝杰杰, 赵小亮, 于广利. 不同1,6-酐衍生度依诺肝素钠结构及其抗凝血活性比较J. 药学学报, 2014,49(7): 1049-1053.
引用本文: 祝贺, 吕友晶, 韩现伟, 刘世龙, 郝杰杰, 赵小亮, 于广利. 不同1,6-酐衍生度依诺肝素钠结构及其抗凝血活性比较J. 药学学报, 2014,49(7): 1049-1053.
ZHU He, LÜ You-jing, HAN Xian-wei, LIU Shi-long, HAO Jie-jie, ZHAO Xiao-liang, YU Guang-li. Comparison of structural characteristics and anticoagulation activity of enoxaparin sodium with different degree of 1, 6-anhydro derivativesJ. Acta Pharmaceutica Sinica, 2014,49(7): 1049-1053.
Citation: ZHU He, LÜ You-jing, HAN Xian-wei, LIU Shi-long, HAO Jie-jie, ZHAO Xiao-liang, YU Guang-li. Comparison of structural characteristics and anticoagulation activity of enoxaparin sodium with different degree of 1, 6-anhydro derivativesJ. Acta Pharmaceutica Sinica, 2014,49(7): 1049-1053.

不同1,6-酐衍生度依诺肝素钠结构及其抗凝血活性比较

Comparison of structural characteristics and anticoagulation activity of enoxaparin sodium with different degree of 1, 6-anhydro derivatives

  • 摘要: 运用聚丙烯酰胺凝胶电泳、高效液相色谱、紫外光谱、红外光谱和核磁共振波谱等手段对不同1,6-酐衍生度的依诺肝素钠的细微结构进行了比较,并进一步测定了它们的抗凝血活性。结果表明,虽然不同1,6-酐衍生度 (20.0%~39.7%) 依诺肝素钠在结构特征方面相似,但它们的抗Xa和抗IIa因子活性却随着1,6-酐衍生度的增大呈现降低趋势,尤其抗Xa因子活性受1,6-酐衍生度的变化较明显。

     

    Abstract: The fine structure of enoxaparin sodium samples with different degree of 1, 6-anhydro derivatives were analyzed with polyacrylamide gel electrophoresis, high performance liquid chromatography, ultraviolet spectroscopy, infrared spectroscopy and nuclear magnetic resonance spectroscopy. A further study of anticoagulation activity of enoxaparins was performed, including those on their inhibition activities of coagulation factor Xa (FXa) and thrombin (FIIa). The results showed that the anti-FXa and -FIIa activities of enoxaparins with different degree of 1, 6-anhydro derivatives (20.0%-39.7%) with similar structure characteristics, had decreasing tendency when the degree of 1, 6-anhydro derivatives increased. Especially, the anti-FXa activity was sensitive to the change of the degree of 1, 6-anhydro derivatives.

     

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