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

作　　者：祝贺[1] 吕友晶[1] 韩现伟[1] 刘世龙[1] 郝杰杰[1] 赵小亮[1] 于广利[1] 

机构地区：[1]中国海洋大学医药学院,海洋药物教育部重点实验室,山东省糖科学与糖工程重点实验室,山东青岛266003

出　　处：《药学学报》2014年第7期1049-1053,共5页Acta Pharmaceutica Sinica

基　　金：国家科技支撑计划(2013BAB01B02);国家自然科学基金资助项目(31070724)

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。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.

关 键 词：依诺肝素钠 1 6-酐衍生物 聚丙烯酰胺凝胶电泳 高效液相色谱 抗凝血活性 

分 类 号：R917[医药卫生—药物分析学]