Antithrombin III-Binding Site Analysis of Low-Molecular-Weight Heparin Fractions

作者：Chen, Yin; Zhao, Jing; Yu, Yanlei; Liu, Xinyue; Lin, Lei; Zhang, Fuming; Linhardt, Robert J.^*

来源：Journal of Pharmaceutical Sciences, 2018, 107(5): 1290-1295.

DOI：10.1016/j.xphs.2018.01.008

• heparin
• LMWH
• gel permeation chromatography
• compositional analysis
• LC-MS
• SPR

Low-molecular-weight heparins (LMWHs) are widely used as clinical anticoagulant drugs. LMWHs are heterogeneous and highly negatively charged glycans prepared by chemical or enzymatic depolymerization of unfractionated heparin. The detailed structural analysis of a LMWH is essential for the drug quality control. In this study, an LMWH, enoxaparin sodium (a generic version of Lovenox) was separated into different molecular weight fractions by a Superdex peptide column. The disaccharide compositions, 3-O-sulfo groupecontaining tetrasaccharides composition, and antithrombin III-binding affinity of the fractions from this LMWH were analyzed. The results showed that all the fractions had very similar disaccharide and 3-O-sulfo groupecontaining tetrasaccharide compositions, but the fraction containing larger-sized chains had higher antithrombin III-binding affinity.

• 出版日期2018-5
• 单位浙江海洋大学