抗凝血酶 III 结合位点分析的低分子量肝素片段。
Antithrombin III-Binding Site Analysis of Low-Molecular-Weight Heparin Fractions.
机构信息
Department of Food and Pharmacy, Zhejiang Ocean University, Zhoushan, China.
Department of Biology, Chemical and Biological Engineering, Biomedical Engineering, and Chemistry and Chemical Biology, Center for Biotechnology and Interdisciplinary Studies, Rensselaer Polytechnic Institute, Troy, New York 12180.
出版信息
J Pharm Sci. 2018 May;107(5):1290-1295. doi: 10.1016/j.xphs.2018.01.008. Epub 2018 Jan 12.
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 group-containing 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 group-containing tetrasaccharide compositions, but the fraction containing larger-sized chains had higher antithrombin III-binding affinity.
低分子量肝素（LMWH）广泛用作临床抗凝药物。LMWH 是通过对未分级肝素进行化学或酶解聚合制备的异质且带高度负电荷的聚糖。LMWH 的详细结构分析对于药物质量控制至关重要。在这项研究中，依诺肝素钠（Lovenox 的一种仿制药）通过 Superdex 肽柱分离成不同分子量的级分。分析了该 LMWH 级分的二糖组成、含 3-O-磺基的四糖组成和抗凝血酶 III 结合亲和力。结果表明，所有级分的二糖和含 3-O-磺基的四糖组成非常相似，但含有较大链的级分具有更高的抗凝血酶 III 结合亲和力。
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