An efficient anticoagulant candidate: Characterization, synthesis and in vivo study of a fondaparinux analogue Rrt1.17.
An efficient anticoagulant candidate: Characterization, synthesis and in vivo study of a fondaparinux analogue Rrt1.17.
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DOI：
10.1016/j.ejmech.2016.12.004
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发表时间：
2017-01
影响因子：
6.7
通讯作者：
Guo-Qiang Zhang;Hongzhen Jin;Yunyan Zhao;Lina Guo;Xue Gao;Xiaoxue Wang;S. Tie;Jie Shen;P. Wang;Hao Gan;Huifei Cui;Wei Zhao
中科院分区：
文献类型：
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作者：
Guo-Qiang Zhang;Hongzhen Jin;Yunyan Zhao;Lina Guo;Xue Gao;Xiaoxue Wang;S. Tie;Jie Shen;P. Wang;Hao Gan;Huifei Cui;Wei Zhao
磺达肝癸钠是一种基于肝素抗凝血酶结合结构域的合成五糖抗凝剂，由50多个步骤的化学合成得到。本文从市售磺达肝癸钠粗品中分离鉴定了9个类似物，并对其体外抗凝活性进行了检测。根据活性结果，化学合成了活性最高的衍生物Rrt 1.17。体外体内生物学特性表明，与磺达肝癸钠相比，定义明确的衍生物Rrt1.17是更有效的抗凝候选药物。
Fondaparinux, a synthetic pentasaccharide anticoagulant based on heparin antithrombin-binding domain, is derived from a chemical synthesis with more than 50 steps. Herein, we identified nine analogues separated from commercially available crude fondaparinux sodium, and tested their anticoagulant activityin vitro. Based on the activity results, the most active derivative Rrt1.17 was chemically synthesized. Biological propertiesin vitroandin vivoindicated that the well-defined derivative Rrt1.17 was a more efficient anticoagulant candidate compared with fondaparinux.