Generation of "Neoheparin" from E coli K5 capsular polysaccharide
Generation of "Neoheparin" from E coli K5 capsular polysaccharide
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DOI：
10.1021/jm049812m
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发表时间：
2005-01-27
影响因子：
7.3
通讯作者：
Casu, B
中科院分区：
文献类型：
--
作者：
Lindahl, U;Li, JP;Casu, B
肝素仍然是预防血栓栓塞性疾病的主要药物。对其动物来源的担忧促使人们寻找肝素类似物。肝素的抗凝活性取决于结合抗凝血酶的特定五糖序列。我们报道了通过对细菌（大肠杆菌 K5）多糖进行化学和酶促修饰的组合，产生了一种具有与肝素相似的抗凝血酶结合、抗凝血和抗血栓特性的产品。该工艺易于大规模生产。
Heparin remains a major drug in prevention of thromboembolic disease. Concerns related to its animal source have prompted search for heparin analogues. The anticoagulant activity of heparin depends on a specific pentasaccharide sequence that binds antithrombin. We report the generation of a product with antithrombin-binding, anticoagulant, and antithrombotic properties similar to those of heparin, through combined chemical and enzymatic modification of a bacterial (E. coli K5) polysaccharide. The process is readily applicable to large-scale production.