Anticoagulant Heparin Mimetics via RAFT Polymerization.,Biomacromolecules

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Anticoagulant Heparin Mimetics via RAFT Polymerization.
Biomacromolecules ( IF 5.5 ) Pub Date : 2019-12-16 , DOI: 10.1021/acs.biomac.9b01688
Abdullah Al Nahain , Vera Ignjatovic _{1,

2} , Paul Monagle _{1,

2,

3} , John Tsanaktsidis ₄ , George Vamvounis ₅ , Vito Ferro

Affiliation

Heparin, a sulfated polysaccharide derived from animal sources, is the most commonly used parenteral anticoagulant drug, but it suffers from significant safety and supply issues. Herein, we describe the preparation of heparin mimetic homo- and copolymers via the reversible addition-fragmentation chain transfer (RAFT) polymerization in water of commercially available (non-carbohydrate) sulfonated and carboxylated monomers. The anticoagulant activities of the polymers were assessed by activated partial thromboplastin time (APTT), thrombin clotting time (TCT), and for the more promising polymers, thrombin generation, antifactor Xa, and antifactor IIa assays. Sulfonated homopolymers studied herein displayed low cytotoxicity and significant anticoagulant activity in APTT, TCT, and thrombin generation assays. In addition, copolymers of sodium styrenesulfonate and acrylic acid [poly(SSS-co-AA)] displayed unprecedented antifactor IIa activity. This study demonstrates the potential of RAFT polymers as alternative anticoagulants for biomedical applications.

中文翻译：

通过RAFT聚合的抗凝肝素模拟物。

肝素，一种源自动物的硫酸化多糖，是最常用的肠胃外抗凝药，但存在严重的安全性和供应问题。在这里，我们描述了可逆的加成-断裂链转移（RAFT）聚合在水中可商购的（非碳水化合物）磺化和羧化单体的肝素模拟均聚物和共聚物的制备。通过活化的部分凝血活酶时间（APTT），凝血酶凝血时间（TCT）评估了聚合物的抗凝活性，对于更有希望的聚合物，还通过凝血酶生成，抗因子Xa和抗因子IIa分析来评估聚合物的抗凝活性。本文研究的磺化均聚物在APTT，TCT和凝血酶生成分析中显示出低细胞毒性和显着的抗凝活性。此外，苯乙烯磺酸钠和丙烯酸的共聚物[poly（SSS-co-AA）]显示出前所未有的抗IIa活性。这项研究证明了RAFT聚合物作为生物医学替代抗凝剂的潜力。

更新日期：2019-12-30

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