Sulfonated RAFT Copolymers as Heparin Mimetics: Synthesis, Reactivity Ratios, and Anticoagulant Activity.,Macromolecular Bioscience

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Sulfonated RAFT Copolymers as Heparin Mimetics: Synthesis, Reactivity Ratios, and Anticoagulant Activity.
Macromolecular Bioscience ( IF 4.4 ) Pub Date : 2020-07-06 , DOI: 10.1002/mabi.202000110
Abdullah Al Nahain _{1,

2} , Vera Ignjatovic _{3,

4} , Paul Monagle _{3,

4,

5} , John Tsanaktsidis ₆ , George Vamvounis ₇ , Vito Ferro _{1,

2}

Affiliation

The glycosaminoglycan heparin is a clinically important anticoagulant drug, primarily used to reduce the risk of blood clots (thrombosis) during surgery. Despite its importance in medicine and its continuous use over many decades, heparin suffers from several limitations associated with its heterogeneity and its extraction from animal tissues. In order to address these limitations, reversible addition‐fragmentation chain transfer polymerization is utilized to prepare a library of heparin mimetic copolymers from the sulfonated monomers sodium 4‐styrene sulfonate, potassium‐3‐sulfopropyl acrylate, potassium‐3‐sulfopropyl methacrylate, and sodium‐2‐acrylamido‐2‐methyl‐1‐propane sulfonate. Copolymers are prepared using combinations of two different monomers in various ratios. Monomer reactivity ratios are also determined for some representative monomer combinations, and all polymers are characterized by ¹H NMR spectroscopy and gel permeation chromatography. The anticoagulant activities of the copolymers are determined by activated partial thromboplastin time and thrombin clotting time assays and structure–activity relationships are explored.

中文翻译：

作为肝素模拟物的磺化 RAFT 共聚物：合成、反应比和抗凝活性。

糖胺聚糖肝素是临床上重要的抗凝药物，主要用于降低手术过程中发生血栓（血栓形成）的风险。尽管肝素在医学中很重要并且其连续使用了几十年，但肝素由于其异质性和从动物组织中提取而受到一些限制。为了解决这些限制，可逆加成断裂链转移聚合被用于从磺化单体 4-苯乙烯磺酸钠、3-磺丙基丙烯酸钾、3-磺丙基甲基丙烯酸钾和钠-2-丙烯酰胺-2-甲基-1-丙烷磺酸盐。使用不同比例的两种不同单体的组合来制备共聚物。¹ H NMR光谱和凝胶渗透色谱。共聚物的抗凝活性由活化的部分凝血活酶时间和凝血酶凝固时间测定确定，并探索了结构-活性关系。

更新日期：2020-07-06

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