Chemical Engineering Department, Wuhan University of Technology, Wuhan 430070, China.
Int J Biol Macromol. 2012 Dec;51(5):808-14. doi: 10.1016/j.ijbiomac.2012.07.029. Epub 2012 Aug 3.
In order to develop a promising substitute for heparin, N-succinyl chitosan (NSC) was chemically modified by sulfating agent N(SO(3)Na)(3), which were synthesized with sodium bisulfite and sodium nitrite in aqueous solution. The N-succinyl chitosan sulfates (NSCS) products were characterized by infrared spectroscopy (FT-IR) and (13)C NMR. The degree of substitution (DS) of NSCS depended on the ratio of sulfating agent to N-succinyl chitosan, reaction temperature, reaction time and pH of sulfation agent. N-succinyl chitosan sulfates with DS of 1.97 were obtained under optimal conditions. The in vitro coagulation assay of NSCS was determined by activated partial thromboplastin time (APTT), prothrombin time (PT) and thrombin time (TT) assays. The results showed that NSCS obviously prolonged APTT. The anticoagulant activity strongly depended on DS, molecular weight (M(w)) and concentration of NSCS. The anticoagulant activity of NSCS promoted with the increase of DS and concentration, and NSCS exhibited the best anticoagulant activity with the M(w) of 1.37×10(4).
为了开发肝素的有前途的替代品，通过磺化剂 N(SO(3)Na)(3)对 N-琥珀酰壳聚糖（NSC）进行了化学修饰，磺化剂 N(SO(3)Na)(3)是在水溶液中由亚硫酸钠和亚硝酸钠合成的。N-琥珀酰壳聚糖硫酸盐（NSCS）产物通过红外光谱（FT-IR）和（13)C NMR 进行了表征。NSCS 的取代度（DS）取决于磺化剂与 N-琥珀酰壳聚糖的比例、反应温度、反应时间和磺化剂的 pH 值。在最佳条件下，得到了 DS 为 1.97 的 N-琥珀酰壳聚糖硫酸盐。通过激活部分凝血活酶时间（APTT）、凝血酶原时间（PT）和凝血时间（TT）测定法测定了 NSCS 的体外凝血测定。结果表明，NSCS 明显延长了 APTT。抗凝活性强烈依赖于 DS、分子量（M(w)）和 NSCS 的浓度。随着 DS 和浓度的增加，NSCS 的抗凝活性得到促进，并且 NSCS 表现出最佳的抗凝活性，M(w)为 1.37×10(4)。
