阳离子淀粉硫酸酯的制备及其抗凝血活性

阳离子淀粉硫酸酯的制备及其抗凝血活性 Synthesis and Anticoagulant Activity of Quaternary Ammonium Cationic Starch Sulfates 樊李红 FAN Lihong 1 first-author 沈元 SHEN Yuan 1 徐咏梅 XU Yongmei 1 江澜 JIANG Lan 1 王晓东 WANG Xiaodong 1 周月 ZHOU Yue 1 潘晓然 PAN Xiaoran 1 武汉理工大学化学工程学院 武汉理工大学化学工程学院 College of Chemical Engineering,Wuhan University of Technology College of Chemical Engineering,Wuhan University of Technology 采用由亚硫酸氢钠和亚硝酸钠在水溶液中合成的近似中性的酯化剂N（SO3Na）3在水溶液中对季铵型阳离子淀粉（QACS）进行改性处理,制备了季铵型阳离子淀粉硫酸酯（QACSS）.通过单因素实验优化得到酯化反应的最佳反应条件:pH=10.0,酯化剂的摩尔量与QACS的质量之比2∶314.5（mol/g）,反应温度40℃,反应时间为22 h.通过测定凝血酶原时间（PT）、凝血活酶时间（APTT）以及凝血酶时间（TT）,证明了QACSS有较优的抗凝血活性.随着QACSS取代度和浓度的增加,APTT明显增长,而TT与PT的增长趋势不明显;随着分子量的增加,APTT先增加而后减小,TT与PT变化不明显.QACSS的抗凝血性能优于QACS,分子量为2.51×104（取代度为1.83）的QACSS样品抗凝血效果最明显. Quaternary ammonium cationic starch sulfate（QACSS） was synthesized by chemical modification of quaternary ammonium cationic starch（QACS） with trisulfonated sodium amine（N（SO 3 Na） 3 ）.This sulfating agent was close to neutral,and synthesized by reaction of sodium bisulfite and sodium nitrite in aqueous solution.The reaction conditions for the sulfonation process were optimized through posttest-only control group design.The optimal pH value of the sulfating agent solution was 10.0,the optimal ratio of sulfating agent to QACS was 2.0/314.5（mol/g）,the reaction temperature was 40 ℃,the reaction time was about 22 h,respectively.The DS of QACSS was measured by barium sulfate nephelometry method,and the biggest DS was 1.83.The molecular weight was determined as 2.51×104 by static light scattering.Anticoagulant activity of QACSS was investigated by APTT,TT and PT assays.The results showed that QACSS exhibited good anticoagulant activity.The results also showed that with the increase of DS and concentration,APTT increased significantly,but TT and PT do not increased obviously.APTT prolonged as the molecular weight rose firstly and then decreased slowly with further increase in molecular weight.The best molecular weight was around 2.51×104.In addition,the anticoagulant activity of QACSS was better than QACS. 阳离子淀粉硫酸酯 取代度 磺酸化 抗凝血 quaternary ammonium cationic starch sulfate degree of substitution sulfonation anticoagulant activity 10.14188/j.1671-8836.2011.04.013 R96;TQ460.1 国家自然科学基金（50503019）;教育部高等学校博士学科点专项科研基金课题（200804971074）;湖北省自然科学基金（2008CDB282）资助项目;武汉市科技攻关（201060623262）;武汉理工大学创新基金（2010-IV-070）资助项目 2011-04-01 2021-04-01 4 57