香草酸酰胺衍生物的制备及其止血活性的动力学法研究

发布时间：2018-03-19 01:12

本文选题：香草酸　切入点：酰胺衍生物　出处：《发光学报》2016年04期 　论文类型：期刊论文

【摘要】：以香草酸为母体,分别与6-氨基己酸(EACA)、止血芳酸(AMBA)和止血环酸(AMCA)反应,合成3种未见文献报道的香草酸酰胺衍生物,并采用IR、ESI-MS、1H NMR和13C NMR进行结构鉴定。以传统方法、荧光动力学法和紫外动力学法测定其对血浆复钙时间(PRT)的影响。为了研究衍生物在血液中的稳定性,在模拟生理条件下,运用荧光光谱、紫外光谱及分子对接技术研究了它分别与人血清白蛋白(HSA)的结合。结果表明,3种衍生物在一定浓度范围内都可以有效缩短PRT,具有显著的止血活性。新的动力学测定方法,不仅有效避免了传统方法引入的人为误差,重现性良好,而且判断标准更加科学,并可以获得更多血浆凝结过程中的信息。3种衍生物均主要通过氢键和范德华力与HSA结合形成稳定的复合物,表明它可通过HSA在血液中传递并运输到相应部位而发生药理作用。
[Abstract]:Three vanilamide derivatives were synthesized from vanillic acid by reacting with 6-amino-caproic acid (EACAA), hemostatic aromatic acid (AMBA) and hemostatic acid (AMCA) respectively. The structures of vanilamide derivatives were identified by IR ESI-MS 1H NMR and 13C NMR. In order to study the stability of derivatives in blood, fluorescence spectra were used under simulated physiological conditions. UV spectra and molecular docking techniques were used to study the binding of HSA with human serum albumin. The results showed that the three derivatives could effectively shorten PRT in a certain concentration range, and had remarkable hemostatic activity. It not only effectively avoids the artificial error introduced by the traditional method, but also has good reproducibility, and the judgment standard is more scientific. More information in plasma coagulation can be obtained. 3 derivatives can form stable complexes by hydrogen bonding and van der Waals force binding with HSA, which indicates that they can be transported to the corresponding sites through HSA and have pharmacological effects.
【作者单位】：广西大学化学化工学院;广西医科大学第一附属医院;南宁市化工研究设计院;广西高校应用化学技术与资源开发重点实验室;
【基金】：广西研究生教育创新计划(YCBZ2013011) 广西自然科学基金重点项目(2013GXNSFDA019005) 国家自然科学基金(21362001)资助项目
【分类号】：R943;R96

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