发光学报2016，Vol.37Issue(4)：487-497,11.DOI:10.3788/fgxb20163704.0487
香草酸酰胺衍生物的制备及其止血活性的动力学法研究
Synthesis of Vanillylamide Derivatives and Their Hemostatic Activity in Vitro by Kinetics Methods
摘要
Abstract
Three novel amide derivatives were designed and prepared by the reaction of vanillic acid with 6-aminocaproic acid ( EACA) , p-aminomethylbeozoic acid ( AMBA) or tranexamic acid ( AM-CA), respectively. The structures were identified by IR, ESI-MS, 1H NMR and 13C NMR. In order to study their hemostatic activity in vitro, the plasma recalcification time ( PRT) was determined by traditional method, fluorescence kinetics method and UV kinetics method, respectively. In order to study the stability of derivatives in blood, the interaction between derivatives and human serum albu-min ( HSA) was investigated under imitated physiological condition by fluorescence spectroscopy, UV-visible absorption spectroscopy and molecular docking, respectively. The results stated clearly that derivatives could reduce PRT significantly and exhibit obvious procoagulant effect in vitro. Mo-reover, in some concentrations, the hemostatic activity of derivativeIIwas better than AMBA. The results obtained by three different methods were in correspondence. New kinetics methods not only avoided artificial error effectually but also had good repeatability. In addition, more reasonable and credible information could be obtained in the process of serum agglutination. On the other hand, the spectra experiments showed that three derivatives could all form stable complexes with HSA respective-ly. The binding types between derivatives and HSA were all van der Waals force and hydrogen bonds. The results were accordant with molecular docking. It indicates that all the derivatives can be trans-ferred and delivered by HSA to play pharmacological effects at corresponding site. Consequently, there is a strong possibility that the three vanillylamide derivatives can be applied to practice.关键词
香草酸/酰胺衍生物/止血/人血清白蛋白(HSA)/光谱法Key words
vanillic acid/amide derivatives/hemostasia/human serum albumin (HSA)/spectroscopic methodology分类
化学化工引用本文复制引用
杜传荣,林发全,逯东伟,陈丹丹,樊希望,林翠梧..香草酸酰胺衍生物的制备及其止血活性的动力学法研究[J].发光学报,2016,37(4):487-497,11.基金项目
广西研究生教育创新计划(YCBZ2013011) （YCBZ2013011）
广西自然科学基金重点项目(2013GXNSFDA019005) （2013GXNSFDA019005）
国家自然科学基金(21362001)资助项目 （21362001）
