关于基于共轭聚合物的α-葡萄糖苷酶抑制剂的荧光传感研究.docVIP

基于共轭聚合物的α－葡萄糖苷酶抑制剂 唐艳丽*，， 应用表面与胶体化学教育部重点实验室， *Email: yltang@snnu.edu.cn 糖尿病是一种代谢紊乱性疾病，是目前世界上发病率高、最严重的慢性病之一。α－葡萄糖苷酶抑制剂((α－glucosidase inhibitor ( α－GI))通过抑制α－葡萄糖苷酶的活性，从而延缓蔗糖向葡萄糖和果糖的转化，减少高血糖对胰腺的刺激，提高胰岛素敏感性，有效预防糖尿病并改善并发症的发生和发展。我们设计了一种基于水溶性共轭聚合物PFP的荧光传感新方法，实现了α－GI的灵敏快速检测。在中性缓冲液中，α－葡萄糖苷酶的底物para-nitrophenyl-α-D-glucoside (PNPG)被α－葡萄糖苷酶水解，释放出具有良好淬灭作用的阴离子型对硝基苯酚，该化合物通过静电相互作用与阳离子PFP相结合，并有效的淬灭了PFP的荧光。在α－GI存在下，PNPG的水解被抑制，从而使得PFP的荧光得以恢复。通过检测PFP的荧光淬灭与恢复，可以简单灵敏的筛选α－GI。该荧光传感新方法有望用于天然产物和合成化合物中α－GI的灵敏快速的体外筛选。 α－ 参考文献 [1] Fernando, B.; Rogelio R.; Robert B.; Martín G.-A.; Rachel M. J. Nat. Prod. 2011, 74:314. [2] Tang, Y. L.; Feng, F. D.; Yu, M. H.; An, L. L.; He, F.; Wang, S.; Li, Y. L.; Zhu, D. B. Adv. Mater. 2008, 20:703. Novel Fluorescent Biosensor for α-glucosidase Inhibitors Screening Based on Cationic Conjugated Polymer Yanli Tang*, Ali Cao, Xiaoteng Mu, Yue Liu Key Laboratory of Applied Surface and Colloid Chemistry, MOE, School of Chemistry and Chemical Engineering, Shaanxi Normal University, 199 South Chang’an road, Xi’an, 710062 A new fluorescent sensor has been developed to screen α-glucosidase inhibitors (AGIs) sensitivel and simply by taking advantage of signal amplification effect of conjugated polymers. The fluorescence intensity of (poly{(1,4-phenylene)-2,7-[9,9-bis(6’-N,N,N-trimethylammonium) hexyl fluorene]diiodide}) (PFP) was found to be quenched effectively by p-nitrophenol in neutral buffer solution. The electrostatic interaction brings cationic PFP and anionic p-nitrophenol to a close proximity, which induces the superquenching phenomenon between them. P-nitrophenol can be released after para-nitrophenyl-α-D-glucoside (PNPG) being hydrolyzed by α-glucosidase. In the presence of AGIs, the activities of α-glucosidase are inactivated and then the cleavage of the substrate PNPG is inhibited. The fluorescence intensity of PFP is recovered without significant decreasing. Thus, a sensitive method is designed to screen AGIs in vitro based on the fluorescence turn-off /