Liu Si-Yao, Wang Huan, He Tian, Qi Liang, Zhang Zhi-Qi
Key Laboratory of Analytical Chemistry for Life Science of Shaanxi Province, School of Chemistry and Chemical Engineering, Shaanxi Normal University, Xi'an, 710062, China.
Luminescence. 2016 Feb;31(1):96-101. doi: 10.1002/bio.2929. Epub 2015 May 12.
A fluorescence method was established for a α-glucosidase activity assay and inhibitor screening based on β-cyclodextrin-coated quantum dots. p-Nitrophenol, the hydrolysis product of the α-glucosidase reaction, could quench the fluorescence of β-cyclodextrin-coated quantum dots via an electron transfer process, leading to fluorescence turn-off, whereas the fluorescence of the system turned on in the presence of α-glucosidase inhibitors. Taking advantage of the excellent properties of quantum dots, this method provided a very simple, rapid and sensitive screening method for α-glucosidase inhibitors. Two α-glucosidase inhibitors, 2,4,6-tribromophenol and acarbose, were used to evaluate the feasibility of this screening model, and IC50 values of 24 μM and 0.55 mM were obtained respectively, which were lower than those previously reported. The method may have potential application in screening α-glucosidase inhibitors.
建立了一种基于β-环糊精包被量子点的α-葡萄糖苷酶活性测定及抑制剂筛选的荧光方法。对硝基苯酚是α-葡萄糖苷酶反应的水解产物,它可通过电子转移过程淬灭β-环糊精包被量子点的荧光,导致荧光猝灭,而在α-葡萄糖苷酶抑制剂存在时体系荧光开启。利用量子点的优异性能,该方法为α-葡萄糖苷酶抑制剂提供了一种非常简单、快速且灵敏的筛选方法。使用两种α-葡萄糖苷酶抑制剂2,4,6-三溴苯酚和阿卡波糖评估该筛选模型的可行性,分别获得IC50值为24 μM和0.55 mM,均低于先前报道的值。该方法在筛选α-葡萄糖苷酶抑制剂方面可能具有潜在应用。