α-葡萄糖苷酶抑制剂体外筛选方法的研究  

Study of Screening Method for α-glucosidase Inhibitors in Vitro

作　　者：朱文佳[1] 寇自农[2] 张曦[1] 付绍平[1] 朱靖博[1,3] 萧伟[3,4] 

机构地区：[1]大连工业大学食品学院植物资源化学与应用研究所,辽宁大连116034 [2]大连工业大学现代教育技术部,辽宁大连116034 [3]中药制药过程新技术国家重点实验室(筹),江苏连云港222001 [4]江苏康缘药业股份有限公司,江苏连云港222001

出　　处：《食品研究与开发》2012年第8期171-175,共5页Food Research and Development

基　　金：中药制药过程新技术国家重点实验室开放基金课题(SKL2010Z0201)

摘　　要：以对-硝基苯-α-D-吡喃葡萄糖苷为底物,通过高效液相色谱定量分析水解产物对-硝基苯酚,确定α-葡萄糖苷酶的活性,建立新的α-葡萄糖苷酶抑制剂的体外筛选方法,为了提高筛选方法的灵敏度,对酶促反应条件进行了优化,并用阿卡波糖验证筛选方法的可靠性,结果测得阿卡波糖的IC50为2.07 mg/mL,与文献报道相近,说明该法可替代传统的Trembly法,并可用于α-葡萄糖苷酶抑制剂的高通量筛选。A novel screening method for a-glucosidase inhibitors has been established by HPLC in vitro. The enzymatic activities of a-glucosidase were determined by monitoring the release of PNP from the substrate PNPG.. In order to improve the detection sensitivity, the conditions of enzyme-catalyzed reaction were optimized. Acarbose was used to validate the established method. The results showed that the IC50 values of a- glucosidase inhibitors activities of Acarbose was 2.07 mg/mL. Which was closed to the experimental date reported in literatures. So this method could be used as an alternative of traditional method of ＂Trembly＇, and it could be used in the high-throughput screening of a-glucosidase inhibitors.

关 键 词：Α-葡萄糖苷酶抑制剂 高效液相色谱 筛选模型 糖尿病 酶动力学 

分 类 号：R587.1[医药卫生—内分泌]