芦荟大黄素对α-葡萄糖苷酶的抑制作用及机理  

Inhibitory effect and mechanism of aloe-emodin on α-glucosidase

作　　者：潘若瑶 任国艳[1,2,3] 马富利 彭琪越 杜鹂莹 PAN Ruoyao;REN Guoyan;MA Fuli;PENG Qiyue;DU Liying(College of Food and Bioengineering,Henan University of Science and Technology,Luoyang 471000,China;Henan Engineering Research Center of Food Material,Luoyang 471000,China;National Demonstration Center for Experimental Food Processing and Safety Education,Luoyang 471000,China)

机构地区：[1]河南科技大学食品与生物工程学院,河南洛阳471000 [2]河南省食品原料工程研究中心,河南洛阳471000 [3]国家实验食品加工与安全教育示范中心,河南洛阳471000

出　　处：《食品与发酵工业》2024年第10期134-140,I0001,共8页Food and Fermentation Industries

基　　金：河南省重点科技攻关项目(182102110345)。

摘　　要：抑制α-葡萄糖苷酶活性是控制机体血糖平衡的有效途径。该文通过酶活性实验、紫外光谱法、荧光光谱法、傅里叶变换红外光谱和分子对接等方法研究了芦荟大黄素(aloe-emodin,AE)对α-葡萄糖苷酶的抑制作用及机理。结果表明,AE对α-葡萄糖苷酶活性有显著抑制作用[IC_(50)=(0.031±0.001)mg/mL],抑制类型为混合型抑制。AE通过一个结合位点与酶结合,使酶中的荧光基团发生静态猝灭。AE改变了酶的构象,使酶的α-螺旋、β-转角含量降低,β-折叠、无规则卷曲含量增加。分子对接深入分析结果显示,AE与Thr290、Leu297、Glu296和Asn2592形成氢键,与Leu297等形成范德华力。AE通过这些分子间作用力结合到α-葡萄糖苷酶的疏水结合腔内,改变了酶的构象,使酶活性降低。Inhibition ofα-glucosidase activity is an effective way to control blood glucose balance.The inhibitory effect of aloe emodin(AE)onα-glucosidase and its mechanism were studied by enzyme activity inhibition experiment,ultraviolet spectroscopy,fluorescence spectrometry,Fourier transform infrared spectroscopy,and molecular docking.Results showed that AE had a significant inhibitory effect onα-glucosidase activity[(IC_(50)=(0.031±0.001)mg/mL)],and the inhibitory type was mixed inhibition.AE bound toα-glucosidase with a binding site by static quenching mechanism.The interaction of AE andα-glucosidase changed the conformation ofα-glucosidase,resulting in a decrease in theα-helix,β-turn content and an increase in theβ-sheet and random coil content.Further analysis by molecular docking showed that AE formed hydrogen bonds with Thr290,Leu297,Glu296,and Asn2592,formed van der Waals forces with Leu297.AE bound to the hydrophobic binding cavity ofα-glucosidase by these intermolecular forces,changing the conformation of the enzyme and reducing enzyme activity.

关 键 词：芦荟大黄素 Α-葡萄糖苷酶 抑制作用 光谱 分子对接 

分 类 号：TS201.4[轻工技术与工程—食品科学]