文献类型：期刊文献

英文题名：alpha-glucosidase immobilization on magnetic core-shell metal-organic frameworks for inhibitor screening from traditional Chinese medicines

作者：Wan, Guang-Zhen[1];Ma, Xiao-Hui[2];Jin, Ling[2];Chen, Juan[1]

第一作者：Wan, Guang-Zhen

通信作者：Chen, J[1];Jin, L[2]

机构：[1]Lanzhou Univ, Sch Pharm, Lanzhou 730000, Peoples R China;[2]Gansu Univ Chinese Med, Coll Pharm, Lanzhou 730000, Peoples R China

第一机构：Lanzhou Univ, Sch Pharm, Lanzhou 730000, Peoples R China

通信机构：[1]corresponding author), Lanzhou Univ, Sch Pharm, Lanzhou 730000, Peoples R China;[2]corresponding author), Gansu Univ Chinese Med, Coll Pharm, Lanzhou 730000, Peoples R China.|[1073501e14fb35863569f]甘肃中医药大学药学院（西北中藏药协同创新中心办公室）;[10735]甘肃中医药大学;

年份：2021

卷号：205

外文期刊名：COLLOIDS AND SURFACES B-BIOINTERFACES

收录：;WOS:【SCI-EXPANDED(收录号:WOS:000703107600005)】；

基金：This work was funded by Special Foundation for National Science and Technology Basic Resources of China (2018FY100701), the Key Program of Natural Science Foundation of Gansu Province, China (20JR10RA584), National Survey of Traditional Chinese Medicine Resources of National Administration of Traditional Chinese Medicine (GZY-KJS-2018-004; GZY-KJS-2019-001), and Special Subsidy for Public Health Services of Traditional Chinese Medicine, China (CS [2018]-43).

语种：英文

外文关键词：alpha-glucosidase; Immobilized enzyme; Magnetic metal-organic frameworks; Capillary electrophoresis; Inhibitor screening

摘要：In this work, a simple and rapid screening strategy was developed combining capillary electrophoresis analysis with enzymatic assay based on immobilized alpha-glucosidase. For alpha-glucosidase immobilization, magnetic core-shell metal-organic frameworks composite (Fe3O4@CS@ZIF-8) was fabricated by a step-by-step assembly method, and alpha-glucosidase was in situ encapsulated in crystal lattice of ZIF-8. The composite was characterized by transmission electron microscopy, Fourier transform infrared spectroscopy, X-ray diffraction and vibrating sample magnetometer. After immobilization, alpha-glucosidase exhibited enhanced tolerance to temperature and pH, and its reusability was greatly improved with 74 % of initial enzyme activity after being recycled 10 times. The Michaelis-Menten constant of immobilized enzyme was calculated to be 0.47 mM and its inhibition constant and IC50 for acarbose were 0.57 mu M and 0.18 mu M, respectively. The immobilized enzyme was subsequently applied to inhibitor screening from 14 TCMs, and Rhei Radix et Rhizoma was screened out. Among the commercially available 10 components presented in Rhei Radix et Rhizoma, gallic acid, (+)-catechin and epicatechin exhibited the strongest inhibitory effect on alpha-glucosidase. Their binding sites and modes with alpha-glucosidase were simulated via molecular docking to further verify the inhibition screening assay results. The positive results indicated that the Fe3O4@CS@ZIF-8-based screening strategy may provide a new avenue for discovering enzyme inhibitors from TCMs.