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New Drug Screening Model Using Enzymes Immobilized on Mesoporous Materials: A Proof-of-Concept Study Using Immobilized α-Glucosidase and Acarbose

Journal 2016 · IF 1.338 · 16(12): 12460-12469 · 发表于 2016 年 12 月 1 日
作者: Hu Yinghui,An Jing,Liu Xiujie,Wang Huiheng,Dai Rongji,Deng Yulin
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摘要

Enzyme immobilization increases the availability of the enzyme to the substrate with a higher turnover over a considerable period. For this purpose, a variety of mesoporous materials with different diameters were synthesized by various methods using different ratios of P123 (template agent) to 1,3,5-trimethylbenzene (expanding agent). These versatile materials were then characterized by transmission electron microscopy and N2 adsorption–desorption analysis. α-Glucosidase was successfully immobilized on all the synthesized materials, but the P123/TMB = 4/3-COOH-PMO material had a higher loading rate and enzyme activity. Furthermore, applications of this material were best performed in a column to immobilize the enzymes. Additionally, the synthesized material was further tested using acarbose as a model compound for drug screening. The immobilized α-glucosidase was packed into a column and connected to HPLC instrument to screen 20 small molecular compounds. Using this method, several drugs that might strongly inhibit α-glucosidase were identified. Therefore, this method can be further used in drug screening for chemical drugs and traditional Chinese medicines to expedite new drug research.