An immobilized acetylcholinesterase as test system to screen new inhibitor drugs to treat alzheimer’s disease

This study presents a rapid and simple method to screen and detect new drugs to treat Alzheimer’s disease. The method uses a test system based on an immobilized acetylcholinesterase from Electrophorus electricus (AChE). The optimal AChE immobilized preparation retained 65% of the original catalytic activity; immobilization improved AChE stability by approximately 200-fold. Inhibition and usability of immobilized AChE in real conditions was studied using tacrine as model inhibitor. The immobilized system enabled to determine variables like IC50, Ki, KD, and ΔGº´ in an uncomplicated way and proved to be an interesting tool for rapid screening of the ability of new target compounds to inhibit AChE. System inertia was also studied to avoid false positives. The system was optimized by making the un-specific interactions between AChE and other compounds from a vegetable extract negligible. Optimization of the immobilized AChE system allowed its efficient application to test mixtures of tacrine, a standard inhibitor, and vegetable extracts as AChE inhibitors. The system was reused at least 15 times with minimal AChE activity loss.Graphical abstract

Source: Sensors and Actuators B: Chemical - September 22, 2018 Category: Chemistry Source Type: research