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A silica gel plate-based qualitative assay for acetylcholinesterase activity: A mass method to screen for potential inhibitors

✍ Scribed by John S. Kiely; Walter H. Moos; Micheal R. Pavia; Roy D. Schwarz; Gail L. Woodard


Publisher
Elsevier Science
Year
1991
Tongue
English
Weight
423 KB
Volume
196
Category
Article
ISSN
0003-2697

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✦ Synopsis


A procedure for the qualitative assessment of inhibitory activity towards acetylcholinesterase for a given compound is described. Solutions of the compounds of interest are spotted on silica gel TLC plates in a matrix pattern. The silica gel plate is sprayed with a solution of acetylthiocholine iodide and 5,5-dithiobis(2-nitrobenzoic acid) followed by a solution of acetylcholinesterase. The enzyme reaction produces a yellow background color with inhibitor compounds exposed as white zones where color has failed to develop. The results for a test set of compounds were compared to those obtained using the standard Ellman assay procedure and found to agree for virtually all of these compounds. The conditions of silica gel plate thickness, reagent concentration, and enzyme source under which this procedure is suitable were investigated. This represents an extremely rapid method to screen large numbers of compounds to uncover new inhibitors of acetylcholinesterase and potentially other enzymes as well.