title: Differential inhibition of human erythrocyte acetylcholinesterase by polyphenols epigallocatechin-3-gallate and resveratrol. Relevance of the membrane-bound form.
abstract: The activity of acetylcholinesterase (AChE) from human erythrocytes was tested in the presence of the phenolic compounds resveratrol and epigallocatechin-3-gallate (EGCG). Even though the stilbene barely changed this enzymatic activity, EGCG did inhibit AChE. Importantly, it preferentially acted on the membrane-bound enzyme rather than on its soluble form. Actually, it was shown that this flavonoid may bind to the red blood cell membrane surface, which may improve the interaction between EGCG and AChE. Therefore, caution should be taken when screening AChE inhibitors. In fact, testing compounds with the soluble form of the enzyme may underestimate the activity of some of these potential inhibitors, hence it would be advisable not to use them as a sole model system for screening. Moreover, erythrocyte AChE is proposed as a good model for these enzymatic assays. © 2016 BioFactors, 43(1):73-81, 2017.
authors: Instituto Superior de Investigaciones Biológicas (CONICET-UNT) and Instituto de Química Biológica ''Dr. Bernabe Bloj'', Facultad de Bioquímica, Química y Farmacia (UNT), Tucumán, Argentina.
authors: Paula B
authors: PB
authors: Salazar
authors: Instituto Superior de Investigaciones Biológicas (CONICET-UNT) and Instituto de Química Biológica ''Dr. Bernabe Bloj'', Facultad de Bioquímica, Química y Farmacia (UNT), Tucumán, Argentina.
authors: Alejandro
authors: A
authors: de Athayde Moncorvo Collado
authors: Instituto Superior de Investigaciones Biológicas (CONICET-UNT) and Instituto de Química Biológica ''Dr. Bernabe Bloj'', Facultad de Bioquímica, Química y Farmacia (UNT), Tucumán, Argentina.
authors: Verónica
authors: V
authors: Canal-Martínez
authors: Instituto Superior de Investigaciones Biológicas (CONICET-UNT) and Instituto de Química Biológica ''Dr. Bernabe Bloj'', Facultad de Bioquímica, Química y Farmacia (UNT), Tucumán, Argentina.
authors: Carlos J
authors: CJ
authors: Minahk
mesh_terms: D000110:Acetylcholinesterase / Q000378:metabolism*; D002392:Catechin / Q000031:analogs & derivatives* / Q000494:pharmacology; D002800:Cholinesterase Inhibitors / Q000494:pharmacology*; D004353:Drug Evaluation, Preclinical; D004910:Erythrocyte Membrane / Q000187:drug effects / Q000201:enzymology*; D006801:Humans; D020128:Inhibitory Concentration 50; D000077185:Resveratrol; D013267:Stilbenes / Q000494:pharmacology*
chemical_list: D002800:Cholinesterase Inhibitors; D013267:Stilbenes; D002392:Catechin; C045651:epigallocatechin gallate; D000110:Acetylcholinesterase; D000077185:Resveratrol
keywords: acetylcholinesterase; epigallocatechin-3-gallate; inhibition; membranes; resveratrol