Kinetic evaluation of the inhibition and reactivation of human acetylcholinesterase
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Effect of Gallic Acid on Reactivation of Acetylcholinesterase and Butyrylcholinesterase Inhibited by Diazinon in Vitro and in Vivo
Background and purpose: Diazinon is an organophosphate insecticide that binds to the acetylcholinesterase enzyme after metabolization causing its inactivation. Galic acid is a polyphenolic compound with nucleophilic properties. The aim of this study was to investigate the effects of gallic acid on reactivation of acetylcholine and butyrylcholinesterase inhibited by diazinon in mice and human se...
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Objective(s): The objective of this study was to evaluate pharmacological effect of Calligonum polygonoides against Krait snake’s venom acetylcholinesterase (AChE) and to extent it for the treatment of Alzheimer’s disease. Materials and Methods: Acetylcholinesterase activity was measured using Ellman method with some modification. The kinetic studies of methanolic extract of C. polygonoides aga...
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Acetylcholinesterase has important role in synaptic cleft. It breaks down the acetylcholineatcholinergic synapsesand terminates the cholinergic effects. Some chemical agents likeorganophosphorus compounds (OPCs) including nerve agents and pesticides react withacetylcholinesteraseirreversibly. They inhibit normal biological enzyme action and resultin accumulation of acetylcholineand show toxic e...
متن کاملThe Length Dependent Activity of Oximes on Reactivation of Tabun Inhibited Acetylcholinesterase; A Theoretical Study
In this work, the effect of ligand's length on interaction energy of six oximes, A [2-(hydroxyimino)-N-((1-(2-(2-((hydroxyimino)methyl)-1H-imidazol-1-yl)ethyl)-1H-1,2,3-triazol-4-yl)methyl)acetamide], B [2-(hydroxyimino)-N-((1-(3-(2-((hydroxyimino)methyl)-1H-imidazol-1-yl)propyl)-1H-1,2,3-triazol-4-yl)methyl)acetamide], C [2-(hydroxyimino)-N-((1-(4-(2-((hydroxyimino)methyl)-1H-imidazol-1-yl)but...
متن کاملKinetic and structural studies on the interaction of cholinesterases with the anti-Alzheimer drug rivastigmine.
Rivastigmine, a carbamate inhibitor of acetylcholinesterase, is already in use for treatment of Alzheimer's disease under the trade name of Exelon. Rivastigmine carbamylates Torpedo californica acetylcholinesterase very slowly (k(i) = 2.0 M(-1) min(-1)), whereas the bimolecular rate constant for inhibition of human acetylcholinesterase is >1600-fold higher (k(i) = 3300 M(-1) min(-1)). For human...
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