Oxime-induced reactivation of acetylcholinesterase inhibited by phosphoramidates |
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| Affiliation: | 1. Laboratoire de Chimie des Matériaux, Faculté des Sciences de Bizerte, 7021 Zarzouna, Tunisie;2. Laboratory of Biochemistry and Molecular Biology, Faculty of Sciences, Risks Related to Environmental Stress, Struggle and Prevention (UR17ES20), University of Carthage, Te Ministry of Higher Education and Scientifc Research, Zarzouna, 7003 Bizerte, Tunisia;3. Laboratoire de Physique des Matériaux, Faculté des Sciences de Bizerte, 7021 Zarzouna, Tunisie;4. Univ Rennes, CNRS, ISCR (Institut des Sciences Chimiques de Rennes) – UMR 6226, F-35000 Rennes, France;5. Aix-Marseille Université, Centrale Marseille CNRS, iSm2 UMR 7313, 13397 Marseille, France;1. Universidad Autónoma de Nuevo León, Facultad de Ciencias Químicas, Av. Universidad S/N, San Nicolás de los Garza, N. L., México;2. Universidad Autónoma de Nuevo León, Facultad de Agronomía, Francisco Villa S/N, Exacienda el Canadá, General Escobedo, N.L., México |
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| Abstract: | The reaction of human erythrocyte acetylcholinesterase (AChE) with a set of structurally related phosphoramidates was studied in order to investigate the properties of phosphorylated enzyme and the effects of 4 oximes PAM-2, TMB-4, HI-6 and BDB-106 on the reactivation of inhibited AChE. Second-order rate constant of the phosphorylation reaction of the compounds towards the active site of AChE ranged between 5.0 × 102 and 4.9 × 106M−1min−1 and their inhibitory power (I50) was from 7.3 × 10−5to 5.7 × 10−9M for 20 min incubation at 37 °C. The oximes used were weak reactivators of inhibited AChE except for (C4H9O)(NH2)P(O)DCP (DCP, -O-2,5-dichlorphenyl group) and (C6H13O)(NH2)P(O)SCH3 where we have obtained good reactivation. Imidazole oxime BDB-106 proved to be a potent reactivator of tabun-inhibited AChE. |
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