Butyrylcholinesterase inhibited by nerve agents is efficiently reactivated with chlorinated pyridinium oximes.
Cholinesterase
Organophosphorus compounds
Pseudo-catalytic scavenger
Quaternary oxime
Reactivators
Journal
Chemico-biological interactions
ISSN: 1872-7786
Titre abrégé: Chem Biol Interact
Pays: Ireland
ID NLM: 0227276
Informations de publication
Date de publication:
01 Jul 2019
01 Jul 2019
Historique:
received:
07
03
2019
revised:
05
04
2019
accepted:
15
04
2019
pubmed:
21
4
2019
medline:
27
6
2019
entrez:
21
4
2019
Statut:
ppublish
Résumé
Bispyridinium oximes with one (K865, K866, K867) or two (K868, K869, K870) ortho-positioned chlorine moiety, analogous to previously known K027, K048 and K203 oximes, and potent reactivators of human acetylcholinesterase (AChE) inhibited by nerve agents, were tested in the reactivation of human butyrylcholinesterase (BChE) inhibited by sarin, cyclosarin, VX, and tabun. A previously highlighted AChE reactivator, dichlorinated bispyridinium oxime with propyl linker (K868), was tested in more detail for reactivation of four nerve agent-BChE conjugates. Its BChE reactivation potency was showed to be promising when compared to the standard oximes used in medical practice, asoxime (HI-6) and pralidoxime (2-PAM), especially in case of sarin and tabun. This finding could be used in the pseudo-catalytic scavenging of the most nerve agents due to its cumulative capacity to reactivate both AChE and BChE.
Identifiants
pubmed: 31004594
pii: S0009-2797(19)30394-1
doi: 10.1016/j.cbi.2019.04.020
pii:
doi:
Substances chimiques
Cholinesterase Inhibitors
0
Nerve Agents
0
Oximes
0
Pyridinium Compounds
0
Sarin
B4XG72QGFM
Butyrylcholinesterase
EC 3.1.1.8
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
16-20Informations de copyright
Copyright © 2019 Elsevier B.V. All rights reserved.