Butyrylcholinesterase inhibited by nerve agents is efficiently reactivated with chlorinated pyridinium oximes
Language English Country Ireland Media print-electronic
Document type Journal Article
PubMed
31004594
DOI
10.1016/j.cbi.2019.04.020
PII: S0009-2797(19)30394-1
Knihovny.cz E-resources
- Keywords
- Cholinesterase, Organophosphorus compounds, Pseudo-catalytic scavenger, Quaternary oxime, Reactivators,
- MeSH
- Enzyme Activation drug effects MeSH
- Butyrylcholinesterase chemistry metabolism MeSH
- Cholinesterase Inhibitors chemistry metabolism MeSH
- Halogenation MeSH
- Kinetics MeSH
- Humans MeSH
- Nerve Agents chemistry metabolism MeSH
- Oximes chemistry metabolism pharmacology MeSH
- Pyridinium Compounds chemistry MeSH
- Sarin chemistry metabolism MeSH
- Check Tag
- Humans MeSH
- Publication type
- Journal Article MeSH
- Names of Substances
- Butyrylcholinesterase MeSH
- Cholinesterase Inhibitors MeSH
- Nerve Agents MeSH
- Oximes MeSH
- Pyridinium Compounds MeSH
- Sarin MeSH
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.
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