Butyrylcholinesterase inhibited by nerve agents is efficiently reactivated with chlorinated pyridinium oximes
| Autor: | Tamara Zorbaz, Kamil Kuca, Zrinka Kovarik, Kamil Musilek, David Malinak |
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| Rok vydání: | 2019 |
| Předmět: |
0301 basic medicine
Sarin Pralidoxime Halogenation Cyclosarin Pyridinium Compounds Toxicology Medicinal chemistry 03 medical and health sciences chemistry.chemical_compound 0302 clinical medicine organophosphorus compounds quaternary oxime reactivators cholinesterase pseudo-catalytic scavenger Oximes medicine Humans Butyrylcholinesterase Cholinesterase Nerve agent Tabun biology General Medicine Oxime Enzyme Activation Kinetics 030104 developmental biology chemistry 030220 oncology & carcinogenesis biology.protein Cholinesterase Inhibitors Nerve Agents medicine.drug |
| Zdroj: | Chemico-biological interactions. 307 |
| ISSN: | 1872-7786 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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