engleski

Butyrylcholinesterase with pralidoximeanalogs scavenges nerve agents

Nerve agents’ (NA) neurotoxicity is primarily induced by phos-phorylation of acetylcholinesterase (AChE), the key enzyme inthe neurotransmitter acetylcholine (ACh) pathway. Its akinenzyme, butyrylcholinesterase (BChE), an enzyme without knownessential physiological function, can serve as a protector ofAChE from inhibition by NAs by binding them in a stoichiomet-ric ratio and thus lower their concentration in the body. Currenttherapy, consisting of compounds containing oxime group (i.e.pralidoxime) as reactivators of phosphorylated AChE, has lim-ited reactivation potency for phosphorylated BChE. Therefore, asearch for a BChE reactivator that would create an enzyme-oxime catalytic scavenging system is still ongoing. With that pur-pose, in this study, several pyridinium oximes were selected, tested, and identified as efficient reactivators for cyclosarin- inhib-ited BChE with up to 300-fold higher overall kinetic reactivation

Organophosphorus compounds, acetylcholinesterase, butyrylcholesterase, pyridinium oximes, bioscavenging

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