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Interactions and kinetics of acetylcholinesterase with selected pesticides (CROSBI ID 724119)

Prilog sa skupa u zborniku | sažetak izlaganja sa skupa | međunarodna recenzija

Kolić, Dora ; Kovarik, Zrinka Interactions and kinetics of acetylcholinesterase with selected pesticides // HDBMB2022: From Science to Knowledge - Book of Abstracts / Dulić, Morana ; Sinčić, Nino ; Vrhovac Madunić, Ivana (ur.). Zagreb: Hrvatsko društvo za kemiju i molekularnu biologiju, 2022. str. 93-93

Podaci o odgovornosti

Kolić, Dora ; Kovarik, Zrinka

engleski

Interactions and kinetics of acetylcholinesterase with selected pesticides

Organophosphate compounds (OPs) comprise an important class of pesticides, chemical agents used in agriculture for management of diseases and pests. Due to their widespread and frequent use as insecticides and herbicides during the last 80 years, they are considered as an increasing environmental and public health concern. The uptake of contaminated food and water or exposure through agricultural activities is harmful to humans and other species because of their low target selectivity and severe toxicity. OPs act mainly by inhibiting enzyme acetylcholinesterase (AChE) which hydrolizes essential neurotransmitter acetylcholine (ACh), leading to a paralysis of cholinergic synaptic transmission in the central and peripheral nervous system which may induce convulsions, respiratory failure, loss of consciousness and death. In this study we investigated in vitro and in silico kinetics of inhibition and interactions of human AChE with four OP herbicides (anilofos, bensulide, butamifos and piperophos) and compared them to a potent AChE inhibitor, insecticide ethoprophos. Their overall rate constants of inhibition (ki) were up to 300-fold lower than ki of ethoprophos and they achieved a maximum inhibition of 85% of enzyme activity. Since medical therapy for restoration of AChE activity in case of poisoning includes oxime reactivators which dephosphylate AChE’s active center, we also evaluated potential of standard pyridinium oximes (2-PAM and HI-6) and a novel zwitterionic oxime RS194B to reactivate selected herbicide- and ethoprophos-inhibited AChE. Our results provide insight into neurotoxic effects of pesticides and facilitate further development of antidotes directed against OP pesticide poisoning. This research was supported by the Croatian Science Foundation (HrZZ-IP-2018-01-7683).

Organophosphorus compounds, acetylcholinesterase, pesticides, herbicides, oxime

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Podaci o prilogu

93-93.

2022.

objavljeno

Podaci o matičnoj publikaciji

HDBMB2022: From Science to Knowledge - Book of Abstracts

Dulić, Morana ; Sinčić, Nino ; Vrhovac Madunić, Ivana

Zagreb: Hrvatsko društvo za kemiju i molekularnu biologiju

1847-7836

Podaci o skupu

Congress of the Croatian Society of Biochemistry and Molecular Biology: From Science to Knowledge (HDBMB22)

poster

05.07.2022-07.07.2022

Brela, Hrvatska

Povezanost rada

Farmacija, Kemija, Temeljne medicinske znanosti