Pregled bibliografske jedinice broj: 1219554
Interactions and kinetics of acetylcholinesterase with selected pesticides
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 (poster, međunarodna recenzija, sažetak, znanstveni)
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Naslov
Interactions and kinetics of acetylcholinesterase with selected pesticides
Autori
Kolić, Dora ; Kovarik, Zrinka
Vrsta, podvrsta i kategorija rada
Sažeci sa skupova, sažetak, znanstveni
Izvornik
HDBMB2022: From Science to Knowledge - Book of Abstracts
/ Dulić, Morana ; Sinčić, Nino ; Vrhovac Madunić, Ivana - Zagreb : Hrvatsko društvo za kemiju i molekularnu biologiju, 2022, 93-93
Skup
Congress of the Croatian Society of Biochemistry and Molecular Biology: From Science to Knowledge (HDBMB22)
Mjesto i datum
Brela, Hrvatska, 28.09.2022. - 01.10.2022
Vrsta sudjelovanja
Poster
Vrsta recenzije
Međunarodna recenzija
Ključne riječi
Organophosphorus compounds, acetylcholinesterase, pesticides, herbicides, oxime
Sažetak
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).
Izvorni jezik
Engleski
Znanstvena područja
Kemija, Temeljne medicinske znanosti, Farmacija
POVEZANOST RADA
Projekti:
IP-2018-01-7683 - Analiza interakcija butirilkolinesteraze s novim inhibitorima i reaktivatorima (AnalyseBChE) (Kovarik, Zrinka, HRZZ - 2018-01) ( CroRIS)
Ustanove:
Institut za medicinska istraživanja i medicinu rada, Zagreb