Nalazite se na CroRIS probnoj okolini. Ovdje evidentirani podaci neće biti pohranjeni u Informacijskom sustavu znanosti RH. Ako je ovo greška, CroRIS produkcijskoj okolini moguće je pristupi putem poveznice www.croris.hr
izvor podataka: crosbi

Assessment of four organophosphorus pesticides as inhibitors of human cholinesterases (CROSBI ID 718017)

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

Kovarik, Zrinka ; Čadež, Tena ; Kolić, Dora ; Šinko, Goran Assessment of four organophosphorus pesticides as inhibitors of human cholinesterases // 17th International Symposium on Cholinergic Mechanisms (ISCM2022) : Programme and Abstracts / Kovarik, Zrinka ; Primožič, Ines (ur.). Zagreb: Institut za medicinska istraživanja i medicinu rada, 2022. str. 45-45

Podaci o odgovornosti

Kovarik, Zrinka ; Čadež, Tena ; Kolić, Dora ; Šinko, Goran

engleski

Assessment of four organophosphorus pesticides as inhibitors of human cholinesterases

Toxicity of organophosphorus compounds remains a major public health concern due to their widespread use as pesticides and the existence of nerve agents. Their common mechanism of action involves inhibition of enzymes acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) which are crucial for neurotransmission. Both chronic and acute poisoning by organophosphates can leave long- lasting health effects even when the patients are treated with standard medical therapy. Therefore, an increasing urgency exists to find more effective oxime reactivators for compounds which are resistant to reactivation, especially phosphoramidates. Here, we investigated in silico and in vitro interactions and kinetics of inhibition for human cholinesterases with four organophosphate pesticides - ethoprophos, fenamiphos, methamidophos and phosalone. Overall, ethoprophos and fenamiphos displayed higher potency as inhibitors for tested cholinesterases. Our results show that methamidophos-inhibited AChE was more susceptible to reactivation than AChE inhibited by fenamiphos by selected oximes. Molecular modelling enabled an evaluation of interactions important for specificity and selectivity of both inhibition and reactivation of cholinesterases. Two newly developed reactivators – bispyridinium triazole oxime 14A and zwitterionic oxime RS194B possess remarkable potential for further development of antidotes directed against pesticides and related phosphoramidate exposures, such as nerve agents tabun or Novichoks.

Organophosphorus compounds ; acetylcholinesterase ; butyrylcholesterase , pyridinium oximes ; bioscavenging

nije evidentirano

nije evidentirano

nije evidentirano

nije evidentirano

nije evidentirano

nije evidentirano

Podaci o prilogu

45-45.

2022.

objavljeno

Podaci o matičnoj publikaciji

17th International Symposium on Cholinergic Mechanisms (ISCM2022) : Programme and Abstracts

Kovarik, Zrinka ; Primožič, Ines

Zagreb: Institut za medicinska istraživanja i medicinu rada

978-953-96817-8-2

Podaci o skupu

17th International Symposium on Cholinergic Mechanisms (ISCM2022)

pozvano predavanje

08.05.2022-12.05.2022

Mlini, Hrvatska; Dubrovnik, Hrvatska

Povezanost rada

Farmacija, Kemija, Temeljne medicinske znanosti

Poveznice