Carbonic anhydrase (CA, EC 4.2.1.1) plays crucial physiological roles in many different organisms, such as in pH regulation, ion transport, and metabolic processes. CA was isolated from the European beeApis mellifera(AmCA) spermatheca and inhibitory effects of pesticides belonging to various classes, such as carbamates, thiophosphates, and pyrethroids, were investigated herein. The inhibitory effects of methomyl, oxamyl, deltamethrin, cypermethrin, dichlorodiphenyltrichloroethane (DDT) and diazinon on AmCA were analysed. These pesticides showed effectivein vitroinhibition of the enzyme, at sub-micromolar levels. The IC(50)values for these pesticides ranged between of 0.0023 and 0.0385 mu M. The CA inhibition mechanism with these compounds is unknown at the moment, but most of them contain ester functionalities which may be hydrolysed by the enzyme with the formation of intermediates that can either react with amino acid residues or bid to the zinc ion from the active site.

Investigation of pesticides on honey bee carbonic anhydrase inhibition / Soydan, Ercan; Olcay, Ahmet Can; Bilir, Gürkan; Taş, Ömer; Şentürk, Murat; Ekinci, Deniz; Supuran, Claudiu T. - In: JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY. - ISSN 1475-6366. - ELETTRONICO. - 35:(2020), pp. 0-0. [10.1080/14756366.2020.1835885]

Investigation of pesticides on honey bee carbonic anhydrase inhibition

Supuran, Claudiu T
2020

Abstract

Carbonic anhydrase (CA, EC 4.2.1.1) plays crucial physiological roles in many different organisms, such as in pH regulation, ion transport, and metabolic processes. CA was isolated from the European beeApis mellifera(AmCA) spermatheca and inhibitory effects of pesticides belonging to various classes, such as carbamates, thiophosphates, and pyrethroids, were investigated herein. The inhibitory effects of methomyl, oxamyl, deltamethrin, cypermethrin, dichlorodiphenyltrichloroethane (DDT) and diazinon on AmCA were analysed. These pesticides showed effectivein vitroinhibition of the enzyme, at sub-micromolar levels. The IC(50)values for these pesticides ranged between of 0.0023 and 0.0385 mu M. The CA inhibition mechanism with these compounds is unknown at the moment, but most of them contain ester functionalities which may be hydrolysed by the enzyme with the formation of intermediates that can either react with amino acid residues or bid to the zinc ion from the active site.
2020
35
0
0
Soydan, Ercan; Olcay, Ahmet Can; Bilir, Gürkan; Taş, Ömer; Şentürk, Murat; Ekinci, Deniz; Supuran, Claudiu T
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Utilizza questo identificatore per citare o creare un link a questa risorsa: https://hdl.handle.net/2158/1307524
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