Faculty of Agriculture, Department of Agricultural Biotechnology, Ondokuz Mayıs University, Samsun, Turkey.
Pharmacy Faculty, Department of Biochemistry, Agri Ibrahim Cecen University, Agri, Turkey.
J Enzyme Inhib Med Chem. 2020 Dec;35(1):1923-1927. doi: 10.1080/14756366.2020.1835885.
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 bee (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 effective inhibition of the enzyme, at sub-micromolar levels. The IC values for these pesticides ranged between of 0.0023 and 0.0385 μM. 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.
碳酸酐酶（CA，EC 4.2.1.1）在许多不同的生物体中发挥着至关重要的生理作用，例如在 pH 调节、离子转运和代谢过程中。本文研究了属于不同类别的杀虫剂，如氨基甲酸酯类、硫代磷酸酯类和拟除虫菊酯类，对欧洲蜜蜂（AmCA）精囊碳酸酐酶的抑制作用。分析了灭多威、涕灭威、溴氰菊酯、氯菊酯、滴滴涕（DDT）和二嗪农对 AmCA 的抑制作用。这些杀虫剂在亚微米水平上对酶表现出有效的抑制作用。这些杀虫剂的 IC 值范围在 0.0023 到 0.0385 μM 之间。目前，这些化合物与 CA 的抑制机制尚不清楚，但它们大多数都含有酯官能团，可能被酶水解，形成中间体，这些中间体要么与氨基酸残基反应，要么与活性部位的锌离子结合。
