The effects of some avermectins on bovine carbonic anhydrase enzyme.

IF 5.6 2区医学 Q1 BIOCHEMISTRY & MOLECULAR BIOLOGY

Journal of Enzyme Inhibition and Medicinal Chemistry Pub Date : 2016-10-01 Epub Date: 2015-07-24 DOI:10.3109/14756366.2015.1064406

Leyla Polat Kose, İlhami Gülçin, Hasan Özdemir, Ali Atasever, Saleh H Alwasel, Claudiu T Supuran

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引用次数: 56

Abstract

Avermectins are effective agricultural pesticides and antiparasitic agents that are widely employed in the agricultural, veterinary and medical fields. The aim of this study was to investigate the inhibitory effects of selected avermectins including abamectin, doramectin, emamectin, eprinomectin, ivermectin and moxidectin that are used as drugs against a wide variety of internal and external mammalian parasites, on the carbonic anhydrase enzyme (CA, EC 4.2.1.1.) purified from fresh bovine erythrocyte. CA catalyses the rapid interconversion of carbon dioxide (CO2) and water (H2O) to bicarbonate ([Formula: see text]) and protons (H(+)) and regulate the acidity of the local tissues. Bovine erythrocyte CA (bCA) enzyme was purified by Sepharose-4B affinity chromatography with a yield of 21.96% and 262.7-fold purification. The inhibition results obtained from this study showed Ki values of 9.73, 17.39, 20.43, 13.39, 16.44 and 17.73 nM for abamectin, doramectin, emamectin, eprinomectin, ivermectin and moxidectin, respectively. However, acetazolamide, well-known clinically established CA inhibitor, possessed a Ki value of 27.68 nM.

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一些阿维菌素对牛碳酸酐酶的影响。

阿维菌素是一种有效的农用农药和抗寄生虫剂，广泛应用于农业、兽医和医疗等领域。摘要本研究旨在探讨阿维菌素、多拉菌素、埃维菌素、依普诺菌素、伊维菌素和莫西菌素等阿维菌素对新鲜牛红细胞中纯化的碳酸水解酶(CA, EC 4.2.1.1.)的抑制作用。CA催化二氧化碳(CO2)和水(H2O)快速相互转化为碳酸氢盐([分子式:见正文])和质子(H(+))，并调节局部组织的酸度。采用Sepharose-4B亲和层析法纯化牛红细胞CA (bCA)酶，产率为21.96%，纯化率为262.7倍。对阿维菌素、doramectin、emamectin、eprinomectin、ivermectin和moxidectin的Ki值分别为9.73、17.39、20.43、13.39、16.44和17.73 nM。然而，临床上公认的CA抑制剂乙酰唑胺的Ki值为27.68 nM。

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来源期刊

Journal of Enzyme Inhibition and Medicinal Chemistry 医学-生化与分子生物学

CiteScore

10.30

自引率

10.70%

发文量

195

审稿时长

4-8 weeks

期刊介绍： Journal of Enzyme Inhibition and Medicinal Chemistry publishes open access research on enzyme inhibitors, inhibitory processes, and agonist/antagonist receptor interactions in the development of medicinal and anti-cancer agents. Journal of Enzyme Inhibition and Medicinal Chemistry aims to provide an international and interdisciplinary platform for the latest findings in enzyme inhibition research. The journal’s focus includes current developments in: Enzymology; Cell biology; Chemical biology; Microbiology; Physiology; Pharmacology leading to drug design; Molecular recognition processes; Distribution and metabolism of biologically active compounds.