Department of Biochemistry, Faculty of Veterinary Medicine, Bingöl University, Bingöl 12000, Turkey.
Department of Chemistry, Faculty of Science, Atatürk University, Erzurum 25240, Turkey.
J Biochem Mol Toxicol. 2018 Jan;32(1). doi: 10.1002/jbt.22010. Epub 2017 Nov 13.
Avermectins are used worldwide as antiparasitic drugs in the field of veterinary medicine and as agricultural pesticides and insecticides. Carbonic anhydrase (CA, E.C. 4.2.1.1) is a zinc-containing metalloenzyme that catalyzes the reversible hydration of carbon dioxide (CO ) to yield protons (H ) and bicarbonate (HCO ). In this study, some avermectins, including abamectin, doramectin, eprinomectin, and moxidectin, were investigated for in vitro inhibitory effects on the CA enzyme purified from goat liver, which was purified (125.00-fold) using sepharose 4B-l-tyrosine-sulfanilamide affinity chromatography, with a yield of 68.27% and a specific activity of 21765.31 EU/mg proteins. The inhibition results obtained from this study showed K values of 0.283, 0.153, 0.232, and 0.317 nM for abamectin, doramectin, eprinomectin, and moxidectin, respectively. On the other hand, acetazolamide, well-known clinically established CA inhibitor, possessed a K value of 0.707 nM against goat liver CA.
阿维菌素类药物在兽医领域被广泛用作抗寄生虫药物，在农业领域被用作农药和杀虫剂。碳酸酐酶（CA，EC 4.2.1.1）是一种含锌的金属酶，可催化二氧化碳（CO ）的可逆水合作用，生成质子（H +）和碳酸氢盐（HCO 3-）。在这项研究中，研究了一些阿维菌素类药物，包括阿维菌素、多拉菌素、埃普里诺菌素和莫昔克丁，它们对从山羊肝脏中纯化的碳酸酐酶（CA）酶的体外抑制作用。该酶通过 sepharose 4B-l-酪氨酸-磺胺亲和层析法（yield 68.27%，specific activity 21765.31 EU/mg proteins）被纯化（125.00 倍）。本研究的抑制结果表明，阿维菌素、多拉菌素、埃普里诺菌素和莫昔克丁对 CA 的 K 值分别为 0.283、0.153、0.232 和 0.317 nM。另一方面，临床上已确立的碳酸酐酶抑制剂乙酰唑胺对山羊肝碳酸酐酶的 K 值为 0.707 nM。
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