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The effects of some avermectins on bovine carbonic anhydrase enzyme

机译:某些阿维菌素对牛碳酸酐酶的影响

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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 ( ) 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.
机译:摘要阿维菌素是有效的农业杀虫剂和抗寄生虫剂,已广泛用于农业,兽医和医学领域。这项研究的目的是研究选定的阿维菌素(包括阿维菌素,多拉菌素,阿莫菌素,依普利菌素,伊维菌素和莫西菌素)对碳酸酐酶(CA, EC 4.2.1.1。)从新鲜的牛红细胞中纯化。 CA催化二氧化碳(CO 2 )和水(H 2 O)快速相互转化为碳酸氢根()和质子(H + )并调节局部组织的酸度。牛红细胞CA(bCA)酶通过Sepharose-4B亲和层析纯化,收率为21.96%,纯化率为262.7倍。从该研究获得的抑制结果显示,阿维菌素,多拉菌素,阿曼菌素,依普诺菌素,伊维菌素和莫昔克丁的K i 值分别为9.73、17.39、20.43、13.39、16.44和17.73?nM。然而,临床上公认的著名CA抑制剂乙酰唑胺的K 值为27.68?nM。

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