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The toxicological impact of some avermectins on human erythrocytes glutathione S‐transferase enzyme

机译:一些Averpectins对人红细胞谷胱甘肽S-转移酶酶的毒理学影响

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Abstract The drugs of the class avermectins are?antiparasitic agents, which are widely used in medical and agricultural fields, especially in veterinary medicine. The aim of this study was to investigate the inhibitory effects of avermectin derivatives such as abamectin, doramectin, eprinomectin, ivermectin, and moxidectin, which are used for internal and external mammalian parasites. Glutathione S‐transferase (GST, E.C. 2.5.1.18) was purified from fresh human erythrocytes. The purification of the GST enzyme was performed separately by affinity chromatography with a yield of 34.81% and 117.94‐fold purification. The control of the pure GST enzyme was performed by sodium dodecyl sulphate‐polyacrylamide gel electrophoresis, and a single band was obtained. The IC 50 values were approximately 0.31, 0.39, 0.13, 0.44, and 0.73?mM for abamectin, doramectin, eprinomectin, ivermectin, and moxidectin, and the K i values were 0.32?±?0.06, 0.39?±?0.09, 0.13?±?0.03, 0.44?±?0.02, 0.73?±?0.04?mM, respectively. This data revealed that the tested avermectins showed significant inhibitory effects on the GST enzyme.
机译:摘要Avermectins类的药物是抗披啶药物,其广泛用于医疗和农业领域,特别是在兽医中。本研究的目的是研究AvaMectin衍生物如Abamectin,Doramectin,ePrinoMectin,Ivermectin和Moxidectin的抑制作用,这些蛋白和莫克利菌素用于内部和外部哺乳动物寄生虫。从新鲜的人红细胞纯化谷胱甘肽S-转移酶(GST,例如2.5.1.18)。通过亲和色谱法分别进行GST酶的纯化,产率为34.81%和117.94倍净化。通过十二烷基硫酸钠 - 聚丙烯酰胺凝胶电泳进行纯GST酶的控制,得到单个带。用于取向蛋白,多拉米菌素,ePrinomectin,伊维菌蛋白和丙二聚酶蛋白和磷酸酯,IC 50值约为0.31,0.39,0.13,0.44和0.73Ω·mm,ki值为0.32≤0.32,0.39?±0.09,0.13? ±0.03,0.44?±0.02,0.73?±0.04?mm。该数据显示,测试的Avermectins对GST酶显示出显着的抑制作用。

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