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Toxicological effects of some antiparasitic drugs on equine liver glutathione S-Transferase enzyme activity.
Journal of Pharmaceutical and Biomedical Analysis ( IF 3.4 ) Pub Date : 2019-12-17 , DOI: 10.1016/j.jpba.2019.113048
Fikret Turkan 1 , Mehmet Harbi Calimli 2 , Ayhan Akgun 2 , Fulya Gulbagca 3 , Fatih Sen 3
Affiliation  

Benzimidazoles are antiparasitic drugs having an extensive application field like agriculture, medicine, and especially in veterinary medicine. In this study, we report the effect of some benzimidazole drugs such as ricobendazole (RBZ), thiabendazole (TBZ), albendazole (ALBA) and oxfendazole (OFZ) on glutathione s-transferase (GST) enzyme activity. The kinetics studies, IC50 and Ki values of the tested drugs on GSTs enzyme activity were investigated. The obtained ranking of IC50 values were found to be approximately RBZ (53.31 μM, r2: 0.9778) < OFZ (57.75 μM, r2: 0.9630) < ALBA (63.00 μM, r2: 0.9443) < TBZ (69.30 μM, r2: 0.9491). And the obtained ranking of Ki values of the tested drugs (RBZ, TBZ, ALBA, and OFZ) for GSTs enzyme activity was found to be approximately 26.37 ± 2.96, 44.01 ± 5.74, 39.82 ± 3.98 and 30.14 ± 3.03 μM, respectively. Experimental results showed that tested the benzimidazoles drugs have some significant inhibitory effect on GSTs enzyme activity. And also, it was determined that RBZ, ALBA, OFZ are competitive inhibition, but TBZ is non-competitive inhibitors on GSTs enzyme activity. RBZ drug showed the best inhibitory effect with the lowest Ki value.

中文翻译:

某些抗寄生虫药对马肝谷胱甘肽S-转移酶活性的毒理作用。

苯并咪唑是具有广泛应用领域的抗寄生虫药,例如农业,医学,尤其是兽医学。在这项研究中,我们报告了一些苯并咪唑药物,如利多拉达唑(RBZ),噻苯达唑(TBZ),阿苯达唑(ALBA)和奥芬达唑(OFZ)对谷胱甘肽S-转移酶(GST)酶活性的影响。研究了动力学研究,测试药物对GSTs酶活性的IC50和Ki值。发现获得的IC50值排名约为RBZ(53.31μM,r2:0.9778)<OFZ(57.75μM,r2:0.9630)<ALBA(63.00μM,r2:0.9443)<TBZ(69.30μM,r2:0.9491) 。所获得的被测药物(RBZ,TBZ,ALBA和OFZ)的GST酶活性的Ki值排名约为26.37±2.96、44.01±5.74、39.82±3.98和30.14±3.03μM,分别。实验结果表明,所测试的苯并咪唑类药物对GSTs的酶活性具有明显的抑制作用。并且,还确定了RBZ,ALBA,OFZ是竞争性抑制,而TBZ是GSTs酶活性的非竞争性抑制剂。RBZ药物显示出最佳的抑制效果,且Ki值最低。
更新日期:2019-12-18
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