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J Pharm Biomed Anal ; 180: 113048, 2020 Feb 20.
Artículo en Inglés | MEDLINE | ID: mdl-31887670

RESUMEN

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 ±â€¯2.96, 44.01 ±â€¯5.74, 39.82 ±â€¯3.98 and 30.14 ±â€¯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.


Asunto(s)
Antiparasitarios/toxicidad , Bencimidazoles/toxicidad , Glutatión Transferasa/antagonistas & inhibidores , Caballos , Hígado/efectos de los fármacos , Drogas Veterinarias/toxicidad , Animales , Antiparasitarios/química , Bencimidazoles/química , Relación Dosis-Respuesta a Droga , Técnicas In Vitro , Concentración 50 Inhibidora , Hígado/enzimología , Estructura Molecular , Especificidad por Sustrato , Drogas Veterinarias/química
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