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Toxicological effects of some antiparasitic drugs on equine liver glutathione S-Transferase enzyme activity.
Abstract: 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, IC and Ki values of the tested drugs on GSTs enzyme activity were investigated. The obtained ranking of IC values were found to be approximately RBZ (53.31 μM, r 0.9778) < OFZ (57.75 μM, r 0.9630) < ALBA (63.00 μM, r 0.9443) < TBZ (69.30 μM, r 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.
Copyright © 2019 Elsevier B.V. All rights reserved.
Publication Date: 2019-12-17 PubMed ID: 31887670DOI: 10.1016/j.jpba.2019.113048Google Scholar: Lookup The Equine Research Bank provides access to a large database of publicly available scientific literature. Inclusion in the Research Bank does not imply endorsement of study methods or findings by Mad Barn.
- Journal Article
Summary
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The research study investigates the effects of certain antiparasitic drugs on the enzyme activity of glutathione s-transferase (GST) in the equine liver. The study’s primary focus is the impact of benzimidazole drugs like ricobendazole (RBZ), thiabendazole (TBZ), albendazole (ALBA), and oxfendazole (OFZ) on GST activity.
Research Background and Purpose
- The background of the research hinges on the widespread application of benzimidazoles as antiparasitic drugs across various fields, mainly in veterinary medicine.
- The aim of the study is to investigate the influence of certain benzimidazole drugs (RBZ, TBZ, ALBA, and OFZ) on the enzyme activity of glutathione s-transferase in the horse liver.
Research Methods and Findings
- Kinetic studies, IC and Ki values of the tested drugs were analyzed to assess their impact on GST enzyme activity.
- According to the results, all the tested benzimidazoles drugs exhibited a significant inhibitory effect on GST enzyme activity.
- The ranking of IC values was RBZ (53.31 μM, r 0.9778) < OFZ (57.75 μM, r 0.9630) < ALBA (63.00 μM, r 0.9443) < TBZ (69.30 μM, r 0.9491), indicating that RBZ has the strongest inhibitory effect.
- The obtained ranking of Ki values for GST enzyme activity from the tested drugs (RBZ, TBZ, ALBA, and OFZ) was approximately 26.37 ± 2.96, 44.01 ± 5.74, 39.82 ± 3.98 and 30.14 ± 3.03 μM, respectively, showing RBZ as the most promising inhibitor.
- It was determined that RBZ, ALBA, and OFZ are competitive inhibitors, meaning they compete with the substrate for binding to the enzyme, but TBZ is a non-competitive inhibitor, implying it binds to the enzyme at a different site than the substrate.
Conclusion
- The study confirmed that the tested benzimidazoles drugs, especially RBZ, significantly impact GSTs enzyme activity.
- This research provides insightful information for the veterinary field, particularly regarding drug interactions with equine liver enzymes.
Cite This Article
APA
Turkan F, Harbi Calimli M, Akgun A, Gulbagca F, Sen F.
(2019).
Toxicological effects of some antiparasitic drugs on equine liver glutathione S-Transferase enzyme activity.
J Pharm Biomed Anal, 180, 113048.
https://doi.org/10.1016/j.jpba.2019.113048 Publication
Researcher Affiliations
- Health Services Vocational School, Igdir University, 76000, Igdir, Turkey. Electronic address: fikret.turkan@igdir.edu.tr.
- Tuzluca Vocational School, Igdir University, 76000, Igdir, Turkey.
- Tuzluca Vocational School, Igdir University, 76000, Igdir, Turkey.
- Sen Research Group, Biochemistry Department, Faculty of Arts and Science, Dumlupinar University, 43100, Kutahya, Turkey.
- Sen Research Group, Biochemistry Department, Faculty of Arts and Science, Dumlupinar University, 43100, Kutahya, Turkey. Electronic address: fatih.sen@dpu.edu.tr.
MeSH Terms
- Animals
- Antiparasitic Agents / chemistry
- Antiparasitic Agents / toxicity
- Benzimidazoles / chemistry
- Benzimidazoles / toxicity
- Dose-Response Relationship, Drug
- Glutathione Transferase / antagonists & inhibitors
- Horses
- In Vitro Techniques
- Inhibitory Concentration 50
- Liver / drug effects
- Liver / enzymology
- Molecular Structure
- Substrate Specificity
- Veterinary Drugs / chemistry
- Veterinary Drugs / toxicity
Conflict of Interest Statement
Declaration of Competing Interest The authors declare no conflict of interest.
Citations
This article has been cited 4 times.- Badawy MAS, Bräse S, Ali TFS, Abdel-Aziz M, Abdel-Rahman HM. Biologically Active Benzimidazole Hybrids as Cancer Therapeutics: Recent Advances. Pharmaceuticals (Basel) 2025 Sep 28;18(10).
- Wang B, Han F, Ding P, Tong J, Liu K, Yan S, Wang S, Chen G, Wu X, Huang K, Geng M, Tao F. Prenatal Environmental Antibiotic Exposure and Autism Spectrum Disorder Symptoms in Children at 3 Years of Age: Findings from the Ma'anshan Birth Cohort Study. Environ Health (Wash) 2024 Sep 20;2(9):651-660.
- Dos Santos Bezerra WA, Tavares CP, Lima VAS, da Rocha CQ, da Silva Vaz Junior I, Michels PAM, Costa Junior LM, Dos Santos Soares AM. In silico and In vitro Assessment of Dimeric Flavonoids (Brachydins) on Rhipicephalus microplus Glutathione S-transferase. Med Chem 2024;20(9):912-919.
- Donmez M, Sekerci M, Adiguzel R, Oğuz E, Türkan F, Yildiko U, Colak N. Synthesis and characterization of novel bis(thiosemicarbazone) complexes and investigation of their acetylcholinesterase and glutathione S-transferase activities with in silico and in vitro studies. Mol Divers 2025 Apr;29(2):1109-1127.
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