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1,2,4-Triazole-based anticonvulsant agents with additional ROS scavenging activity are effective in a model of pharmacoresistant epilepsy
B. Kaproń, R. Czarnomysy, M. Wysokiński, R. Andrys, K. Musilek, A. Angeli, CT. Supuran, T. Plech,
Language English Country Great Britain
Document type Journal Article
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from 2020-01-01 to 2020-12-31
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- MeSH
- Acetylcholinesterase metabolism MeSH
- Anticonvulsants chemical synthesis chemistry pharmacology MeSH
- Antioxidants chemical synthesis chemistry pharmacology MeSH
- Biphenyl Compounds antagonists & inhibitors MeSH
- Butyrylcholinesterase metabolism MeSH
- Cholinesterase Inhibitors chemical synthesis chemistry pharmacology MeSH
- Epilepsy drug therapy metabolism MeSH
- Carbonic Anhydrase Inhibitors chemical synthesis chemistry pharmacology MeSH
- Carbonic Anhydrases metabolism MeSH
- Humans MeSH
- Models, Molecular MeSH
- Molecular Structure MeSH
- Mice MeSH
- Cell Line, Tumor MeSH
- Oxidative Stress drug effects MeSH
- Picrates antagonists & inhibitors MeSH
- Reactive Oxygen Species metabolism MeSH
- Triazoles chemical synthesis chemistry pharmacology MeSH
- Cell Survival drug effects MeSH
- Dose-Response Relationship, Drug MeSH
- Structure-Activity Relationship MeSH
- Animals MeSH
- Check Tag
- Humans MeSH
- Mice MeSH
- Animals MeSH
- Publication type
- Journal Article MeSH
There are numerous studies supporting the contribution of oxidative stress to the pathogenesis of epilepsy. Prolonged oxidative stress is associated with the overexpression of ATP-binding cassette transporters, which results in antiepileptic drugs resistance. During our studies, three 1,2,4-triazole-3-thione derivatives were evaluated for the antioxidant activity and anticonvulsant effect in the 6 Hz model of pharmacoresistant epilepsy. The investigated compounds exhibited 2-3 times more potent anticonvulsant activity than valproic acid in 6 Hz test in mice, which is well-established preclinical model of pharmacoresistant epilepsy. The antioxidant/ROS scavenging activity was confirmed in both single-electron transfer-based methods (DPPH and CUPRAC) and during flow cytometric analysis of total ROS activity in U-87 MG cells. Based on the enzymatic studies on human carbonic anhydrases (CAs), acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), one can assume that the herein investigated drug candidates will not impair the cognitive processes mediated by CAs and will have minimal off-target cholinergic effects.
References provided by Crossref.org
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- $a Kaproń, Barbara $u Department of Clinical Genetics, I Faculty of Medicine with Dentistry Division, Medical University of Lublin, Lublin, Poland.
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- $a There are numerous studies supporting the contribution of oxidative stress to the pathogenesis of epilepsy. Prolonged oxidative stress is associated with the overexpression of ATP-binding cassette transporters, which results in antiepileptic drugs resistance. During our studies, three 1,2,4-triazole-3-thione derivatives were evaluated for the antioxidant activity and anticonvulsant effect in the 6 Hz model of pharmacoresistant epilepsy. The investigated compounds exhibited 2-3 times more potent anticonvulsant activity than valproic acid in 6 Hz test in mice, which is well-established preclinical model of pharmacoresistant epilepsy. The antioxidant/ROS scavenging activity was confirmed in both single-electron transfer-based methods (DPPH and CUPRAC) and during flow cytometric analysis of total ROS activity in U-87 MG cells. Based on the enzymatic studies on human carbonic anhydrases (CAs), acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), one can assume that the herein investigated drug candidates will not impair the cognitive processes mediated by CAs and will have minimal off-target cholinergic effects.
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- $a Czarnomysy, Robert $u Department of Synthesis and Technology of Drugs, Faculty of Pharmacy, Medical University of Białystok, Bialystok, Poland.
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- $a Wysokiński, Mariusz $u Department of Basic Nursing and Medical Teaching, Chair of Development in Nursing, Faculty of Health Sciences, Medical University of Lublin, Lublin, Poland.
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- $a Angeli, Andrea $u Department of Neuroscience, Psychology, Drug Research and Child Health (NEUROFARBA), Section of Pharmaceutical and Nutraceutical Sciences, University of Florence, Firenze, Italy.
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