Please use this identifier to cite or link to this item:
http://repo.knmu.edu.ua/handle/123456789/31466
Title: | Evaluation of 5-[(Z)-(4-nitrobenzylidene)]-2-(thiazol-2-ylimino)-4-thiazolidinone (Les-6222) as Potential Anticonvulsant Agent |
Authors: | Mishchenko, Mariia Shtrygol, Sergiy Lozynskyi, Andrii Hoidyk, Mykhailo Khyluk, Dmytro Gorbach, Tetiana Lesyk, Roman |
Keywords: | antiepileptic drugs thiazolidinones pentylenetetrazole kindling inflammation molecular docking |
Issue Date: | 2022 |
Publisher: | Sci. Pharm. 2022 |
Citation: | Evaluation of 5-[(Z)-(4-nitrobenzylidene)]-2-(thiazol-2-ylimino)-4-thiazolidinone (Les-6222) as Potential Anticonvulsant Agent / M. Mishchenko, S. Shtrygol, A. Lozynskyi, M. Hoidyk, D. Khyluk, T. Gorbach, R. Lesyk // Scientia Pharmaceutica. – 2022. – Vol. 90, issue 3. – DOI: 10.3390/scipharm90030056. |
Abstract: | It was determined that the studied 5-[(Z)-(4-nitrobenzylidene)]-2-(thiazol-2-ylimino)-4-thiazolidinone (Les-6222) affects the cyclooxygenase pathway of the arachidonic acid cascade, the markers of damage to neurons on models of PTZ kindling. In the model of chronic epileptogenesis in mice (pentylenetetrazole kindling), a 4-thiazolidinone derivative showed high anticonvulsant activity, which is weaker than the effect of sodium valproate and higher than Celecoxib. The mentioned compound has a pronounced anti-inflammatory effect in the brain on the background of the PTZ kindling, reliably inhibiting COX-1 and COX-2. The predominant inhibition of COX-2 by 44.5% indicates this enzyme’s high selectivity of Les-6222. According to the molecular docking study results, the studied compound revealed the properties of COX-1/COX-2 inhibitor and especially 5-LOX/FLAP. The decreasing content of 8-isoprostane in the brain of mice of the Les-6222 group indicates a beneficial effect on cell membranes in the background of oxidative stress during the long-term administration of PTZ. In addition, Les-6222 significantly decreased the content of neuronspecific enolase, indicating neuroprotective properties in the background of chronic epileptogenesis. The obtained results experimentally substantiate the feasibility of further developing Les-6222 as a promising anticonvulsant agent. |
URI: | http://repo.knmu.edu.ua/handle/123456789/31466 |
Appears in Collections: | Наукові праці. Кафедра біологічної хімії |
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Горбач_англ_13.pdf | 1,48 MB | Adobe PDF | View/Open |
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