GABA A and serotonergic receptors participation in anxiolytic effect of chalcones in adult zebrafish.

Autor:	Mendes FRS; Department of Biological Chemistry, Regional University of Cariri, Crato, Ceará, Brazil., da Silva AW; Graduate Program of Biotechnology, State University of Ceara, Fortaleza, Ceará, Brazil., Ferreira MKA; Graduate Program in Natural Sciences, State University of Ceara, Fortaleza, Ceará, Brazil., Rebouças EL; Graduate Program of Biotechnology, State University of Ceara, Fortaleza, Ceará, Brazil., Moura Barbosa I; Graduate Program in Natural Sciences, State University of Ceara, Fortaleza, Ceará, Brazil., da Rocha MN; Department of Chemistry, Limoeiro do Norte, State University of Ceara, Limoeiro do Norte, Ceará, Brazil., Henrique Ferreira Ribeiro W; Chemistry Course, State University of Vale do Acaraú, Sobral, Ceará, Brazil., Menezes RRPPB; Department of Clinical and Toxicological Analysis, Federal University of Ceará, Fortaleza, Ceará, Brazil., Magalhães EP; Department of Clinical and Toxicological Analysis, Federal University of Ceará, Fortaleza, Ceará, Brazil., Marinho EM; Department of Analytical and Physical Chemistry, Federal University of Ceara, Fortaleza, Ceará, Brazil., Marinho MM; Department of Biological Chemistry, Regional University of Cariri, Crato, Ceará, Brazil., Bandeira PN; Chemistry Course, State University of Vale do Acaraú, Sobral, Ceará, Brazil., de Menezes JESA; Graduate Program in Natural Sciences, State University of Ceara, Fortaleza, Ceará, Brazil., Marinho ES; Graduate Program in Natural Sciences, State University of Ceara, Fortaleza, Ceará, Brazil.; Department of Chemistry, Limoeiro do Norte, State University of Ceara, Limoeiro do Norte, Ceará, Brazil., Dos Santos HS; Department of Biological Chemistry, Regional University of Cariri, Crato, Ceará, Brazil.; Graduate Program of Biotechnology, State University of Ceara, Fortaleza, Ceará, Brazil.; Graduate Program in Natural Sciences, State University of Ceara, Fortaleza, Ceará, Brazil.; Chemistry Course, State University of Vale do Acaraú, Sobral, Ceará, Brazil.
Jazyk:	angličtina
Zdroj:	Journal of biomolecular structure & dynamics [J Biomol Struct Dyn] 2023; Vol. 41 (21), pp. 12426-12444. Date of Electronic Publication: 2023 Jan 16.
DOI:	10.1080/07391102.2023.2167116
Abstrakt:	The prevalence of anxiety is a significant public health problem, being the 24th leading cause of disability in individuals affected by this disorder. In this context, chalcones, a flavonoid subclass obtained from natural or synthetic sources, interact with central nervous system (CNS) receptors at the same binding site as benzodiazepines, the primary drugs used in the treatment of anxiety. Thus, our study investigates the anxiolytic effect of synthetic chalcones derived from the natural product 2-hydroxy-3,4,6-trimethoxyacetophenone isolated from Croton anisodontus Müll.Arg. in modulating anxiolytic activity via GABAergic and serotoninergic neurotransmission in an adult zebrafish model. Chalcones 1 and 2 were non-toxic to adult zebrafish and showed anxiolytic activity via GABA A receptors. Chalcone 2 also had its anxiolytic action reversed by the antagonist granisetron, indicating the participation of serotonergic receptors 5HTR 3A/3B in the anxiolytic effect. In addition, molecular docking results showed that chalcones have a higher affinity for the GABA A receptor than DZP and binding in the same region of the DZP binding site, indicating a similar effect to the drug. Furthermore, the interaction of chalcones with GABA A and 5-HT 3A receptors demonstrates the anxiolytic effect potential of these molecules.Communicated by Ramaswamy H. Sarma.
Databáze:	MEDLINE
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