Anxiolytic-like effect of chalcone N-{4’[(2E)-3-(3-nitrophenyl)-1-(phenyl)prop-2-en-1-one]} acetamide on adult zebrafish (Danio rerio): Involvement of the 5-HT system
| Autor: | Débora Hellen Almeida de Brito, Emanuela de Lima Rebouças, Alexandre Magno Rodrigues Teixeira, Adriana Rolim Campos, Sacha Aubrey Alves Rodrigues Santos, Jane Eire Silva Alencar de Menezes, Francisco Ernani Alves Magalhães, Paulo Nogueira Bandeira, Antônio Eufrásio Vieira Neto, Francisca Crislândia Oliveira Silva, Carlos Emídio Sampaio Nogueira, Hélcio Silva dos Santos, Jayze da Cunha Xavier, Antonio Wlisses da Silva, Maria Kueirislene Amâncio Ferreira |
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| Rok vydání: | 2020 |
| Předmět: |
0301 basic medicine
Serotonin Chalcone medicine.drug_class Biophysics Danio Anxiety Pharmacology Serotonergic Biochemistry Anxiolytic Open field 03 medical and health sciences chemistry.chemical_compound 0302 clinical medicine Acetamides Drug Discovery medicine Animals Receptor Molecular Biology Zebrafish 5-HT receptor biology Cell Biology Zebrafish Proteins biology.organism_classification Molecular Docking Simulation 030104 developmental biology Anti-Anxiety Agents Mechanism of action chemistry 030220 oncology & carcinogenesis medicine.symptom Receptors Serotonin 5-HT1 Locomotion |
| Zdroj: | Biochemical and Biophysical Research Communications. 526:505-511 |
| ISSN: | 0006-291X |
| Popis: | The action of anxiolytic compounds that act on selective serotonin receptors (SSRIs) have been scarcely evaluated. Serotonergic drugs have been shown to be effective in treating anxiety without presenting adverse effects as benzodiazepines. However, the anxiolytic effects take days to occur. This study aimed to evaluate the anxiolytic effect of the synthetic chalcone, 4’-[(2E) -3- (3-nitrophenyl) -1- (phenyl) prop-2-en-1-one] acetamide (PAAMNBA), and its possible mechanism of action in adult zebrafish (Danio rerio). PAAMNBA was synthesized with a yield of 51.3% and its chemical structure was determined by 1H and 13C NMR. Initially, PAAPMNBA was intraperitoneally administered to zebrafish (n = 6/group) at doses of 4, 12, or 40 mg/kg, and the animals were subsequently subjected to acute and open field toxicity tests. PAAMNBA was administered to the other groups (n = 6/group) for analyzing its effect in the light and dark test. The involvement of the serotonergic (5HT) system was also evaluated using 5-HTR 1, 5-HTR 2A/2C, and 5-HTR 3A/3B receptor antagonists, namely, pizotifeo, granizetron, and ciproeptadina, respectively. Molecular coupling was performed using the 5-HT1 receptor. PAAMNBA was found to be non-toxic, reduced the locomotor activity, and had an anxiolytic effect in adult zebrafish. The effect was reduced by pretreatment with pizotifene and was not reversed by treatment with granizetron and cyproeptadine. A previous in vivo molecular coupling study indicated that chalcones interact with the 5-HT1 receptor. The results suggested that the chalcone, PAAPMNBA, has anxiolytic activity, that is mediated by the serotonergic system via the 5-HT1 receptor. The interaction of PAAPMNBA with the 5-HT1 receptor was confirmed by molecular docking studies. |
| Databáze: | OpenAIRE |
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