Anxiolytic-like effect of brominated compounds from the marine sponge Aplysina fulva on adult zebrafish (Danio rerio): Involvement of the GABAergic system
| Autor: | Francisca Crislândia Oliveira Silva, Carlos Emídio Sampaio Nogueira, Edilberto R. Silveira, Otília Deusdênia L. Pessoa, Hélcio Silva dos Santos, Maria Kueirislene Amâncio Ferreira, Karísia S.B. de L. Silva, Hozana Patrícia S. de F. Cesário, Eduardo Hajdu, Jane Eire Silva Alencar de Menezes |
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| Rok vydání: | 2021 |
| Předmět: |
Bromides
Male 0301 basic medicine medicine.drug_class Danio Pharmacology Anxiolytic Protein Structure Secondary Open field 03 medical and health sciences Cellular and Molecular Neuroscience 0302 clinical medicine medicine Animals GABA Modulators Zebrafish Biological Products Dose-Response Relationship Drug biology Chemistry GABAA receptor Age Factors Biological activity Cell Biology Receptors GABA-A biology.organism_classification Porifera 030104 developmental biology Anti-Anxiety Agents Flumazenil GABAergic Female Locomotion 030217 neurology & neurosurgery medicine.drug |
| Zdroj: | Neurochemistry International. 146:105021 |
| ISSN: | 0197-0186 |
| DOI: | 10.1016/j.neuint.2021.105021 |
| Popis: | Benzodiazepines are commonly used to treat disorders of the central nervous system, including anxiety. However, due to their adverse effects, there is a continuing interest in discovering new safe and effective drugs. Marine natural products have emerged as a prolific source of bioactive nitrogenated compounds. Aiming to discover new biologically active natural compounds, the marine sponge Aplysina fulva, a nitrogen-bearing heterocyst producer, was investigated. The main isolated compounds (4, 6, and 9) were evaluated on adult zebrafish (Danio rerio). A group of fishes (n = 6) was preliminarily subjected to acute toxicity, and open field tests using 0.1, 0.5, and 1.0 mg/mL (v. o.) of those compounds was performed. The anxiolytic effect was further investigated in the light/dark assay based on the locomotor response at zebrafish. Interactions through the GABAergic system were investigated using flumazenil, a silent modulator of GABA receptors. To improve the results, a study of molecular docking using the GABAA receptor also was performed. Based on the results, the bromotyrosine derivative compounds 4, 6, and 9 exhibited anxiolytic-like effects mediated by the GABAergic system. |
| Databáze: | OpenAIRE |
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