Effect of Cinnamaldehyde Chalcone on Behavior in Adult Zebrafish (Danio rerio): In Silico Approach

The study focuses on the anxiolytic potential of chalcone (2E,4E)‐1‐(2‐hydroxyphenyl)‐5‐phenylpenta‐2,4‐dien‐1‐one (CHALCNM) in adult zebrafish. Successfully synthesized in 58 % yield, CHALCNM demonstrated no toxicity after 96 h of exposure. In behavioral tests, CHALCNM (40 mg/kg) reduced locomotor...

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Bibliographic Details
Published in:Chemistry & biodiversity 2024-08, Vol.21 (8), p.e202400935-n/a
Main Authors: Carneiro Romão, Ivana, Costa Siqueira, Sônia Maria, Amâncio Ferreira, Maria Kueirislene, Wlisses da Silva, Antonio, Machado Marinho, Márcia, Ferreira Ribeiro, Walber Henrique, Castro Gomes, Andreia Ferreira, Alencar de Menezes, Jane Eire Silva, Santos, Hélcio Silva
Format: Article
Language:English
Subjects:
Anxiety
Aquariums
Benzodiazepines
Bioavailability
Chalcone
Cinnamaldehyde
Coupling (molecular)
Danio rerio
Diazepam
Flumazenil
GABAergic
Hepatotoxicity
Locomotor activity
Pharmacology
Receptors
Virtual memory systems
Zebrafish
γ-Aminobutyric acid A receptors
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Summary:The study focuses on the anxiolytic potential of chalcone (2E,4E)‐1‐(2‐hydroxyphenyl)‐5‐phenylpenta‐2,4‐dien‐1‐one (CHALCNM) in adult zebrafish. Successfully synthesized in 58 % yield, CHALCNM demonstrated no toxicity after 96 h of exposure. In behavioral tests, CHALCNM (40 mg/kg) reduced locomotor activity and promoted less anxious behavior in zebrafish, confirmed by increased permanence in the light zone of the aquarium. Flumazenil reversed its anxiolytic effect, indicating interaction with GABAA receptors. Furthermore, CHALCNM (4 and 20 mg/kg) preserved zebrafish memory in inhibitory avoidance tests. Virtual screening and ADMET profile studies suggest high oral bioavailability, access to the CNS, favored by low topological polarity (TPSA≤75 Å2) and low incidence of hepatotoxicity, standing out as a promising pharmacological agent against the GABAergic system. In molecular coupling, CHALCNM demonstrated superior affinity to diazepam for the GABAA receptor. These results reinforce the therapeutic potential of CHALCNM in the treatment of anxiety, highlighting its possible future clinical application.
ISSN:1612-1872
1612-1880
1612-1880
DOI:10.1002/cbdv.202400935