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Anxiolytic-like effect of chalcone N-{(4'-[(E)-3-(4-fluorophenyl)-1-(phenyl) prop-2-en-1-one]} acetamide on adult zebrafish (Danio rerio): Involvement of the GABAergic system.
Ferreira, Maria Kueirislene A; da Silva, Antonio Wlisses; Silva, Francisca Crislândia O; Holanda, Carlos Leone A; Barroso, Sheila M; Lima, Joyce Dos Reis; Vieira Neto, Antônio Eufrásio; Campos, Adriana R; Bandeira, Paulo N; Dos Santos, Hélcio S; de Lemos, Telma Leda G; Siqueira, Sônia Maria C; Magalhães, Francisco Ernani A; de Menezes, Jane Eire S A.
Affiliation
  • Ferreira MKA; State University of Ceará, Science and Technology Center (CCT), Itaperi Campus, Laboratory of Natural Products Chemistry - LQPN-S, CEP 60741-000, Fortaleza, Ceará, Brazil. Electronic address: kueirislene.ferreira@aluno.uece.br.
  • da Silva AW; State University of Ceará, Science and Technology Center (CCT), Itaperi Campus, Laboratory of Natural Products Chemistry - LQPN-S, CEP 60741-000, Fortaleza, Ceará, Brazil.
  • Silva FCO; State University of Ceará, Science and Technology Center (CCT), Itaperi Campus, Laboratory of Natural Products Chemistry - LQPN-S, CEP 60741-000, Fortaleza, Ceará, Brazil.
  • Holanda CLA; State University of Ceará, Science and Technology Center (CCT), Itaperi Campus, Laboratory of Natural Products Chemistry - LQPN-S, CEP 60741-000, Fortaleza, Ceará, Brazil.
  • Barroso SM; State University of Ceará, Science and Technology Center (CCT), Itaperi Campus, Laboratory of Natural Products Chemistry - LQPN-S, CEP 60741-000, Fortaleza, Ceará, Brazil.
  • Lima JDR; State University of Ceará, Science and Technology Center (CCT), Itaperi Campus, Laboratory of Natural Products Chemistry - LQPN-S, CEP 60741-000, Fortaleza, Ceará, Brazil.
  • Vieira Neto AE; University of Fortaleza, Experimental Biology Nucleus (NUBEX), CEP 60811650, Fortaleza, Ceará, Brazil.
  • Campos AR; University of Fortaleza, Experimental Biology Nucleus (NUBEX), CEP 60811650, Fortaleza, Ceará, Brazil.
  • Bandeira PN; State University of Vale do Acaraú, Chemistry Course, Laboratory of Natural Products Chemistry, Synthesis and Biocatalysis of Organic Compounds - LBPNSB, Betânia Campus, CEP 62040370, Sobral, Ceará, Brazil.
  • Dos Santos HS; State University of Vale do Acaraú, Chemistry Course, Laboratory of Natural Products Chemistry, Synthesis and Biocatalysis of Organic Compounds - LBPNSB, Betânia Campus, CEP 62040370, Sobral, Ceará, Brazil.
  • de Lemos TLG; Department of Organic and Inorganic Chemistry, Federal University of Ceará, CEP 60451-970, Fortaleza, Ceará, Brazil.
  • Siqueira SMC; State University of Ceará, Science and Technology Center (CCT), Itaperi Campus, Laboratory of Natural Products Chemistry - LQPN-S, CEP 60741-000, Fortaleza, Ceará, Brazil.
  • Magalhães FEA; State University of Ceará, Science and Technology Center (CCT), Itaperi Campus, Laboratory of Natural Products Chemistry - LQPN-S, CEP 60741-000, Fortaleza, Ceará, Brazil; University of Fortaleza, Experimental Biology Nucleus (NUBEX), CEP 60811650, Fortaleza, Ceará, Brazil; State University of Ceará
  • de Menezes JESA; State University of Ceará, Science and Technology Center (CCT), Itaperi Campus, Laboratory of Natural Products Chemistry - LQPN-S, CEP 60741-000, Fortaleza, Ceará, Brazil. Electronic address: jane.menezes@uece.br.
Behav Brain Res ; 374: 111871, 2019 11 18.
Article in En | MEDLINE | ID: mdl-30922939
ABSTRACT
Benzodiazepines are the standard drugs for the treatment of anxiety, but their undesirable side effects make it necessary to develop new anxiolytic drugs. The objective of this study was to evaluate the possible anxiolytic-simile effect of synthetic chalcone N-{(4'-[(E)-3-(4-fluorophenyl)-1-(phenyl) prop-2-en-1-one]} acetamide (PAAPFBA) on adult zebrafish (Danio rerio). PAAPFBA was synthesized with an 88.21% yield and its chemical structure was determined by 1H and 13C NMR. Initially, animals (n = 6/group) were treated (4 or 12 or 40 mg/kg, intraperitoneal) with PAAPFBA and were submitted to acute toxicity and open field tests. Then, other groups (n = 6/each) received PAAPFBA for the analysis of its effect on the Light & Dark Test. The participation of the GABAergic system was also assessed using the GABAA antagonist flumazenil. Molecular docking was performed using the GABAA receptor. The effect of PAAPFBA on anxiety induced by alcohol withdrawal was analyzed. PAAPFBA was non-toxic, reduced the locomotor activity, and showed an anxiolytic-like effect in both models. This effect was reduced by pre-treatment with the flumazenil. In agreement with in vivo studies, molecular docking indicated an interaction between chalcone and the GABAA receptor. The results suggest that PAAPFBA is an anxiolytic agent mediated via the GABAergic system.
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Full text: 1 Database: MEDLINE Main subject: Anxiety / Chalcones Limits: Animals Language: En Year: 2019 Type: Article
Fulltext
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PubMed Links
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Full text: 1 Database: MEDLINE Main subject: Anxiety / Chalcones Limits: Animals Language: En Year: 2019 Type: Article