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| 1. |  | OLIVEIRA, D. R. de; TODO, A. H.; REGO, G. M.; CERUTTI, J. M.; CAVALHEIRO, A. J.; RANDO, D. G. G.; CERUTTI, S. M. Flavones-bound in benzodiazepine site on GABAA receptor: concomitant anxiolytic-like and cognitive-enhancing effects produced by Isovitexin and 6-C-glycoside-Diosmetin. European Journal of Pharmacology, v. 831, p. 77-86, July 2018.| Biblioteca(s): Embrapa Florestas. |
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 | Acesso ao texto completo restrito à biblioteca da Embrapa Florestas. Para informações adicionais entre em contato com cnpf.biblioteca@embrapa.br. |
Registro Completo
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Biblioteca(s): |
Embrapa Florestas. |
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Data corrente: |
29/05/2018 |
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Data da última atualização: |
30/05/2018 |
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Tipo da produção científica: |
Artigo em Periódico Indexado |
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Circulação/Nível: |
A - 2 |
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Autoria: |
OLIVEIRA, D. R. de; TODO, A. H.; REGO, G. M.; CERUTTI, J. M.; CAVALHEIRO, A. J.; RANDO, D. G. G.; CERUTTI, S. M. |
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Afiliação: |
Daniela Rodrigues de Oliveira, Universidade Federal de São Paulo; Andréia Hatsue Todo, Universidade Federal de São Paulo; GIZELDA MAIA REGO, CNPF; Janete Maria Cerutti, Universidade Federal de São Paulo; Alberto José Cavalheiro, UNESP; Daniela Gonçales Galasse Rando, Universidade Federal de São Paulo; Suzete Maria Cerutti, Universidade Federal de São Paulo. |
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Título: |
Flavones-bound in benzodiazepine site on GABAA receptor: concomitant anxiolytic-like and cognitive-enhancing effects produced by Isovitexin and 6-C-glycoside-Diosmetin. |
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Ano de publicação: |
2018 |
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Fonte/Imprenta: |
European Journal of Pharmacology, v. 831, p. 77-86, July 2018. |
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DOI: |
10.1016/j.ejphar.2018.05.004 |
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Idioma: |
Inglês |
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Conteúdo: |
Increasing evidence suggests that flavones can modulate memory and anxiety-like behaviour. However, these therapeutic effects are inconsistent and induce of adverse effects, which have been associated with interactions at the Benzodiazepine (BZ)-binding site. To improve our understanding of flavone effects on memory and anxiety, we employed a plus-maze discriminative avoidance task. Furthermore, we evaluated the potential of the compounds in modulating GABAA receptors via BZ-binding site using molecular modelling studies. Adult male Wistar rats were treated 30 min before training session with Vicenin-2 (0.1 and 0.25 mg/kg), Vitexin (0.1 and 0.25 mg/kg), Isovitexin (0.1 and 0.25 mg/kg) and 0.1 mg/kg 6-C-glycoside-Diosmetin, vehicle and a GABAA receptor agonist. The analysis of the time spent in the non-aversive vs aversive enclosed arms during the test session and percentage of time in the open arms within the training session revealed that treatment with Isovitexin and 6-C-glycoside-Diosmetin had memory-enhancing and anxiolytic-like effects (P < 0.001). In contrast, treatment with a higher dose of Diazepam impaired short-and long-term memory when it alleviated anxiety level. Docking studies revealed that flavones docked in a very similar way to that observed to the Diazepam, except by a lack of interaction in residue α1His101 in the BZ-binding site on GABAA receptors, which may be related to memory-enhancing effect. The occurrence of the α1His101 interaction could justify the memory-impairing observed following Diazepam treatment. These findings provide the first evidence that Isovitexin and 6-C-glycoside-Diosmetin could exert their memory-enhancing and anxiolytic-like effects via GABAA receptor modulation, which likely occurs via their benzodiazepine-binding site. MenosIncreasing evidence suggests that flavones can modulate memory and anxiety-like behaviour. However, these therapeutic effects are inconsistent and induce of adverse effects, which have been associated with interactions at the Benzodiazepine (BZ)-binding site. To improve our understanding of flavone effects on memory and anxiety, we employed a plus-maze discriminative avoidance task. Furthermore, we evaluated the potential of the compounds in modulating GABAA receptors via BZ-binding site using molecular modelling studies. Adult male Wistar rats were treated 30 min before training session with Vicenin-2 (0.1 and 0.25 mg/kg), Vitexin (0.1 and 0.25 mg/kg), Isovitexin (0.1 and 0.25 mg/kg) and 0.1 mg/kg 6-C-glycoside-Diosmetin, vehicle and a GABAA receptor agonist. The analysis of the time spent in the non-aversive vs aversive enclosed arms during the test session and percentage of time in the open arms within the training session revealed that treatment with Isovitexin and 6-C-glycoside-Diosmetin had memory-enhancing and anxiolytic-like effects (P < 0.001). In contrast, treatment with a higher dose of Diazepam impaired short-and long-term memory when it alleviated anxiety level. Docking studies revealed that flavones docked in a very similar way to that observed to the Diazepam, except by a lack of interaction in residue α1His101 in the BZ-binding site on GABAA receptors, which may be related to memory-enhancing effect. The occurrence of the α1His101 interaction could ... Mostrar Tudo |
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Palavras-Chave: |
Ácido gama aminobutírico; Ansiedade; Anxiety and memory; Efeito ansiolítico; GABA; GABAAR; Memória; Neurotransmissor; PM-DAT; Receptor. |
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Thesagro: |
Erythrina Falcata; Farmacologia; Flavonóide. |
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Thesaurus NAL: |
Flavones. |
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Categoria do assunto: |
F Plantas e Produtos de Origem Vegetal |
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Marc: |
LEADER 02929naa a2200373 a 4500
001 2092046
005 2018-05-30
008 2018 bl uuuu u00u1 u #d
024 7 $a10.1016/j.ejphar.2018.05.004$2DOI
100 1 $aOLIVEIRA, D. R. de
245 $aFlavones-bound in benzodiazepine site on GABAA receptor$bconcomitant anxiolytic-like and cognitive-enhancing effects produced by Isovitexin and 6-C-glycoside-Diosmetin.$h[electronic resource]
260 $c2018
520 $aIncreasing evidence suggests that flavones can modulate memory and anxiety-like behaviour. However, these therapeutic effects are inconsistent and induce of adverse effects, which have been associated with interactions at the Benzodiazepine (BZ)-binding site. To improve our understanding of flavone effects on memory and anxiety, we employed a plus-maze discriminative avoidance task. Furthermore, we evaluated the potential of the compounds in modulating GABAA receptors via BZ-binding site using molecular modelling studies. Adult male Wistar rats were treated 30 min before training session with Vicenin-2 (0.1 and 0.25 mg/kg), Vitexin (0.1 and 0.25 mg/kg), Isovitexin (0.1 and 0.25 mg/kg) and 0.1 mg/kg 6-C-glycoside-Diosmetin, vehicle and a GABAA receptor agonist. The analysis of the time spent in the non-aversive vs aversive enclosed arms during the test session and percentage of time in the open arms within the training session revealed that treatment with Isovitexin and 6-C-glycoside-Diosmetin had memory-enhancing and anxiolytic-like effects (P < 0.001). In contrast, treatment with a higher dose of Diazepam impaired short-and long-term memory when it alleviated anxiety level. Docking studies revealed that flavones docked in a very similar way to that observed to the Diazepam, except by a lack of interaction in residue α1His101 in the BZ-binding site on GABAA receptors, which may be related to memory-enhancing effect. The occurrence of the α1His101 interaction could justify the memory-impairing observed following Diazepam treatment. These findings provide the first evidence that Isovitexin and 6-C-glycoside-Diosmetin could exert their memory-enhancing and anxiolytic-like effects via GABAA receptor modulation, which likely occurs via their benzodiazepine-binding site.
650 $aFlavones
650 $aErythrina Falcata
650 $aFarmacologia
650 $aFlavonóide
653 $aÁcido gama aminobutírico
653 $aAnsiedade
653 $aAnxiety and memory
653 $aEfeito ansiolítico
653 $aGABA
653 $aGABAAR
653 $aMemória
653 $aNeurotransmissor
653 $aPM-DAT
653 $aReceptor
700 1 $aTODO, A. H.
700 1 $aREGO, G. M.
700 1 $aCERUTTI, J. M.
700 1 $aCAVALHEIRO, A. J.
700 1 $aRANDO, D. G. G.
700 1 $aCERUTTI, S. M.
773 $tEuropean Journal of Pharmacology$gv. 831, p. 77-86, July 2018.
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