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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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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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Embrapa Florestas (CNPF) |
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| Registros recuperados : 3 | |
| 2. |  | COELHO, M. do S. E.; LIMA, B. M. F. V.; ASSIS, J. S. de; MELO, N. F. de. Efeito da benzilaminopurina (BAP) na multiplicação in vitro de onze genótipos de oliveira (Olea europaea L.). Magistra, Cruz das Almas, v. 18, p.77, out. 2006. Número especial. Edição de Resumos do 2º Workshop de Recursos Genéticos Vegetais no Estado da Bahia, Ilheus, out. 2006.| Tipo: Resumo em Anais de Congresso |
| Biblioteca(s): Embrapa Semiárido. |
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| 3. | | COELHO, M. do S. E.; LIMA, B. M. F. V.; ASSIS, J. S. de; MELO, N. F. de. Estabelecimento in vitro de genótipos de oliveira (Olea europaea L.) cultivadas no semi-árido brasileiro. Magistra, Cruz das Almas, v. 18, p.87, out. 2006. Número especial. Edição de Resumos do 2º Workshop de Recursos Genéticos Vegetais no Estado da Bahia, Ilheus, out. 2006.| Tipo: Resumo em Anais de Congresso |
| Biblioteca(s): Embrapa Semiárido. |
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| Registros recuperados : 3 | |
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| Nenhum registro encontrado para a expressão de busca informada. |
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