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Quercetin and/or Ascorbic Acid Modulatory Effect on Phenobarbital-Induced Sleeping Mice Possibly through GABA(A) and GABA(B) Receptor Interaction Pathway
Depressive disorder is a recurrent illness that affects large numbers of the general population worldwide. In recent years, the goal of depression treatment has moved from symptomatic response to that of full remission. However, treatment-resistant depression is a major challenge in the treatment of...
Autores principales: | , , , , , , , , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2021
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8398796/ https://www.ncbi.nlm.nih.gov/pubmed/34451819 http://dx.doi.org/10.3390/ph14080721 |
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author | Hossain, Rajib Al-Khafaji, Khattab Khan, Rasel Ahmed Sarkar, Chandan Islam, Md. Shahazul Dey, Dipta Jain, Divya Faria, Farhana Akbor, Rukaya Atolani, Olubunmi Oliveira, Sónia M. R. Siyadatpanah, Abolghasem Pereira, Maria de Lourdes Islam, Muhammad Torequl |
author_facet | Hossain, Rajib Al-Khafaji, Khattab Khan, Rasel Ahmed Sarkar, Chandan Islam, Md. Shahazul Dey, Dipta Jain, Divya Faria, Farhana Akbor, Rukaya Atolani, Olubunmi Oliveira, Sónia M. R. Siyadatpanah, Abolghasem Pereira, Maria de Lourdes Islam, Muhammad Torequl |
author_sort | Hossain, Rajib |
collection | PubMed |
description | Depressive disorder is a recurrent illness that affects large numbers of the general population worldwide. In recent years, the goal of depression treatment has moved from symptomatic response to that of full remission. However, treatment-resistant depression is a major challenge in the treatment of depression or depression-related disorders. Consensus opinion, therefore, suggests that effective combined aggressive initial treatment is the most appropriate strategy. This study aimed to evaluate the effects of quercetin (QUR) and/or ascorbic acid (AA) on Phenobarbital-induced sleeping mice. QUR (50 mg/kg) and/or AA (25 mg/kg) with or without intraperitoneally pre-treated with GABA receptor agonist (diazepam: 2 mg/kg, i.p.) or antagonist (Flumazenil: 2.5 mg/kg, i.p.) to underscore the effects, as well as the possible involvement of the GABA receptor in the modulatory action of QUR and AA in sleeping mice. Additionally, an in silico study was undertaken to predict the involvement of GABA receptors in the sleep mechanism. Findings suggest that the pretreatment of QUR and AA modulated the onset and duration of action of the standard drugs in experimental animals. The acute administration of QUR and/or AA significantly (p < 0.05) reversed the DZP-mediated onset of action and slightly reversed the duration of sleep time in comparison to the vehicle (control) group. A further combination of QUR or AA with the FLU resulted in an enhancement of the onset of action while reducing the duration of action, suggesting a FLU-like effect on the test animals. In in silico studies, AA and QUR showed good to moderate binding affinities with GABA(A) and GABA(B) receptors. Both QUR and AA produced a stimulatory-like effect on mice, possibly through the GABA(A) and GABA(B) receptor interaction pathways. Further studies are necessary to verify this activity and clarify the exact mechanism of action(s) involved. |
format | Online Article Text |
id | pubmed-8398796 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2021 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-83987962021-08-29 Quercetin and/or Ascorbic Acid Modulatory Effect on Phenobarbital-Induced Sleeping Mice Possibly through GABA(A) and GABA(B) Receptor Interaction Pathway Hossain, Rajib Al-Khafaji, Khattab Khan, Rasel Ahmed Sarkar, Chandan Islam, Md. Shahazul Dey, Dipta Jain, Divya Faria, Farhana Akbor, Rukaya Atolani, Olubunmi Oliveira, Sónia M. R. Siyadatpanah, Abolghasem Pereira, Maria de Lourdes Islam, Muhammad Torequl Pharmaceuticals (Basel) Article Depressive disorder is a recurrent illness that affects large numbers of the general population worldwide. In recent years, the goal of depression treatment has moved from symptomatic response to that of full remission. However, treatment-resistant depression is a major challenge in the treatment of depression or depression-related disorders. Consensus opinion, therefore, suggests that effective combined aggressive initial treatment is the most appropriate strategy. This study aimed to evaluate the effects of quercetin (QUR) and/or ascorbic acid (AA) on Phenobarbital-induced sleeping mice. QUR (50 mg/kg) and/or AA (25 mg/kg) with or without intraperitoneally pre-treated with GABA receptor agonist (diazepam: 2 mg/kg, i.p.) or antagonist (Flumazenil: 2.5 mg/kg, i.p.) to underscore the effects, as well as the possible involvement of the GABA receptor in the modulatory action of QUR and AA in sleeping mice. Additionally, an in silico study was undertaken to predict the involvement of GABA receptors in the sleep mechanism. Findings suggest that the pretreatment of QUR and AA modulated the onset and duration of action of the standard drugs in experimental animals. The acute administration of QUR and/or AA significantly (p < 0.05) reversed the DZP-mediated onset of action and slightly reversed the duration of sleep time in comparison to the vehicle (control) group. A further combination of QUR or AA with the FLU resulted in an enhancement of the onset of action while reducing the duration of action, suggesting a FLU-like effect on the test animals. In in silico studies, AA and QUR showed good to moderate binding affinities with GABA(A) and GABA(B) receptors. Both QUR and AA produced a stimulatory-like effect on mice, possibly through the GABA(A) and GABA(B) receptor interaction pathways. Further studies are necessary to verify this activity and clarify the exact mechanism of action(s) involved. MDPI 2021-07-26 /pmc/articles/PMC8398796/ /pubmed/34451819 http://dx.doi.org/10.3390/ph14080721 Text en © 2021 by the authors. https://creativecommons.org/licenses/by/4.0/Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/). |
spellingShingle | Article Hossain, Rajib Al-Khafaji, Khattab Khan, Rasel Ahmed Sarkar, Chandan Islam, Md. Shahazul Dey, Dipta Jain, Divya Faria, Farhana Akbor, Rukaya Atolani, Olubunmi Oliveira, Sónia M. R. Siyadatpanah, Abolghasem Pereira, Maria de Lourdes Islam, Muhammad Torequl Quercetin and/or Ascorbic Acid Modulatory Effect on Phenobarbital-Induced Sleeping Mice Possibly through GABA(A) and GABA(B) Receptor Interaction Pathway |
title | Quercetin and/or Ascorbic Acid Modulatory Effect on Phenobarbital-Induced Sleeping Mice Possibly through GABA(A) and GABA(B) Receptor Interaction Pathway |
title_full | Quercetin and/or Ascorbic Acid Modulatory Effect on Phenobarbital-Induced Sleeping Mice Possibly through GABA(A) and GABA(B) Receptor Interaction Pathway |
title_fullStr | Quercetin and/or Ascorbic Acid Modulatory Effect on Phenobarbital-Induced Sleeping Mice Possibly through GABA(A) and GABA(B) Receptor Interaction Pathway |
title_full_unstemmed | Quercetin and/or Ascorbic Acid Modulatory Effect on Phenobarbital-Induced Sleeping Mice Possibly through GABA(A) and GABA(B) Receptor Interaction Pathway |
title_short | Quercetin and/or Ascorbic Acid Modulatory Effect on Phenobarbital-Induced Sleeping Mice Possibly through GABA(A) and GABA(B) Receptor Interaction Pathway |
title_sort | quercetin and/or ascorbic acid modulatory effect on phenobarbital-induced sleeping mice possibly through gaba(a) and gaba(b) receptor interaction pathway |
topic | Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8398796/ https://www.ncbi.nlm.nih.gov/pubmed/34451819 http://dx.doi.org/10.3390/ph14080721 |
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