Quercetin and/or Ascorbic Acid Modulatory Effect on Phenobarbital-Induced Sleeping Mice Possibly through GABA(A) and GABA(B) Receptor Interaction Pathway
authors Hossain, R; Al-Khafaji, K; Khan, RA; Sarkar, C; Islam, MS; Dey, D; Jain, D; Faria, F; Akbor, R; Atolani, O; Oliveira, SMR; Siyadatpanah, A; Pereira, MD; Islam, MT
nationality International
journal PHARMACEUTICALS
author keywords ascorbic acid; quercetin; Mus musculus; stimulatory-like activity; GABA receptor; molecular docking
keywords MAJOR DEPRESSIVE DISORDER; SYSTEMIC-LUPUS-ERYTHEMATOSUS; COGNITIVE DYSFUNCTION; VITAMIN-C; OXIDATIVE STRESS; ANTIDEPRESSANT; ANXIETY; FLAVONOIDS; MODEL; ANTIOXIDANT
abstract 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 DZPmediated 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 GABAA and GABAB receptors. Both QUR and AA produced a stimulatory-like effect on mice, possibly through the GABAA and GABAB receptor interaction pathways. Further studies are necessary to verify this activity and clarify the exact mechanism of action(s) involved.
publisher MDPI
isbn 1424-8247
year published 2021
volume 14
issue 8
digital object identifier (doi) 10.3390/ph14080721
web of science category 22
subject category Chemistry, Medicinal; Pharmacology & Pharmacy
unique article identifier WOS:000689859200001
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journal analysis (jcr 2019):
journal impact factor 4.286
5 year journal impact factor Not Available
category normalized journal impact factor percentile 82.037
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