Anxiolytic-like Effect of Quercetin Possibly through GABA Receptor Interaction Pathway: In Vivo and In Silico Studies
Scientific evidence suggests that quercetin (QUR) has anxiolytic-like effects in experimental animals. However, the mechanism of action responsible for its anxiolytic-like effects is yet to be discovered. The goal of this research is to assess QUR’s anxiolytic effects in mouse models to explicate th...
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| Format: | Article |
| Language: | English |
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MDPI AG
2022-10-01
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| Series: | Molecules |
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| Online Access: | https://www.mdpi.com/1420-3049/27/21/7149 |
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| author | Md. Shahazul Islam Rajib Hossain Taukir Ahmed Md. Mizanur Rahaman Khattab Al-Khafaji Rasel Ahmed Khan Chandan Sarkar Mehedi Hasan Bappi Edlane Martins de Andrade Isaac Moura Araújo Henrique Douglas Melo Coutinho Grażyna Kowalska Radosław Kowalski Muhammad Asif Hanif Muhammad Torequl Islam |
| author_facet | Md. Shahazul Islam Rajib Hossain Taukir Ahmed Md. Mizanur Rahaman Khattab Al-Khafaji Rasel Ahmed Khan Chandan Sarkar Mehedi Hasan Bappi Edlane Martins de Andrade Isaac Moura Araújo Henrique Douglas Melo Coutinho Grażyna Kowalska Radosław Kowalski Muhammad Asif Hanif Muhammad Torequl Islam |
| author_sort | Md. Shahazul Islam |
| collection | DOAJ |
| description | Scientific evidence suggests that quercetin (QUR) has anxiolytic-like effects in experimental animals. However, the mechanism of action responsible for its anxiolytic-like effects is yet to be discovered. The goal of this research is to assess QUR’s anxiolytic effects in mouse models to explicate the possible mechanism of action. After acute intraperitoneal (i.p.) treatment with QUR at a dose of 50 mg/kg (i.p.), behavioral models of open-field, hole board, swing box, and light–dark tests were performed. QUR was combined with a GABAergic agonist (diazepam) and/or antagonist (flumazenil) group. Furthermore, in silico analysis was also conducted to observe the interaction of QUR and GABA (α5), GABA (β1), and GABA (β2) receptors. In the experimental animal model, QUR had an anxiolytic-like effect. QUR, when combined with diazepam (2 mg/kg, i.p.), drastically potentiated an anxiolytic effect of diazepam. QUR is a more highly competitive ligand for the benzodiazepine recognition site that can displace flumazenil (2.5 mg/kg, i.p.). In all the test models, QUR acted similar to diazepam, with enhanced effects of the standard anxiolytic drug, which were reversed by pre-treatment with flumazenil. QUR showed the best interaction with the GABA (α5) receptor compared to the GABA (β1) and GABA (β2) receptors. In conclusion, QUR may exert an anxiolytic-like effect on mice, probably through the GABA-receptor-interacting pathway. |
| first_indexed | 2024-03-09T18:48:42Z |
| format | Article |
| id | doaj.art-2c4d93a892b5446cbaee401dc481abee |
| institution | Directory Open Access Journal |
| issn | 1420-3049 |
| language | English |
| last_indexed | 2024-03-09T18:48:42Z |
| publishDate | 2022-10-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Molecules |
| spelling | doaj.art-2c4d93a892b5446cbaee401dc481abee2023-11-24T05:59:28ZengMDPI AGMolecules1420-30492022-10-012721714910.3390/molecules27217149Anxiolytic-like Effect of Quercetin Possibly through GABA Receptor Interaction Pathway: In Vivo and In Silico StudiesMd. Shahazul Islam0Rajib Hossain1Taukir Ahmed2Md. Mizanur Rahaman3Khattab Al-Khafaji4Rasel Ahmed Khan5Chandan Sarkar6Mehedi Hasan Bappi7Edlane Martins de Andrade8Isaac Moura Araújo9Henrique Douglas Melo Coutinho10Grażyna Kowalska11Radosław Kowalski12Muhammad Asif Hanif13Muhammad Torequl Islam14Department of Pharmacy, Life Science Faculty, Bangabandhu Sheikh Mujibur Rahman Science and Technology University, Gopalganj 8100, BangladeshDepartment of Pharmacy, Life Science Faculty, Bangabandhu Sheikh Mujibur Rahman Science and Technology University, Gopalganj 8100, BangladeshDepartment of Pharmacy, Life Science Faculty, Bangabandhu Sheikh Mujibur Rahman Science and Technology University, Gopalganj 8100, BangladeshDepartment of Pharmacy, Life Science Faculty, Bangabandhu Sheikh Mujibur Rahman Science and Technology University, Gopalganj 8100, BangladeshCollege of Dentistry, The University of Mashreq, Baghdad 10022, IraqPharmacy Discipline, Life Science School, Khulna University, Khulna 9280, BangladeshDepartment of Pharmacy, Life Science Faculty, Bangabandhu Sheikh Mujibur Rahman Science and Technology University, Gopalganj 8100, BangladeshDepartment of Pharmacy, Life Science Faculty, Bangabandhu Sheikh Mujibur Rahman Science and Technology University, Gopalganj 8100, BangladeshCECAPE—College of Dentistry, Av. Padre Cícero 3917, São José 63024-015, BrazilDepartment of Biological Chemistry, Regional University of Cariri—URCA, Crato 63105-000, BrazilDepartment of Biological Chemistry, Regional University of Cariri—URCA, Crato 63105-000, BrazilDepartment of Tourism and Recreation, University of Life Sciences in Lublin, 15 Akademicka Str., 20-950 Lublin, PolandDepartment of Analysis and Food Quality Assessment, University of Life Sciences in Lublin, 8 Skromna Str., 20-704 Lublin, PolandNano and Biomaterials Lab, Department of Chemistry, University of Agriculture, Faisalabad 38040, PakistanDepartment of Pharmacy, Life Science Faculty, Bangabandhu Sheikh Mujibur Rahman Science and Technology University, Gopalganj 8100, BangladeshScientific evidence suggests that quercetin (QUR) has anxiolytic-like effects in experimental animals. However, the mechanism of action responsible for its anxiolytic-like effects is yet to be discovered. The goal of this research is to assess QUR’s anxiolytic effects in mouse models to explicate the possible mechanism of action. After acute intraperitoneal (i.p.) treatment with QUR at a dose of 50 mg/kg (i.p.), behavioral models of open-field, hole board, swing box, and light–dark tests were performed. QUR was combined with a GABAergic agonist (diazepam) and/or antagonist (flumazenil) group. Furthermore, in silico analysis was also conducted to observe the interaction of QUR and GABA (α5), GABA (β1), and GABA (β2) receptors. In the experimental animal model, QUR had an anxiolytic-like effect. QUR, when combined with diazepam (2 mg/kg, i.p.), drastically potentiated an anxiolytic effect of diazepam. QUR is a more highly competitive ligand for the benzodiazepine recognition site that can displace flumazenil (2.5 mg/kg, i.p.). In all the test models, QUR acted similar to diazepam, with enhanced effects of the standard anxiolytic drug, which were reversed by pre-treatment with flumazenil. QUR showed the best interaction with the GABA (α5) receptor compared to the GABA (β1) and GABA (β2) receptors. In conclusion, QUR may exert an anxiolytic-like effect on mice, probably through the GABA-receptor-interacting pathway.https://www.mdpi.com/1420-3049/27/21/7149anxietyquercetinGABAergic systemin vivo studymolecular docking |
| spellingShingle | Md. Shahazul Islam Rajib Hossain Taukir Ahmed Md. Mizanur Rahaman Khattab Al-Khafaji Rasel Ahmed Khan Chandan Sarkar Mehedi Hasan Bappi Edlane Martins de Andrade Isaac Moura Araújo Henrique Douglas Melo Coutinho Grażyna Kowalska Radosław Kowalski Muhammad Asif Hanif Muhammad Torequl Islam Anxiolytic-like Effect of Quercetin Possibly through GABA Receptor Interaction Pathway: In Vivo and In Silico Studies Molecules anxiety quercetin GABAergic system in vivo study molecular docking |
| title | Anxiolytic-like Effect of Quercetin Possibly through GABA Receptor Interaction Pathway: In Vivo and In Silico Studies |
| title_full | Anxiolytic-like Effect of Quercetin Possibly through GABA Receptor Interaction Pathway: In Vivo and In Silico Studies |
| title_fullStr | Anxiolytic-like Effect of Quercetin Possibly through GABA Receptor Interaction Pathway: In Vivo and In Silico Studies |
| title_full_unstemmed | Anxiolytic-like Effect of Quercetin Possibly through GABA Receptor Interaction Pathway: In Vivo and In Silico Studies |
| title_short | Anxiolytic-like Effect of Quercetin Possibly through GABA Receptor Interaction Pathway: In Vivo and In Silico Studies |
| title_sort | anxiolytic like effect of quercetin possibly through gaba receptor interaction pathway in vivo and in silico studies |
| topic | anxiety quercetin GABAergic system in vivo study molecular docking |
| url | https://www.mdpi.com/1420-3049/27/21/7149 |
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