Anxiolytic-like effect of succinic acid: A possible GABAergic intervention

Mia, Md. Nayem; Smrity, Shanita Zaman; Bappi, Mehedi Hasan; Kamli, Hossam; Islam, Tawhida; Prottay, Abdullah Al Shamsh; Akbor, Md. Showkoth; Latif, Md. Abdul; Islam, Shoriful; Bhakta, Kushal; Shill, Manik Chandra; Sousa, Francisco Claudeni Pereira de; Luna, Gilberto de; Coutinho, Henrique Douglas Melo; Islam, Muhammad Torequl

doi:10.1016/j.fbio.2023.103044

Cited by 10 publications

(2 citation statements)

References 70 publications

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“…Findings of docking show how strongly a target molecule is bound to its catalytic domain. The characteristics of the ligands in the initial target protein grids for these active binding regions of the target protein were examined using PyMOL (v2.50, accessed on May 11, 2023) (Kamli et al, 2023; Lill & Danielson, 2011) and BIOVIA Discovery Studio (v21.1.0, Dassault Systemes, accessed on November 10, 2022) (Chaturvedi et al, 2021; Mia et al, 2023).…”

Section: Methodsmentioning

confidence: 99%

Quercetin increases the antidepressant‐like effects of sclareol and antagonizes diazepam in thiopental sodium‐induced sleeping mice: A possible GABAergic transmission intervention

Bappi,

Mia,

Ansari

et al. 2024

Phytotherapy Research

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Quercetin is the most common polyphenolic flavonoid present in fruits and vegetables demonstrating versatile health‐promoting effects. This study aimed to examine the effects of quercetin (QR) and sclareol (SCL) on the thiopental sodium (TS)‐induced sleeping and forced swimming test (FST) mouse models. SCL (1, 5, and 10 mg/kg, p.o.) or QR (50 mg/kg, p.o.) and/or diazepam (DZP) (3 mg/kg, i.p.) were employed. After 30 min of TS induction, individual or combined effects on the animals were checked. In the FST test, the animals were subjected to forced swimming after 30 min of administration of the test and/or controls for 5 min. In this case, immobility time was measured. In silico studies were conducted to evaluate the involvement of GABA receptors. SCL (5 and 10 mg/kg) significantly increased the latency and decreased sleeping time compared to the control in the TS‐induced sleeping time study. DZP (3 mg/kg) showed a sedative‐like effect in animals in both sleeping and FST studies. QR (50 mg/kg) exhibited a similar pattern of activity as SCL. However, its effects were more prominent than those of SCL groups. SCL (10 mg/kg) altered the DZP‐3‐mediated effects. SCL‐10 co‐treated with QR‐50 significantly (p < 0.05) increased the latency and decreased sleep time and immobility time, suggesting possible synergistic antidepressant‐like effects. In silico studies revealed that SCL and QR demonstrated better binding affinities with GABAA receptor, especially α2, α3, and α5 subunits. Both compounds also exhibited good ADMET and drug‐like properties. In animal studies, the both compounds worked synergistically to provide antidepressant‐like effects in a slightly different fashion. As a conclusion, the combined administration of SCL and QR may be used in upcoming neurological clinical trials, according to in vivo and in silico findings. However, additional investigation is necessary to verify this behavior and clarify the potential mechanism of action.

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Section: Methodsmentioning

confidence: 99%

Quercetin increases the antidepressant‐like effects of sclareol and antagonizes diazepam in thiopental sodium‐induced sleeping mice: A possible GABAergic transmission intervention

Bappi,

Mia,

Ansari

et al. 2024

Phytotherapy Research

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“…Input files for docking were prepared by setting appropriate docking algorithms and parameters. Ligands were docked with prepared protein structures, and the docking results were analyzed using PyMOL (version 2.5.5, Schrodinger Inc., New York, NY, United States) and BIOVIA Discovery Studio ( Mia et al, 2023 ; Prottay et al, 2024 ). The docking analysis involved the visualization of ligand-protein interactions, the calculation of binding energy and other parameters, and the identification of potential binding sites and key amino acid residues.…”

Section: Methodsmentioning

confidence: 99%

Anti-inflammatory activity of d-pinitol possibly through inhibiting COX-2 enzyme: in vivo and in silico studies

Haque,

El-Nashar,

Akbor

et al. 2024

Front. Chem.

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Introduction: D-pinitol, a naturally occurring inositol, has diverse biological activities like antioxidant, antimicrobial and anticancer activities. This study aimed to evaluate anti-inflammatory effect of d-pinitol in a chick model. Additionally, in silico studies were performed to evaluate the molecular interactions with cyclooxygenase-2 (COX-2).Methods: The tested groups received d-pinitol (12.5, 25, and 50 mg/kg) and the standard drugs celecoxib and ketoprofen (42 mg/kg) via oral gavage prior to formalin injection. Then, the number of licks was counted for the first 10 min, and the paw edema diameter was measured at 60, 90, and 120 min.Results and Discussion: The d-pinitol groups significantly (p < 0.05) reduced the number of paw licks and paw edema diameters, compared to negative control. When d-pinitol was combined with celecoxib, it reduced inflammatory parameters more effectively than the individual groups. The in silico study showed a promising binding capacity of d-pinitol with COX-2. Taken together, d-pinitol exerted anti-inflammatory effects in a dose-dependent manner, possibly through COX-2 interaction pathway.

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Anxiolytic Effect of Sesamol, Possibly Through the GABAkine Interaction Pathway

Islam,

Malik,

Alshememry

et al. 2024

Drug Development Research

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Plant‐based components have helped generate novel lead molecules and scaffolds for anxiety research in psychopharmacology. The present study examined the anxiolytic properties of sesamol (SES), a phenolic lignan derived from Sesamum indicum, employing both in vivo and computational methods to understand its mechanisms of action. In this experiment, adult Swiss albino mice received various doses of SES (25 and 50 mg/kg, p.o.) orally. Afterward, a series of behavioral assessments, including open field, swing, hole cross, and light–dark testing, were conducted. The impact of the GABAergic agonist diazepam (DZP‐1 mg/kg, i.p.) along with the antagonist flumazenil (FLU‐0.1 mg/kg, i.p.) has been studied as provided concurrently with the SES‐50 group. Computational studies were performed to comprehend the interaction between SES and GABAA receptor subunits (α2 and α3). The results of our investigation revealed that SES dose‐dependently and significantly (p < 0.05) reduced the number of square crosses, hole crosses, swings, grooming, and rearing along with a reduction of light residence time in animals. When combined with DZP, SES‐50 significantly reduced all these parameters, while altering with FLU‐0.1. The molecular docking analysis showed that the SES has a relatively good binding score (−5.03 ± 0.15 and −5.25 ± 0.23 kcal/mol) with GABAA receptor α2 and α3 subunits, respectively. The SES triggers anxiolytic effects via GABAA receptor α2 and α3 subunit interactions. Furthermore, precise and comprehensive preclinical research must be considered to validate potential SES targets for anxiolytic impact, clinical trial efficacy, and safety.

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Anxiolytic-like effect of succinic acid: A possible GABAergic intervention

Cited by 10 publications

References 70 publications

Quercetin increases the antidepressant‐like effects of sclareol and antagonizes diazepam in thiopental sodium‐induced sleeping mice: A possible GABAergic transmission intervention

Quercetin increases the antidepressant‐like effects of sclareol and antagonizes diazepam in thiopental sodium‐induced sleeping mice: A possible GABAergic transmission intervention

Anti-inflammatory activity of d-pinitol possibly through inhibiting COX-2 enzyme: in vivo and in silico studies

Anxiolytic Effect of Sesamol, Possibly Through the GABAkine Interaction Pathway

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