Isolation And Characterization Of A Novel Chalcone Derivative From Arisaema Utile A Selective MAO-B Inhibitor In Sodium Azide-Induced Rat Model

This study aims to investigate the neuroprotective effects of Utilito, a novel chalcone derivative isolated from Arisaema utile in a sodium azide-induced Alzheimer's disease (AD) rat model. Anti-alzheimer activities were assessed through in silico molecular docking, simulation studies and in vivo studies. Utilito at doses of 100, 200, 300 mg/kg was administered in Wistar rats (n=6/group) for 14 days. Cognitive performance and locomotion were assessed through behavioural tests (Morris water maze, Y-maze, and open field). Biochemical assays measured the levels of oxidative stress biomarker including catalase (CAT) superoxide dismutase (SOD), reduced glutathione (GSH), and malondialdehyde (MDA). Molecular docking studies revealed a strong binding affinity of Utilito with monoamine oxidase (MAO-B), with a docking score of -41.4 kJ/mol. Conventional hydrogen bond interactions were observed between the MAO-B residues LEU171, TYR398, and TYR435 and the phenol ring of Utilito. Utilito also showed 71 ± 0.11% anti-oxidant activity in the DPPH assay. Behavioural tests utilizing animal models demonstrate the cognitive-enhancing effects of Utilito. Biochemical evaluations underscore the antioxidant properties of Utilito, offering valuable insights into their mechanisms of action at the cellular level. Utilito exhibits antioxidant activity and cognitive improvement in a rat AD model, suggesting its promise as a therapeutic candidate for AD.

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Publication Details

Journal
Pakistan Journal of Pharmaceutical Sciences
Published
2025-01-01
DOI
https://doi.org/10.36721/pjps.2025.38.5.reg.14310.1
Primary Topic
Cholinesterase and Neurodegenerative Diseases
Type
article
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article

Isolation And Characterization Of A Novel Chalcone Derivative From Arisaema Utile A Selective MAO-B Inhibitor In Sodium Azide-Induced Rat Model

Malik Saadullah, Muhammad Kamran Khan
Pakistan Journal of Pharmaceutical Sciences
Cholinesterase and Neurodegenerative Diseases
article

Isolation And Characterization Of A Novel Chalcone Derivative From Arisaema Utile A Selective MAO-B Inhibitor In Sodium Azide-Induced Rat Model

Malik Saadullah, Muhammad Kamran Khan
article en

Abstract

This study aims to investigate the neuroprotective effects of Utilito, a novel chalcone derivative isolated from Arisaema utile in a sodium azide-induced Alzheimer's disease (AD) rat model. Anti-alzheimer activities were assessed through in silico molecular docking, simulation studies and in vivo studies. Utilito at doses of 100, 200, 300 mg/kg was administered in Wistar rats (n=6/group) for 14 days. Cognitive performance and locomotion were assessed through behavioural tests (Morris water maze, Y-maze, and open field). Biochemical assays measured the levels of oxidative stress biomarker including catalase (CAT) superoxide dismutase (SOD), reduced glutathione (GSH), and malondialdehyde (MDA). Molecular docking studies revealed a strong binding affinity of Utilito with monoamine oxidase (MAO-B), with a docking score of -41.4 kJ/mol. Conventional hydrogen bond interactions were observed between the MAO-B residues LEU171, TYR398, and TYR435 and the phenol ring of Utilito. Utilito also showed 71 ± 0.11% anti-oxidant activity in the DPPH assay. Behavioural tests utilizing animal models demonstrate the cognitive-enhancing effects of Utilito. Biochemical evaluations underscore the antioxidant properties of Utilito, offering valuable insights into their mechanisms of action at the cellular level. Utilito exhibits antioxidant activity and cognitive improvement in a rat AD model, suggesting its promise as a therapeutic candidate for AD.

Pakistan Journal of Pharmaceutical SciencesVol. 38(5)
Openalex Percentile: Top 70%
Cholinesterase and Neurodegenerative Diseases
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