Sclareol antagonizes the sedative effect of diazepam in thiopental sodium-induced sleeping animals: In vivo and in silico studies

Hassan, SM Hafiz; El-Nashar, Heba A.S.; Rahman, Md Anisur; Polash, Md Jannatul Islam; Bappi, Mehedi Hasan; Mondal, Milon; Abdel-Maksoud, Mostafa A.; Malik, Abdul; Aufy, Mohammed; El-Shazly, Mohamed; Islam, Muhammad Torequl

doi:10.1016/j.biopha.2024.116939

Biomedicine & Pharmacotherapy

2024

DOI: 10.1016/j.biopha.2024.116939

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Sclareol antagonizes the sedative effect of diazepam in thiopental sodium-induced sleeping animals: In vivo and in silico studies

SM Hafiz Hassan,

Heba A.S. El-Nashar,

Md Anisur Rahman

et al.

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2024

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Caffeine and sclareol reduce the sedative effects of linalool, possibly through the GABA A interaction pathway: molecular insights through in vivo and in silico studies

Islam,

Hasan,

Ferdous

et al. 2024

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Study background: Linalool (LIN) has some important neuropharmacological activities, including anxiolytic and sedative effects. It is also clear that it protects experimental animals from convulsions and Alzheimer's disease. On the other hand, caffeine (CAF) and sclareol (SCL) have neurostimulatory potential. Aim To evaluate the sedative effect and possible molecular mechanisms of CAF with LIN and/or SCL through in vivo and in silico studies. Methodology: CAF (10 mg/kg) alone or with LIN (50 mg/kg) and/or SCL (10 mg/kg) were intraperitoneally (i.p.) treated before thirty minutes of pentobarbital sodium (TS) injection (40 mg/kg, i.p.) to the mice and observed for latency and duration of sleep up to 4 hours. To understand the possible action mechanisms of these drugs, we also performed molecular docking studies with GABAA receptor respective submits. Results Findings suggest that LIN exerted significant (p < 0.05) sedative effects on the animals. CAF and SCL alone or in their combinations significantly reduced LIN’s effects in mice. CAF, LIN, and SCL showed binding affinities of ‒5.7, ‒4.7, ‒7.4 kcal/mol with 6X3X of the GABAA receptor (α1 and β2 subunits), respectively. Conclusion LIN exerted significant sedative effects, while CAF and/or SCL reduced this effect in animals. We suppose these drugs may exert their sedative effects through the GABAA receptor intrecation pathway. Further studies are required to confirm these results.

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Caffeine and sclareol reduce the sedative effects of linalool, possibly through the GABA A interaction pathway: molecular insights through in vivo and in silico studies

Islam,

Hasan,

Ferdous

et al. 2024

Preprint

View full text Add to dashboard Cite

show abstract

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Sclareol antagonizes the sedative effect of diazepam in thiopental sodium-induced sleeping animals: In vivo and in silico studies

Cited by 1 publication

References 42 publications

Caffeine and sclareol reduce the sedative effects of linalool, possibly through the GABA A interaction pathway: molecular insights through in vivo and in silico studies

Caffeine and sclareol reduce the sedative effects of linalool, possibly through the GABA A interaction pathway: molecular insights through in vivo and in silico studies

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