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<p>Insomnia is a common sleep disorder characterized by difficulties in falling asleep, staying asleep, or getting restful sleep. This study aimed to assess the sedative properties of helicide using thiopental sodium-induced sleep mice model. Helicide (5 and 10&#xa0;mg/kg) and diazepam (2&#xa0;mg/kg) were administered to the animals. After 30&#xa0;min, thiopental sodium (20&#xa0;mg/kg) was given (<i>i.p.</i>) to induce sleep, and onset and duration of their sleep were recorded over a 4-h period. Molecular docking was also performed to investigate the potential interactions of helicide with GABA<sub>A</sub> (PDB: 6X3X, containing α1 and β2 subunits) receptors and assess its pharmacokinetics and toxicity. The results demonstrated that helicide significantly (<i>p</i> &gt; 0.05) extended the duration of sleep (174.8 ± 10.47&#xa0;min) and provided fast sleeping onset (9.40 ± 1.71&#xa0;min) compared to control. The combination of helicide and diazepam elevated sedation duration (191.40 ± 3.86&#xa0;min) and lowered onset (5.20 ± 0.58&#xa0;min), indicating a synergistic effect. Helicide exerted binding affinity of − 7.7&#xa0;kcal/mol, while diazepam had a slightly higher affinity of − 8.7&#xa0;kcal/mol with 6X3X. Helicide also displayed favorable pharmacokinetics and drug-likeness. Overall, Helicide exhibited a moderate sedative effect in the mice model, likely through its interaction with the GABAergic system.</p> Graphical Abstract <p></p>

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Modulatory Sedative Activity of Helicide on Diazepam in Thiopental Sodium Mediated Sleeping Mice: An In Vivo Approach With Molecular Docking

  • 期刊论文

  • 发表日期：

    2025年3月18日

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  • Mst Muslima Khatun,
  • Md Shimul Bhuia,
  • Mizanur Rahaman,
  • Hossam Kamli,
  • Siddique Akber Ansari,
  • Muhammad Torequl Islam

摘要

Insomnia is a common sleep disorder characterized by difficulties in falling asleep, staying asleep, or getting restful sleep. This study aimed to assess the sedative properties of helicide using thiopental sodium-induced sleep mice model. Helicide (5 and 10 mg/kg) and diazepam (2 mg/kg) were administered to the animals. After 30 min, thiopental sodium (20 mg/kg) was given (i.p.) to induce sleep, and onset and duration of their sleep were recorded over a 4-h period. Molecular docking was also performed to investigate the potential interactions of helicide with GABAA (PDB: 6X3X, containing α1 and β2 subunits) receptors and assess its pharmacokinetics and toxicity. The results demonstrated that helicide significantly (p > 0.05) extended the duration of sleep (174.8 ± 10.47 min) and provided fast sleeping onset (9.40 ± 1.71 min) compared to control. The combination of helicide and diazepam elevated sedation duration (191.40 ± 3.86 min) and lowered onset (5.20 ± 0.58 min), indicating a synergistic effect. Helicide exerted binding affinity of − 7.7 kcal/mol, while diazepam had a slightly higher affinity of − 8.7 kcal/mol with 6X3X. Helicide also displayed favorable pharmacokinetics and drug-likeness. Overall, Helicide exhibited a moderate sedative effect in the mice model, likely through its interaction with the GABAergic system.

Graphical Abstract