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<p>Physcion (PHY), an anthraquinone derivative, has demonstrated various biological properties, including antioxidant and anti-inflammatory effects. This study aimed to evaluate the sedative activity of PHY in Swiss mice using in vivo and in silico approaches. The thiopental sodium (TS)-induced sleep model, fireplace test, and hole cross test were employed to assess sedation along with molecular docking studies. PHY significantly (<i>p</i> &lt; 0.05) reduced sleep latency (17.29 ± 2.33&#xa0;min) and increased sleep duration (162.85 ± 8.38&#xa0;min) compared to controls at higher doses. It also significantly increased (<i>p</i> &lt; 0.05) jump time and decreased the number of hole crosses. Co-administration of PHY with diazepam (DZP) enhanced sedation, while Co-administration with flumazenil (FLN) attenuated it, suggesting modulation of GABA<sub>A</sub> receptors. In silico molecular docking revealed a strong binding affinity (− 8.1 kcal/mol) of PHY with GABA<sub>A</sub> receptor subunits α1 and β2, comparable to DZP. Pharmacokinetic and toxicity predictions showed favorable profiles, supporting the potential of PHY as a sedative agent. Overall, PHY exhibited significant sedative effects likely mediated through the GABAergic pathway.</p>

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Sedative effects of physcion and its modulatory interaction with diazepam: in vivo and in silico evaluation

  • 期刊论文

  • 发表日期：

    2026年3月9日

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  • Md. Shadin,
  • Md. Shimul Bhuia,
  • Mohammed Alfaifi,
  • Abdullah H. Altemani,
  • Faisal H. Altemani,
  • Faisal Alsenani,
  • Raihan Chowdhury,
  • Muhammad Torequl Islam

摘要

Physcion (PHY), an anthraquinone derivative, has demonstrated various biological properties, including antioxidant and anti-inflammatory effects. This study aimed to evaluate the sedative activity of PHY in Swiss mice using in vivo and in silico approaches. The thiopental sodium (TS)-induced sleep model, fireplace test, and hole cross test were employed to assess sedation along with molecular docking studies. PHY significantly (p < 0.05) reduced sleep latency (17.29 ± 2.33 min) and increased sleep duration (162.85 ± 8.38 min) compared to controls at higher doses. It also significantly increased (p < 0.05) jump time and decreased the number of hole crosses. Co-administration of PHY with diazepam (DZP) enhanced sedation, while Co-administration with flumazenil (FLN) attenuated it, suggesting modulation of GABAA receptors. In silico molecular docking revealed a strong binding affinity (− 8.1 kcal/mol) of PHY with GABAA receptor subunits α1 and β2, comparable to DZP. Pharmacokinetic and toxicity predictions showed favorable profiles, supporting the potential of PHY as a sedative agent. Overall, PHY exhibited significant sedative effects likely mediated through the GABAergic pathway.