整合生物学期刊网

应用天然产物 ›› 2021, Vol. 11 ›› Issue (2): 223-233.DOI: 10.1007/s13659-020-00284-8

• ORIGINAL ARTICLES • 上一篇    下一篇

Identification of Anxiolytic Potential of Niranthin: In-vivo and Computational Investigations

Atul R. Chopade1, Prakash M. Somade2, Pratik P. Somade2, Suraj N. Mali3   

  1. 1 Department of Pharmacology, Rajarambapu College of Pharmacy, Kasegaon, Sangli, Maharashtra 415404, India;
    2 Dept. of Physiology, Krishna Institute of Medical Sciences, Karad, Maharashtra, India;
    3 Government College of Pharmacy, Karad, Maharashtra, India
  • 收稿日期:2020-10-10 修回日期:2020-11-02 出版日期:2021-04-24 发布日期:2021-04-07
  • 通讯作者: Atul R. Chopade, Prakash M. Somade

Identification of Anxiolytic Potential of Niranthin: In-vivo and Computational Investigations

Atul R. Chopade1, Prakash M. Somade2, Pratik P. Somade2, Suraj N. Mali3   

  1. 1 Department of Pharmacology, Rajarambapu College of Pharmacy, Kasegaon, Sangli, Maharashtra 415404, India;
    2 Dept. of Physiology, Krishna Institute of Medical Sciences, Karad, Maharashtra, India;
    3 Government College of Pharmacy, Karad, Maharashtra, India
  • Received:2020-10-10 Revised:2020-11-02 Online:2021-04-24 Published:2021-04-07
  • Contact: Atul R. Chopade, Prakash M. Somade

摘要: Anxiety is an unpleasant state, which can critically decrease the quality of life is often accompanied by nervous behaviour and rumination. Niranthin is a lignan isolated from various Phyllanthus sources. The literature survey on niranthin highlights wide ranges of the therapeutic potentials. In a present study, based on our previous investigations, we evaluated pure, isolated and characterized niranthin as an anxiolytic agent. The niranthin[6-[(2R,3R)-3-[(3,4-dimethoxyphenyl)methyl]-4-methoxy-2-(methoxymethyl)butyl]-4-methoxy-1,3-benzodioxole] was purchased from commercial source and further subjected for assessment of its anxiolytic potentials using popular animal models including Elevated plus-maze model/test (EPM) and Light & Dark Exploration test (L&D). GABA-A receptor mediation was evaluated by pretreating the mice with the GABAA receptor antagonist Flumazenil before the EPM task. Molecular docking simulation studies (pdb id:4COF) carried out by Vlife QSAR software showed that niranthin (docking score:-62.1714 kcal/mol) have shown comparatively best docking score compared to the standard drug Diazepam (docking score:-63.1568 kcal/mol). To conclude, Niranthin has probable potential in the management of anxiety disorder. Our in-silico and in-vivo analysis (indirectly) indicated the plausible role of GABA mediation for anxiolytic activity. Although, these studies are preliminary, future in depth experimental explorations will be required to use Niranthin as anti-anxiety drug in near future.

关键词: Pharmacology, Phytoconstituents, Niranthin, Lignan, Anxiolytic activity, EPM models

Abstract: Anxiety is an unpleasant state, which can critically decrease the quality of life is often accompanied by nervous behaviour and rumination. Niranthin is a lignan isolated from various Phyllanthus sources. The literature survey on niranthin highlights wide ranges of the therapeutic potentials. In a present study, based on our previous investigations, we evaluated pure, isolated and characterized niranthin as an anxiolytic agent. The niranthin[6-[(2R,3R)-3-[(3,4-dimethoxyphenyl)methyl]-4-methoxy-2-(methoxymethyl)butyl]-4-methoxy-1,3-benzodioxole] was purchased from commercial source and further subjected for assessment of its anxiolytic potentials using popular animal models including Elevated plus-maze model/test (EPM) and Light & Dark Exploration test (L&D). GABA-A receptor mediation was evaluated by pretreating the mice with the GABAA receptor antagonist Flumazenil before the EPM task. Molecular docking simulation studies (pdb id:4COF) carried out by Vlife QSAR software showed that niranthin (docking score:-62.1714 kcal/mol) have shown comparatively best docking score compared to the standard drug Diazepam (docking score:-63.1568 kcal/mol). To conclude, Niranthin has probable potential in the management of anxiety disorder. Our in-silico and in-vivo analysis (indirectly) indicated the plausible role of GABA mediation for anxiolytic activity. Although, these studies are preliminary, future in depth experimental explorations will be required to use Niranthin as anti-anxiety drug in near future.

Key words: Pharmacology, Phytoconstituents, Niranthin, Lignan, Anxiolytic activity, EPM models