Chopade Atul R, Somade Prakash M, Somade Pratik P, Mali Suraj N
Department of Pharmacology, Rajarambapu College of Pharmacy, Kasegaon, Sangli, Maharashtra, 415404, India.
Dept. of Physiology, Krishna Institute of Medical Sciences, Karad, Maharashtra, India.
Nat Prod Bioprospect. 2021 Apr;11(2):223-233. doi: 10.1007/s13659-020-00284-8. Epub 2020 Nov 11.
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 GABA-A 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.
焦虑是一种令人不适的状态,会严重降低生活质量,常伴有紧张行为和反复思考。尼兰辛是从多种叶下珠属植物中分离出的一种木脂素。关于尼兰辛的文献综述突出了其广泛的治疗潜力。在本研究中,基于我们之前的调查,我们评估了纯净、分离并表征的尼兰辛作为一种抗焦虑剂的效果。尼兰辛[6-[(2R,3R)-3-[(3,4-二甲氧基苯基)甲基]-4-甲氧基-2-(甲氧基甲基)丁基]-4-甲氧基-1,3-苯并二氧杂环戊烯]购自商业来源,并使用包括高架十字迷宫模型/试验(EPM)和明暗探索试验(L&D)等常用动物模型进一步评估其抗焦虑潜力。在EPM任务前,通过用GABA-A受体拮抗剂氟马西尼预处理小鼠来评估GABA-A受体介导作用。由Vlife QSAR软件进行的分子对接模拟研究(pdb编号:4COF)表明,与标准药物地西泮(对接分数:-63.1568 kcal/mol)相比,尼兰辛(对接分数:-62.1714 kcal/mol)显示出相对最佳的对接分数。总之,尼兰辛在焦虑症管理方面可能具有潜力。我们的计算机模拟和体内分析(间接)表明GABA介导作用在抗焦虑活性中可能发挥的作用。尽管这些研究是初步的,但未来需要进行更深入的实验探索,以便在不久的将来将尼兰辛用作抗焦虑药物。