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Identification of Anxiolytic Potential of Niranthin: In-vivo and Computational Investigations
Natural Products and Bioprospecting Pub Date : 2020-11-11 , DOI: 10.1007/s13659-020-00284-8
Atul R. Chopade , Prakash M. Somade , Pratik P. Somade , Suraj N. Mali

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.

Graphic Abstract



中文翻译:

烟碱抗焦虑潜力的鉴定:体内和计算研究。

焦虑是一种令人不快的状态,可能严重降低生活质量,通常伴随着神经行为和反省。Niranthin是从各个分离的木酚素余甘来源。关于烟碱的文献调查强调了广泛的治疗潜力。在当前的研究中,基于我们以前的研究,我们评估了纯的,分离的和表征的烟碱为抗焦虑剂。烟碱[6-[(2 R,3 R)-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-苯并二恶唑]购自商业来源,并进一步对其抗焦虑性进行评估使用流行的动物模型(包括高架迷宫模型/测试(EPM)和光暗探索测试(L&D))的潜力。通过在EPM任务之前用GABA-A受体拮抗剂氟马西尼预处理小鼠来评估GABA-A受体的介导作用。Vlife QSAR进行的分子对接模拟研究(pdb id:4COF)软件显示,与标准药物地西p(对接分数:− 63.1568 kcal / mol)相比,尼古丁(对接分数:− 62.1714 kcal / mol)显示出相对最佳的对接分数。总之,尼兰丁在焦虑症的治疗中具有潜在的潜力。我们的计算机分析和体内分析(间接)表明,GABA介导的抗焦虑活性似乎是合理的。尽管这些研究是初步的,但仍需要在将来进行深入的实验探索,以便在不久的将来使用尼兰丁作为抗焦虑药。

图形摘要

更新日期:2020-11-12
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