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

Atul R Chopade,Prakash M Somade,Pratik P Somade,Suraj N Mali

doi:10.1007/s13659-020-00284-8

Atul R Chopade, Prakash M Somade + Show 2 more

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https://doi.org/10.1007/s13659-020-00284-8

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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 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

Highlights

Anxiety, which has neurobiological, cognitive, and behavioral aspects, is one of the leading mental disorders of modern world experienced by children and adolescents [1,2,3,4]
The number of entries in open and closed arms of the Elevated plus-maze model/test (EPM) apparatus after drug treatment in Control, Niranthin and Diazepam 2 mg/kg treated animals is presented in the (Fig. 1a)
The number of entries reported in open arm of EPM paradigm for Niranthin was comparable with the number of entries observed for diazepam

Summary

Introduction

Anxiety, which has neurobiological, cognitive, and behavioral aspects, is one of the leading mental disorders of modern world experienced by children and adolescents [1,2,3,4]. It has been noted that in certain conditions, stress and anxiety might find helpful as they will motivate individuals, but when it becomes excessive, it leads disturbances in psychological states of individuals. Like other CNS disorders, is linked with CNS neurotransmitter imbalances. There are four neurotransmitters playing key roles in mood regulations, which are norepinephrine, gamma-aminobutyric acid (GABA), serotonin, and dopamine. GABA, glycine, and serotonin are considered as inhibitory neurotransmitters. Gamma-aminobutyric acid is found to be assisting neurons to recover after impulse transmission and thereby reducing the stress and anxiety. GABA regulates both epinephrine and norepinephrine in order to reduce neuronal excitability during neuronal transmission

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