ORIGINAL ARTICLES |
|
|
|
|
|
Identification of Anxiolytic Potential of Niranthin: In-vivo and Computational Investigations |
Atul R. Chopade1, Prakash M. Somade2, Pratik P. Somade2, Suraj N. Mali3 |
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 |
|
|
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.
|
Keywords
Pharmacology
Phytoconstituents
Niranthin
Lignan
Anxiolytic activity
EPM models
|
Corresponding Authors:
Atul R. Chopade, Prakash M. Somade
E-mail: atulrchopade@gmail.com;saishaprakash@gmail.com
|
Issue Date: 07 April 2021
|
|
|
1. S. Kasper, Wien. Med. Wochenschr. 165, 217-228 (2015) 2. A.V. Dwyer, D.L. Whitten, J.A. Hawrelak, Altern Med Rev. 16, 40-49 (2011) 3. V. Gupta, R. Sharma, P. Bansal, G. Kaur, Ayu. 39, 21 (2018) 4. O. Gureje, M. Von Korff, G. Simon, R. Gater, JAMA 280, 147-151 (1998) 5. A.S. Raakhee, N. Aparna, Educ Sci Psychol. 1, 33-37 (2011) 6. S. Sahoo, CR. Khess, C.R., J Nerv Ment Dis. 198, 901-904 (2010) 7. DK. Moser, Am J Crit Care. 16:361-369 (2007) 8. G.P. Rauniar, S. Deo, S.K. Bhattacharya, Kathmandu Univ Med J. 5, 188-194 (2007) 9. RG. Lister, Pharmacol Ther. 46, 321-340 (1990) 10. B.S. Thippeswamy, B. Mishra, VP. Veerapur, G. Gupta, G., Indian J Pharmacol. 43, 50 (2011) 11. R.K. Romana, A. Sharma, V. Gupta, R. Kaur, S. Kumar, P. Bansal, J Relig Health. 59, 1-17 (2017) 12. B. Bandelow, J. Zohar, E. Hollander, S. Kasper, H.J. Möller, World J Psychiatr. 9, 248-312 (2008) 13. G. van der Watt, J. Laugharne, A. Janca, Curr. Opin. Psychiatry. 21, 37-42 (2008) 14. C.W. Fennell, K.L. Lindsey, L. McGaw, S.G. Sparg, G. Stafford, E. Elgorashi, O.M. Grace, J. Van Staden, J Ethnopharmacol. 94, 205-217 (2004) 15. W.D. MacRae, G.N. Towers, Phytochemistry 23, 1207-1220 (1984) 16. J.B. Calixto, A.R. Santos, V.C. Filho, R.A. Yunes, Med. Res. Rev. 18, 225-258 (1998) 17. A.R. Chopade, F.J. Sayyad, Phytother Res. 29, 1202-1210 (2015) 18. J.R. Patel, P. Tripathi, V. Sharma, N.S. Chauhan, V.K. Dixit, J Ethnopharmacol. 138, 286-313 (2011) 19. H. Harikrishnan, I. Jantan, M.A. Haque, E. Kumolosasi, Inflammation. 41, 984-995 (2018) 20. S. Chowdhury, T. Mukherjee, R. Mukhopadhyay, B. Mukherjee, S. Sengupta, S. Chattopadhyay, P. Jaisankar, S. Roy, H.K. Majumder, EMBO Mol Med. 4, 1126-1143 (2012) 21. G.G. Conrado, N. Grazzia, S. Adriana da Silva, C.H. Franco, C.B. Moraes, F.R. Gadelha, D.C. Miguel, V.L. Garcia, Planta Med. 86, 782-789 (2020) 22. A.R. Chopade, R.P. Pol, P.A. Patil, V. Dharanguttikar, N. Naikwade, R.J. Dias, S.N. Mali, Comb Chem. High Through Screen. (2020). https://doi.org/10.2174/1386207323666200605150915 23. A.R. Chopade, P.A. Patil, S.N. Mali, Open Pain J. 13, 22-34 (2020). https://doi.org/10.2174/1876386302013010022 24. A.R. Chopade, R.P. Pol, P.A. Patil, V. Dharanguttikar, N. Naikwade, R.J. Dias, S.N. Mali, Curr Enzym Inhib. 16, 1 (2020). https://doi.org/10.2174/1573408016999201026200650 25. S. Pellow, P. Chopin, S.E. File, M. Briley, J Nuerosci methods. 14, 149-167 (1985) 26. R.G. Lister, Psychopharmacol. 92, 180-185 (1987) 27. S.K. Kulkarni, Hand Book of Experimental Pharmacology, 3rd edn. (Vallabh Prakashan, Delhi, 2005), pp. 36-38 28. C.A. Lorenzini, C. Bucherelli, A. Giachetti, Physiol Behav. 36, 97-101 (1986) 29. A.R. Chopade, F.J. Sayyad, Y.V. Pore, Sci Pharm. 83, 243-267 (2015) 30. V.R. Mishra, C.W. Ghanavatkar, S.N. Mali, H.K. Chaudhari, N. Sekar, J. Biomol. Struct. Dyn. 38, 1772-1785 (2020) 31. S.N. Mali, S. Sawant, H.K. Chaudhari, M.C. Mandewale, Curr. Comput. Aided Drug Des. 15, 445-455 (2019) 32. B.R. Thorat, S. Mali, D. Rani, R. Yamgar, Curr. Comput. Aided Drug Des. 16, 1 (2020). https://doi.org/10.2174/1573409916666200302120942 33. B.R. Thorat, S.N. Mali, D. Rani, R. Yamgar, Comb. Chem. High Throughput Screen. 23, 392-401 (2020) 34. P.B. Shelke, S.N. Mali, H.K. Chaudhari, A.P. Pratap, J. Het. Chem. 56, 3048-3054 (2019) 35. S.N. Mali, A.P. Pratap, B. Thorat, EJMO 4, 34-41 (2020) 36. Molsoft, L. L. C. Drug-Likeness and Molecular Property Prediction, https://www.molsoft.com/about.html. Accessed 27 August 2018 37. Protein Database, https://www.rcsb.org/. Accessed 27 August 2019 38. S. Razack, H.K. Kandikattu, M.P. Venuprasad, N. Amruta, F. Khanum, K. Chuttani, A.K. Mishra, Metab Brain Dis. 33, 1533-1549 (2018) 39. D. Kumar, S.K. Gupta, A. Ganeshpurkar, R. Singh, D. Kumar, N. Das, S. Krishnamurthy, S.K. Singh, Pharmacol Biochem Behav. 176, 63-71 (2019) 40. N.Y. Yuan, M.M. Poe, C. Witzigmann, J.M. Cook, D. Stafford, L.A. Arnold, J Pharmacol Toxicol Methods. 82, 109-114 (2016) |
|
Viewed |
|
|
|
Full text
|
|
|
|
|
Abstract
|
|
|
|
|
Cited |
|
|
|
|
|
Shared |
|
|
|
|
|
Discussed |
|
|
|
|