Evaluation of phytoconstituents of hygrophila auriculata as sedatives and hypnotics: in-vivo and in silico studies

Authors

  • Nidhi Hareshkumar Jadav Department of Pharmacy, L.J. Institute of Pharmacy, L J University, Ahmedabad, Gujarat 382210, India, Department of Pharmaceutical Chemistry. Arihant School of Pharmacy & Bio-Research Institute, Swarrnim Startup & Innovation University, Bhoyan Rathod, Gandhinagar, Gujarat-382422, India
  • Jignesh Suresh Shah Department of Pharmacy, L.J. Institute of Pharmacy, L J University, Ahmedabad, Gujarat 382210, India
  • Dipa Kavi Israni Department of Pharmacy, L.J. Institute of Pharmacy, L J University, Ahmedabad, Gujarat 382210, India

DOI:

https://doi.org/10.1590/s2175-97902025e24582

Keywords:

Hygrophila auriculata, Sedative-hypnotic, In-vivo study, Molecular docking, Diazepam, Gas chromatography-mass spectrometry

Abstract

The study explores the potential of Hygrophila auriculata, also known as “Ikshugandha” in Ayurvedic literature, to alleviate insomnia by extracting phytoconstituents and investigating its in-vivo sedativehypnotic activity. GC-MS analysis of seed and leaf extracts revealed the presence of phytoconstituents like β-stigmasterol, lupeol, and gamma-sitosterol. The receptor alpha1-beta2-gamma2 subtype in combination with GABA and diazepam was selected for the docking investigation. The highest docking scores were -9.46 Kcal/mol for stigmasterol and -9.40 Kcal/mol for lupeol. The in-vivo sedative-hypnotic activity was assessed using the Hole cross test, Hole board test, open field test, and the thiopental-induced sleeping duration test. The oral administration of ethyl acetate subextract and unsaponifiable fraction resulted in a significant reduction in the number of holes traversed and dips and a similar reaction for the open field test. In the thiopental-induced sleeping test, the hydroalcoholic extract, ethyl acetate subextract, and unsaponifiable fraction were observed to improve sleep time compared to the control group. The substance was considered safe up to 400 mg/kg for leaf extract and 200 mg for seed extract. These findings suggest the plant is a promising candidate for future pharmacological studies.

Downloads

Download data is not yet available.

References

Ahmed S, Rahman A, Mathur M, Athar M, Sultana S. Anti tumor promoting activity of Asteracantha longifolia against experimental hepatocarcinogenesis in rats. Food Chem Toxicol. 2001;39:19-28.

Biovia DS Biovia Discovery Studio Visualizer, v16. 1.0. 15350, San Diego: Dassault Systemes; 2015 [Computer Program].

Chauhan NS, Dixit VK. Asteracantha longifolia (L.) Nees, Acanthaceae: chemistry, traditional, medicinal uses and its pharmacological activities - a review. Rev Braz Farmacogn. 2010;20(5):812-817.

Colovos C, Yeates TO. Verification of protein structures: Patterns of nonbonded atomic interactions. Protein Science 1993;2:1511-9.

Dallakyan S, Olson AJ. Small-Molecule Library Screening by Docking with PyRx. Methods. Mol Biol. 2015;1263:243-50.

Neubauer MD, Flaherty MS. Chronic insomnia. Semin Neurol. 2009;29(4):340-343.

Ganeshpurkar A, Singh R, Gore PG, Kumar D, Gutti G, Kumar A. Structure-based screening and molecular dynamics simulation studies for the identification of potential acetylcholinesterase inhibitors. Mol Simul. 2019;46:169-85.

Gupta BD, Dandiya PC, Gupta ML. A psychopharmacological analysis of behaviour in rats. Jpn J Pharmacol. 1971;21(3):293-298.

Islam MS, Parvin MS, Islam ME. The protective and antioxidant effects of Hygrophila schulli seeds on oxidative damage of DNA and RBC cellular membrane. Heliyon. 2022;8(1):e08767.

Katariya V, Gajera V, Shah LD, Joshi H. Evaluation of anxiolytic activity of Hygrophila auriculata seeds on experimental animals. Int J Pharm Biol. 2021;11(2):01-12.

Kim JJ, Gharpure A, Teng J, Zhuang Y, Howard RJ, Zhu S. Human GABAA receptor alpha1-beta2-gamma2 subtype in complex with GABA plus diazepam Nature. 2020;585:303-308.

Kuru P. Tamarindus indica and its health-related effects. Asian Pac J Trop Biomed. 2014;4(9):676-681.

Laskowski RA, MacArthur MW, Moss DS, Thornton JM. PROCHECK: a program to check the stereochemical quality of protein structures. J Appl Crystallogr. 1993;26:283-91.

Mohanty SP, Rautaray KT. Pharmacognostic review of Astercantha longifolia (L.) Nees, & its possible use in prevention of COVID-19. J Ayurveda Holist Med. 2020;6(4):231-236.

Moniruzzaman M, Rahman A, Ferdous A. Evaluation of sedative and hypnotic activity of ethanolic extract of Scoparia dulcis Linn. Evid Based Complement Alternat Med. 2015; 2015:873954.

Morris GM. Software News and Updates AutoDock4 and AutoDockTools4: Automated Docking with Selective Receptor Flexibility. J Comput Chem. 2009;30:2785-2791 [Computer program].

Neharkar V, Gautam G, Pandhare R. Cardioprotective potential of Hygrophila auriculata (l.) leaves methanolic extract and its sub-fraction against doxorubicin induced cardiotoxicity in rats. World J Pharm Pharm Sci. 2016;5:1574-1590.

Ozturk Y, Aydine S, Baser KHC, Berberoglu H. Effects of Hypericum perforatum L. And Hypericum calycinum L. extracts on the central nervous system in mice. Phytomedicine. 1996;3(2):139–146.

Panara K, Nishteswar K, Nariya MK. Sedative and hypnotic activity of the leaves of bijapura (Citrus Medica L.) Indian J Nat Prod Resour. 2021;12(4):605-609.

Patra A, Jha S, Murthy PN, Sharone MA. Isolation and characterization of stigmast-5-en-3β-ol (β-sitosterol) from the leaves of Hygrophila spinosa T. Anders. Int J Pharm Sci Res. 2010;1(2):95-100.

Patra A, Jha S, Murthy PN, Vaibhav AD, Chattopadhyay P, Panigrahi G et al. Anti-inflammatory and antipyretic activities of hygrophila spinosa t. anders leaves (acanthaceae). Trop J Pharm. Res. 2009;8(2):133-137.

Patra A, Jha S, Murthy PN, Phytochemical and Pharmacological Potential of Hygrophila spinosa T. anders. Phcog Rev. 2009;3(6):330-341.

Pattanayak SP, Sunita P. Antitumor potency and toxicology of an indian ayurvedic plant, Hygrophila spinosa. Pharmacology online. 2008;2(1):361-371.

Prut L, Belzung C. The open field as a paradigm to measure the effects of drugs on anxiety-like behaviors: a review. Eur J Pharmacol. 2003;463(1-3):3-33.

Ralte L, Khiangte L, Thangjam NM, Kumar A, Singh YT. GC-MS and molecular docking analyses of phytochemicals from the underutilized plant, Parkia timoriana revealed candidate anti-cancerous and anti-inflammatory agents. Sci Rep. 2022;12(1):3395.

Roth T. Prevalence, associated risks, and treatment patterns of insomnia. J Clin Psychiatry. 2005;66 Suppl 9:10-43.

Saeed N, Khan MR, Shabbir M. Antioxidant activity, total phenolic and total flavonoid contents of whole plant extracts Torilis leptophylla L. BMC Complement Altern Med. 2012;12:1-2.

Saha S, Paul S. Potential of Hygrophila auriculata (schumach.) heine as a source of future anti-cancer drugs: a comprehensive review. J Pharmacogn Phytochem. 2017;6(4):1725-1740.

Sahu D, Rathor LS, Dwivedi SD, Shah K, Chauhan NS, Singh MR, Singh D. A review on molecular docking as an interpretative tool for molecular targets in disease management. Assay Drug Dev Techn. 2024;22(1):40-50.

Salve SD, Bhuktar AS. Pharmacognosy and phytochemical evaluation of Hygrophila auriculata (Schumach.) Heine. Root. J Phytopharmacol. 2017;6(4):210-216.

Sarvananda L, Premarathna AD. Ethnopharmacolological potential and medicinal uses of Hygrophila auriculata, J Ayurveda Holist Med. 2018;4(4):185-188.

Silva GO, Abeysundara AT, Aponso MM. Extraction methods, qualitative and quantitative techniques for screening of phytochemicals from plants. Am J Essent Oil Nat Prod. 2017;5(2):29-32.

Satpathy S, Patra A, Ahirwar B. Development and validation of a novel high-performance thin-layer chromatography method for the simultaneous determination of apigenin and luteolin in Hygrophila spinosa T. Anders. J planar chromat. 2018;31(6):437–43.

Satpathy S, Patra A, Hussain MD, Ahirwar B. Amelioration of postmenopausal osteoporosis and anticancer properties of an antioxidant enriched fraction from Hygrophila spinosa T. Anders. S Afr J Bot. 2018;117:247–55.

Sivam SP, Nabeshima T, Ho IK. Acute and chronic effects of pentobarbital in relation to postsynaptic GABA receptors: a study with muscimol. Neurosci Res. 1982;7(1):37-47.

Steinbach JH, Akk G. Modulation of GABAA receptor channel gating by pentobarbital. J Physiol. 2001;537(3):715-733.

Takagi K, Watanabe M, Saito H. Studies of the spontaneous movement of animals by the hole cross test; effect of 2-dimethyl-aminoethanol and its acyl esters on the central nervous system. Jpn J Pharmacol. 1971;21(6):797-810.

Takeda H, Tsuji M, Matsumiya T. Changes in head-dipping behavior in the hole-board test reflect the anxiogenic and/or anxiolytic state in mice. Eur J Pharmacol. 1998; 350(1):21-29.

Tejashri S, Hasabe AR, Dhole A. Potential herbal plant-Asteracantha longifolia. Int J Res Sci Innov Appl Sci. 2018;3(3):7-8.

Thamer FT, Thamer N. Gas chromatography – mass spectrometry (gc-ms) profiling reveals newly described bioactive compounds in citrullus colocynthis (l.) seeds oil extracts. Helyion. 2023;9(6):e16861.

Tiwari S, Kartikay P. Unrevealing the complex interplay: molecular docking: a comprehensive review on current scenario, upcoming difficulties, forthcoming initiatives, and viewpoints. Int J Chem Res. 2024;8(1):1-9.

Turner RA. Screening Methods in Pharmacology 1st. New York, USA, Academic Press. 1965;158.

Viola H, Wasowski C, Stein LD, Wolfman C, Silveira R, Dajas F, Paladini AC. Apigenin, a component of Matricaria recutita flowers, is a central benzodiazepine receptors-ligand with anxiolytic effects. Planta Med. 1995;61(03):213-216.

Vyas N, Gamit K, Raval M. Aphrodisiac and spermatogenic potential of unsaponifiable fraction from seeds of Hygrophila spinosa t. Ander in rats. Int J Pharm Sci Res. 2020;11(10):4902-9.

Downloads

Published

2025-11-10

Data Availability Statement

Not informed.

Issue

Section

Article

How to Cite

Evaluation of phytoconstituents of hygrophila auriculata as sedatives and hypnotics: in-vivo and in silico studies. (2025). Brazilian Journal of Pharmaceutical Sciences, 61, e24582. https://doi.org/10.1590/s2175-97902025e24582