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Licensed Unlicensed Requires Authentication Published by De Gruyter June 4, 2015

Antihistamine from Tragia involucrata L. leaves

  • Sangilimuthu Alagar Yadav EMAIL logo , Sathishkumar Ramalingam , Anitha Jabamalai Raj and Ravi Subban


Background: Synthetic antihistamine drugs cause various adverse effects to overcome these problems with natural phytomedicine or phytoconstituents.

Methods: Tragia involucrata leaves were extracted with soxhlet apparatus and fractionated with column chromatography the homogenized fractions were monitored with thin layer chromatography (TLC) and characterized by using UV-visible, FT-IR, 1H NMR, 13C NMR and MS spectral studies. Isolated compounds were screened their antihistamine activity on ileum preparation, bronchoconstriction and triple response on histamine-induced guinea pig.

Results: Antihistamine 5-hydroxy-1-methylpiperidin-2-one has been isolated and characterized from the leaves of Tragia involucrata L. A promising muscle relaxant, bronchorelaxant and anti-allergic effect of 5-hydroxy-1-methylpiperidin-2-one was observed in histamine-induced guinea pig and found to be 55.54±2.78% protection at the dose level of 12.5 mg/kg in bronchoconstriction effect and 49.05±2.45% protection in triple response. These findings were confirmed by in silico molecular docking also against histamine H1 receptor compared with chlorpheniramine maleate and mepyramine. This shows that the 5-hydroxy-1-methylpiperidine-2-one possess good inhibitory effect on histamine-induced guinea pig. The muscle relaxant, bronchodilating and anti-allergic potency of 5-hydroxy-1-methylpiperidin-2-one has been discussed in context with its probable profile as an anti-asthmatic agent from T. involucrata L. leaves.

Conclusions: We can conclude that isolated 5-hydroxy-1-methylpiperidin-2-one from T. involucrata L. has potent antihistamine agent on histamine-induced guinea pig.


The authors gratefully acknowledge the authorities of Karpagam University for providing necessary facilities to carry out this research work. We also extend our thanks to Co-ordinators of Karpagam University Instrument Facility (KUIF) and SAIF-STIC, CUSAT, Cochin for providing the facility.

Author contributions: All the authors have accepted responsibility for the entire content of this submitted manuscript and approved submission.

Research funding: None declared.

Employment or leadership: None declared.

Honorarium: None declared.

Competing interests: The funding organization(s) played no role in the study design; in the collection, analysis and interpretation of data; in the writing of the report or in the decision to submit the report for publication.


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Received: 2015-3-4
Accepted: 2015-4-29
Published Online: 2015-6-4
Published in Print: 2015-9-1

©2015 by De Gruyter

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