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.
2. GopumadhavanS, RafiqM, VenkatarangannaMV, MitraSK. Antihistaminic and antianaphylactic activity of HK-07, a herbal formulation. Indian J Pharmacol2005;37:300–3.10.4103/0253-7613.16853Search in Google Scholar
3. AgnihotriS, WakodeS, AgnihotriA. An overview on anti-inflammatory properties and chemo-profile of plants used in traditional medicine. Indian J Nat Prod Resour2009;2:150–67.Search in Google Scholar
4. MaheshwariU. Molecular docking of human histamine H1 receptor with chlorpheniramine to alleviate cat allergies. J Bioinform Seq Anal2011;3:6–10.Search in Google Scholar
5. ThurmondRL, GelfandEW, DunfordPJ. The role of histamine H1 and H4 receptors in allergic inflammation: the search for new antihistamines. Nat Rev Drug Discov2008;7:41–53.10.1038/nrd2465Search in Google Scholar
6. DharaAK, SubaV, SenT, PalS, ChaudhuriAK. Preliminary studies on the anti-inflammatory and analgesic activity of the methanolic fraction of the root extract of Tragia involucrata Linn. J Ethnopharmacol2000;72:265–8.10.1016/S0378-8741(00)00166-5Search in Google Scholar
7. ShanmugamS, RajendranK, SureshK. Traditional uses of medicinal plants among the rural people in Sivagangai district of Tamil Nadu, Southern India. Asian Pac J Trop Biomed2012;2:S429–34.10.1016/S2221-1691(12)60201-9Search in Google Scholar
8. RahmatullahM, HasanME, IslamMA, IslamMT, JahanFI, SerajS, et al. A survey on medicinal plants used by the folk medicinal practitioners in three villages of Panchagarh and Thakurgaon District, Bangladesh. AM Eurasian J Sustain Agric2010;4:291–301.Search in Google Scholar
10. FengL, JiH, GuH, WangD, CuiJ, LiuR, et al. An efficient method for extraction, separation and purification of naphthoquinone pigments from Lithospermum erythrorhizon Sieb. Chromatographia2009;70:1197–200.10.1365/s10337-009-1283-9Search in Google Scholar
11. ShamsaF, AhmadianiA, KhosrokhavarR. Antihistaminic and anticholinergic activity of barberry fruit (Berberis vulgaris) in the guinea-pig ileum. J. Ethnopharmacol1999;64:161–6.10.1016/S0378-8741(98)00122-6Search in Google Scholar
13. ParmarNS, PrakashS. Screening methods in pharmacology, 1st ed. Bodakdev, India: Alpha Science Intl Ltd, 2006.Search in Google Scholar
14. ShimamuraT, ShiroishiM, WeyandS, TsujimotoH, WinterG, KatritchV, et al. Structure of the human histamine H1 receptor complex with doxepin. Nature2011;475:65–70.10.1038/nature10236Search in Google Scholar PubMed PubMed Central
17. WangL, WangT, YangB, ChenYH. Design, synthesis, and anti-allergic activities of novel (R)(-)-1-[(4-chlorophenyl)phenyl methyl] piperazine derivatives. Med Chem Res2012;21:124–32.10.1007/s00044-010-9512-1Search in Google Scholar
19. NayampalliSS, DesaiNK, AinapureSS. Anti-allergic properties of Tinospora cardifolia in animal models. Indian J Pharm1986;18:250–2.Search in Google Scholar
20. BarnesPJ, ChungKF, PageCP. Inflammatory mediators of asthma; an update. Pharmacol Rev1998;50:515–96.Search in Google Scholar
21. RaffertyP, JacksonL, SmithR, HolgateST. Terfenadine, a potent histamine H1-receptor antagonist in the treatment of grass pollen sensitive asthma. Br J Clin Pharmacol1990;30:229–35.10.1111/j.1365-2125.1990.tb03769.xSearch in Google Scholar
22. RussellT, StoltzM, PharmacokineticsWS. Pharmacodynamics, and tolerance of single- and multiple-dose fexofenadine hydrochloride in healthy male volunteers. Clin Pharmacol Ther1998;64:612–21.10.1016/S0009-9236(98)90052-2Search in Google Scholar
23. DockhornRJ, BergnerA, ConnellJT, FalliersCJ, GrabiecSV, WeilerJM, et al. Safety and efficacy of loratadine (Sch-29851): a new non-sedating antihistamine in seasonal allergic rhinitis. Ann Allergy1987;58:407–11.Search in Google Scholar
24. MitaH, ShidaT. Comparison of anti-allergic activities of the histamine H1 receptor antagonists epinastine, ketotifen and oxatomide in human leukocytes. Arzneimittelforschung1995;45:36–40.Search in Google Scholar
25. SalataJJ, JurkiewiczNK, WallaceAA, StupienskiRF, GuinossoPJ, LynchJJ. Cardiac electrophysiological actions of the histamine H1-receptor antagonists astemizole and compared with chlorpheniramine and pyrilamine. Circ Res1995;76:110–19.10.1161/01.RES.76.1.110Search in Google Scholar PubMed
26. YanniJM, StephensDJ, ParnellDW, SpellmanJM. Preclinical efficacy of emedastine, a potent, selective histamine H1 antagonist for topical ocular use. J Ocul Pharmacol1994;10:665–75.10.1089/jop.1994.10.665Search in Google Scholar PubMed
©2015 by De Gruyter