Antihistamine from Tragia involucrata L. leaves.

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.