Antispasmodic effects and composition of the essential oils from two South American chemotypes of Lippia alba

Aug 20, 2013Journal of ethnopharmacology

Muscle-relaxing effects and makeup of essential oils from two South American types of Lippia alba

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Abstract

Essential oils from Lippia alba chemotypes exhibit differing potencies, with citral essential oil (CEO) showing five times more potency than linalool essential oil (LEO) in inhibiting intestinal contractions.

CEO and LEO both caused a non-competitive inhibition of acetylcholine-induced contractions in isolated rat intestine.
The IC50 for CEO was 7.0±0.3 mg CEO/mL, while for LEO it was 37.2±4.2 mg LEO/mL.
Both essential oils non-competitively inhibited calcium-induced contractions, with IC50 values of 6.3±1.7 mg CEO/mL and 7.0±2.5 mg LEO/mL.
The potency of both CEO and LEO was about 28 times lower than that of verapamil, a known calcium channel blocker.
CEO was found to stimulate nitric oxide production partially, indicating potential differences in their effects on intestinal function.

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ETHOPHARMACOLOGY RELEVANCE: Lippia alba (Mill.) N. E. Brown (Verbenaceae) is an aromatic species used in Central and South America as eupeptic for indigestion. In Argentina, it is used by the "criollos" from the Chaco province. There are several chemotypes which differ in the chemical composition of the essential oils. Nowadays, it is experimentally cultivated in some countries of the region, including Argentina.

AIM OF THE STUDY: To compare the chemical composition and pharmacology of the essential oils from two chemotypes: "citral" (CEO) and "linalool" (LEO), in isolated rat duodenum and ileum.

METHODS: Contractile concentration-response curves (CRC) of acetylcholine (ACh) and calcium in 40mM K(+)-medium (Ca(2+)-CRC) were done in isolated intestine portions, in the absence and presence of CEO or LEO at different concentrations.

RESULTS: Likewise verapamil, CEO and LEO induced a non-competitive inhibition of the ACh-CRC, with IC50 of 7.0±0.3mg CEO/mL and 37.2±4.2mg LEO/mL. l-NAME, a NO-synthase blocker, increased the IC50 of CEO to 26.1±8.7mg CEO/mL. Likewise verapamil, CEO and LEO non-competitively inhibited the Ca(2+)-CRC, with IC50 of 6.3±1.7mg CEO/mL, 7.0±2.5mg LEO/mL and 0.24±0.04mg verapamil/mL (pIC50: 6.28). CEO was proved to possess limonene, neral, geranial and (-)-carvone as the major components, while LEO was rich in linalool.

CONCLUSIONS: Results suggest that CEO has five times more potency than LEO to inhibit muscarinic contractions. The essential oils of both chemotypes interfered with the Ca(2+)-influx, but with an IC50 about 28 times higher than that of verapamil. Moreover, CEO partially stimulated the NO production. These results show the medicinal usefulness of both Lippia alba chemotypes, thus validating its traditional use, potency and mechanism of action.

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Antispasmodic effects and composition of the essential oils from two South American chemotypes of Lippia alba

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