Vasorelaxant effect of the Lippia alba essential oil and its major constituent, citral, on the contractility of isolated rat aorta.

The Lippia alba (Mill.) N.E. Brown (Verbenaceae) species popularly known as lemon balm has sedative, analgesic and spasmolytic properties. This study aimed to evaluate the vasorelaxant effect of the L. alba essential oil (EOLa) and its major constituent, citral, rat on aorta. Isometric muscle contraction were induced by potassium (K 60 mM) or phenylephrine (PHE, 0.1 µM) in isolated aortic rings. EOLa and citral promoted a smooth muscle relaxant action, which was potentiated by the presence of the endothelium; PHE-induced contractions (0.1 µM) in aorta with endothelium, had EC50 values of 352.73 ± 19.39 µg/mL and 99.34 ± 7.2 µg/mL for EOLa and citral, respectively. In the presence of a nitric oxide synthase inhibitor, L-NAME, the EC50 values were 654.19 ± 10.46 µg/mL and 601.66 ± 10.922 µg/mL for EOLa and citral, respectively. EOLa and citral dose-dependently relaxed contractions induced by BAY-K 8644, a calcium channel agonist, and by Phorbol 12,13-dibutyrate an activator of protein kinase C. EOLa and citral produced a vasorelaxant effect in isolated aorta which was potentiated by the presence of endothelium. In summary, EOLa and citral, probably using several mechanisms of action, relaxed aortic smooth muscle with maximal pharmacologic efficacy.

Essential oil of Lippia alba and its main constituent citral block the excitability of rat sciatic nerves.

Lippia alba is empirically used for infusions, teas, macerates, and hydroalcoholic extracts because of its antispasmodic, analgesic, sedative, and anxiolytic effects. Citral is a mixture of trans-geranial and cis-neral and is the main constituent of L. alba essential oil and possesses analgesic, anxiolytic, anticonvulsant, and sedative effects. The present study evaluated the effects of the essential oil of L. alba (EOLa) and citral on compound action potentials (CAPs) in Wistar rat sciatic nerves. Both drugs inhibited CAP in a concentration-dependent manner. The calculated half-maximal inhibitory concentrations (IC50) of peak-to-peak amplitude were 53.2 µg/mL and 35.00 µg/mL (or 230 µM) for EOLa and citral, respectively. Peak-to-peak amplitude of the CAP was significantly reduced by 30 µg/mL EOLa and 10 µg/mL citral. EOLa and citral (at 60 and 30 µg/mL, values close to their respective IC50 for CAP blockade) significantly increased chronaxy and rheobase. The conduction velocity of the first and second CAP components was statistically reduced to ∼86% of control with 10 µg/mL EOLa and ∼90% of control with 3 µg/mL citral. This study showed that EOLa inhibited nerve excitability and this effect can be explained by the presence of citral in its composition. Both EOLa and citral showed inhibitory actions at lower concentrations compared with other essential oils and constituents with local anesthetic activity. In conclusion, these data demonstrate that EOLa and citral are promising agents in the development of new drugs with local anesthetic activity.

Antimicrobial activity and chemical composition of fixed oil extracted from the body fat of the snake Spilotes pullatus.

CONTEXT: Ethnozoological studies have shown that Spilotes pullatus Linn. (Colubridae: Ophidia), is associated with medicinal and magic-religious uses in Brazil. OBJECTIVES: This study was designed to determine the chemical composition of the oil extracted from the body fat of S. pullatus and to test its antimicrobial properties, alone and in association with aminoglycosides, against fungi and bacterial strains in concentrations ranging between 1024 and 0.5 µg/mL. MATERIAL AND METHODS: The snakes were collected in the Chapada do Araripe, county of Crato, Ceará State, Brazil. The oil was extracted in a Soxhlet apparatus using hexane. The methyl esters of the fatty acids present in the samples were identified using GC-MS. The antimicrobial and drug modulatory activities of oil were tested by microdilution against fungal and bacterial strains. RESULTS: The chemical composition of the fixed oils of S. pullatus identified 10 constituents representing 94.97% of the total sample. The percentages of saturated and unsaturated fatty acids were 33.59 and 61.38%, respectively, with the most abundant components being elaidic (37.26%). The oil did not demonstrate any antimicrobial or antifungal activity when tested alone, presenting MIC values ≥ 1024 µg/mL. However, when associated with antibiotics, it demonstrated synergistic effects with gentamicin against all the bacterial lineages assayed, and antagonistic effects with amikacin and neomycin against strains of Escherichia coli. CONCLUSIONS: Oil extracted from the body fat of S. pullatus did not demonstrate any inhibitory effects on bacterial or fungal activities, but was effective in modulating the effects of certain antibiotics.

Chemical composition, toxicological aspects and antifungal activity of essential oil from Lippia sidoides Cham.

OBJECTIVES: The aims of this study were to test the essential oil from Lippia sidoides Cham. for antifungal activity, in vitro, against Candida spp. and Microsporum canis, to evaluate its acute and subchronic toxicological effects, in vivo, and to determine its chemical constituents. METHODS: The antifungal activity, in vitro, was initially evaluated by the agar-well diffusion technique, and the MIC and minimum fungicidal concentration (MFC) were determined by the broth microdilution method. The acute and subchronic toxicological effects were determined in mice and rats, respectively. The chemical composition of the essential oil was determined by gas chromatography coupled to mass spectroscopy. RESULTS: The essential oil obtained from L. sidoides was effective against all tested strains by the agar-well diffusion method. The MICs of L. sidoides essential oil for strains of M. canis ranged from 4 to 70 mg/L and the MFCs ranged from 9 to 150 mg/L. The MICs for strains of Candida spp. ranged from 620 to 2500 mg/L and the MFCs ranged from 1250 to 5000 mg/L. The main constituents of L. sidoides essential oil were thymol (59.65%), E-caryophyllene (10.60%) and p-cymene (9.08%). The acute administration of the essential oil up to 3 g/kg by the oral route to mice was devoid of overt toxicity. The 30 day oral administration of L. sidoides oil (117.95 mg/kg/day) to rats did not induce any significant histopathological, haematological or serum biochemical alterations. CONCLUSIONS: The essential oil from L. sidoides may be a promising source in the search for new antifungal drugs due to its efficacy and low toxicity.