Antibacterial Activity and Reversal of Multidrug Resistance of Tumor Cells by Essential Oils from Fresh Leaves, Flowers, and Stems of Montanoa quadrangularis Schultz Bipontinus (Asteraceae) Collected in Mérida-Venezuela.

Essential oils obtained by hydrodistillation of Montanoa quadrangularis leaves, flowers, and stems were analyzed by GC and GC/MS techniques revealing myrcene, limonene, ß-phellandrene, and sabinene among the main components. The aim of the present study was to evaluate the MDR modulator activity on human MDR1 gene transfected mouse lymphoma cell line and the antimicrobial activity on the essential oils obtained from different parts of the species under investigation. The results revealed that MQL caused a similar increase in the fluorescence activity of the cells at 0.02 µL/mL comparing to the Verapamil® value. The antimicrobial assay was carried out according to the disc diffusion method. Five different bacterial strains (Staphylococcus epidermidis, Bacillus subtilis, Pseudomonas aeruginosa, Escherichia coli AG 100, and Escherichia coli AG100A) were treated with the essential oils and the zones of inhibition were determined on TSA plates and TSA agar plates supplemented with Tween 20. MQF and MQL showed activity against B. subtilis, S. epidermidis, and E. coli AG 100A while MQS was only active against E. coli AG 100A on TSA agar plates experiment. In case of TSA agar plates supplemented with 0.1 v/v% Tween 20 detergent, MQF showed inhibition on B. subtilis, S. epidermidis, and E. coli AG 100A; MQL was active against B. subtilis, E. coli AG 100, and E. coli AG 100A while MQS was only active against E. coli AG 100A.

Oxytocin neuron activation by acute infusion of Montanoa genus plants in the Wistar rats / Activación de neuronas de oxitocina por la infusión aguda de plantas del género de Montanoa en la rata Wistar

In tradition al Mexican medicine, plants from the Montanoa genus, family Asteraceae ( Montanoa tomentosa , Montanoa grandiflora , and Montanoa frutescens ) have been used to induce labor owing to their uterotonic properties like those produced by oxytocin (OXT). However, w hether infusions of these plants can activate hypothalamic OXT - producing neurons is unknown. To test this possibility, five independent groups of Wistar rats (n=4) were included: intact, vehicle, and three groups that received 50 mg/kg p.o. of M. tomentosa , M. grandiflora , and M. frutescens infusions, respectively. Ninety min after treatment, the brains were obtained and processed using double - labeled immunohistochemistry for Fos protein and oxytocin (Fos/OXT - ir). Rats that received Montanoa infusions had s ignificantly greater number of Fos/OXT - ir cells in the paraventricular (PVN) and supraoptic (SON) nuclei, with respect to intact and vehicle groups. These findings demonstrate that Montanoa infusions activated OXT neurons, an effect that may be related to the reported pharmacological properties.

En la medicina tradicional mexicana, plantas del género Montanoa , familia Asteraceae ( Montanoa tomentosa , Montanoa grandiflora y Montanoa frutescens ), se han utilizado para inducir el parto debido a sus propiedades uterotónicas, aparentemente similares a las producidas por la hormona oxitocina (OXT). Sin embargo, se desconoce si las infusiones de estas plantas pueden activar neuronas hipotalámicas productoras de OXT. Para probar esta posibilidad, se incluyeron cinco grupos independientes (n=4): intacto, vehículo y tres grupos que recibieron 50 mg/kg p.o. de infusiones de M. tomentosa , M. grandiflora , y M. frute scens , respectivamente. Noventa minutos después del tratamiento, los cerebros fueron obtenidos y procesados por doble marcaje de inmunohistoquímica para la proteína Fos y oxitocina (Fos/OXT - ir). Las ratas que recibieron infusiones de Montanoa aumentaron si gnificativamente el número de células Fos/OXT - ir en los núcleos paraventricular (PVN) y supraóptico (SON), respecto a los grupos intacto y vehículo. Estos hallazgos demuestran que las infusiones de Montanoa activan neuronas de OXT, lo que podría estar rela cionado con sus propiedades farmacológicas

Pro-ejaculatory effect of the aqueous crude extract of cihuapatli (Montanoa tomentosa) in spinal male rats.

In the present study, the pro-sexual effect of the cihuapatli (Montanoa tomentosa) and its possible pro-ejaculatory properties in spinal male rats were examined. Systemic administration of the aqueous crude extracts of Montanoa tomentosa exerted a pro-ejaculatory effect and produced an increase in the number of discharges in the ejaculatory motor patterns in the spinal rats. The cihuapatli-induced ejaculatory responses included the expression of penile erections and penile movements and the potent expulsion of urethral contents and in some cases the expulsion of seminal plugs. The cihuapatli-induced ejaculatory motor patterns were similar to that obtained after systemic oxytocin. Cihuapatli- and oxytocin-induced ejaculatory motor responses and the penile erections and movements were abolished by the pre-treatment with hexamethonium, a selective oxytocin antagonist. Present data show that the cihuapatli extract acts directly at the spinal system in charge of the expression of the ejaculatory motor patterns and suggest that the aqueous crude extract exerts its aphrodisiacs properties by increasing sexual potency acting as an oxytocic agent.

GABAA/benzodiazepine receptor complex mediates the anxiolytic-like effect of Montanoa tomentosa.

ETHNOPHARMACOLOGICAL RELEVANCE: Montanoa tomentosa also named Cihuapatli is a native plant of Mexico that has been used in traditional medicine for the last five centuries mainly as a remedy for reproductive impairments. However, there are reports indicating that this plant was also consumed by Mexican ancient people for its relaxing properties. In order to corroborate this information, the present study was conducted to evaluate the effect of Montanoa tomentosa lyophilisate (MT) on rat׳s anxiety-like behavior and to analyze its mechanism of action. MATERIALS AND METHODS: The anxiolytic-like action of MT (1.5, 3.0, 6.0 and 12.0 mg/kg) was investigated in male Wistar rats tested in three animal models of anxiety: the burying behavior, the elevated plus maze and the hole-board tests. As a positive control, the anti-anxiety effects of different doses of the selective GABAA receptor agonist muscimol were also analyzed. In order to evaluate the participation of the GABAA and oxytocin receptors in the anxiolytic-like actions of MT, the GABAA receptors blockers picrotoxin (0.25 and 0.50 mg/kg), bicuculline (2.0 mg/kg) and flumazenil (5.00 and 10.0 mg/kg), the neurosteroid inhibitor finasteride (50.0 and 100 mg/kg) and the oxytocin receptor antagonist atosiban (0.25 µg) were used. Finally, to evaluate general activity, and motor coordination, the open field and rota-rod tests were used. RESULTS: MT at 3.0 mg/kg showed anxiolytic-like effects in the three anxiety paradigms without affecting reactivity, general motor activity or motor coordination; however, at higher doses sedative effects were observed. Picrotoxin (0.25 and 0.50 mg/kg), flumazenil (10.0 mg/kg) and finasteride (100 mg/kg) antagonized the anxiolytic-like actions of MT in the burying behavior test. In the plus maze and hole-board tests bicuculline (2.0 mg/kg) blocked the effects of the plant as well. Atosiban (0.25 µg) did not antagonize the anxiolytic-like actions of MT. CONCLUSIONS: The results corroborate the anxiolytic-like actions of Montanoa tomentosa and suggest that this effect is mediated through GABAA receptors but not oxytocin receptors.

Increase of the ejaculatory potency by the systemic administration of aqueous crude extracts of cihuapatli (Montanoa genus) plants in spinal male rats.

In the present study, evidence on the aphrodisiac activity of Montanoa frutescens and Montanoa grandiflora and a comparison with the aphrodisiac activity of Montanoa tomentosa is presented. By using the fictive ejaculation model in spinal male rats, electromyographic recordings of the genital motor pattern of ejaculation were obtained in the bulbospongiosus muscles and analyzed after the intravenous injection of aqueous crude extracts of Montanoa tomentosa, Montanoa frutescens, and Montanoa grandiflora. Results showed that the systemic administration of the aqueous crude extracts of Montanoa plants elicits a significant increase in the ejaculatory capacity of spinal male rats with very robust ejaculatory motor patterns that included the expression of tonic penile erections and penile movements and the potent expulsion of urethral contents. In conclusion, Montanoa frutescens and Montanoa grandiflora increase the ejaculatory potency with aphrodisiac activity similar to Montanoa tomentosa.

Montanoa frutescens and Montanoa grandiflora extracts reduce anxiety-like behavior during the metestrus-diestrus phase of the ovarian cycle in Wistar rats.

In previous studies, the anxiolytic-like effects of Montanoa tomentosa and Montanoa frutescens were reported in male rats, but the potential anxiolytic-like effects of Montanoa plants during the different phases of the ovarian cycle in rats remain to be explored. The anxiolytic-like effects of the aqueous crude extracts of M. frutescens (25 and 50 mg/kg) and M. grandiflora (25 and 50 mg/kg) in the elevated plus maze were investigated in Wistar rats during the estrous cycle and compared with 2 mg/kg diazepam as a reference anxiolytic drug. To investigate any motor effect (i.e., hyperactivity, no changes, or hypoactivity) associated with the treatments, the rats were evaluated in the open field test. The M. frutescens (25 and 50 mg/kg) and M. grandiflora (50 mg/kg) extracts exerted anxiolytic-like effects during the metestrus-diestrus phase, similar to diazepam, without disrupting spontaneous motor activity. No significant effects of the extracts were detected in either behavioral test during the proestrus-estrus phase, whereas diazepam produced motor hypoactivity in the open field test. These results indicate that the M. frutescens and M. grandiflora extracts possess anxiolytic-like effects that depend on the ovarian cycle phase, supporting the Mexican ancient medicinal use of these plants to ameliorate anxiety disorders.

Anti-fertility and other biological activities of zoapatle (Montanoa spp. )with biotechnological application / Anti-fertilidad y otras actividades biológicas del zoapatle (Montanoa spp. ) con aplicación biotecnológica

Species from the Montanoa genus have been used for hundreds of years in Mexican traditional medicine. The Náhuatl name given by Aztecs to this plant was “cihuapahtli”, meaning “woman’s medicine” (cihua, woman; pahtli, medicine), because M. tomentosa has been used to treat female health disorders since pre-Hispanic times due to its uterotonic properties. Later on, the Spanish pronunciation transformed the word into “zoapatle”, the name still used by herb sellers in México. Despite its use in folk medicine, intensive scientific research on this plant did not begin until the early 1970’s. The only two available reviews exclusively focused on the Montanoa species cover the period from 1529 to 1985. However, in the last two decades, important phytochemical, biochemical and biotechnological advances were achieved. This is a review of the history, botany, most relevant chemistry, biological activity and biotechnology of the secondary metabolites from the Montanoa genus so far.

Especies del género Montanoa han sido empleadas por siglos en la medicina tradicional Mexicana. El nombre asignado a esta planta por los Aztecas fue “cihuapahtli”, ó “medicina para la mujer” (cihua, mujer; pahtli, medicina). Específicamente, M. tomentosa es usada para tratar desordenes de la mujer desde tiempos prehispánicos por sus propiedades uterotónicas. La castellanización transformó esta palabra en “zoapatle”, este nombre sigue siendo usado por los curanderos en México. A pesar de su uso en la medicina folklórica, la investigación científica intensa en esta planta comenzó desde inicios de 1970. Las únicas dos revisiones disponibles y dedicadas exclusivamente a las especies de Montanoa cubren el periodo de 1529 a 1985. Sin embargo, en las últimas dos décadas, se han logrado importantes avances fitoquímicos, bioquímicos y biotecnológicos. Este trabajo presenta una revisión de la historia, botánica, química más relevante, actividades biológicas y biotecnología de los metabolitos secundarios del género Montanoa a la fecha.

Montanoa tomentosa glandular trichomes containing kaurenoic acids chemical profile and distribution.

Montanoa tomentosa has been used in traditional medicine in Mexico to treat diverse female health disorders; it is particularly useful in inducing childbirth. Microscopic analysis of leaf surfaces of M. tomentosa revealed the presence of glandular trichomes. The chemical profile and distribution of glandular trichomes from different developmental stages of M. tomentosa leaves were investigated. Two diterpenic acids, kaurenoic and grandiflorenic were detected in glandular trichomes through the glandular microsampling technique and GC/MS analysis. In the glandular trichomes of the leaves also up to twenty-six volatile terpenes were identified, where beta-eudesmol and valencene were the most abundant terpenes.

Sesquiterpene lactones from Montanoa hibiscifolia that inhibit the transcription factor NF-kappa B.

The reinvestigation of the aerial parts of Montanoa hibiscifolia afforded four new eudesmanolides (1-4), three of them with a rare endoperoxide structural element and the fourth with a rare carbonyl function. It also afforded three unusual montabibisciolides (5-7), two (5 and 7) of which are new natural compounds. Additionally, seven germacrolides (8-10 and 12-15) and one melampolide (11) could be isolated, including two new germacrolides (8 and 9). Their structures were elucidated using 1D and 2D NMR measurement as well as ESI, CIMS, and HRMS analyses. Low-energy conformations were obtained by molecular mechanics calculations. The (13)C NMR data of five compounds are reported for the first time. Six sesquiterpene lactones (4, 6, 10, 11, 12, and 14) were investigated for their inhibitory activity on DNA binding of the transcription factor NF-kappa B using Jurkat T cells as well as RAW 264.7 cells. Besides the alpha-methylene-gamma-butyrolactone moiety the epoxy group in the acyl residue might take part in the NF-kappa B inhibitory activity of sesquiterpene lactones.