Desarrollo inicial de un fitofármaco derivado del jugo de Citrus limón (limón) para el tratamiento de crisis hipertensivas

Objetivo: Obtener un fitofármaco a base de extracto seco de limón con estándares de calidad, procesamiento amigable con el medio ambiente y con antecedentes de efectividad y seguridad, evaluando sus efectos en pacientes hipertensos con frecuentes crisis hipertensivas. Métodos y resultados: Se seleccionó la población de limónes de las Regiones Metropolitana y Coquimbo con las concentraciones más altas de ácido ascórbico y flavonoides totales, respectivamente. Se utilizó liofilización para obtener jugo de limón en polvo. Sólo durante el período de estudio, se informó un caso de aumento/ crisis hipertensiva. La formulación con la concentración más alta de ácido ascórbico disminuyó la presión arterial sistólica y diastólica en 16 mmHg desde 10 minutos hasta 60 minutos. Por otro lado, la formulación con mayor concentración de flavonoides disminuyó la presión arterial en 12 a 30 mmHg desde 5 a 60 minutos. Conclusión: Se obtuvo un producto innovador como complemento al manejo de los aumentos de presión arterial. Los principios activos con mayor contribución al mecanismo antihipertensivo del jugo de limón corresponden a compuestos fenólicos, específicamente, flavonoides.

Aim: To obtain a product based on a dry extract of standardized phytodrug lemon with high quality standards, using an environmentally friendly process; to evaluate its effects in hypertensive patients suffering frequent episodes of hypertensive crisis. Methods and Results: Lemons with high concentration of ascorbic acid (Coquimbo Region) or total flavonoids (Metropolitan Region) were selected. Lyophilization was used to obtain juice powder. During the study period only one case of hypertensive crisis was reported. The formula with the highest concentration of ascorbic acid decreased systolic and diastolic blood pressure by 16 mmHg from 10 minutes up to 60 minutes. On the other hand, the formula with the highest concentration of flavonoids decreased blood pressure from 12 to 30 mmHg between 5 and 60 minutes. Conclusion: An novel product to help decrease acutely elevated blood pressure was obtained that can be used as a complement to the management of acute blood pressure rises. The active principles with greater contribution to the antihypertensive mechanism of lemon juice corresponded to phenolic compounds, specifically flavonoids.

Improvement of endothelial function by Gunnera tinctoria extract with antioxidant properties

BACKGROUND: Gunnera tinctoria has been collected by Mapuche-Pewenche people for food and medicinal purposes. The high polyphenol content of methanolic extract from G. tinctoria leaves with chemical constituents such as ellagic acid and quercetin derivatives suggests its application to prevent endothelial dysfunction and oxidative stress. The aim of this study was to provide evidence of the protective effect of this extract on endothelial function by reducing oxidative stress induced by high D-glucose and H2O2, as well as by stimulating nitric oxide (NO) levels in human umbilical vein endothelial cells (HUVECs). RESULTS: A methanolic extract with a high content of polyphenols (520 ± 30 mg gallic acid equivalents/g dry extract) was obtained from G. tinctoria leaves. Its main constituent was ellagic acid. The results of Ferric reducing antioxidant power and 2,2-diphenyl-1-picrylhydrazyl radical scavenging assays of the extract confirmed its antioxidant activity by inhibition pathway of radical species. The incubation of HUVECs with the extract decreased the apoptosis and reactive oxygen species (ROS) synthesis induced by high extracellular concentration of D-glucose or hydrogen peroxide. The extract increased endothelial NO levels and reduced vasoconstriction in human placental vessels. CONCLUSIONS: This study provides evidence about the antioxidant and endothelial protective properties of methanolic G. tinctoria leaf extract. The extract improves the availability of NO in HUVECs, inhibiting the production of ROS and vasoconstriction.

Propolis polyphenolic compounds affect the viability and structure of Helicobacter pylori in vitro

ABSTRACT To evaluate the anti-Helicobacter pylori activity of the major polyphenol compounds of propolis and their cellular damage, both as single molecule or in combination. Honey bees propolis were fractionated by using CPC and preparative HPLC. Four major polyphenols (chrysin, pinocembrin, galangin and caffeic acid phenethyl ester) were identified by thin layer chromatography-mass spectroscopy and liquid chromatography-mass spectroscopy. These compounds inhibited both ATCC and clinical H. pylori strains, with caffeic acid phenethyl ester being the most active. The four compounds presented minimum inhibitory concentration in the range 256-1024 µg ml−1 and a fractional inhibitory concentration of 64-512 µg ml−1. In mixtures all compounds showed an indifference effect (FIC < 0.15) but chrysin + galangin which was synergistic (FIC = 2.0). Killing curves show a similar behavior as the antibiotic amoxycillin. On the other hand, analyses by transmission electron microscopy at sub inhibitory concentration show vesicle formation and cell lysis after exposition to both individual polyphenol compounds and in mixture. The major compounds of propolis show anti-H. pylori activity both as individual compounds and in mixture. When combined they present mainly indifference but exert a lytic activity upon H. pylori, suggesting a potential bactericidal activity of propolis.

Characterization of Lactobacillus fermentum UCO-979C, a probiotic strain with a potent anti-Helicobacter pylori activity

Background: Helicobacter pylori is considered as the main risk factor in the development of gastric cancer. In the present study, we performed a detailed characterization of the probiotic properties and the anti-H. pylori activity of a previously isolated lactobacillus strain ­ Lactobacillus fermentum UCO-979C ­ obtained from human gut. Results: The strain tolerated pH 3.0; grew in the presence of 2% bile salts; produced lactic acid and hydrogen peroxide; aggregated in saline solution; showed high hydrophobicity; showed high adherence to glass; Caco-2 and gastric adenocarcinoma human cells (AGS) cells; showed an efficient colonization in Mongolian Gerbils; and potently inhibited the growth and urease activity of H. pylori strains. L. fermentum UCO-979C significantly inhibited H. pylori-induced IL-8 production in AGS cells and reduced the viability of H. pylori. With regard to innocuousness, the strain UCO-979C was susceptible to several antibiotics and did not produce histamine or beta-haemolysis in blood agar containing red blood cells from various origins. Conclusion: The results demonstrated that L. fermentum UCO-979C is a very good candidate as a probiotic for the protection of humans against H. pylori infections.

Efecto pediculicida de una formulación en base a Eucaliptus globulus L / Pediculicide effect of a Eucaliptus globulus L formulation

Introduction: Pediculosis capitis is a public health problem with a high prevalence. The emergence of parasite resistance to conventional pediculicide is of great concern worldwide. Objective: To develop alternatives pediculicide, effective and safe, based on the essential oil of Eucaliptus globulus. Method: Through bioassays active concentrations ranges of the essential oil were established, and proceeded to develop a standardized, stable, pharmaceutical form, evaluating its effects on our population. Results: The results showed 100% effectiveness; short time of death, ovicidal action, activity on the adhesion of the egg, and low toxicity. Discussion: In addition to great effect, the inability of the parasite to become resistant to the chemical composition of the essential oil makes this formulation an alternative to the problem of head lice solution.

Introducción: La pediculosis capitis es un problema de salud pública con una alta prevalencia. La aparición de resistencia del parásito a los pediculicidas convencionales es de gran preocupación a nivel mundial. Objetivo: Desarrollar alternativas pediculicidas, efectivas y seguras, en base al aceite esencial de Eucaliptus globulus. Método: A través de bioensayos se establecieron rangos de concentraciones activas del aceite esencial, y se procedió al desarrollo de una forma farmacéutica, estandarizada, estable, evaluando sus efectos en nuestra población. Resultados: Los resultados mostraron 100% de efectividad; corto tiempo de muerte, acción ovicida, actividad sobre la adherencia del huevo, y baja toxicidad. Discusión: Además de la gran efectividad, la imposibilidad del parásito de adquirir resistencia a la composición química del aceite esencial hace de esta formulación una solución alternativa al problema de la pediculosis.

Variation in phenolic compounds of Ugni molinae populations and their potential use as antioxidant supplement

In the present work we carried out a comparative study of total phenolic contents and antioxidant capacity of aqueous leaf extracts of Ugni molinae Turcz., Myrtaceae (infusion and Soxhlet extracted) prepared from continent and Juan Fernández Island samples. The results revealed that total phenol content (TPC), tannins (TTC) and flavonoids (TFC) for U. molinae extracts (infusion and Soxhlet extracts) from island leaves were 38.5, 56.7 and 37.5% higher than those obtained with leaves from the continent, respectively. Also, HPLC profiles showed important differences between U. molinae populations. In vitro antioxidant capacity (scavenging of DPPH radical) for 1% infusion and aqueous extract (Soxhlet method) of U. molinae from island samples, was 15% greater than from continent samples. Further, in vivo impact of U. molinae intake (1% infusion) was studied in plasma samples obtained from healthy volunteers. Participants that consumed tea prepared with leaves from island population showed higher TBARS reduction and plasma antioxidant capacity (TEAC-CUPRAC) than those who consumed tea prepared with leaves from continental population. The conditions of the territory in which U. molinae populations growth could explain the differences in their composition and activity. According to results, island U. molinae populations could be an important source of study for the development of an antioxidant supplement, and thereby contribute to the use of this species that has becoming an ecological problem in the island.

Los polifenoles antioxidantes extraídos del epicarpio de Palta (Persea americana var. Hass) inhiben la ureasa de Helicobacter pylori / Antioxidant polyphenols extracted from Avocado epicarp (Persea americana var. Hass) inhibit Helicobacter pylori urease

Chronic infection by Helicobacter pylori produce chronic gastritis leading to other more severe pathologies as peptic ulcer and gastric adenocarcinoma. New anti-H. pylori agents has been found in natural products, particularly polyphenols. The inhibition of enzymes such us urease appears to be an interesting strategy by which polyphenols could limit the colonization by H. pylori. From the exocarp of Persea americana (avocado fruit), we obtain a procyanidin-rich extract with a 77 percent of gallic acid equivalents (GAE). Such procyanidins derived from epicatechin. with a mean degree of polymerization DPm = 6.10. The antioxidant capacity was assessed by different methods as TEAC-DPPH, TEAC-CUPRAC, TEAC-FRAP, TEAC-crocin. The extract shown inhibitory activity against H. pylori urease with an IC50 = 1.02 ug GAE/mL. In order to obtain clusters of procyanidins with different molecular weights, avocado peel extract was fractioned. A clear relation between the molecular size of procyanidins and their urease inhibitory activity was observed.

La infección crónica por Helicobacter pylori produce gastritis crónica o patologías más severas como la úlcera péptica y adenocarcinoma gástrico. Nuevos agentes anti-H. pylori se han encontrado en los productos naturales, donde destacan los polifenoles. La inhibición de enzimas como la ureasa, resulta ser una estrategia interesante mediante la cual los polifenoles pueden limitar la colonización por H. pylori. A partir del epicarpio del fruto de Persea americana (palto) se obtuvo un extracto polifenólico (77 por ciento de EAG), rico en procianidinas derivadas de epicatequina, con un grado de polimerización DPm = 6.10. La capacidad antioxidante fue evaluada mediante TEAC-DPPH, TEAC-CUPRAC, TEAC-FRAP, TEAC-crocina. El extracto mostró una actividad inhibitoria de la ureasa de H. pylori con un IC50 = 1.02 ug EAG/mL. El fraccionamiento de las procianidinas permitió agruparlas según su peso molecular, observándose una clara relación entre su tamaño y la capacidad de inhibir la ureasa.

Propagación y descripción morfo-anatómica de salvia chilena (Lepechinia chamaedryoides) / Propagation and morpho-anatomical description of Chilean salvia (Lepechinia chamaedryoides)

The aim of this work was to identify an effective method to improve the rate and percentage of germination and the rooting of seeds and cuttings of Lepechinia chamaedryoides (Balb.) Epling. Morphological changes experienced by the seed during the germination process also were followed by microscopy. This research was conducted during 2009 and 2010 in the Faculty of Agronomy of the University of Concepción. Four germination tests were assayed: a) sulfuric acid scarification and further stratification, b) leaching of inhibitors with different water temperatures plus different concentrations of gibberellic acid, c) thermal scarification plus stratification and d) gibberellic acid application at different concentrations. The highest percentage of germination was obtained with thermal scarification and stratification. Vegetative propagation test consisted of different concentrations of indole butyric acid (IBA) applied to the stem base. Significant differences between treatments were not found. The morphological changes of the seed during the germination process were observed by scanning electron microscope (SEM). These findings allowed identifying characteristics of highly lignified pericarp.

Con el propósito de identificar un método efectivo para obtener un alto porcentaje de germinación y enraizamiento en semillas y estacas de Lepechinia chamaedryoides (Balb.) Epling y observar los cambios morfológicos que experimenta la semilla durante el proceso de germinación, se realizó esta investigación durante el año 2009 y 2010 en la Facultad de Agronomía de la Universidad de Concepción. Se efectuaron cuatro ensayos de germinación: a) escarificación con ácido sulfúrico y estratificación, b) lixiviación de inhibidores con agua a diferentes temperaturas más concentraciones de ácido giberélico, c) escarificación térmica más estratificación y d) aplicación de ácido giberélico, en diferentes concentraciones. El mayor porcentaje de germinación se obtuvo con el tratamiento de escarificación térmica y estratificación. Con respecto a la propagación vegetativa, se realizaron ensayos con diferentes concentraciones de ácido indolbutírico (IBA) aplicado a la base de las estacas, no observándose diferencias significativas entre tratamientos. Los cambios morfológicos de la semilla durante el proceso de germinación se observaron mediante Microscopio Electrónico de Barrido (MEB) lo que permitió identificar características anatómicas y estructurales de un pericarpio altamente lignificado.