Chemical profile and anti-leishmanial activity of three Ecuadorian propolis samples from Quito, Guayaquil and Cotacachi regions.

Three propolis samples were collected from different regions of Ecuador (Quito, Guayaquil and Cotacachi) and their methanolic extracts were prepared. Preliminary information supplied by TLC and NMR data, allowed us to define two main types of propolis: Cotacachi propoli sample (CPS), rich in flavonoids and Quito and Guayaquil samples (QPS and GPS) containing triterpenic alcohols and acetyl triterpenes as the main constituents. Two different approaches based on RP-HPLC preparative procedure and NMR structural determination (CPS) and GC-MS analysis (QPS and GPS) were successfully used for the chemical characterization of their major compounds. All three propolis extracts were able to inhibit Leishmania amazonensis growth but propolis sample rich in flavonoids was the most active (IC50=17.1±1.7µg/mL). In the literature this is the first study on propolis from Ecuador.

Estudio farmacognóstico preliminar de tallo y raíz de la especie Moringa Oleífera lam cosechada en Machala / Preliminary pharmacognostic study of the stem and root of the species Moringa Oleifera lam grown in Machala

Introducción: la composición química de las especies vegetales está sujeta a cambios, dependiendo, entre otros factores, de la localización geográfica. Moringa oleífera Lam., que crece en Machala, Ecuador, puede diferir de especies de otras regiones geográficas. Objetivo: realizar un estudio farmacognóstico preliminar del tallo y raíz (corteza y pulpa) de la planta M. oleífera cultivada en las áreas de la Unidad Académica de Ciencias Agropecuarias, de la Universidad Técnica de Machala. Métodos: se desarrolla el control de la calidad de la droga cruda según la metodología establecida por la Organización Mundial de la Salud, mediante determinación de la humedad residual, el porciento de cenizas y el porciento de sustancias solubles en el tallo y la raíz. Se cuantificaron algunos metales mediante espectrometría de emisión óptica con plasma acoplado inductivamente. El estudio químico preliminar se efectuó a través de ensayos de tamizaje fitoquímico y mediante cromatografía en capa delgada. Resultados: la humedad residual para ambos órganos y los valores de cenizas obtenidos para la raíz se encuentran dentro de los límites establecidos. Las cenizas totales para el tallo resultaron elevadas. La determinación de metales descartó la presencia de metales tóxicos en los órganos...(AU)

Introduction: The chemical composition of plant species is subject to changes which depend, among other factors, on their geographic location. The Moringa oleifera Lam. growing in Machala, Ecuador, may differ from species from other geographic regions. Objective: Conduct a preliminary pharmacognostic study of the stem and root (bark and pulp) of the plant M. oleifera grown in areas from the Agricultural Sciences Academic Unit of the Technical University of Machala. Methods: Quality control was performed of the crude drug following the methodology set up by the World Health Organization to determine residual humidity, percentage of ashes and percentage of soluble substances in the stem and the root. Several metals were quantified by inductively coupled plasma atomic emission spectroscopy. The preliminary chemical study was conducted by phytochemical screening testing and thin layer chromatography. Results: Both the residual humidity for both organs and the ash values obtained for the root are within the limits established. Total ashes for the stem were high. Metal determination discarded the presence of toxic metals in the organs studied. Values for soluble substances awarded a greater extraction capacity to water. Phytochemical screening pointed to the presence of triterpenes and steroids, reducing sugars, alkaloids, flavonoids, amino acids and saponins in root extracts. The stem was found to also contain catechins, mucilages and phenolic compounds, but not flavonoids. Thin layer chromatography pointed to the presence of alkaloids derived from phenyl methylamine. Conclusions: The study made it possible to set up crude drug quality parameters for the study species, make preliminary suggestions about similarities between the chemical composition of the plant analyzed and other plants of different geographic origin, and verify the absence of toxic metals in the organs studied(AU)

Estudio farmacognóstico preliminar de tallo y raíz de la especie Moringa Oleífera lam cosechada en Machala / Preliminary pharmacognostic study of the stem and root of the species Moringa Oleifera lam grown in Machala

Introducción: la composición química de las especies vegetales está sujeta a cambios, dependiendo, entre otros factores, de la localización geográfica. Moringa oleífera Lam., que crece en Machala, Ecuador, puede diferir de especies de otras regiones geográficas. Objetivo: realizar un estudio farmacognóstico preliminar del tallo y raíz (corteza y pulpa) de la planta M. oleífera cultivada en las áreas de la Unidad Académica de Ciencias Agropecuarias, de la Universidad Técnica de Machala. Métodos: se desarrolla el control de la calidad de la droga cruda según la metodología establecida por la Organización Mundial de la Salud, mediante determinación de la humedad residual, el porciento de cenizas y el porciento de sustancias solubles en el tallo y la raíz. Se cuantificaron algunos metales mediante espectrometría de emisión óptica con plasma acoplado inductivamente. El estudio químico preliminar se efectuó a través de ensayos de tamizaje fitoquímico y mediante cromatografía en capa delgada. Resultados: la humedad residual para ambos órganos y los valores de cenizas obtenidos para la raíz se encuentran dentro de los límites establecidos. Las cenizas totales para el tallo resultaron elevadas. La determinación de metales descartó la presencia de metales tóxicos en los órganos estudiados. Los valores de sustancias solubles indicaron mayor poder extractivo para el agua. La evaluación mediante tamizaje fitoquímico sugirió triterpenos y esteroides, azúcares reductores, alcaloides, flavonoides, aminoácidos y saponinas, en los extractos de la raíz. En el tallo se detectaron, además, catequinas, mucílagos y compuestos fenólicos, no así flavonoides. La cromatografía en capa delgada sugirió la existencia de alcaloides derivados de la fenilmetilamina. Conclusiones: el estudio permitió establecer parámetros de calidad de la droga cruda para la especie estudiada; sugerir, en principio, semejanzas en composición química de la planta analizada con otras de orígenes geográficos diferentes, y comprobar la ausencia de metales tóxicos en los órganos estudiados(AU)

Introduction: The chemical composition of plant species is subject to changes which depend, among other factors, on their geographic location. The Moringa oleifera Lam. growing in Machala, Ecuador, may differ from species from other geographic regions. Objective: Conduct a preliminary pharmacognostic study of the stem and root (bark and pulp) of the plant M. oleifera grown in areas from the Agricultural Sciences Academic Unit of the Technical University of Machala. Methods: Quality control was performed of the crude drug following the methodology set up by the World Health Organization to determine residual humidity, percentage of ashes and percentage of soluble substances in the stem and the root. Several metals were quantified by inductively coupled plasma atomic emission spectroscopy. The preliminary chemical study was conducted by phytochemical screening testing and thin layer chromatography. Results: Both the residual humidity for both organs and the ash values obtained for the root are within the limits established. Total ashes for the stem were high. Metal determination discarded the presence of toxic metals in the organs studied. Values for soluble substances awarded a greater extraction capacity to water. Phytochemical screening pointed to the presence of triterpenes and steroids, reducing sugars, alkaloids, flavonoids, amino acids and saponins in root extracts. The stem was found to also contain catechins, mucilages and phenolic compounds, but not flavonoids. Thin layer chromatography pointed to the presence of alkaloids derived from phenyl methylamine. Conclusions: The study made it possible to set up crude drug quality parameters for the study species, make preliminary suggestions about similarities between the chemical composition of the plant analyzed and other plants of different geographic origin, and verify the absence of toxic metals in the organs studied(AU)

Análisis farmacognóstico preliminar de las semillas de Moringa Oleifera Lam cosechadas en Cuba / Preliminary pharmacognitive analysis of Moringa oleifera Lam seeds harvested in Cuba

Introducción: la Moringa oleífera Lam. (moringa) es una especie de reconocido uso tanto para humanos como para animales. Sus semillas constituyen una fuente de aceites fijos con un elevado contenido de ácidos grasos insaturados y en particular de ácido oleico. Este aceite se puede emplear en la industria alimenticia, farmacéutica, cosmética, incluso como biodiesel. Objetivo: desarrollar el análisis farmacognóstico preliminar de las semillas de Moringa oleífera Lam cosechadas en el municipio Jovellanos, provincia de Matanzas, Cuba. Métodos: las semillas de moringa fueron evaluadas según algunos parámetros farmacognósticos como: características organolépticas, descripción micromorfológica, pérdida por desecación y cenizas totales. La extracción de las semillas y la nuez, previo proceso de secado en estufa, se realizó mediante Soxhlet y maceración, utilizando hexano como menstruo. Adicionalmente, se efectuó el análisis químico de los aceites obtenidos por cromatografía gaseosa acoplada a espectrometría de masas (CG-EM). Resultados: los parámetros farmacognósticos evaluados se encuentran dentro de los límites establecidos por las monografías oficiales. La descripción micromorfológica de la droga, mostró la presencia de almidón, cristales de oxalato de calcio y aceites o grasas. El análisis por CG-EM, de los aceites extraídos a partir de la semilla y la nuez, mostró que el ácido oleico, con un porcentaje superior al 50 por ciento, el ácido palmítico, el ácido esteárico y el ácido behénico, son los ácidos grasos mayoritarios. Conclusiones: independientemente del método de extracción utilizado, la composición química cualitativa de los aceites obtenidos es similar. En todos los casos el ácido oleico resulta el de mayor proporción. El resto de los componentes se mantienen en niveles similares en todas las muestras analizadas(AU)

Introduction: Moringa oleifera Lam (moringa) is a species of recognized use for both humans and animals. The seeds are a source of fixed oils with high content of unsaturated fatty acids and especially oleic acid. This oil can be used in food, pharmaceutical and cosmetic products and as well as in biodiesel. Objective: to develop preliminary pharmacognostic analysis using seeds of Moringa oleifera Lam harvested in Jovellanos municipality, Matanzas, Cuba. Methods: moringa seeds were evaluated according to some pharmacognostic parameters: organoleptic, micromorphological description, loss on drying and total ash. The extraction of the seeds and nuts, after oven drying process, was performed by Soxhlet and maceration, using hexane as solvent. Furthermore, the analysis of oils obtained by gas chromatography coupled to mass spectrometry (GC-MS) was performed. Results: pharmacognitive parameters are within the limits set by the official monographs. Micromorphological description of the drug showed grain starch, calcium oxalate crystals and, oils or fats. The GC-MS analysis of the oil obtained from the seed and nut showed that oleic acid (percentage greater than 50 percent), palmitic acid, stearic acid and behenic acid, are the main fatty acids. Conclusions: regardless of the extraction method used, the qualitative chemical composition of oils obtained is similar. In all cases, the oleic acid proves to be the major component. The remaining components are kept at similar levels in all tested samples(AU)

In vitro antimicrobial assessment of Cuban propolis extracts

Propolis is a resinous mixture of different plant exudates collected by honeybees. Currently, propolis is widely used as a food supplement and in folk medicine. We have evaluated 20 Cuban propolis extracts of different chemical types, brown (BCP), red and yellow (YCP), with respect to their in vitro antibacterial, antifungal and antiprotozoal properties. The extracts inhibited the growth of Staphylococcus aureus and Trichophyton rubrum at low µg/mL concentrations, whereas they were not active against Escherichia coli and Candida albicans. The major activity of the extracts was found against the protozoa Leishmania, Trypanosoma and Plasmodium, although cytotoxicity against MRC-5 cells was also observed. The BCP-3, YCP-39 and YCP-60 extracts showed the highest activity against P. falciparum, with 50% of microbial growth (IC50) values of 0.2 µg/mL. A positive correlation between the biological activity and the chemical composition was observed for YCP extracts. The most promising antimicrobial activity corresponds to YCP subtype B, which contains acetyl triterpenes as the main constituents. The present in vitro study highlights the potential of propolis against protozoa, but further research is needed to increase selectivity towards the parasite. The observed chemical composition-activity relationship of propolis can contribute to the identification of the active principles and standardisation of this bee product.

In vitro antimicrobial assessment of Cuban propolis extracts.

Propolis is a resinous mixture of different plant exudates collected by honeybees. Currently, propolis is widely used as a food supplement and in folk medicine. We have evaluated 20 Cuban propolis extracts of different chemical types, brown (BCP), red and yellow (YCP), with respect to their in vitro antibacterial, antifungal and antiprotozoal properties. The extracts inhibited the growth of Staphylococcus aureus and Trichophyton rubrum at low µg/mL concentrations, whereas they were not active against Escherichia coli and Candida albicans. The major activity of the extracts was found against the protozoa Leishmania, Trypanosoma and Plasmodium, although cytotoxicity against MRC-5 cells was also observed. The BCP-3, YCP-39 and YCP-60 extracts showed the highest activity against P. falciparum, with 50% of microbial growth (IC50) values of 0.2 µg/mL. A positive correlation between the biological activity and the chemical composition was observed for YCP extracts. The most promising antimicrobial activity corresponds to YCP subtype B, which contains acetyl triterpenes as the main constituents. The present in vitro study highlights the potential of propolis against protozoa, but further research is needed to increase selectivity towards the parasite. The observed chemical composition-activity relationship of propolis can contribute to the identification of the active principles and standardisation of this bee product.

Activity of Cuban propolis extracts on Leishmania amazonensis and Trichomonas vaginalis.

In this paper we analyzed the antiprotozoal effects of eighteen Cuban propolis extracts (brown, red and yellow type) collected in different geographic areas, using Leishmania amazonensis (as a model of intracellular protozoa) and Trichomonas vaginalis (as a model of extracellular protozoa). All evaluated propolis extracts caused inhibitory effect on intracellular amastigotes of L. amazonensis. However, cytotoxicity on peritoneal macrophages from BALB/c mice was observed. Only five samples decreased the viability of T. vaginalis trophozoites at concentrations lower than 10 microg/mL. No correlation between the type of propolis and antiprotozoal activity was found. Cuban propolis extracts demonstrated activity against both intracellular and extracellular protozoa model, as well as the potentialities of propolis as a natural source to obtain new antiprotozoal agents.

Cuban and Brazilian red propolis: botanical origin and comparative analysis by high-performance liquid chromatography-photodiode array detection/electrospray ionization tandem mass spectrometry.

Chemical composition of propolis depends on the specificity of the local flora at the site of collection and thus on the geographic and climatic characteristics of this place. This paper describes a comparative analysis of Cuban red propolis (CRP), Brazilian red propolis (BRP), and Dalbergia ecastophyllum exudates (DEE) by high-performance liquid chromatography with diode-array detection and tandem mass spectrometry. The aim of this study was to investigate the overall chemical profile and the botanical origin of red propolis and to suggest similarities and differences between samples collected in different tropical regions. Isoliquiritigenin (1), liquiritigenin and naringenin (2 and 17), isoflavones (3-4 and 16), isoflavans (5-7 and 18), and pterocarpans (8-13) were detected in CRP, BRP, and DEE, whereas polyisoprenylated benzophenones (PPBs) guttiferone E/xanthochymol (14a,b) and oblongifolin A (15) were detected only in BRP. Pigments responsible for the red color of DEE and red propolis were also identified as two C30 isoflavans, the new retusapurpurin B (19) and retusapurpurin A (20). PPBs and pigments were isolated and unambiguously characterized by 1D and 2D NMR analysis. These results show that red propolis samples from different tropical zones have a similar chemical composition. DEE is the main red propolis source, but the presence of PPBs in BRP suggests the contribution of different botanical sources for Brazilian samples. This chemical information is important for quality control of red propolis and its commercial products and for biological study.

Diseño tecnológico de tabletas de Desipramina de liberación controlada / Technological design of controlled-release desipramine tablets

Se realizó un estudio preliminar con la finalidad de obtener tabletas de clorhidrato de desipramina (75 mg) de liberación controlada de lo cual no existen antecedentes de elaboración en la literatura universal. Se diseñaron 5 variantes tecnológicas de formulación, y se obtuvieron resultados muy alentadores al emplear como agentes retardantes dextrana técnica cubana e hidroxipropilmetilcelulosa (HPMC) en la masa y aglutinarla con una solución clorofórmica de alcohol cetílico, con lo cual se obtienen tabletas con excelentes propiedades físico--mecánicas y tecnológicas, y una satisfactoria cinética de disolución con un t100 porciento de aproximadamente 14 h de ensayo in vitro