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The crude drug ysypó hû (Adenocalymma marginatum DC., Bignoniaceae) is used traditionally by the Guarani of Eastern Paraguayan as a male sexual enhancer. The aim of the present study was to identify the main constituents of the crude drug and to evaluate the in vitro inhibitory activity towards the enzyme phosphodiesterase-5 (PDE-5). The main compounds were isolated by counter-current chromatography (CCC). The metabolites were identified by spectroscopic and spectrometric means. The chemical profiling of the extracts was assessed by high-performance liquid chromatography coupled to mass spectrometry (HPLC-MS/MS). The crude extract and main isolated compounds were tested for their PDE-5 inhibitory activity using commercial kits. The iridoid theviridoside and 4-hydroxy-1-methylproline were isolated as the main constituent of the crude drug. Four chlortheviridoside hexoside derivatives were detected for the first time as natural products. Chemical profiling by HPLC-MS/MS led to the tentative identification of nine iridoids, six phenolics, and five amino acids. The crude extracts and main compounds were inactive towards PDE-5 at concentrations up to 500 µg/mL. Iridoids and amino acid derivatives were the main compounds occurring in the Paraguayan crude drug. The potential of ysypó hû as a male sexual enhancer cannot be discarded, since other mechanisms may be involved.

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ETHNOPHARMACOLOGICAL RELEVANCE: Fabiana imbricata (Solanaceae) is a Patagonian medicinal plant with a long tradition of use. The aim of this review is to provide an integrative overview of the traditional uses, chemistry, bioactivity and chemical profiling of the crude drug. MATERIALS AND METHODS: The information was collected from scientific databases searching with the keywords Fabiana imbricata, Fabiana species, Fabiana (Solanaceae) and includes local literature and books. RESULTS: The indications of use reported in literature show little variation from the data published as early as 1889. The chemical studies showed a rich diversity in metabolites including phenolics, coumarins, flavonoids, phenylpropanoids, terpenes, alkaloids and sugars. Bioactivity studies supported the traditional use as diuretic and also the potential of the crude drug as a gastroprotective agent. The plant can be used as a source of compounds with effect on gastric ulcers and shows enzyme inhibitory activity. While the germination rate of the plant is very low, protocols were developed for the rapid in vitro propagation of the species. The toxicity of the crude drug extracts was low and did not show clastogenic effect in human lymphocytes. Further research is needed to disclose the potential of the F. imbricata sesquiterpenes on other relevant biological targets.

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Introducción: las hojas de Justicia secunda Vahl. son ampliamente utilizadas en las poblaciones rurales de la costa ecuatoriana. Los pobladores la utilizan con fines medicinales sin que se hayan comprobado las propiedades que se le atribuye. El presente estudio se realizó con los extractos hidroalcohólico, alcohólico y etéreo de las hojas. Objetivos: caracterizar la droga cruda y varios extractos de J. secunda para determinar la presencia de metabolitos o principios activos con potencial medicinal y de esta manera analizar la posible utilidad en la elaboración de productos farmacéuticos. Métodos: se analizaron parámetros físico-químicos de la droga cruda, las hojas se recolectaron en la noche, se secaron hasta peso constante en una estufa a 30 °C ± 1 °C por 5 días y posteriormente se trituraron con un mortero, se pesaron y se obtuvieron los extractos por maceración con diversos solventes orgánicos; como etanol al 90 por ciento, éter dietílico y una solución hidroalcohólica al 50 por ciento v/v como menstruos. En el análisis fitoquímico se utilizaron técnicas cualitativas para la determinación de los principales metabolitos presentes en los extractos así como técnicas gravimétricas para determinación de cenizas totales, sólidos totales y porciento de humedad. Resultados: se constató que el contenido de cenizas totales y la humedad residual halladas en la droga cruda se encuentra dentro de los límites establecidos en la USP 37 para artículos de origen botánico. Además, se comprobó la presencia de alcaloides, cumarinas y glucósidos fenólicos en el extracto hidroalcohólico; taninos, glucósidos fenólicos y triterpenos y/o esteroides en el extracto alcohólico y alcaloides y triterpenos y/o esteroides en el extracto etéreo. Conclusión: la gran variedad de componentes químicos presentes en las hojas de J. secunda, le confieren un alto potencial para su uso medicinal como antiséptico, antiinflamatorio, antioxidante, entre otros(AU)

Introduction: Justicia secunda Vahl. leaves are widely used by rural populations from the Ecuadorian coast for medicinal purposes, but the properties attributed to it have not been verified. A study was conducted of hydroalcoholic, alcoholic and etheric leaf extracts. Objectives: Characterize the crude drug and several extracts of J. secunda to determine the presence of metabolites or active principles with medicinal potential, and analyze their possible usefulness to produce pharmaceutical products. Methods: An analysis was conducted of the physicochemical parameters of the crude drug. The leaves were collected at night and dried to constant weight in a stove at 30 °C ± 1 °C for 5 days. They were then crushed in a mortar and weighed. The extracts were obtained by maceration in various organic solvents, such as 90 percent ethanol, diethyl ether and a 50 percent v/v hydroalcoholic solution. For phytochemical analysis, qualitative techniques were applied to determine the main metabolites present in the extracts. Gravimetric techniques were used for determination of total ashes, total solids and percentage of humidity. Results: It was found that content of total ashes and residual humidity in the crude drug are within the limits established by USP 37 for items of botanical origin. Additionally, alkaloids, coumarins and phenolic glucosides were found to be present in the hydroalcoholic extract; tannins, phenolic glucosides and triterpenes and/or steroids in the alcoholic extract; and alkaloids and triterpenes and/or steroids in the etheric extract. Conclusion: The great variety of chemical components present in the leaves of J. secunda grants them high potential for medicinal use as antiseptic, antiinflammatory and antioxidant, among others(AU)

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