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The methanolic extracts of Pterocaulon alopecuroides and Pterocaulon angustifolium were assayed for antibacterial activity and biofilm formation inhibition of four community-acquired-MRSA isolates representative of ST30 t975, ST30 t021, ST5 t311, and ST4335 t008 clones that are responsible for invasive infections in Paraguayan children. Both Pterocaulon extracts showed significant antibacterial activity with a minimum inhibitory concentration of 200 µg/mL against the four isolates. P. angustifolium showed inhibition of biofilm formation for the four isolates, whereas P. alopecuroides showed inhibition for three of them. The chemical constituents were identified by liquid chromatography coupled to tandem mass spectrometry. Phenolic compounds were detected in the two species as well as coumarins. These results showed that these plants are sources of compounds with activity against MRSA.

In Paraguay, healers from the Mbya culture treat cancer with a recipe prepared with the native toad Rhinella schneideri. However, the chemical composition and biological effects of the recipe remain unknown.The aim is to determine the composition of the traditional preparation made using the toad R. schneideri and to evaluate its effect on human breast cancer (BC) cells.The metabolites contained in the preparation were concentrated using XAD-7 resin, and the concentrate was analyzed by HPLC-MS/MS. The effect of the preparation was assessed in normal (MCF10F) and BC cells (MDA-MB-231 and MCF7). The mitochondrial membrane potential (Δψm), reactive oxygen species (ROS) levels, and cell cycle progression were determined by flow cytometry. The oxygen consumption rate (OCR) was measured by Clark electrode, and fibronectin-dependent migration in normoxia and hypoxia-like conditions were evaluated by transwell assay.From the Amberlite-retained extract from the preparation, 24 compounds were identified, including alkaloids, amino acids, bufadienolides, and flavonoids, among others. The crude extract (CE) did not affect cell cycle progression and viability of BC cell lines. Moreover, it did not make cancer cells more sensitive to the cytotoxic effect of the chemotherapeutics doxorubicin and teniposide. On the other hand, the CE reduced the menadione-induced ROS production and increased NADH, Δψm, and the OCR. Respiratory complexes I and III as well as ATP synthase levels were increased in an AMPK-dependent manner. Moreover, the CE inhibited the migration of BC cells in normoxia and a hypoxia-like condition using CoClThe Paraguayan toad recipe contains metabolites from the toad ingredient, including alkaloids and bufadienolide derivatives. The CE lacks cytotoxic effects alone or in combination with chemotherapeutics. However, it increases mitochondrial bioenergetics and inhibits the cancer cell migration in an AMPK-dependent manner in BC cells. This is the first report of the in vitro anticancer effect of a traditional Rhinella sp. toad preparation based on Mbya tradition.

Ethnopharmacological relevance Selected Peruvian Amazon plants are macerated into sugar cane distillates to prepare alcoholic beverages used to improve male sexual performance. The tree bark from Campsiandra angustifolia Spruce ex Benth (Fabaceae), Swartzia polyphylla DC (Fabaceae), Minquartia guianensis Aubl. (Olacaceae) and Thynantus panurensis (Bureau) Sandwith (Bignoniaceae) usually are used as crude drugs in mixtures of several ingredients. Aim of study Describe the chemical composition of the most traded traditional male enhancer beverages, namely “Levantate Lazaro” and “Siete veces sin sacarla”, and their single crude drug constituents, as well as their inhibitory activity towards the enzyme phosphodiesterase-5. The presence of pro-sexual drugs such as Sildenafil® and derivatives was assessed in the samples. Materials and methods Single plant constituents and the preparation mixtures were purchased in the Mercado Belen (Iquitos, Peru). Chemical profiling was carried out by HPLC-DAD-ESI-MS/MS. The extracts were assessed for phosphodiesterase-5 inhibition. The occurrence of pro-sexual drugs was determined by HPLC-DAD-ESI-MS/MS. Results Chemical profiling allowed the identification of condensed tannins as the main constituents of C. angustifolia and S. polyphylla, hydrolysable tannins for M. guianensis, and C-glycosides for T. panurensis. The traditional preparations showed similar composition compared to the crude drugs. At 200 µg/mL, the traditional preparation “Levantate Lazaro” and “Siete veces sin sacarla” inhibited the phosphodiesterase-5 by 49.88% and 27.90%, respectively. No adulterations with pro-sexual drugs were found in the samples. From the crude drugs, low effect was found for the extracts of S. polyphylla and T. panurensis and high activity for C. angustifolia which inhibited the enzyme by 89.37% and 81.32% at 200 and 100 µg/mL, respectively. Conclusion The traditional preparations used to improve sexual performance in the Peruvian Amazon showed activity as phosphodiesterase-5 inhibitors. The most active ingredient of the traditional preparations was C. angustifolia, with some contribution from T. panurensis. These results encourage additional studies, including animal models to confirm the male enhancer effect of the preparations.

The Araucaria araucana kernels are a traditional food in southern Chile and Argentina. The aim of this work was to determine the composition of the phenolic-enriched extracts (PEEs) of the boiled kernels as well as their antioxidant capacity, inhibitory activity on metabolic syndrome-associated enzymes and effect on postprandial oxidative stress in a simulated gastric digestion model. The PEEs composition was assessed by HPLC-DAD-MS/MS. The main PEEs constituents were catechin and epicatechin in the unbound form, while hydroxybenzoic acids occurred mainly in the bound form. The unbound phenolics from boiled kernels showed significant correlations with DPPH, FRAP, TEAC (Pearson’s r of 0.481, 0.331 and 0.417, respectively) and lipid peroxidation (r = 0.381) and were more active than the bound phenolics. The extracts were highly active against α-glucosidase (IC50: 0.33–3.15 µg/mL) and reduced lipoperoxidation. Traditional processing increases the flavan-3-ol content. Our results suggest that this traditional food has potential health promoting properties.

The crude drug ysyp&oacute, h&ucirc, (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 &micro, g/mL. Iridoids and amino acid derivatives were the main compounds occurring in the Paraguayan crude drug. The potential of ysyp&oacute, as a male sexual enhancer cannot be discarded, since other mechanisms may be involved.

The protective effect of polyphenols from Chilean currants (Ribes spp.) in human epithelial gastric cells (AGS) against oxidative induced-stress has been recently reported. The aim of the present study was to assess the ability of polyphenol-enriched extracts (PEE) from three Chilean Ribes species to modify the activities of the intracellular antioxidant enzymes: catalase (CAT), glutathione peroxidase (GSH-Px), glutathione reductase (GSH-R) and superoxide dismutase (SOD) in AGS cells. The PEE of each species was fractionated using membrane chromatography to give an anthocyanin-enriched fraction (AF) and a copigment fraction (CF). A significant increase in the SOD activity was observed with a dose-response effect after an overnight incubation of AGS cells with the PEE, AF and CF from the selected species. The activity of CAT was enhanced by the CF of Ribes magellanicum and R. cucullatum, and by the AF of R. punctatum. For the GSH-R, a dose-response effect was observed in the extracts of R. magellanicum, while for the GSH-Px activity, only the AF of R. magellanicum and R. cucullatum had a significant increase. The studied samples were not able to increase the intracellular GSH content. Only the R. magellanicum samples raised the intracellular total antioxidant activity. These results suggested that the increase in the activity of the antioxidant response enzymes is associated with the cytoprotective effect of these native currants.

The Chilean wild currants Ribes magellanicum and R. punctatum are a good source of polyphenols. Polyphenolic-enriched extracts (PEEs) from both species were submitted to in vitro colonic fermentation to assess the changes in phenolic composition, antioxidant capacity and inhibition of metabolic syndrome-associated enzymes. The phenolic profiles of the fermented samples showed significant changes after 24 h incubation. Nine metabolites, derived from the microbial fermentation, were tentatively identified, including dihydrocaffeic acid, dihydrocaffeoyl-, dihydroferuloylquinic acid, 1-(3,4-dihydroxyphenyl)-3-(2,4,6-trihydroxyphenyl)propan-2-ol (3,4-diHPP-2-ol), among others. The content of anthocyanins and hydroxycinnamic acids was most affected by simulated colonic conditions, with a loss of 71–92% and 90–100% after 24 h incubation, respectively. The highest antioxidant capacity values (ORAC) were reached after 8 h incubation. The inhibitory activity against the enzyme α-glucosidase was maintained after the fermentation process. Our results show that simulated colonic fermentation exerts significant changes on the polyphenolic composition of these berries, modifying their health-promoting properties.

Ethnopharmacological relevance: The Argentinean medicinal plant Tetraglochin andina Ciald, formerly classified as T. cristatum (Britton) Rothm is used in traditional medicine by inhabitants from Argentinean northwestern highlands (Puna) to treat candidiasis and as anti-inflammatory. Aim of the study: To assess the potential of the crude drug as an anti-Candida agent with anti-inflammatory properties. The bioactivity and phytochemical composition of a dry extract of the plant was investigated. Material and methods: The pharmacognostic description of the crude drug is carried out for the first time, including macroscopic and microscopic examinations of the different organs, physicochemical and extractive values (petroleum ether-, ethanol- and water-soluble). The dry extract from T. andina was evaluated as antifungal against pathogenic Candida sp. and Saccharomyces cerevisiae isolated from vaginal infections and reference strains, by the macrodilution and microdilution assays. The normal vaginal microbiome in women is characterized by the dominance of lactic acid-producing bacteria, mainly Lactobacillus spp. The effect of T. andina extract on Lactobacillus strains was also assayed. The inhibitory effect on proinflammatory enzymes (cyclooxygenase, lipoxygenase and phospholipase A2) and antioxidant capacity was studied. The chemical profile was analyzed by HPLC-ESI-MS. Results: The hydroalcoholic extract inhibited the growth of all yeasts with Minimal Inhibitory Concentration (MIC) values between 12.5 and 400 µg GAE/mL and the MIC values on Lactobacillus were higher than the MIC values against Candida isolates (> 400 µg GAE/mL). These results indicate that the hydroalcoholic extract could be used without affecting the normal microbiota of vaginal fluid. The extract showed antioxidant activity and could modulate the inflammatory process by three pathways (sPLA2, COX-2, LOX). The plant extract contained high total phenolic levels (386.9±1.7 mg GAE/g dry extract) and flavonoid levels (260.4±2.7 mg GAE/g dry extract). Fifty phenolic compounds were identified by HPLC-ESI-MS. They were mainly hydrolysable and condensed tannins. The dry extract was chemically and biologically stable during one year at room temperature or 4 °C. Conclusions: The presence of anti-Candida and anti-inflammatory activities in Tetraglochin andina extracts give support to their traditional use for treating conditions associated with microorganism infections and inflammatory process in humans. This plant preparation could be used to design phytopharmaceutical preparations to inhibit yeast growth and moderate the inflammatory and oxidative process. Fil: Moreno, María Alejandra. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Tucumán; Argentina. Universidad Nacional de Tucumán. Facultad de Ciencias Naturales e Instituto Miguel Lillo; Argentina Fil: Córdoba, Susana Beatríz. Dirección Nacional de Instituto de Investigación. Administración Nacional de Laboratorio e Instituto de Salud “Dr. C. G. Malbrán”; Argentina Fil: Zampini, Iris Catiana. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Tucumán; Argentina. Universidad Nacional de Tucumán. Facultad de Ciencias Naturales e Instituto Miguel Lillo; Argentina Fil: Mercado, Maria Ines. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Tucumán; Argentina. Fundación Miguel Lillo. Dirección de Botánica. Instituto de Ecología Vegetal. Área Botánica; Argentina Fil: Ponessa, Graciela Ines. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Tucumán; Argentina. Fundación Miguel Lillo. Dirección de Botánica. Instituto de Ecología Vegetal. Área Botánica; Argentina Fil: Alberto, Maria Rosa. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Tucumán; Argentina. Universidad Nacional de Tucumán. Facultad de Ciencias Naturales e Instituto Miguel Lillo; Argentina Fil: Nader, Maria Elena Fatima. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Tucumán. Centro de Referencia para Lactobacilos; Argentina Fil: Sayago, Jorge Esteban. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Tucumán; Argentina. Universidad Nacional de Tucumán. Facultad de Ciencias Naturales e Instituto Miguel Lillo; Argentina Fil: Burgos Edwards, Alberto. Universidad de Talca; Chile Fil: Schmeda Hirschmann, Guillermo. Universidad de Talca; Chile Fil: Isla, Maria Ines. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Tucumán; Argentina. Universidad Nacional de Tucumán. Facultad de Ciencias Naturales e Instituto Miguel Lillo; Argentina

The wild Chilean currants Ribes magellanicum and R. punctatum are a good source of polyphenolic compounds. The effect of simulated gastrointestinal digestion (GID) on phenolic content, composition and antioxidant capacity was determined. The inhibitory activity of the non-digested and digested samples towards metabolic syndrome-associated enzymes (α-amylase, α-glucosidase and lipase) was evaluated. The total phenolic (TP) and flavonoid contents (TF) decreased by about 50% at the end of the in vitro GID. Main anthocyanins and hydroxycinnamic acids were strongly affected by this process, with a loss of about 80%. A decrease in the antioxidant activity was observed throughout the digestion steps, which was correlated with the reduction in the TP and TF content. After the in vitro GID of the samples, only the inhibition of α-glucosidase was preserved. Our results show that the simulated GID modified the health-promoting properties of the studied currants.

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.

International audience; Roasted cotyledons of the Chilean hazelnut (Gevuina avellana) are appreciated as snacks. The aim of our work was to assess the fatty acid, oxylipin and phenolic composition using gas chromatography (GC) coupled to mass spectrometry (MS), ultra- high performance liquid chromatography (UHPLC) coupled to MS and HPLC coupled to diode array detector (HPLC-DAD). Additionally, various antioxidant activities were assessed. The inhibition of α-glucosidase, α-amylase, lipase, cyclooxygenases-1 and -2 (COX-1/COX-2), and lipoxygenase was determined. The main fatty acids were oleic and 7-hexadecenoic acids. Eight phytoprostanes and three phytofurans were identified and quantified. Hydroxybenzoic and hydroxycinnamic acids were the main phenolic compounds. Oils showed antioxidant activity determined by EPR, and inhibition of COX-1/COX-2. The statistical analysis showed that the roasting does not affect the composition of the samples. The occurrence of oxylipins in this species is reported for the first time. Chilean hazelnuts can be considered a source of health promoting compounds.

Chilean currants (Ribes magellanicum and Ribes punctatum) are wild polyphenol-rich berries with interesting bioactivities in several in vitro models. The aim of this study was to investigate the effects of the pre-digested PEE (polyphenol-enriched extract) in a simulated colon model. Fruits were extracted, submitted to simulated gastrointestinal digestion and further colonic fermentation with feces from healthy human donors. Samples were taken at 1, 4, 8 and 24 h of incubation, monitoring pH, ammonia, branched-chain fatty acids (BCFA), short-chain fatty acids (SCFA) and bacterial growth. FOS (fructooligosaccharides) and fecal slurry without treatments were positive and negative control, respectively. Both Ribes species reduced (p < 0.05) both BCFA and SCFA at 24 h. R. punctatum promoted the growth (p < 0.05) of beneficial bacteria such as Clostridium cluster XIVa, and Faecalibacterium prausnitzii; while a trend to increase Akkermansia muciniphila was observed. R. magellanicum increased (p < 0.05) Clostridium cluster XIVa population. Escherichia coli, Lactobacillus spp. and Bifidobacterium spp. remained unaffected. Our results suggest that polyphenols from R. punctatum and R. magellanicum may modulate both bacterial metabolism and some selected gut beneficial bacteria under simulated conditions. Therefore, Chilean currants might be useful as supplements to maintain a healthy colon; however, further in vivo studies are needed to confirm their effect and their mechanisms. Ministry of Economy and Competitiveness Ramón y Cajal Fellowship 2012_11910 MINECO (Project AGL2016-75878-R) National Commission for Scientific and Technological Research of Chile CONICYT-PCHA/Doctorado Nacional/2015-21151561 6.475 JCR (2020) Q1, 9/143 Food Science and Technology 1.479 SJR (2020) Q1, 16/332 Food Science No data IDR 2020 UEM