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The COVID-19 pandemic has led to the search for new molecules with antiviral activity against SARS-CoV-2. The entry of the virus into the cell is one of the main targets for inhibiting SARS-CoV-2 infection. Natural products are an important source of new therapeutic alternatives against diseases. Pseudotyped viruses allow the study of SARS-CoV-2 viral entry inhibitors, and due to their simplicity, they allow the screening of a large number of antiviral candidates in Biosafety Level 2 facilities. We used pseudotyped HIV-1 with the D614G SARS-CoV-2 spike glycoprotein to test its ability to infect ACE2-expressing HEK 293T cells in the presence of diverse natural products, including 21 plant extracts, 7 essential oils, and 13 compounds from plants and fungi. The 50% cytotoxic concentration (CC50) was evaluated using the resazurin method. From these analyses, we determined the inhibitory activity of the extract of Stachytarpheta cayennensis, which had a half-maximal inhibitory concentration (IC50) of 91.65 µg/mL, a CC50 of 693.5 µg/mL, and a selectivity index (SI) of 7.57, indicating its potential use as an inhibitor of SARS-CoV-2 entry. Moreover, our work indicates the usefulness of the pseudotyped-virus system in the screening of SARS-CoV-2 entry inhibitors.

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.

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

The Chilean white strawberry (Fragaria chiloensis spp. chiloensis f. chiloensis) is a semi-domesticated strawberry with high polyphenol content and antioxidant activity occurring in southern Chile. The aim of this work was to compare the composition and bioactivity of the polyphenol-enriched fruit extract (PEE) before and after simulated gastrointestinal digestion (GID). Results show a decrease by >50% in the total phenolic (TP) content at the end of the GID, compared to the non-digested PEE. A reduction in the antioxidant capacity of the PEEs was observed after GID by means of DPPH, FRAP, TEAC and anion superoxide assays. After simulated GID the PEE significantly inhibited α-glucosidase with an IC50 value of 3.13μg/mL. The inhibition of pancreatic lipase was reduced by 95% after GID. All the PEEs did not show inhibitory effect towards α-amylase throughout the GID. In the same way, the PEEs did not significantly protect human gastric adenocarcinoma (AGS) cells against H2O2-induced stress. Thirty eight compounds were tentatively identified in the non-digested PEE. The compounds that were more affected by the simulated GID were simple phenolics. After the GID, only 33 and 25 compounds were detected, in the gastric and intestinal steps, respectively. These results evidence the changes elicited by GID on the bioactivity and polyphenolic composition of the white strawberry.