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Herbal teas are used in South Africa as digestives to lower glycaemia and for other indications. However, the chemical composition of the infusions and their effect on enzymes related to metabolic syndrome is poorly known. The composition of infusions and methanol extracts of B. saligna (Scrophulariaceae), Lippia javanica, L. scaberrima, and Phyla dulcis (Verbenaceae) was assessed and the effect of the infusions and extract was determined towards α-glucosidase, α-amylase, and pancreatic lipase. The commercial herbal products were extracted separately with MeOH or hot water to obtain the extract/infusion for comparative studies. Total phenolic, total flavonoid and antioxidant capacity were assessed. The fingerprints of the MeOH extracts and infusions were compared by HPLD-DAD. The extract constituents were tentatively identified by HPLC-MS/MS and NMR analyses. From the extracts/infusions, 57 compounds were identified, including iridoids, phenylpropanoid glycosides, flavonoids, and caffeic acid derivatives, among others. The MeOH extracts and infusions showed strong inhibition towards α-glucosidase with IC50 in the range of 0.13–0.84 µg/mL for the phenolic-enriched infusion extract (PEI) and 0.47–0.50 µg/mL for the MeOH extracts, respectively. The P. dulcis PEI showed higher inhibition towards α-glucosidase, and the MeOH extract of L. scaberrima was better than the PEI. At 100 µg/mL, the PEI from the four herbal teas reduces the activity of α-amylase by 23.03–28.61%, with L. javanica as the most active tea. Three of the species are high in phenylpropanoid glycosides, while P. dulcis contains rosmarinic acid. Some 26 compounds were identified in the infusion from B. saligna, 28 from L. scaberrima, and 21 from P. dulcis. Four of them are common in all the teas, namely decaffeoylverbascoside, verbascoside, isoverbascoside, and tuberonic acid hexoside. Ten compounds occur in two of the teas and seventeen, fifteen, and eleven compounds were detected only in B. saligna, L. scaberrima, and P. dulcis, respectively. Most of the compounds are reported for the first time from the crude drug infusions. The results give some support for the traditional use of herbal teas as digestives and/or indications for diabetes. The chemical fingerprints set the basis for quality control of the crude drugs, based on the main constituents and differential compounds occurring in the samples. [ABSTRACT FROM AUTHOR]

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. [ABSTRACT FROM AUTHOR]

Featured Application: The scope of the work is the hydroalcoholic extraction of total anthocyanins from the S. odorifera peel for their purification and foods applications.Sicana odorifera is a native fruit of South America large in size. Its dark-colored skin constitutes a useful byproduct for obtaining bioactive molecules because it is rich in polyphenolic compounds, such as anthocyanins. Obtaining appropriate extracts for obtaining anthocyanins can be useful for multiple applications in the food industry or for obtaining phytopharmaceuticals. In this work, the fruit and its peel composition were evaluated, an anthocyanin extraction system was designed and optimized, and the extract obtained was characterized. The peel composition of S. odorifera ripe fruits from the black accession growing in Paraguay was rich in polyphenol compounds and anthocyanins. Ultrasound-assisted extractions of total anthocyanins were studied, and the extraction variables were optimized. First, a screening design was considered to analyze time, pH, liquid–solid ratio, solvent concentration, and temperature. From the screening design, the significant variables were considered in a Box–Behnken design, and a response surface methodology was applied. The resulting total anthocyanin extract was characterized by UPLC-DAD-MS / MS-ESI. The most efficient system for the extraction of anthocyanins from the peel was at 15 min, 20 °C, pH = 6, 60% ethanol, and 80 mL/g of liquid–solid ratio. The highest concentration obtained was 61.908 mg C3G/g peel extract. In the extract, 12 main compounds were tentatively identified, including five anthocyanin derivatives, five flavonol derivatives, and two flavonol aglycones. This study provides information for the obtention of an anthocyanin-based dye from black kurugua peel, possibly useful for future applications as a natural colorant in high-added-value foods due to its antioxidant characteristics. [ABSTRACT FROM AUTHOR]

Simple Summary: This research highlights the prospect of kurugua seed by-product as a nutraceutical and functional food ingredient. Nutritional and bioactive profiling revealed that kurugua is rich in excellent nutritional compounds that can be exploited for human food development or in animal feed formulations. The seed by-product has shown great promise as an effective hepatoprotective agent and could be targeted for drug development. The "Kurugua" (Sicana odorifera) is a native fruit that demonstrates attractive nutritional, coloring, flavoring, and antioxidant properties. The main by-products from the processing and consumption of kurugua fruit are epicarp and seeds. In this work, the properties of the seeds of S. odorifera were evaluated. The nutritional composition of the fruit seeds was determined through AOAC official methods and UHPLC-ESI-MS/MS profiling. The antioxidant activities were determined using in vitro methods, and the acute toxicity and hepatoprotective properties were investigated in Swiss albino mice. Quercetin derivatives and cucurbitacins were the main phytochemicals in the seeds' methanolic extract and demonstrated some biological activities. GC-MS analysis revealed the essential fatty acids linolenic and linoleic as the main compounds present in seeds oil. The methanolic extract significantly reduced the serum levels of glutamic-pyruvic transaminase (GPT) and glutamic-oxaloacetic transaminase (GOT) in mice with induced hepatotoxicity (GPT p < 0.05; GOT p < 0.001) at the minor concentration tested (100 mg/kg EMSo). The results suggest that the S. odorifera seeds as by-products show potential use as a source of phytochemicals and in the production of oils with application in food supplements and nutraceuticals. Their integral use could contribute to waste reduction from kurugua fruits processing within the food safety and environmental sustainability framework. [ABSTRACT FROM AUTHOR]

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. [ABSTRACT FROM AUTHOR]