Larrea ameghinoi Speg., an endemic species of Argentine Patagonia traditionally used in folk medicine to treat fever, stomach disorders, respiratory conditions, back pain, and as an emmenagogue, among others, still remains chemically and biologically underexplored compared to the other four members of the genus. This study aimed to perform a comprehensive metabolomic characterization of methanolic extracts from two populations (EMLaSAO and EMLaMAQ) using ultra-high-resolution liquid chromatography coupled with electrospray ionization quadrupole time-of-flight mass spectrometry (UHPLC-ESI-QTOF-MS) and to evaluate their antioxidant, antimicrobial, and enzyme-inhibitory activities of relevance to human health. Thirty-three compounds were tentatively identified by extensive UHPLC-MS analysis, including flavones, two major lignans, and oleanane-type triterpenes. Both extracts exhibited high phenolic content (215-239 mg of gallic acid equivalents (GAE)/g extract) and strong free radical scavenging activity, as evidenced by 2,2-diphenyl-1-picrylhydrazyl (DPPH, EC50 ≈ 10 μg/mL), ferric-reducing antioxidant power (FRAP), and Trolox equivalent antioxidant activity (TEAC) assays. In addition, significant inhibition of butyrylcholinesterase (IC50 ≈ 50 μg extract/mL) and α-glucosidase, together with selective antibacterial activity against methicillin-sensitive and resistant Staphylococcus aureus (MIC = 125 μg extract/mL), were recorded. These findings suggest that L. ameghinoi possesses a distinctive phytochemical composition conferring multitarget bioactivity, differing from other Larrea species dominated by lignans such as nordihydroguaiaretic acid (NDGA) and its derivatives. Overall, this work supports the potential of L. ameghinoi as a novel source of bioactive metabolites for managing oxidative stress-related disorders and opportunistic infections. This warrants future in vivo studies investigating biological activities associated with oxidative stress and their relevance to human health.

The growing environmental pollution and the imminent depletion of natural resources highlight the need for alternative building materials derived from renewable sources, including those that promote waste recycling and biodegradability. One promising alternative is biocomposites produced from filamentous fungal mycelium. In Argentina, orange and lemon peels are among the most abundant organic waste generated by the citrus industry. This study explores the development of a sustainable insulating biocomposite using Pleurotus ostreatus mycelium grown on mixtures of citrus peels, paper, and cardboard. The test specimens were prepared using varying concentrations of these components. The resulting fungal biocomposite exhibited a density approximately ten times higher than expanded polystyrene, with drying shrinkage ranging from 28% to 51%, depending on the formulation. Key properties were evaluated, including compressive strength (σ10 = 7–33 kPa), bulk density (ρ = 152–181 kg/m3), and thermal conductivity (λ = 0.29–0.36 W/mK), indicating advantageous performance for thermal insulation in construction applications. Specimens containing orange peel also demonstrated repellent activity against Triatoma infestans, main vector of transmission of Chagas’ disease, attributed to the residual limonene content retained from the citrus peels. This fungal biocomposite aligns with principles of green chemistry and circular economy, offering a biodegradable, low-impact solution with potential use in construction. The citrus waste proved to be an effective substrate for mycelial growth, producing a material with desirable mechanical and thermal properties, and added resistance to biodeterioration.

Pistachio nuts are among the 50 best foods with the highest antioxidant potential. They have a balanced content of mono- (~70%) and polyunsaturated (~20%) fatty acids, minerals, and bioactive compounds such as tocopherols, phytosterols, and phenolic compounds, which have shown rapid accessibility in the stomach. Pistachio consumption provides several health benefits, primarily due to its antioxidant properties and high content of essential nutrients. In this study, we analyzed the mineral composition, total phenolic content (TP), antioxidant activity (AA), and UHPLC/MS-MS polyphenolic profile of three Argentinian pistachio crops. Additionally, the physicochemical parameters and the elemental profiles of the growing soils were determined, as they influence mineral uptake and the synthesis of bioactive compounds in pistachio kernels. The TP was not significantly modified by the growing soils, with Crop3 presenting the highest TP content (276 ± 14 mg GA/100 g DW). Crop3 exhibited 18% higher TP content compared to Crop2. Similarly, FRAP values ranged from 28.0 to 36.5 mmol TE/100 g DW, with Crop1 showing a 30% increase compared to Crop2. DPPH values varied from 19.0 to 24.3 mmol TE/100 g DW, with Crop1 displaying 28% higher activity than Crop2. However, the polyphenolic profile was similar for all crops analyzed. Thirty compounds were identified; only Crop 1 contained the flavanone eriodyctiol and the isoflavone genistein, while the flavanone naringenin and the flavone luteolin were identified in Crop1 and Crop3. Regarding mineral content, the pistachio kernels mainly contained K, Ca, and Mg. Multivariate analyses revealed distinct elemental and antioxidant profiles among crops. LDA achieved classification accuracies of 77.7% for soils and 74.4% for kernels, with Pb, Zn, Cu, Rb, Sr, and Mn as key discriminants. CCA confirmed strong soil–kernel mineral correlations (r = 1), while GPA showed higher congruence between antioxidant traits and kernel composition than with soil geochemistry. These findings underscore the importance of soil composition in determining the nutritional quality of pistachio kernels, thereby supporting the beneficial health effects associated with pistachio consumption.

This research was designed to investigate the metabolite profiling, phenolics content, and the trypanocidal, nematicidal, antibacterial, antifungal, and free radical scavenging properties of Usnea lethariiformis Motyka. The air-dried U. lethariiformis material was extracted successively with dichloromethane and methanol (UlMeOH). Two phases were obtained from the extract with dichloromethane, one soluble in methanol (UlDCM-s) and the other insoluble (UlDCM-i). The metabolite profiling was obtained using ultra-high-resolution liquid chromatography coupled with electrospray ionization quadrupole time-of-flight mass spectrometry (UHPLC-ESI-QTOF-MS) system. The trypanocidal and nematicidal activities were determined according to standardized protocols. The antimicrobial activity was evaluated according to the Clinical and Laboratory Standards Institute (CLSI) rules. The total phenolic content of lichen extracts was determined by the Folin–Ciocalteu method. Antioxidant properties were assessed through 2,2-diphenyl-1-picrylhydrazyl (DPPH), Trolox equivalent antioxidant activity (TEAC), ferric-reducing antioxidant power (FRAP), and inhibition of lipid peroxidation in erythrocytes (ILP) assays, and the extracts exhibited robust antioxidant activity. Seventeen compounds were detected, of which thirteen were identified by UHPLC-ESI-QTOF-MS analysis, including depsides, depsidones, fatty acids, dibenzofurans, benzoic acids, and triterpenes. The UlDCM-s and UlMeOH extracts displayed strong trypanocidal activity against Trypanosoma cruzi epimastigotes at 50 μg/mL and 100 μg/mL and a nematicidal activity toward J2 Meloidogyne incognita, an important nematode infecting horticultural crops. Regarding the antimicrobial activity, the results showed that all bacteria and yeasts tested were inhibited by the different extracts with minimum inhibitory concentration (MIC) values between 25 μg/mL and 500 μg/mL. The UlDCM-s and UlMeOH extracts showed phenolic content of 107 mg and 48 mg gallic acid equivalents (GAE)/g dried extract, respectively. The UlDCM-s, UIDCM-i, and UlMeOH extracts showed moderate free radical scavenging activity in the DPPH, FRAP, and TEAC assays until 1 mg/mL and ILP tests at 250 μg/mL. The results indicated that U. lethariiformis may constitute a potential source of diverse bioactivities with application in the food, pharmaceutical, and agronomic industries.

Recently, we reported the chemical profile and the hypocholesterolemic effects of a decoction of Tessaria absinthioides (Hook. & Arn.) DC. (Asteraceae). In this study, we evaluated a methanolic extract (METa) instead. Metabolite profiling was conducted using ultra-high-resolution liquid chromatography coupled with electrospray ionization quadrupole time-of-flight mass spectrometry (UHPLC-ESI-QTOF-MS), identifying thirty compounds, including flavonoids, phenolic acids, fatty acids, and phorbolesters. Antioxidant properties were assessed through 2,2-diphenyl-1-picrylhydrazyl (DPPH), Trolox equivalent antioxidant activity (TEAC), ferric-reducing antioxidant power (FRAP), and inhibition of lipid peroxidation in erythrocytes (ILP) assays, exhibiting robust antioxidant activity. The in vivo impact of METa on serum lipid parameters and liver X receptors (LXRs) was evaluated in a hypercholesterolemic animal model. After 14 days on a high-fat diet, male rats received either a vehicle (V) or METa100, METa200 or METa500 (100; 200 and 500 mg METa/kg animal, respectively) for an additional two weeks. METa500 reduced total cholesterol levels (17.62%; p < 0.05) and all doses increased high-density lipoprotein cholesterol levels (METa100: 86.27%; METa200: 48.37%, and METa500: 29.42%; p < 0.0001). However, METa did not alter LXRs expression. The observed antioxidant and hypocholesterolemic properties of METa may be linked to the presence of six di-caffeoylquinic acids. These findings underscore T. absinthioides as a potential candidate for the treatment of metabolic disease.

In this work, a decoction (DOe) and a methanolic global extract (MGEOe), obtained with the aerial parts of Oxalis erythrorhiza Gillies ex Hooker et Arnott (Oxalidaceae), were evaluated. The high-resolution liquid chromatography in conjunction with electrospray ionization quadrupole time-of-flight mass spectrometry (UHPLC-ESI-QTOF-MS) analysis showed forty compounds in MGEOe and twenty-nine in DOe, including flavones, C-glycosyl flavones, isoflavones, fatty acids, terpenes, phenolic acids, and sterols. The antioxidant properties were evaluated by DPPH, TEAC, FRAP, and ILP assays. Both DOe and MGEOe showed stronger antioxidant activities. The anti-inflammatory effects were evaluated by COX inhibition method, where DOe demonstrated a significant inhibitory effect. The cytotoxic effects were evaluated in the tumoral HCT-116 and non-tumoral HBL-100 cell lines, revealing a selective action from DOe and MGOe on cancer cells. DOe was evaluated in an animal model of insulin resistance, which is characterized by alterations in glucose and lipid metabolism, as well as cognitive impairments, including anxiety-like behavior and memory deficits. Male SD rats received sucrose (10% w/v, SUC), a half dilution of DOe (5% w/v) with sucrose (HDOeS) or DOe with sucrose (DOeS) from PND21 to PND61. Then, anxiety-like behavior and spatial memory were assessed using the open field (OF), elevated plus maze (EPM) and the novel object location (NOL) tests, respectively. Serum parameters basal glycemia, total cholesterol (TC) and tryglicerides were measured using commercial kits. The lipid peroxidation was determined in homogenates of cerebral cortex, hippocampus and hypothalamus by TBAR assay. Only HDOeS exhibited lower anxiety-like behavior in OF and improved performance in NOL compared to SUC. Furthermore, DOeS showed reduced serum parameters, while HDOeS presented lower TC levels than SUC. No differences were observed on TBAR assay. The beneficial properties of these preparations could be attributed to the identified metabolites. These findings highlighted O. erythrorhiza as a potential source of compounds to improve human health; however, further research is required to elucidate its mechanisms of action.

This research was designed to investigate the metabolite profiling, phenolics, and flavonoids content as well as the potential nematicidal properties of decoction (ZpDe), orange-yellow resin (ZpRe) and essential oil (ZpEO) from Argentinean medicinal plant Zuccagnia punctata Cav. Additionally, the antioxidant and antibacterial properties of ZpDe and ZpEO were determined. Metabolite profiling was obtained by an ultrahigh-resolution liquid chromatography MS analysis (UHPLC-ESI-QTOF/OT-MS-MS) and GCMS. The nematicidal activity was assayed by a standardized method against Meloidogyne incognita. The antioxidant properties were screened by four methods: (2,2-diphenyl-1-picrylhydrazyl assay (DPPH), Trolox equivalent antioxidant activity assay (TEAC), ferric-reducing antioxidant power assay (FRAP), and lipid peroxidation in erythrocytes (ILP). The antibacterial activity was evaluated according to the Clinical and Laboratory Standards Institute (CLSI) rules. The ZpDe, ZpRe and ZpEO displayed a strong nematicidal activity with an LC50 of 0.208, 0.017 and 0.142 mg/mL, respectively. On the other hand, the ZpDe showed a strong DPPH scavenging activity (IC50 = 28.54 µg/mL); ILP of 87.75% at 250 µg ZpDe/mL and moderated antimicrobial activity. The ZpEO showed promising activity against a panel of yeasts Candida albicans and non-albicans (ATCC and clinically isolated) with MIC values from 750 to 1500 µg/mL. The ZpDe showed a content of phenolics and flavonoid compounds of 241 mg GAE/g and 10 mg EQ/g, respectively. Fifty phenolic compounds were identified in ZpDe by ultrahigh-resolution liquid chromatography (UHPLC–PDA– Q-TOF-MS) analysis, while forty-six phenolic compounds were identified in ZpRe by UHPLC-ESI-Q-OT-MS-MS and twenty-nine in ZpEO using a GC-MS analysis, updating the knowledge on the chemical profile of this species. The results support and standardize this medicinal plant mainly as a potential environmentally friendly and sustainable bionematicide for the control of Argentinean horticultural crops including tomatoes and peppers and as a source of antimicrobial and antioxidant compounds which could be further explored and exploited for potential applications.

Azara dentata Ruiz & Pav. is a small Chilean native plant from Patagonia, a producer of small white reddish berries. For the first time, the proximal analysis of the fruits, phenolic fingerprinting, the antioxidant activity, and the enzymatic inhibition and relaxation effects in rat aorta induced by the ethanolic extract of these fruits were investigated. The proximal composition and the mineral (Ca: 2434 ± 40 mg/kg; Mg: 702 ± 13 mg/kg; Fe: 117.1 ± 1.6 mg/kg; Zn: 16.1 ± 0.4 mg/kg) and heavy metal (As: 121 ± 11 µg/kg; Cd: 152 ± 5 µg/kg; Hg: 7.7 ± 1.3 µg/kg; Pb 294 ± 4 µg/kg) contents were analyzed. Anthocyanins, flavonoids, phenolic acids, and coumarins were identified using UHPLC-PDA-QTOF-MS. The ethanolic extracts showed a total phenolic content of 23.50 ± 0.93 mg GAE/g extract. In addition, the antioxidant activity was assessed using both DPPH and TEAC (28.64 ± 1.87 and 34.72 ± 2.33 mg Trolox/g of dry fruit, respectively), FRAP (25.32 ± 0.23 mg Trolox equivalent/g dry fruit), and ORAC (64.95 ± 1.23 mg Trolox equivalents/g dry fruit). The inhibition of enzymatic activities (acetylcholinesterase IC50: 2.87 + 0.23 µg extract/mL, butyrylcholinesterase IC50: 6.73 + 0.07 µg extract/mL, amylase IC50: 5.6 ± 0.0 µg extract/mL, lipase IC50: 30.8 ± 0.0 µg extract/mL, and tyrosinase IC50: 9.25 ± 0.15 µg extract/mL) was also assessed. The extract showed 50–60% relaxation in rat aorta (intact), mediated thorough the release of endothelial nitric oxide. Our results suggest that A. dentata is a good source of compounds with the capacity to inhibit important enzymes, can be hypotensive, and can thus have good potentiality as supplements in the amelioration of neurodegenerative diseases and could also have potential to be used to develop new functional foods. The study highlights the benefits of these neglected small fruits and could boost their consumption.

The appearance of antifungal resistance promotes the investigation of therapeutic options. There are few studies on the combined effect of antifungal drugs and essential oils (EOs). In the present work, regarding the association of eight EOs Andean plants with antifungal agents against a panel of fungi strains. Combinatorial effects were determined using the Fractional Inhibitory Concentration Index (FICI) and Dose Reduction Index (DRI). A combination of A. cryptantha-B EO with fluconazole showed a synergistic effect against C. Albicans (FIC = 0.31 and DRI = 16.25). EOs from A. cryptantha-A and L. integrifolia showed an additive effect (FICI = 0.75) against C. neoformans. A combination of EOs from A. seriphioides and A. cryptantha-A with terbinafine showed an additive effect on T. rubrum (FIC = 0.56; DRI = 16) and M. gypseum (FICI = 1.03; DRI = 32). In conclusion, combinations between EOs of species from Andean plants and commercial antifungal drugs yielded some interesting findings, as potential antifungal strategies used for treating infections associated with C. Albicans and T. rubrum.

BACKGROUND:Chagas disease, caused by the parasite Trypanosoma cruzi, affects over six million people worldwide, mainly in Latin American countries. Currently available drugs have variable efficacy in the chronic phase and significant side effects, so there is an urgent need for safer chemotherapeutic treatments. Natural products provide privileged structures that could serve as templates for the synthesis of new drugs. Among them, Amaryllidaceae plants have proved to be a potential natural source of therapeutical agents due to their rich diversity in alkaloids.PURPOSE:To identify alkaloids with anti-T. cruzi activity from Habranthus brachyandrus (Baker) Sealy (Amaryllidaceae, subfamily Amaryllidoideae) collected in Argentina.METHODS:An H. brachyandrus alkaloid extract was tested against T. cruzi, and its cytotoxicity profile was evaluated against two mammalian cell lines to ascertain its selectivity against the parasite and potential liver toxicity. It was also assessed by a stage-specific anti-amastigote assay and analysed by GC/MS to determine its alkaloid profile. The isolated alkaloids were also tested using the aforementioned assays.RESULTS:The extract showed high and specific activity against T. cruzi. The alkaloids lycoramine, galanthindole, 8-O-demethylmaritidine, 8-O-demethylhomolycorine, nerinine, trisphaeridine, deoxytazettine, and tazettamide were identified by means of GC-MS. In addition, hippeastidine (also named aulicine), tazzetine, ismine, and 3-epimacronine were isolated. The alkaloid ismine was specifically active against the parasite and had low toxicity against HepG2 cells, but did not show anti-amastigote activity.CONCLUSION:The extract had specific anti-T. cruzi activity and the isolated alkaloid ismine was partially responsible of it. These results encourage further exploration of H. brachyandrus alkaloids in search of novel starting points for Chagas disease drug development.

This research was designed to investigate the metabolite profiling, phenolics and flavonoids content and the potential antioxidant, antibacterial and nematicidal activities of “yellow-brown resins” from Larrea divaricata Cav (LdRe) and L. nitida Cav (LnRe). Metabolite profiling was obtained using an ultrahigh resolution liquid chromatography orbitrap MS analysis (UHPLC-ESI-OT-MS). The antioxidant properties were screened by four methods: 2,2-diphenyl-1-picrylhydrazyl assay (DPPH), trolox equivalent antioxidant activity assay (TEAC), ferric-reducing antioxidant power assay (FRAP) and lipid peroxidation in erythrocytes (LP). The antibacterial activity was evaluated according to the Clinical and Laboratory Standards Institute (CLSI) guidelines. In addition, the potential combinatory effect was analyzed with the fractional inhibitory concentration index (FICI) values using the checkerboard design. The nematicidal activity was carried out according to a standardized protocol. LdRe and LnRe showed a strong capture of the DPPH radical withvalues around 8.4 µg resin/mL; FRAP (1.69–1.94 mgTE/ g resin), TEAC (1.08–1.09 mgTE/g resin) and LP (81–82% at 100 µg of resin/mL) assays. A strong antimicrobial activity was displayed by both resins against methicillin-sensitive Staphylococcus aureus ATCC 25923(MSSA) and methicillin-resistant S. aureus ATCC 43300(MRSA) (MICs = 16–32 µg resin/mL). Additionally, the combination of LdRe or LnRe with the antibiotic cefotaxime showed an indifferent effect (FICI values = 1–1.25), however, this combinationcould be a potential strategy to reduce the drug doses, and in this way can be a potential alternative to reduce bacterial resistance. On the other hand, the resins showed a scarce nematicidal potential toward J2 Meloidogyne incognita; an important nematode infecting horticultural crops. Phenolics compounds were identified by UHPLC-PDA-OT-MS analysis, updating the knowledge on the chemical profile of these species. These results, together with the high content of quantified phenolics and flavonoids, allow the phenolics-enriched resins of these two Larrea species to be considered as a promising sustainable source of compounds of pharmacological interest.

The main strategies against Triatoma infestans (primary vector responsible for the Chagas disease transmission) are the elimination or reduction of its abundance in homes through the application of insecticides or repellents with residual power, and environmental management through the improvement of housing. The use of plant-derived compounds as a source of therapeutic agents (i.e., essential oils from aromatic plants and their components) is a valuable alternative to conventional insecticides and repellents. Essential oil-based insect repellents are environmentally friendly and provide reliable personal protection against the bites of mosquitoes and other blood-sucking insects. This study investigates, for the first time to our knowledge, the potential repellent activity of Zuccagnia punctata essential oil (ZEO) and poly(ε-caprolactone) matrices loaded with ZEO (ZEOP) prepared by solvent casting. The analysis of its essential oil from aerial parts by GC–FID and GC-MS, MS allowed the identification of 25 constituents representing 99.5% of the composition. The main components of the oil were identified as (−)-5,6-dehydrocamphor (62.4%), alpha-pinene (9.1%), thuja-2, 4 (10)-diene (4.6%) and dihydroeugenol (4.5%). ZEOP matrices were homogeneous and opaque, with thickness of 800 ± 140 µm and encapsulation efficiency values above 98%. ZEO and ZEOP at the lowest dose (0.5% wt./wt., 96 h) showed a repellency of 33 and 73% respectively, while at the highest dose (1% wt./wt., 96 h) exhibited a repellent activity of 40 and 66 %, respectively. On the other hand, until 72 h, ZEO showed a strong repellent activity against T. infestans (88% repellency average; Class V) to both concentrations, compared with positive control N-N diethyl-3-methylbenzamide (DEET). The essential oils from the Andean flora have shown an excellent repellent activity, highlighting the repellent activity of Zuccagnia punctata. The effectiveness of ZEO was extended by its incorporation in polymeric systems and could have a potential home or peridomiciliary use, which might help prevent, or at least reduce, Chagas’ disease transmission.

Plants in the Amaryllidaceae family synthesize a diversity of bioactive alkaloids. Some of these plant species are not abundant and have a low natural multiplication rate. The aims of this work were the alkaloids analysis of a Habranthus cardenasianus bulbs extract, the evaluation of its inhibitory activity against cholinesterases, and to test several propagation strategies for biomass production. Eleven compounds were characterized by GC-MS in the alkaloid extract, which showed a relatively high proportion of tazettine. The known alkaloids tazettine, haemanthamine, and the epimer mixture haemanthidine/6-epi-haemanthidine were isolated and identified by spectroscopic methods. Inhibitory cholinesterases activity was not detected. Three forms of propagation were performed: bulb propagation from seed, cut-induced bulb division, and micropropagated bulbs. Finally, different imbibition and post-collection times were evaluated in seed germination assays. The best propagation method was cut-induced bulb division with longitudinal cuts into quarters (T1) while the best conditions for seed germination were 0-day of post-collection and two days of imbibition. The alkaloids analyses of the H. cardenasianus bulbs showed that they are a source of anti-tumoral alkaloids, especially pretazettine (tazettine) and T1 is a sustainable strategy for its propagation and domestication to produce bioactive alkaloids.

Chronic high-fat diet consumption induces hypercholesterolemia. The effect of Tessaria absinthioides (Hook. & Arn.) DC. (Asteraceae) was studied on the levels of total cholesterol (TC), high-density lipoprotein cholesterol (HDL-c), and triglycerides, and on the expression of liver X receptors (LXRs) in a hypercholesterolemic model. Adult male rats received a normal diet (ND) or a high-fat diet (HFD; normal diet + bovine fat + cholesterol). After 14 days, rats received water (W) or a decoction of the aerial parts of T. absinthioides (Ta; 10% w/v) for 2, 4, or 6 weeks. Four and six weeks of Ta improved the levels of TC and HDL-c in HFD. After 6 weeks of Ta, the expression of LXRs in HFD was the same as that in ND in both tissues. The Ta chemical profile was studied with an ultrahigh resolution liquid chromatography Orbitrap MS analysis (UHPLC–PDA–OT-MS/MS). Fifty-one compounds were identified, of which twelve are reported for the first time. Among these compounds, caffeoylquinic acid and its derivatives could modify the lipid profile and the expression of LXRs. This is the first in vivo report of T. absinthioides, which may be a potential candidate against hypercholesterolemia.

A library of embelin derivatives has been synthesized through a multicomponent reaction from embelin (1), aldehydes and privileged structures such as 4-hydroxycoumarin, 4-hydroxy-2H-pyran-2-one and 2-naphthol, in the presence of InCl3 as catalyst. This multicomponent reaction implies Knoevenagel condensation, Michael addition, intramolecular cyclization and dehydration. Many of the synthesized compounds were active and selective against Gram-positive bacteria, including one important multiresistant Staphylococcus aureus clinical isolate. It was found how the conjugation of diverse privileged substructure with embelin led to adducts having enhanced antibacterial activities.

This research was designed to investigate the metabolite profiling, phenolics, and flavonoids content as well as the potential antioxidant and antibacterial, properties of orange-yellow resin from Zuccagnia punctata Cav (ZpRe). Metabolite profiling was obtained by a ultrahigh resolution liquid chromatography orbitrap MS analysis (UHPLC-ESI-OT-MS-MS). The antioxidant properties were screened by four methods: 2,2-diphenyl-1-picrylhydrazyl assay (DPPH), trolox equivalent antioxidant activity assay (TEAC), ferric-reducing antioxidant power assay (FRAP), and lipid peroxidation in erythrocytes (LP)). The antibacterial activity was evaluated according to the Clinical and Laboratory Standards Institute (CLSI) rules. The resin displayed a strong DPPH scavenging activity (IC50 = 25.72 µg/mL) and showed a percentage of inhibition of LP close to that of the reference compound catechin (70% at 100 µg ZpRe/mL), while a moderated effect was observed in the FRAP and TEAC assays. The resin showed a content of phenolic and flavonoid compounds of 391 mg GAE/g and 313 mg EQ/g respectively. Fifty phenolics compounds were identified by ultrahigh resolution liquid chromatography orbitrap MS analysis (UHPLC-PDA-OT-MS) analysis. Thirty-one compounds are reported for the first time, updating the knowledge on the chemical profile of this species. The importance of the biomolecules identified support traditional use of this endemic plant. Furthermore, additional pharmacological data is presented that increase the potential interest of this plant for industrial sustainable applications.

The aqueous extract of the Argentinean native plant, Prosopis strombulifera (PsAE), presents cytotoxicity against human cancer cell lines by inducing cytostasis, necrosis and apoptosis; with diminution of clonogenic survival; without genotoxic effects nor oral animal toxicity. Until now, the chemical extract composition and its in vivo antitumoral properties remain unknown; these studies are the aim of the current work. The PsAE was characterized by chemical fingerprinting and the metabolome was identified by tandem UHPLC-PDA-HESI-Q-orbitrap® mass spectrometry. Colorectal tumors were induced by DMH administration and melanomas resulted from B16-F0 S.C. cells injection; then, animals were treated orally with PsEA. To correlate in vivo results with in vitro cytotoxicity, B16-F0 cell were cultured to determine: cell proliferation and viability by dye exclusion assays, MTT and CFSE dilution; cell cycle distribution by flow cytometry; and immunoblotting of p21cip1, PCNA, cleaved caspase 3, cleaved PARP and TUBA1A. Based on UHPLC-OT-MS and PDA analysis, twenty-six compounds were identified, including: 5 simple organic acids, 4 phenolic acids, 4 procyanidins, 11 flavonoids, and 2 oxylipins. On C57BL6 mice, PsAE significantly increases the median survival on colorectal cancer and reduces the final volume and weight of melanomas. Over cultured cells, the treatment induce over-expression of p21, cytostasis by G2/M cell cycle arrest and apoptosis; while, on in vivo melanomas, treatment up-regulates p21 and slightly decreases PCNA. In conclusion, PsAE is composed by phenolic compounds which demonstrate cytotoxic and antitumoral properties when is orally administrated. Presented results support future research of PsAE as a potential phytomedicine for cancer treatment.

The decoction of Tessaria absinthioides is used in traditional medicine of South America as hypocholesterolemic, balsamic, and expectorant; but it is also useful for the prevention of hepatitis, renal insufficiency, and diabetes, and is used as digestive. A lyophilized decoction from the aerial parts of this plant (TLD) collected in San Juan (TLDSJ) and Mendoza (TLDM) provinces (Argentina) and one collection from Antofagasta, Chile (TLDCH) were characterized regarding antioxidant and antibacterial activities, phenolics and flavonoids content, and ultrahigh resolution liquid chromatography Orbitrap MS analysis UHPLC–PDA–OT-MS/MS metabolite profiling. The antioxidant properties were carried out "in vitro" using 2,2-diphenyl-1-picrylhydrazyl (DPPH) and trolox equivalent antioxidant activity (TEAC) methods, ferric-reducing antioxidant power (FRAP), and lipoperoxidation in erythrocytes (LP). The antibacterial activity was evaluated following the Clinical and Laboratory Standards Institute (CLSI) rules. TLDSJ, TLDM, and TLDCH displayed a strong DPPH scavenging activity (EC50 = 42, 41.6, and 43 µg/mL, respectively) and inhibition of lipoperoxidation in erythrocytes (86–88% at 250 µg TLD/mL), while a less effect in the FRAP and TEACantioxidant assays was found. Additionally, the decoctions showed a content of phenolics compounds of 94 mg gallic acid equivalents (GAE)/g, 185 GAE/g, and 64 GAE/g, for TLDSJ, TLDM, and TLDCH samples, respectively. Regarding the flavonoid content, the Chilean sample was highlighted with 19 mg quercetin equivalents (QE)/g. In this work, several phenolic compounds, including sesquiterpenes, flavonoids, and phenolic acids, were rapidly identified in TLDSJ, TLDM, and TLDCH extracts by means UHPLC–PDA–OT-MS/MS for the first time, which gave a first scientific support to consider this medicinal decoction from both countries as a valuable source of metabolites with antioxidant effects, some with outstanding potential to improve human health.

A new series of furan embelin derivatives was synthesized and characterized as ATP-competitive CK2 inhibitors. The new compounds were efficiently synthesized using a multicomponent approach from embelin (1), aldehydes and isonitriles through a Knoevenagel condensation/Michael addition/heterocyclization. Several compounds with inhibitory activities in the low micromolar or even submicromolar were identified. The most active derivative was compound 4l (2-(tert-butylamino)-3-(furan-3-yl)-5-hydroxy-6-undecylbenzofuran-4,7-dione) with an IC50 value of 0.63 mu M. It turned out to be an ATP competitive CK2 inhibitor with a K-i value determined to be 0.48 mu M. Docking studies allowed the identification of key ligand-CK2 interactions, which could help to further optimize this family of compounds as CK2 inhibitors.

The decoction of the local plant Baccharis grisebachii is used as a digestive, gastroprotective, external cicatrizing agent and antiseptic in Argentine. A lyophilized decoction (BLD) from the aerial parts of this plant was evaluated regarding its anti-ulcer, antioxidant and cytotoxic activities and the bioactivities were supported by UHPLC-MS metabolome fingerprinting which revealed the presence of several small bioactive compounds. The antioxidant properties were evaluated by DPPH, TEAC, FRAP and lipoperoxidation inhibition in erythrocytes methods, and the antibacterial activity was evaluated according to the Clinical and Laboratory Standards Institute (CLSI) guidelines. The BLD showed a moderate free radical scavenging activity in the DPPH (EC50 = 106 µg/mL) and lipid peroxidation in erythrocytes assays (67%, at 250 µg/mL). However, the BLD had the highest gastroprotective effect at a dose of 750 mg/kg with a ninety-three percent inhibition of damage through a mechanism that involve NO and prostaglandins using the ethanol-induced gastric damage in a standard rat model. On the other hand, BLD does not induce cytotoxic changes on human tumor and no-tumor cell lines at the concentrations assayed. Regarding the metabolomic analysis, thirty-one compounds were detected and 30 identified based on UHPLC-OT-MS including twelve flavonoids, eleven cinnamic acid derivatives, one coumarin, one stilbene and two other different phenolic compounds. The results support that the medicinal decoction of Baccharis grisebachii is a valuable natural product with gastroprotective effects and with potential to improve human health that opens a pathway for the development of important phytomedicine products.