Search Results (39)

The pisco industry generates significant environmental waste, particularly grape pomace, which is a rich source of phenolic compounds. Emerging extraction technologies offer promising alternatives for recovering these bioactive components. This study evaluated enzyme-assisted extraction (EAE) and pressurized liquid extraction (PLE) techniques using response surface methodology to optimize phenolic compound yield and antioxidant capacity. Specifically, a D-optimal design was applied for EAE, and a Box–Behnken design was applied for PLE. The optimal extraction conditions for EAE were 0.75 U/mL of tannase, 40 U/mL of cellulase, 20 °C, and 15 min. For PLE, the optimal parameters were 54% ethanol, 113 °C, and three extraction cycles. These conditions yielded 38.49 mg GAE g⁻¹ dw and 50.03 mg GAE g⁻¹ dw of total polyphenols and antioxidant capacities of 342.47 μmol TE g⁻¹ dw and 371.00 μmol TE g⁻¹ dw, respectively. The extracts obtained under optimal conditions were further characterized through chromatographic techniques to determine their phenolic profiles. Seven phenolic compounds were identified: gallic acid, catechin, epicatechin, 4-hydroxybenzoic acid, quercetin-3-rutinoside hydrate, quercetin-3-O-rhamnoside, and kaempferol. PLE extracts exhibited the highest concentration of these compounds. These findings demonstrate that recovering antioxidant-rich phenolic compounds from pisco grape pomace using innovative extraction methods is a viable strategy for obtaining functional ingredients and supporting sustainable industrial practices. Full article

Bioactive extracts from living plants (LR) and beach deposits (NR) of the submerged brackish water angiosperm Ruppia maritima were examined for their antioxidant activity and anticancer potential. LR extract scavenged effectively free radicals with IC₅₀ values of 38.00 μg/mL (DPPH^•), 12.00 μg/mL (ABTS^•+), 281.00 μg/mL (OH^•), and 53.00 μg/mL (O₂^•), and exhibited reducing activity with an RP_0.5AU value of 37.00 μg/mL. NR extract retained a significant part of LR extract’s antioxidant activity by scavenging free radicals with IC₅₀ values of 180.00 μg/mL (DPPH^•), 60.00 μg/mL (ABTS^•+), and 164.00 μg/mL (O₂^•), and exhibited reducing activity with an RP_0.5AU value of 107.00 μg/mL. Importantly, NR extract (IC₅₀ value: 60.00 μg/mL) exhibited much higher inhibitory activity than LR extract (IC₅₀ value: 1100.00 μg/mL) in XTT assay. HPLC analysis revealed that both R. maritima extracts contained phenolics, such as chicoric acid, quercetin-3-O-glucopyranoside, p-coumaric acid, 3,5-dimethoxy-4-hydroxicinnanic acid, trans-ferulic acid, and rutin hydrate, possessing antioxidant and/or anticancer activity. Thus, the present study showed for the first time that R. maritima extracts from either LR or NR are a promising source of bioactive compounds having beneficial properties for human health. Full article

(1) Background: The onset of inflammation and oxidative stress after biomaterial implantation can lead to complications and prolonged recovery times. To address this, bioactive mesoporous glasses doped with cerium (0, 3.6 and 5.3 mol%) were loaded with three different biomolecules—3-hydroxyflavone, quercetin and morin hydrate—to enhance antioxidant properties while preserving bioactivity. (2) Methods: Elemental analysis, specific surface area determination, spectroscopic techniques, evaluation of antioxidant activity and in vitro bioactivity assessment were performed to characterize mesoporous glass loaded with biomolecules. (3) Results: Biomolecule loading gives values in the range of 0.5–2.0% and 10.3–39.6% for loading content and loading efficiency, respectively. The loading order is quercetin > morine hydrate > 3-hydroxyflavone, and a cerium percentage of 3.6 seems to be a good compromise. The antioxidant properties evaluated on both solids and solutions in contact with simulated biological fluids improve markedly over loaded glasses, and the most promising results are obtained with quercetin. In the most efficient systems, the bioactivity results were delayed and more evident at longer times (168 h) but were still retained. (4) Conclusions: We obtained new materials still bioactive with improved antioxidant properties that can be proposed for the regeneration of both hard and soft tissues. Full article

Many important drugs in pharmaceutical applications are poorly soluble. Solubilization, which is diffusion through biological barriers, and the control of local administration are crucial steps for bioavailability and to avoid cytotoxic effects. Hybrid organic/inorganic biomaterials can incorporate drugs for in situ release after implantation. Molecular Mechanics (MM) and Molecular Dynamics (MD) simulations are useful tools for investigating intermolecular interactions between drug and biomaterial surfaces at the atomistic level for these applications. This work studies quercetin, a flavonoid drug important for its anti-inflammatory, antioxidant, and anticancer properties, and the amorphous SiO₂ surface using a simulation protocol proposed in previous work related to ketoprofen drugs. After adsorption on the amorphous silica surface, the adsorption process of quercetin drug molecules at two different drug concentrations near a hydrated and then dried silica surface is investigated. Interestingly, these theoretical results are compared with experimental data obtained via Fourier Transform Infrared Spectroscopy (FT–IR) spectra related to quercetin molecules homogenously entrapped in a silica matrix obtained via the Sol–Gel method. Favorable H– bonds and some π–π interactions among drug molecules are crucial surface interactions for the new generation of biocompatible materials capable of incorporating anti-inflammatory agents for release into the human body. Full article

The identification of natural remedies for the management of the skin aging process is an increasingly growing issue. In this context, ursolic acid (UA), a ubiquitous molecule, mainly contained in Annurca apple (AA) fruit, has demonstrated valuable cosmetic potential. To this end, in the current study, the AA oleolite (AAO, extract in sunflower oil containing 784.40 ± 7.579 µg/mL of UA) was evaluated to inhibit porcine elastase enzymatic reactions through a validated spectrophotometric method. AAO has shown a valuable capacity to contrast the elastase enzyme with a calculated IC₅₀ of 212.76 mg/mL, in comparison to UA (IC₅₀ of 135.24 μg/mL) pure molecules and quercetin (IC₅₀ of 72.47 μg/mL) which are used as positive controls. In this context and in view of the valuable antioxidant potential of AAO, its topical formulation with 2.5% (w/w) AAO was tested in a placebo-controlled, double-blind, two-arm clinical study on 40 volunteers. Our results indicated that after 28 days of treatment, a significant reduction of the nasolabial fold (−7.2 vs. baseline T0, p < 0.001) and forehead wrinkles (−5.3 vs. baseline T0, p < 0.001) were registered in combination with a valuable improvement of the viscoelastic skin parameters, where skin pliability/firmness (R₀) and gross elasticity (R₂) were significantly ameliorated (−13% vs. baseline T0, p < 0.001 for R₀ and +12% vs. baseline T0, p < 0.001 for R₂). Finally, considering the positive correlation between skin elasticity and hydration, the skin moisture was evaluated through the estimation of Trans epidermal water loss (TEWL) and skin conductance. Full article

The presented study is focused on the modification of commercially available epoxy resin with flame retardants by means of using natural substances, including quercetin hydrate and potato starch. The main aim was to obtain environmentally friendly material dedicated to rail transport that is resistant to the aging process during exploitation but also more prone to biodegradation in environmental conditions after usage. Starch is a natural biopolymer that can be applied as a pro-ecological filler, which may contribute to degradation in environmental conditions, while quercetin hydrate is able to prevent a composite from premature degradation during exploitation. To determine the aging resistance of the prepared materials, the measurements of hardness, color, mechanical properties and surface free energy were performed before and after solar aging. To assess the mechanical properties of the composite material, one-directional tensile tests were performed for three directions (0, 90, 45 degrees referred to the plate edges). Moreover, the FT-IR spectra of pristine and aged materials were obtained to observe the changes in chemical structure. Furthermore, thermogravimetric analysis was conducted to achieve information about the impact of natural substances on the thermal resistance of the achieved composites. Full article

Aristotelia chilensis or “maqui” is a tree native to Chile used in the folk medicine of the Mapuche people as an anti-inflammatory agent for the treatment of digestive ailments, fever, and skin lesions. Maqui fruits are black berries which are considered a “superfruit” with notable potential health benefits, promoted to be an antioxidant, cardioprotective, and anti-inflammatory. Maqui leaves contain non-iridoid monoterpene indole alkaloids which have previously been shown to act on nicotinic acetylcholine receptors, potassium channels, and calcium channels. Here, we isolated a new alkaloid from maqui leaves, now called makomakinol, together with the known alkaloids aristoteline, hobartine, and 3-formylindole. Moreover, the polyphenols quercetine, ethyl caffeate, and the terpenes, dihydro-β-ionone and terpin hydrate, were also obtained. In light of the reported analgesic and anti-nociceptive properties of A. chilensis, in particular a crude mixture of alkaloids containing aristoteline and hobartinol (PMID 21585384), we therefore evaluated the activity of aristoteline and hobartine on Na_V1.8, a key Na_V isoform involved in nociception, using automated whole-cell patch-clamp electrophysiology. Aristoteline and hobartine both inhibited Nav1.8 with an IC₅₀ of 68 ± 3 µM and 54 ± 1 µM, respectively. Hobartine caused a hyperpolarizing shift of the voltage-dependence of the activation, whereas aristoteline did not change the voltage-dependence of the activation or inactivation. The inhibitory activity of these alkaloids on Na_V channels may contribute to the reported analgesic properties of Aristotelia chilensis used by the Mapuche people. Full article

This study aimed at establishing the optimal conditions for the classic extraction of phenolic compounds from Prunus spinosa L. fruits. The effects of different parameters, i.e., ethanol concentration in the extraction solvent (mixture of ethanol and water), operation temperature, and extraction time, on process responses were evaluated. Total phenolic content (TPC), total anthocyanin content (TAC), antioxidant capacity (AC), and contents of protocatechuic acid (PA), caffeic acid (CA), vanillic acid (VA), rutin hydrate (RH), and quercetin (Q) of fruit extracts were selected as process responses. A synergistic effect of obtaining high values of TPC, TAC, AC, PA, and VA was achieved for the extraction in 50% ethanol at 60 °C for 30 min. At a higher level of process temperature, the extraction of protocatechuic acid and vanillic acid was enhanced, but the flavonoids, i.e., rutin hydrate and quercetin, were degraded. A lower temperature should be used to obtain a higher amount of flavonoids. TPC, TAC, AC, and phenolic acid contents (PA, CA, and VA) in the extract samples obtained at an ethanol concentration of 50–100%, a temperature of 30–60 °C, and an extraction time of 30 min were strongly directly correlated. Full article

In the frame of reformulating food products for valorizing underutilized crops and enhancing both the nutritional and sensory characteristics of traditional foods, this study explored the potential impact of sprouting on some features of couscous prepared from buckwheat. Specifically, the impact of two sprouting times (48 h and 72 h) and two enrichment levels (25% and 50%) on physical properties (bulk density, hydration properties), cooking behavior (e.g., texture), chemical features (e.g., total phenolic content, rutin and quercetin), antioxidant activity (DPPH assay), and sensory traits (by means of electronic nose, tongue, and eye) was considered. Results showed that the replacement of 50% of pre-gelatinized buckwheat flour with 72 h-sprouted buckwheat flour resulted in a couscous with a higher content of phenolic compounds (including rutin and quercetin) and antioxidant activity; the related values further increased upon cooking. Moreover, except for the hardness and gumminess that were worsened (i.e., their values increased), cohesiveness and resilience improved in the presence of sprouted buckwheat (i.e., their values increased). Finally, the overall sensory traits improved with the addition of 50% sprouted buckwheat, since both bitterness and astringency decreased in the reformulated couscous. Full article

Filipendula ulmaria, commonly known as meadowsweet, is a wild herbaceous flowering plant that is widely distributed in Europe. A range of salicylic acid derivatives and flavonol glycosides have been previously associated with the antirheumatic and diuretic properties of F. ulmaria. In the present work, a hydroalcoholic extract from F. ulmaria aerial parts was extensively profiled using an efficient NMR-based dereplication strategy. The approach involves the fractionation of the crude extract by centrifugal partition chromatography (CPC), ¹³C NMR analysis of the fractions, 2D-cluster mapping of the entire NMR dataset, and, finally, structure elucidation using a natural metabolite database, validated by 2D NMR data interpretation and liquid chromatography coupled with mass spectrometry. The chemodiversity of the aerial parts was extensive, with 28 compounds unambiguously identified, spanning various biosynthetic classes. The F. ulmaria extract and CPC fractions were screened for their potential to enhance skin epidermal barrier function and skin renewal properties using in vitro assays performed on Normal Human Epidermal Keratinocytes. Fractions containing quercetin, kaempferol glycosides, ursolic acid, pomolic acid, naringenin, β-sitosterol, and Tellimagrandins I and II were found to upregulate genes related to skin barrier function, epidermal renewal, and stress responses. This research is significant as it could provide a natural solution for improving hydration and skin renewal properties. Full article

The Oropouche virus is an orthobunyavirus responsible for causing Oropouche fever, a disease that primarily affects thousands of people in South and Central America. Currently, no specific antiviral treatments or vaccines are available against this virus, highlighting the urgent need for safe, affordable, and effective therapies. Natural products serve as an important source of bioactive compounds, and there is growing interest in identifying natural bioactive molecules that could be used for treating viral diseases. Quercetin hydrate is a compound classified as a flavonoid, which has garnered scientific attention due to its potential health benefits and its presence in various plant-based foods. In this study, we aim to evaluate the in vitro antiviral activity of quercetin hydrate against the Oropouche virus (OROV). Furthermore, we intend to explore its mode of action through in silico approaches. The cytotoxicity and antiviral activity of the compound were assessed using Vero cells. In addition, in silico studies were also performed through molecular docking, molecular dynamics simulations, Molecular Mechanics Poisson–Boltzmann surface area (MM/PBSA), and quantum-mechanical analysis in order to evaluate the interaction with the Gc protein of OROV. The assay revealed that the compound was highly active against the virus, inhibiting OROV with an EC50 value of 53.5 ± 26.5 µM under post-infection treatment conditions. The present study demonstrates that the compound is a promising antiviral agent; however, the mechanisms of action proposed in this study need to be experimentally verified by future assays. Full article

Zika virus (ZIKV) has re-emerged in recent decades, leading to outbreaks of Zika fever in Africa, Asia, and Central and South America. Despite its drastic re-emergence and clinical impact, no vaccines or antiviral compounds are available to prevent or control ZIKV infection. This study evaluated the potential antiviral activity of quercetin hydrate against ZIKV infection and demonstrated that this substance inhibits virus particle production in A549 and Vero cells under different treatment conditions. In vitro antiviral activity was long-lasting (still observed 72 h post-infection), suggesting that quercetin hydrate affects multiple rounds of ZIKV replication. Molecular docking indicates that quercetin hydrate can efficiently interact with the specific allosteric binding site cavity of the NS2B-NS3 proteases and NS1-dimer. These results identify quercetin as a potential compound to combat ZIKV infection in vitro. Full article

Brassica rapa L. ssp. pekinensis (Lour.) Hanelt (kimchi cabbage) is a major vegetable cultivated in Korea, and its hairy roots (HRs) are rich in glucosinolates and phenolic compounds. This study aimed to induce HRs from cotyledon explants via the transformation of the Agroacterium rhizogenes strain R1000 and examine the glucosinolate and phenolic compounds present in the HRs of two kimchi cabbage (green and red) cultivars after exposure to 16 h light/8 h dark conditions (photosynthetic photon flux density of 54.6 µmol m⁻² s⁻¹) and continuous dark conditions. The highest HR production was achieved in the green kimchi cabbage grown under dark conditions (0.37 ± 0.01 DW g/30 mL). The highest glucosinolate and phenolic contents were neoglucobrassicin and catechin hydrate, which were highest in the green kimchi HRs grown under dark (GKHD) conditions (5268.29 ± 292.84 µg/g DW) and green HRs grown under light (GKHL) conditions (203.49 ± 4.70 µg/g DW), respectively. A heat map showed that the red kimchi HRs grown under dark conditions (RKHD) and the GKHL condition accumulated the highest glucosinolate and phenolic contents. Principal component (PCA) and partial least-squares discriminant (PLS-DA) analyses of the 13 identified metabolites showed a clear separation. According to a variable importance in projection (VIP) analysis, quercetin was the most important metabolite, leading to a clear separation. The most suitable conditions for enhancing the glucosinolate and phenolic contents were the GKHD and GKHL conditions, respectively, whereas both compounds were enhanced in the RKHD condition. HRs cultures cultivated under light and dark conditions are a promising method to enhance the production of specific health-promoting bioactive metabolites, which might be helpful in the pharmaceutical and nutraceutical industries. Full article

There are a plethora of plant species in India, which have been widely used in vegetable dishes, soups, desserts and herbal medicine. In addition to these traditional uses, today there is the extra possibility of also being able to use these plants in the nutritional supplements industry due to their favorable antioxidant and mineral composition. In this sense, thirteen vegetable species—Chanania lanzan, Ziziphus mauritiana, Nilumbo nucifera, Terminalia catappa, Terminalia arjuna, Terminalia bellirica, Terminalia chebula, Lagenaria siceraria, Luffa aegyptiaca, Praecitrullus fistulosus, Benincasa hispida, Citrullus lanatus var. lanatus and Cucurbita maxima—have been analyzed. In this paper we discuss the distribution of polyphenols and minerals (Na, K, Mg, Ca, Al, P, S, Cr, Mn, Fe, Cu, Zn, Mo, As and Pb) in different seed parts (the rhizome, pericarp, carpel, seed coat and kernel) of the above species and their possible use in the nutritional supplements industry. The concentrations of total polyphenols, flavonoids and minerals ranged from 407 to 3144 mg rutin hydrate/100 g, 24 to 3070 mg quercetin/100 g and 1433 to 7928 mg/100 g, respectively. K, Ca, P and S were abundant in these herbal fruits. In two species of herbal fruits, Terminalia arjuna and Terminalia chebula, only part of the seed structure was suitable for use in nutritional supplements. Full article

With the aim to develop essential oil (EO) multi-antioxidant systems, combinatorial interactions of selected phenol and terpene-rich EOs (from Pimento Berry, Ceylon Cinnamon, Clove, Sage, White thyme; Oregano) enriched with individual polyphenols, crude plant extracts, and mixtures of their major polyphenols were investigated using single electron transfer (SET)-based DPPH and hydrogen atom transfer (HAT)-based ORAC assays. Polyphenols that enriched Eos the most favorably were rosmarinic acid (IC₅₀ of 0.0891–0.1448 mg enriched EO/mg DPPH; 5772–17,879 µmol TE/g enriched EO) and quercetin (IC₅₀ of 0.0682–0.1060 mg enriched EO/mg DPPH; Trolox Equivalents (TE) of 9776–14,567µmol /g enriched EO), whereas p-coumaric acid (IC₅₀ of 0.1865–1.1424 mg enriched EO/mg DPPH; 7451.00–11,588 µmol TE/g enriched EO) and rutin hydrate (IC₅₀ of 0.1140–0.3112 mg enriched EO/mg DPPH; 2298–6227 µmol TE/g enriched EO) were the least favorable. Enrichments with polyphenol mixes and crude extracts exhibited synergistic and additive effects in the SET-based DPPH assay. In the HAT-based ORAC assay, EO enrichments with crude extracts exhibited more additive effects, as well as less antagonistic effects, than enrichments with their major polyphenol mixes, revealing the significant contributions of minor compounds. EOs enriched with crude green tea and apple extracts exhibited synergistic or additive effects, whereas EOs enriched with grape seed and rosemary extracts exhibited equal antagonistic effects. Predictive models were developed to explain the variability between the observed and predicted antioxidant activities of enriched EOs. Full article