•Antioxidant and anti-inflammatory activities of quercetin derivatives were studied.•Quercetin metabolites present in systemic circulation have potent biopotential.•Derivatization quercetin resulted ...in decrease of antioxidant activity.•Derivatization of quercetin does not significantly defines anti-inflammatory potential.•Metabolites should be included in defining biopotential of quercetin-rich diet.
Quercetin is hardly bioavailable and largely transformed to different metabolites. Although little is known about their biological activities, these metabolites are crucial for explanation of health benefits associated with quercetin dietary intake. In this study, the antioxidant and anti-inflammatory activities of six quercetin derivatives (quercetin-3-O-glucuronide, tamarixetin, isorhamnetin, isorhamnetin-3-O-glucoside, quercetin-3,4′-di-O-glucoside, quercetin-3,5,7,3′,4′-pentamethylether) were compared with the activity of common onion extract as the main source of dietary quercetin and standards (butylated hydroxytoluene and aspirin). The quercetin derivatives demonstrated notable bioactivities, similar to standards and onion. Derivatization of quercetin hydroxyl groups resulted in decrease of antioxidant potency. However, the number of quercetin free hydroxyl groups was not in direct correlation with its potential to inhibit inflammatory mediators production. To conclude, quercetin derivatives present in systemic circulation after consumption of quercetin may act as potent antioxidant and anti-inflammatory agents and can contribute to overall biological activity of quercetin-rich diet.
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•Efficacy of 6 solvents for natural products extraction from grape pomace was studied.•Ethyl acetate is the most efficient solvent for a wide range of phenolic classes.•Acidified 50% ...methanol proved to be the best option for extraction of anthocyanins.•Pomaces contain high amounts of triterpenoid ursolic acid, efficiently extracted with acetone.•80% MeOH is best for obtaining highest yield of phenolics for large scale industries.
Pomace is a winemaking by-product, rich in bioactive compounds which exert various health benefits and are used as dietary supplements, cosmetic ingredients, food colorants and preservatives. Isolation and further utilization of these compounds is an important issue in pomace waste management. Different industries have different requirements for specific classes of compounds and thus, selective extraction methods for isolation of these classes should be developed. In this work, the efficacy of six solvents (80% MeOH, 80% EtOH, EtOAc, acetone, acidified 50% and 80% MeOH) for the extraction of polyphenolic and triterpenoid compounds was examined. Pomaces of different grape varieties from Fruška Gora winery region in Serbia were used for extraction. 47 phenolics and 3 triterpenoids were analyzed by LC–MS/MS and 5 anthocyanin glucosides by LC-UV/VIS, while contents of total phenols and flavonoids were determined spectrophotometrically in obtained extracts. The most efficient solvent for each class and each compound was defined: EtOAc was the best for obtaining an extract rich in polyphenols, acidified 50% MeOH for isolation of anthocyanins, and acetone for ursolic acid. For industries that work on a large scale and aim at the highest utilization of raw material, 80% MeOH was found to be a solvent of choice, providing the highest yield of all polyphenols. This study confirmed that pomaces from Fruška Gora vineyards are a promising source of bioactive compounds, suggesting that their utilization could be very attractive for pharmaceutical, food and cosmetic industries.
Can Polyphenols Inhibit Ferroptosis? Lesjak, Marija; Simin, Nataša; Srai, Surjit K S
Antioxidants,
01/2022, Letnik:
11, Številka:
1
Journal Article
Recenzirano
Odprti dostop
Polyphenols, a diverse group of naturally occurring molecules commonly found in higher plants, have been heavily investigated over the last two decades due to their potent biological activities-among ...which the most important are their antioxidant, antimicrobial, anticancer, anti-inflammatory and neuroprotective activities. A common route of polyphenol intake in humans is through the diet. Since they are subjected to excessive metabolism in vivo it has been questioned whether their much-proven in vitro bioactivity could be translated to in vivo systems. Ferroptosis is a newly introduced, iron-dependent, regulated mode of oxidative cell death, characterized by increased lipid peroxidation and the accumulation of toxic lipid peroxides, which are considered to be toxic reactive oxygen species. There is a growing body of evidence that ferroptosis is involved in the development of almost all chronic diseases. Thus, ferroptosis is considered a new therapeutic target for offsetting many diseases, and researchers are putting great expectations on this field of research and medicine. The aim of this review is to critically analyse the potential of polyphenols to modulate ferroptosis and whether they can be considered promising compounds for the alleviation of chronic conditions.
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•Extracts increase Dox cytotoxicity against cancer cells, while protect normal cells.•Extracts had cardioprotective and myeloprotective effect in Dox-treated embryos.•Extracts ...increase the survival of Dox-treated zebrafish embryos.•Extracts inhibited angiogenesis better than sunitinib-malate and auranofin.•Extracts markedly potentiated inhibition of angiogenesis by Dox.
The objective of this study was to evaluate potential of two chemically characterized edible wild onion species, Allium flavum and Allium carinatum, to reduce side effects of cytostatic doxorubicin (Dox). Since Dox application is mainly limited due to its high cardiotoxicity, while there are no approved cardioprotective agents for the prevention of Dox adverse effects, new co-treatments are urgently needed. Here, we showed that methanol extracts expressed high antioxidant activity and synergistically increased Dox anticancer activity against human hepatoma (HepG2) and lung carcinoma (A549) cells, while protected normal human fibroblasts (MRC-5) from Dox cytotoxicity. Analysis of the antioxidative enzymes level (catalase and superoxide dismutases) showed that the catalase level was differently altered in cancer cells compared to normal cells upon applied treatments. In vivo toxicity evaluation in the zebrafish model revealed significantly lower toxicity of extracts compared to Dox, and no teratogenic effects at applied doses. We found that extracts successfully rescued the Dox-treated embryos of life-threating cardiomyopathy, while at the same time reduced developmental toxicity and neutropenia. Further analysis demonstrated that extracts had higher anti-angiogenic activity than sunitinib or auranofin, clinically used antiangiogenic drugs. In addition, angiogenesis was markedly more suppressed in Dox-extract cotreatments than upon single treatments.
Herbal products such as essential oils may play a promising role in the treatment of infections caused by gastrointestinal nematodes (GINs). The aim of this study was to evaluate the in vitro ...potential of 11 essential oils (EOs) and one binary combination of isolated EO compounds, as well as the in vivo anthelmintic efficacy of two EO formulations. Four GIN genera were identified in the coproculture examination:
,
,
and
. The in vitro egg hatch test (EHT) was performed at six different concentrations (50, 12.5, 3.125, 0.781, 0.195 and 0.049 mg/mL) for each EO, whereas in the in vivo faecal egg count reduction test (FECRT), each EO sample was diluted in sunflower oil and orally administrated at a dose of 100 mg/kg to the different group of animals. In the EHT, the EOs of
,
,
,
and two types of
were the most effective. The dominant compounds of these EOs were carvacrol, thymol, anethol, p-cymene and γ-terpinene, indicating their importance for the anthelmintic activity. In the FECRT, both
EO type 1 and linalool:estragole combination show an anthelmintic potential with a mean effect on FECR of approximately 25%. The results suggest the possible role of tested EOs as anthelmintic agents in sheep farms, although further in vivo tests are needed.
The development of anthelmintic resistance in sheep gastrointestinal nematodes (GINs) requires novel strategies for the sustainable control of these parasites. This study aimed to evaluate the ...anthelmintic efficacy of the
(L.) essential oil (EO) against sheep GINs and to evaluate the possibility of its use in control practice. The in vitro egg hatch test was conducted at eight different concentrations (50, 12.5, 3.125, 0.781, 0.195, 0.049, 0.025, and 0.0125 mg/mL) of the tested EO. For the in vivo fecal egg count reduction test, the EO of
was administrated orally at a mean single dose of 150 mg/kg to sheep from two farms in Southern Italy, whereby potential toxic effects to the hosts were also evaluated. In the egg hatch test, the inhibition of egg hatchability varied from 71.3% to 93.7%, depending on the concentration used. The high anthelmintic potential was confirmed in the fecal egg count reduction test with an average reduction of nematode eggs in feces of 43.2% and 60.1% on days 7 and 14 after treatment, respectively. In addition, no toxic effects were noticed during the clinical examination of sheep or by observing blood count and liver or kidney function test results. The obtained results suggest the strong activity of the
EO against sheep GINs, probably due to a high percentage of carvacrol (76.21%), whereby it can be considered safe for sheep at the dose tested in vivo. Therefore, it is suitable for use in veterinary practice as a part of an integrated strategy for the control of sheep GINs.
Ferroptosis is a recently discovered type of programmed cell death that is mechanistically different from other types of programmed cell death such as apoptosis, necroptosis, and autophagy. It is ...characterized by the accumulation of intracellular iron, overproduction of reactive oxygen species, depletion of glutathione, and extensive lipid peroxidation of lipids in the cell membrane. It was discovered that ferroptosis is interconnected with many diseases, such as neurodegenerative diseases, ischemia/reperfusion injury, cancer, and chronic kidney disease. Polyphenols, plant secondary metabolites known for many bioactivities, are being extensively researched in the context of their influence on ferroptosis which resulted in a great number of publications showing the need for a systematic review. In this review, an extensive literature search was performed. Databases (Scopus, Web of Science, PubMed, ScienceDirect, Springer) were searched in the time span from 2017 to November 2023, using the keyword "ferroptosis" alone and in combination with "flavonoid", "phenolic acid", "stilbene", "coumarin", "anthraquinone", and "chalcone"; after the selection of studies, we had 311 papers and 143 phenolic compounds. In total, 53 compounds showed the ability to induce ferroptosis, and 110 compounds were able to inhibit ferroptosis, and out of those compounds, 20 showed both abilities depending on the model system. The most researched compounds are shikonin, curcumin, quercetin, resveratrol, and baicalin. The most common modes of action are in the modulation of the Nrf2/GPX4 and Nrf2/HO-1 axis and the modulation of iron metabolism.
Rosehips are processed and consumed in numerous forms, such as juice, wine, herbal tea, yogurt, preserved fruit, and canned products. The seeds share in fruit is 30–35% and they have recently been ...recognized as an important source of oil rich in unsaturated fatty acids. However, after defatting, seed waste may still contain some polar polyphenolic compounds, which have been scarcely investigated. The aim of this study was to examine the potential of the defatted seed waste as a source of polyphenols. For the defatting process, supercritical carbon dioxide extraction at 300 bar and 40 °C was applied. The capacity of eight different natural deep eutectic solvents (NADES) for the recovery of phenolics from defatted rosehip seed powder (dRSP) was examined. In the extracts obtained with ultrasound-assisted NADES extraction, twenty-one phenolic compounds were identified with LC-MS/MS, among which the most abundant were quinic acid (22.43 × 103 µg/g dRSP) and catechin (571.93 µg/g dRSP). Ternary NADES formulations based on lactic acid proved to be superior. Potential correlations between identified chemical compounds, solvent polarity and viscosity, as well as the compound distributions across studied solvent combinations in PCA hyperspace, were also investigated. PCA demonstrated that more polar NADES mixtures showed improved extraction potential. The established environmentally friendly process represents an approach of transforming rosehip seed waste into value-added products with the potential to be applied in the food industry and to contribute to sustainable production.
Modern roses (Rosa × hybrida) are among the most important and economically profitable horticultural plants. Besides their beauty and remarkable fragrance, they are also rich sources of biologically ...active compounds with potential health benefits. The aim of this study was to valorize the prospective of six new genotypes of edible roses to be utilized as functional foods. Rose flowers were subjected to detailed characterization of morphological traits, fragrance analysis, GC-MS analysis of aroma carriers, determination of phenolic profile and vitamin C content, and evaluation of biological activities. The results showed that all the investigated cultivars have a favorable aroma for human consumption (pear-like, strawberry-like or fruity), high contents of phenolics and vitamin C, strong antioxidant content and moderate neuroprotective activity. They are characterized by large amounts of quercetin 3-O-glycosydes and quinic acid. The genotype ‘Marija Frayla’ stands out from others due to facilitated flower morphology, the highest level of total phenolics (217 mg of galic acid equivalents/g of dry extract) and the strongest antioxidant activity (in the DPPH assay, IC50 = 9.24 µg/mL; and antioxidant potential in the FRAP assay was 220 mg ascorbic acid equivalents/g of dry extract), thus represents the most valuable amendment to the development of novel functional food products. The ‘Eveline Wild’ genotype has the highest neuroprotective activity (68.5 ng of eserine equivalents/g of dry extract), thus might be applied in the prevention of dementia. The ‘Pear’ cultivar with the lowest phenolics content and biological activity has a mild, fruity aroma, thus can be used in everyday eating.
Garden roses, known as
×
, hold a prominent position as one of the most important and economically valuable plants in horticulture. Additionally, their products-essential oil, rose water, concrete, ...and concentrate-find extensive use in the cosmetic, pharmaceutical, and food industries, due to their specific fragrances and potential health benefits. Rose flowers are rich in biologically active compounds, such as phenolics, flavonoids, anthocyanins, and carotenoids. This study aims to investigate the potential of five new garden rose genotypes with intensely colored flowers to serve as sources of biologically active compounds. Phenolic profile was evaluated by determination of total phenolic (TPC), flavonoid (TFC), and monomeric anthocyanins (TAC) contents and LC-MS/MS analysis of selected compounds. Antioxidant activity was evaluated via DPPH and FRAP assays, neuroprotective potential via acethylcholinesterase inhibition assay, and antidiabetic activity viaα-amylase and α-glucosidase inhibition assays. The flowers of investigated genotypes were rich in phenolics (TPC varied from 148 to 260 mg galic acid eq/g de, TFC from 19.9 to 59.7 mg quercetin eq/g de, and TAC from 2.21 to 13.1 mg cyanidin 3-
-glucoside eq/g de). Four out of five genotypes had higher TPC than extract of
, the most famous rose cultivar. The dominant flavonoids in all investigated genotypes were glycosides of quercetin and kaempferol. The extracts showed high antioxidant activity comparable to synthetic antioxidant BHT, very high α-glucosidase inhibitory potential, moderate neuroprotective activity, and low potential to inhibit α-amylase.
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