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1.
Molecules ; 27(4)2022 Feb 15.
Artigo em Inglês | MEDLINE | ID: mdl-35209106

RESUMO

Quercetin, a flavonoid with promising therapeutic potential, has been shown to protect from cisplatin nephrotoxicity in rats following intraperitoneal injection, but its low bioavailability curtails its prospective clinical utility in oral therapy. We recently developed a micellar formulation (P-quercetin) with enhanced solubility and bioavailability, and identical nephroprotective properties. As a first aim, we herein evaluated the oral treatment with P-quercetin in rats, which displayed no nephroprotection. In order to unravel this discrepancy, quercetin and its main metabolites were measured by HPLC in the blood and urine after intraperitoneal and oral administrations. Whilst quercetin was absorbed similarly, the profile of its metabolites was different, which led us to hypothesize that nephroprotection might be exerted in vivo by a metabolic derivate. Consequently, we then aimed to evaluate the cytoprotective capacity of quercetin and its main metabolites (quercetin 3-O-glucoside, rutin, tamarixetin, isorhamnetin and quercetin 3-O-glucuronide) against cisplatin toxicity, in HK-2 and NRK-52E tubular cell lines. Cells were incubated for 6 h with quercetin, its metabolites or vehicle (pretreatment), and subsequently 18 h in cotreatment with 10-300 µM cisplatin. Immediately after treatment, cell cultures were subject to the MTT technique as an index of cytotoxicity and photographed under light microscopy for phenotypic assessment. Quercetin afforded no direct cytoprotection and quercetin-3-O-glucuronide was the only metabolite partially preventing the effect of cisplatin in cultured tubule cells. Our results identify a metabolic derivative of quercetin contributing to its nephroprotection and prompt to further explore exogenous quercetin-3-O-glucuronide in the prophylaxis of tubular nephrotoxicity.


Assuntos
Cisplatino/farmacologia , Citoproteção/efeitos dos fármacos , Células Epiteliais/efeitos dos fármacos , Túbulos Renais/efeitos dos fármacos , Substâncias Protetoras/farmacologia , Quercetina/análogos & derivados , Animais , Linhagem Celular , Células Cultivadas , Cromatografia Líquida de Alta Pressão , Cisplatino/efeitos adversos , Taxa de Filtração Glomerular , Testes de Função Renal/métodos , Túbulos Renais/citologia , Quercetina/farmacologia , Ratos
2.
Compr Rev Food Sci Food Saf ; 21(1): 453-476, 2022 01.
Artigo em Inglês | MEDLINE | ID: mdl-34773427

RESUMO

The wastes generated during the olive oil extraction process, even if presenting a negative impact for the environment, contain several bioactive compounds that have considerable health benefits. After suitable extraction and purification, these compounds can be used as food antioxidants or as active ingredients in nutraceutical and cosmetic products due to their interesting technological and pharmaceutical properties. The aim of this review, after presenting general applications of the different types of wastes generated from this industry, is to focus on the olive pomace produced by the two-phase system and to explore the challenging applications of the main individual compounds present in this waste. Hydroxytyrosol, tyrosol, oleuropein, oleuropein aglycone, and verbascoside are the most abundant bioactive compounds present in olive pomace. Besides their antioxidant activity, these compounds also demonstrated other biological properties such as antimicrobial, anticancer, or anti-inflammatory, thus being used in formulations to produce pharmaceutical and cosmetic products or in the fortification of food. Nevertheless, it is mandatory to involve both industries and researchers to create strategies to valorize these byproducts while maintaining environmental sustainability.


Assuntos
Olea , Antioxidantes , Resíduos Industriais/análise , Azeite de Oliva , Extratos Vegetais
3.
Molecules ; 26(14)2021 Jul 12.
Artigo em Inglês | MEDLINE | ID: mdl-34299493

RESUMO

Dietary polyphenols have been associated with health benefits in the prevention of a range of degenerative and age-related diseases that constitute the major causes of death and incapacitation in developed countries [...].


Assuntos
Polifenóis/farmacologia , Antioxidantes/metabolismo , Flavonoides/farmacologia , Humanos , Extratos Vegetais/farmacologia
4.
Molecules ; 26(18)2021 Sep 12.
Artigo em Inglês | MEDLINE | ID: mdl-34577008

RESUMO

A considerable amount of literature has been published claiming the cardiovascular benefits of moderate (red) wine drinking, which has been considered a distinguishing trait of the Mediterranean diet. Indeed, red wine contains relevant amounts of polyphenols, for which evidence of their biological activity and positive health effects are abundant; however, it is also well-known that alcohol, even at a low level of intake, may have severe consequences for health. Among others, it is directly related to a number of non-communicable diseases, like liver cirrhosis or diverse types of cancer. The IARC classifies alcohol as a Group 1 carcinogen, causally associated with the development of cancers of the upper digestive tract and liver, and, with sufficient evidence, can be positively associated with colorectum and female breast cancer. In these circumstances, it is tricky, if not irresponsible, to spread any message on the benefits of moderate wine drinking, about which no actual consensus exists. It should be further considered that other hallmarks of the Mediterranean diet are the richness in virgin olive oil, fruits, grains, and vegetables, which are also good sources of polyphenols and other phytochemicals, and lack the risks of wine. All of these aspects are reviewed in this article.


Assuntos
Dieta Mediterrânea , Polifenóis/química , Polifenóis/farmacologia , Vinho , Animais , Dieta Mediterrânea/efeitos adversos , Humanos , Azeite de Oliva/química , Azeite de Oliva/farmacologia , Resveratrol/farmacologia , Meio Social , Vinho/efeitos adversos
5.
Molecules ; 26(6)2021 Mar 10.
Artigo em Inglês | MEDLINE | ID: mdl-33802064

RESUMO

Caffeic and dihydrocaffeic acid are relevant microbial catabolites, being described as products from the degradation of different phenolic compounds i.e., hydroxycinnamoyl derivatives, anthocyanins or flavonols. Furthermore, caffeic acid is found both in free and esterified forms in many fruits and in high concentrations in coffee. These phenolic acids may be responsible for a part of the bioactivity associated with the intake of phenolic compounds. With the aim of progressing in the knowledge of the health effects and mechanisms of action of dietary phenolics, the model nematode Caenorhabditis elegans has been used to evaluate the influence of caffeic and dihydrocaffeic acids on lifespan and the oxidative stress resistance. The involvement of different genes and transcription factors related to longevity and stress resistance in the response to these phenolic acids has also been explored. Caffeic acid (CA, 200 µM) and dihydrocaffeic acid (DHCA, 300 µM) induced an increase in the survival rate of C. elegans under thermal stress. Both compounds also increased the mean and maximum lifespan of the nematode, compared to untreated worms. In general, treatment with these acids led to a reduction in intracellular ROS concentrations, although not always significant. Results of gene expression studies conducted by RT-qPCR showed that the favorable effects of CA and DHCA on oxidative stress and longevity involve the activation of several genes related to insulin/IGF-1 pathway, such as daf-16, daf-18, hsf-1 and sod-3, as well as a sirtuin gene (sir-2.1).


Assuntos
Ácidos Cafeicos/farmacologia , Estresse Fisiológico/efeitos dos fármacos , Animais , Antioxidantes/farmacologia , Caenorhabditis elegans/efeitos dos fármacos , Caenorhabditis elegans/metabolismo , Proteínas de Caenorhabditis elegans/efeitos dos fármacos , Proteínas de Caenorhabditis elegans/metabolismo , Ácidos Cafeicos/metabolismo , Expressão Gênica/efeitos dos fármacos , Expressão Gênica/genética , Longevidade/efeitos dos fármacos , Estresse Oxidativo/efeitos dos fármacos , Transdução de Sinais/efeitos dos fármacos , Estresse Fisiológico/genética , Fatores de Transcrição/efeitos dos fármacos
6.
Molecules ; 25(14)2020 Jul 13.
Artigo em Inglês | MEDLINE | ID: mdl-32668705

RESUMO

The nematode Caernohabditis elegans was introduced as a model organism in biological research by Sydney Brenner in the 1970s. Since then, it has been increasingly used for investigating processes such as ageing, oxidative stress, neurodegeneration, or inflammation, for which there is a high degree of homology between C. elegans and human pathways, so that the worm offers promising possibilities to study mechanisms of action and effects of phytochemicals of foods and plants. In this paper, the genes and pathways regulating oxidative stress in C. elegans are discussed, as well as the methodological approaches used for their evaluation in the worm. In particular, the following aspects are reviewed: the use of stress assays, determination of chemical and biochemical markers (e.g., ROS, carbonylated proteins, lipid peroxides or altered DNA), influence on gene expression and the employment of mutant worm strains, either carrying loss-of-function mutations or fluorescent reporters, such as the GFP.


Assuntos
Antioxidantes/farmacologia , Biomarcadores/metabolismo , Caenorhabditis elegans/fisiologia , Modelos Animais de Doenças , Estresse Oxidativo/efeitos dos fármacos , Compostos Fitoquímicos/farmacologia , Animais , Proteínas de Caenorhabditis elegans/metabolismo , Espécies Reativas de Oxigênio/metabolismo
7.
J Sci Food Agric ; 100(10): 3789-3802, 2020 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-32167171

RESUMO

Interactions between polyphenols and gut microbiota are indeed a major issue of current interest in food science research. Knowledge in this subject is progressing as the experimental procedures and analysis techniques do. The aim of this article is to critically review the more leading-edge approaches that have been applied so far in the study of the interactions between grape/wine polyphenols and gut microbiota. This is the case of in vitro dynamic gastrointestinal simulation models that try to mitigate the limitations of simple static models (batch culture fermentations). More complex approaches include the experimentation with animals (mice, rats, pigs, lambs and chicks) and nutritional intervention studies in humans. Main advantages and limitations as well as the most relevant findings achieved by each approach in the study of how grape/wine polyphenols can modulate the composition and/or functionality of gut microbiota, are detailed. Also, common findings obtained by the three approaches (in vitro, animal models and human nutritional interventions) such as the fact that the Firmicutes/Bacteroidetes ratio tends to decrease after the feed/intake/consumption of grape/wine polyphenols are highlighted. Additionally, a nematode (Caenorhabditis elegans) model, previously used for investigating the mechanisms of processes such as aging, neurodegeneration, oxidative stress and inflammation, is presented as an emerging approach for the study of polyphenols interacting gut microbiota. © 2020 Society of Chemical Industry.


Assuntos
Bactérias/metabolismo , Microbioma Gastrointestinal , Polifenóis/metabolismo , Vitis/química , Vinho/análise , Animais , Bactérias/classificação , Bactérias/genética , Bactérias/isolamento & purificação , Humanos , Modelos Animais , Vitis/metabolismo
8.
J Enzyme Inhib Med Chem ; 34(1): 519-527, 2019 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-30688117

RESUMO

Phytolacca, which belongs to the family of Phytolaccaceae, are known for their use in popular medicine. Bioactivity of five extracts from Phytolacca dioica seeds were evaluated in four bioassays. A selected group of compounds from the extract that displayed the best bioactivity was analysed. The ethyl acetate extract (EAE) possessed the highest content of phenolics, the highest inhibitory activity on the tyrosinase and xanthine oxidase enzymes and showed a high antioxidant activity. HPLC-DAD-MS was employed to identify the phenolics profile of the most active one (EAE). HSCCC analysis of the EAE led to the isolation of phytolaccoside B and a mixture of 4 isomers, isoamericanol B1, B2, C1 and C2. These isoamericanol isomers presented activity against tyrosinase and xanthine oxidase. Our results revealed for the first time an interesting biological activity of the extract and isolated compounds from P. dioica seeds, which could be considered as a source of bioactive molecules.


Assuntos
Antioxidantes/farmacologia , Inibidores Enzimáticos/farmacologia , Monofenol Mono-Oxigenase/antagonistas & inibidores , Phytolacca/química , Extratos Vegetais/farmacologia , Xantina Oxidase/antagonistas & inibidores , Antioxidantes/química , Antioxidantes/isolamento & purificação , Relação Dose-Resposta a Droga , Inibidores Enzimáticos/química , Inibidores Enzimáticos/isolamento & purificação , Humanos , Estrutura Molecular , Monofenol Mono-Oxigenase/metabolismo , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Relação Estrutura-Atividade , Xantina Oxidase/metabolismo
9.
Int J Mol Sci ; 20(2)2019 Jan 11.
Artigo em Inglês | MEDLINE | ID: mdl-30641871

RESUMO

Quercetin (Q) has rapid metabolism, which may make it worthwhile to focus on the potential activity of its metabolites. Our aim was to evaluate the triglyceride-lowering effects of Q metabolites in mature and pre-adipocytes, and to compare them to those induced by Q. 3T3-L1 mature and pre-adipocytes were treated with 0.1, 1 and 10 µM of Q, tamarixetin (TAM), isorhamnetin (ISO), quercetin-3-O-glucuronide (3G), quercetin-3-O-sulfate (3S), as well as with 3S and quercetin-4-O-sulfate (4S) mixture (3S+4S). Triglyceride (TG) content in both cell types, as well as free fatty acid (FFA) and glycerol in the incubation medium of mature adipocytes were measured spectrophotometrically. Gene expression was assessed by RT-PCR. In mature adipocytes, Q decreased TG at 1 and 10 µM, 3S metabolite at 1 and 10 µM, and 3S+4S mixture at 10 µM. 3S treatment modified the glucose uptake, and TG assembling, but not lipolysis or apoptosis. During differentiation, only 10 µM of ISO reduced TG content, as did Q at physiological doses. In conclusion, 3S metabolite but not ISO, 3G, 4S and TAM metabolites can contribute to the in vivo delipidating effect of Q.


Assuntos
Adipócitos/citologia , Quercetina/análogos & derivados , Quercetina/farmacologia , Triglicerídeos/metabolismo , Células 3T3-L1 , Adipócitos/efeitos dos fármacos , Adipócitos/metabolismo , Animais , Diferenciação Celular/efeitos dos fármacos , Dissacarídeos/química , Dissacarídeos/farmacologia , Relação Dose-Resposta a Droga , Ácidos Graxos não Esterificados/metabolismo , Perfilação da Expressão Gênica , Regulação da Expressão Gênica/efeitos dos fármacos , Glicerol/metabolismo , Metabolismo dos Lipídeos/efeitos dos fármacos , Camundongos , Quercetina/química
10.
Molecules ; 24(2)2019 Jan 16.
Artigo em Inglês | MEDLINE | ID: mdl-30654476

RESUMO

Protocatechuic acid (3,4-dihydroxybenzoic acid; PCA) is a phenolic acid present in plants as a secondary metabolite and is also produced in the human organism as a metabolite from the degradation of polyphenols by the intestinal microbiota, particularly of flavonoids. However, PCA, like most polyphenols, is biotransformed in the human body to different conjugates as sulfates, which are found circulating in blood and could be involved in the bioactivity of the original compound. This paper describes a simple process for the preparation of PCA monosulfates with satisfactory yields. Two compounds were obtained that were identified as PCA-3-sulfate and PCA-4-sulfate by mass spectrometry and ¹H and 13C nuclear magnetic resonance using one- and two-dimensional techniques (heteronuclear single-quantum coherence and heteronuclear multiple-bond correlation). Differential MS fragmentation behavior and UV spectra were observed for each compound, which could be used for their identification in samples of unknown composition. The described procedure can be used for the preparation of these polyphenol metabolites in view of their use in in vivo and in vitro studies, as well as standards for their analysis in biological fluids, to contribute to the elucidation of biological effects of dietary polyphenols.


Assuntos
Hidroxibenzoatos/síntese química , Sulfatos/síntese química , Espectroscopia de Ressonância Magnética Nuclear de Carbono-13 , Hidroxibenzoatos/química , Espectrometria de Massas , Estrutura Molecular , Espectroscopia de Prótons por Ressonância Magnética , Sulfatos/química
11.
BMC Microbiol ; 17(1): 159, 2017 Jul 14.
Artigo em Inglês | MEDLINE | ID: mdl-28709400

RESUMO

BACKGROUND: Many plants have been used in traditional medicine for their antibacterial, antifungal, antiprotozoal, antiviral, antidiarrhoeal, analgesic, antimalarial, antioxidant, anti-inflammatory and anticancer activities. In order to find novel antimicrobial and antiviral agents, the aim of the present study was the evaluation of the antibacterial and antibiofilm susceptibility of Asphodelus microcarpus leaves extract. Moreover, the antiviral activity and the phytochemical composition of the active extract were also determined. METHODS: Antimicrobial and antibiofilm activities of leaves ethanol extract of A. microcarpus were evaluated on 13 different microbial strains. We selected three different sets of microorganisms: (i) Gram-positive bacteria, (ii) Gram-negative bacteria and (iii) yeasts. The potential antiviral activity of A. microcarpus leaves ethanol extract was evaluated with a luciferase reporter gene assay in which the dsRNA-dependent RIG-I-mediated IFN-ß activation was inducted or inhibited by the Ebola virus VP35 protein. HPLC-DAD-MS was used to identify phenolic profile of the active extract. RESULTS: A. microcarpus leaves extract showed a potent inhibitory activity on Gram-positive bacteria while only a reduced inhibition was observed on Gram-negative bacteria. No activity was detected against Yeasts. The extract also showed an interesting antibiofilm motif on various bacterial strains (E. coli, S. aureus, S. haemolyticus and B. clausii). Moreover, this extract significantly affected the Ebola virus VP35 inhibition of the viral RNA (vRNA) induced IFN response. CONCLUSIONS: The overall results provide supportive data on the use of A. microcarpus as antimicrobial agent and a potential source of anti-viral natural products. Data collected set the bases for further studies for the identification of single active components and the development of new pharmaceuticals.


Assuntos
Anti-Infecciosos/farmacologia , Antivirais/farmacologia , Magnoliopsida/química , Extratos Vegetais/farmacologia , Anti-Infecciosos/química , Antivirais/química , Bactérias/efeitos dos fármacos , Bactérias/crescimento & desenvolvimento , Testes de Sensibilidade Microbiana , Extratos Vegetais/química , Folhas de Planta/química , Vírus/efeitos dos fármacos , Vírus/crescimento & desenvolvimento , Leveduras/efeitos dos fármacos , Leveduras/crescimento & desenvolvimento
12.
Chem Biodivers ; 14(8)2017 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-28488389

RESUMO

Neuroprotective potential of V. teucrium and V. jacquinii methanol extracts was analyzed. Chemical analysis of investigated extracts showed the presence of phenolic acid derivatives, flavonoids and one secoiridoid. The detected flavonoids derived from flavones (luteolin and isoscutellarein in V. jacquinii; apigenin, isoscutellarein and luteolin in V. teucrium) and flavonol (quercetin in V. jacquinii). Acteoside was the dominant compound in V. jacquinii, while plantamajoside and isoscutellarein 7-O-(6‴-O-acetyl)-ß-allosyl (1‴→2‴)-ß-glucoside were the major phenolics in V. teucrium. Additionally, the antineurodegenerative activity was tested at concentrations of 25, 50, and 100 µg/ml using acetylcholinesterase (AChE) and tyrosinase (TYR) assays. The inhibition of both enzymes was achieved with the investigated extracts, ranging from 22.78 to 35.40% for AChE and from 9.57 to 16.38% for TYR. There was no statistical difference between the activities of the analyzed extracts. Our data indicate that V. teucrium and V. jacquinii may have beneficial effects against Alzheimer's and Parkinson's disease.


Assuntos
Antioxidantes/química , Fármacos Neuroprotetores/química , Extratos Vegetais/química , Veronica/química , Acetilcolinesterase/química , Acetilcolinesterase/metabolismo , Antioxidantes/análise , Cromatografia Líquida de Alta Pressão , Flavonas/química , Flavonas/isolamento & purificação , Concentração Inibidora 50 , Monofenol Mono-Oxigenase/química , Monofenol Mono-Oxigenase/metabolismo , Fármacos Neuroprotetores/análise , Fármacos Neuroprotetores/metabolismo , Fenóis/análise , Fenóis/química , Extratos Vegetais/análise , Ligação Proteica , Espectrometria de Massas por Ionização por Electrospray , Veronica/metabolismo
13.
Int J Mol Sci ; 18(6)2017 May 28.
Artigo em Inglês | MEDLINE | ID: mdl-28555032

RESUMO

Dyslipidemia and oxidation of low density lipoproteins (LDL) are recognized as critical factors in the development of atherosclerosis. Healthy dietary patterns, with abundant fruit and vegetable consumption, may prevent the onset of these risk factors due to the presence of phytochemical compounds. Strawberries are known for their high content of polyphenols; among them, flavonoids are the major constituents, and it is presumed that they are responsible for the biological activity of the fruit. Nevertheless, there are only a few studies that actually evaluate the effects of different fractions isolated from strawberries. In order to assess the effects of two different strawberry extracts (whole methanolic extract/anthocyanin-enriched fraction) on the lipid profile and antioxidant status in human hepatocellular carcinoma (HepG2) cells, the triglycerides and LDL-cholesterol content, lipid peroxidation, intracellular reactive oxygen species (ROS) content and antioxidant enzymes' activity on cell lysates were determined. Results demonstrated that both strawberry extracts not only improved the lipid metabolism by decreasing triglycerides and LDL-cholesterol contents, but also improved the redox state of HepG2 cells by modulating thiobarbituric acid-reactive substances production, antioxidant enzyme activity and ROS generation. The observed effects were more pronounced for the anthocyanin-enriched fraction.


Assuntos
Antocianinas/química , Fragaria/química , Metanol/química , Extratos Vegetais/farmacologia , Antioxidantes/metabolismo , Células Hep G2 , Humanos , Peroxidação de Lipídeos/efeitos dos fármacos , Extratos Vegetais/química , Espécies Reativas de Oxigênio/metabolismo
14.
Molecules ; 22(3)2017 Feb 23.
Artigo em Inglês | MEDLINE | ID: mdl-28241497

RESUMO

This study aimed to determine the effect of gamma radiation on the preservation of phenolic compounds and on decontamination of dry herbs in terms of ochratoxin A (OTA) and aflatoxin B1 (AFB1), using Aloysia citrodora Paláu as a case study. For this purpose, artificially contaminated dry leaves were submitted to gamma radiation at different doses (1, 5, and 10 kGy; at dose rate of 1.7 kGy/h). Phenolic compounds were analysed by HPLC-DAD-ESI/MS and mycotoxin levels were determined by HPLC-fluorescence. Eleven phenolic compounds were identified in the samples and despite the apparent degradation of some compounds (namely verbasoside), 1 and 10 kGy doses point to a preservation of the majority of the compounds. The mean mycotoxin reduction varied between 5.3% and 9.6% for OTA and from 4.9% to 5.2% for AFB1. It was not observed a significant effect of the irradiation treatments on mycotoxin levels, and a slight degradation of the phenolic compounds in the irradiated samples was observed.


Assuntos
Cromatografia Líquida de Alta Pressão/métodos , Micotoxinas/efeitos da radiação , Fenóis/análise , Verbenaceae/química , Aflatoxina B1/efeitos da radiação , Animais , Linhagem Celular , Sobrevivência Celular/efeitos dos fármacos , Raios gama , Ocratoxinas/efeitos da radiação , Fenóis/farmacologia , Extratos Vegetais/química , Extratos Vegetais/efeitos da radiação , Folhas de Planta/química , Folhas de Planta/efeitos da radiação , Suínos , Verbenaceae/efeitos da radiação
15.
Molecules ; 22(2)2017 Feb 07.
Artigo em Inglês | MEDLINE | ID: mdl-28178217

RESUMO

Bee bread (BB) is a fermented mixture of plant pollen, honey, and bee saliva that worker bees use as food for larvae, and for young bees to produce royal jelly. In the present study, five BB samples, collected from Apis mellifera iberiensis hives located in different apiaries near Bragança, in the northeast region of Portugal, and one BB commercial sample were characterized by high-performance liquid chromatography coupled to a diode array detector and electrospray mass spectrometry (HPLC-DAD-ESI/MS) in terms of phenolic compounds, such as flavonoid glycoside derivatives. Furthermore, the samples were screened, using in vitro assays, against different human tumor cell lines, MCF-7 (breast adenocarcinoma), NCI-H460 (non-small cell lung cancer), HeLa (cervical carcinoma) and HepG2 (hepatocellular carcinoma), and also against non-tumor liver cells (porcine liver cells, PLP2). The main phenolic compounds found were flavonol derivatives, mainly quercetin, kaempferol, myricetin, isorhamnetin and herbacetrin glycoside derivatives. Thirty-two compounds were identified in the six BB samples, presenting BB1 and BB3 with the highest contents (6802 and 6480 µg/g extract, respectively) and the highest number of identified compounds. Two isorhamnetin glycoside derivatives, isrohamnetin-O-hexosyl-O-rutinoside and isorhamnetin-O-pentosyl-hexoside, were the most abundant compounds present in BB1; on the other hand, quercetin-3-O-rhamnoside was the most abundant flavonol in BB3. However, it was not possible to establish a correlation between the flavonoids and the observed low to moderate cytotoxicity (ranging from >400 to 68 µg/mL), in which HeLa and NCI-H460 cell lines were the most susceptible to the inhibition. To the authors' knowledge, this is the first report characterizing glycosidic flavonoids in BB samples, contributing to the chemical knowledge of this less explored bee product.


Assuntos
Antineoplásicos/química , Flavonoides/química , Própole/química , Antineoplásicos/farmacologia , Linhagem Celular Tumoral , Sobrevivência Celular/efeitos dos fármacos , Ensaios de Seleção de Medicamentos Antitumorais , Flavonoides/farmacologia , Humanos , Concentração Inibidora 50 , Portugal , Própole/farmacologia
16.
Molecules ; 22(1)2017 Jan 06.
Artigo em Inglês | MEDLINE | ID: mdl-28067835

RESUMO

Over the last few decades, polyphenols, and flavonoids in particular, have attracted the interest of researchers, as they have been associated with the health-promoting effects derived from diets rich in vegetables and fruits, including moderate wine consumption. Recent scientific evidence suggests that wine polyphenols exert their effects through interactions with the gut microbiota, as they seem to modulate microbiota and, at the same time, are metabolized by intestinal bacteria into specific bioavailable metabolites. Microbial metabolites are better absorbed than their precursors and may be responsible for positive health activities in the digestive system (local effects) and, after being absorbed, in tissues and organs (systemic effects). Differences in gut microbiota composition and functionality among individuals can affect polyphenol activity and, therefore, their health effects. The aim of this review is to integrate the understanding of the metabolism and mechanisms of action of wine polyphenols at both local and systemic levels, underlining their impact on the gut microbiome and the inter-individual variability associated with polyphenols' metabolism and further physiological effects. The advent of promising dietary approaches linked to wine polyphenols beyond the gut microbiota community and metabolism are also discussed.


Assuntos
Carboidratos da Dieta/administração & dosagem , Flavonoides/administração & dosagem , Microbioma Gastrointestinal/efeitos dos fármacos , Trato Gastrointestinal/efeitos dos fármacos , Polifenóis/administração & dosagem , Vinho/análise , Disponibilidade Biológica , Vasos Sanguíneos/efeitos dos fármacos , Doenças Cardiovasculares/prevenção & controle , Carboidratos da Dieta/metabolismo , Flavonoides/metabolismo , Microbioma Gastrointestinal/fisiologia , Trato Gastrointestinal/microbiologia , Humanos , Doenças Metabólicas/prevenção & controle , Polifenóis/metabolismo , Ensaios Clínicos Controlados Aleatórios como Assunto , Simbiose/fisiologia , Infecções Urinárias/prevenção & controle
17.
J Sci Food Agric ; 97(10): 3433-3444, 2017 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-28026017

RESUMO

BACKGROUND: Currently, there is growing interest in extracts derived from winery by-products because of their beneficial health properties, which are associated with the presence of bioactive compounds. In this paper, we have carried out the chemical characterization and in vitro colonic fermentation of four grape pomace (GP) extracts rich in polyphenols and dietary fibre. RESULT: Firstly, phenolic and dietary fibre composition of the GP extracts was determined. The highest individual phenolic concentrations corresponded to gallic and ellagic acids, followed by catechins and flavonols. The non-digestible fibre fraction ranged from 66% to 83% of the GP extracts, which indicated that they mainly contained non-digestible cell wall components. Secondly, when GP extracts were subjected to fermentation by faecal microbiota, a total of 16 bacterial phenolic metabolites were found in the fermented samples, confirming that polyphenols contained in the GP extracts were metabolized to different active metabolites by microbiota. In addition, the GP extracts tended to promote the growth of intestinal microbiota, although it was only significant for the Enterococcus group. CONCLUSION: These findings, together with other information available in the literature, support the high added value of products obtained from winery by-products. © 2016 Society of Chemical Industry.


Assuntos
Bactérias/metabolismo , Colo/metabolismo , Colo/microbiologia , Vitis/metabolismo , Resíduos/análise , Fezes/microbiologia , Fermentação , Frutas/química , Frutas/metabolismo , Humanos , Modelos Biológicos , Extratos Vegetais/química , Extratos Vegetais/metabolismo , Vitis/química
18.
BMC Complement Altern Med ; 16(1): 453, 2016 Nov 09.
Artigo em Inglês | MEDLINE | ID: mdl-27829416

RESUMO

BACKGROUND: Asphodelus microcarpus belongs to the family Liliaceae that include several medicinal plants. In the traditional medicine plants of the genus Asphodelus are used to treat skin disorders such as ectodermal parasites, psoriasis, microbial infection and for lightening freckles. In order to find novel skin depigmenting agents, the present work was carry out to evaluate antioxidant activity and tyrosinase inhibitory potential of leaves, flowers and tubers extracts of A. microcarpus. The phytochemical composition of the active extract was also evaluated. METHODS: Three different extracts (water, methanol and ethanol) from leaves, flowers and tubers of A. microcarpus were evaluated for their inhibitory effect on tyrosinase activity using L-3,4-dihydroxyphenylalanine (L-DOPA) as substrate. Inhibition of cellular tyrosinase activity and melanin production was also investigated in melanoma B16F10 cells. Antioxidant activity, total phenolic and flavonoids contents were determined using standard in vitro methods. HPLC-DAD-MS was used to identify phenolic profile of the active extract. RESULTS: The results showed that all extracts have a direct inhibitory anti-tyrosinase activity, with ethanolic extract from flowers (FEE) exhibiting the stronger effect. Kinetic analysis revealed that FEE acts as an uncompetitive inhibitor with a Ki value of 0.19 mg/mL. The same effect was observed in murine melanoma B16F10 cells. Cellular tyrosinase activity as well as melanin content were reduced in FEE-treated cells. The results were comparable to that of the standard tyrosinase inhibitor (kojic acid). Furthermore, the same extract showed the highest antioxidant activity and an elevated levels of total phenolics and flavonoid content. Eleven phenolic components were identified as chlorogenic acid, luteolin derivates, naringenin and apigenin. CONCLUSIONS: Our findings showed that FEE from A. microcarpus inhibits tyrosinase and exerted antimelanogenesis effect in B16F10 cells. This extract also showed the highest scavenging activity, which could be mainly attributed to its high levels of total polyphenols and flavonoids. These results suggest that A. microcarpus has a great potential as sources of bioactive compounds which could be used as depigmenting agents in skin disorders.


Assuntos
Antioxidantes/química , Liliaceae/química , Monofenol Mono-Oxigenase/antagonistas & inibidores , Extratos Vegetais/química , Preparações Clareadoras de Pele/química , Animais , Linhagem Celular Tumoral , Cinética , Melaninas/biossíntese , Camundongos , Monofenol Mono-Oxigenase/análise , Folhas de Planta/química
19.
Plant Physiol ; 166(4): 1972-84, 2014 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-25315603

RESUMO

Nitric oxide (NO) is a unique reactive nitrogen molecule with an array of signaling functions that modulates plant developmental processes and stress responses. To explore the mechanisms by which NO modulates root development, we used a pharmacological approach and NO-deficient mutants to unravel the role of NO in establishing auxin distribution patterns necessary for stem cell niche homeostasis. Using the NO synthase inhibitor and Arabidopsis (Arabidopsis thaliana) NO biosynthesis mutants (nitric oxide-associated1 [noa1], nitrate reductase1 [nia1] and nia2, and nia1 nia2 noa1), we show that depletion of NO in noa1 reduces primary root elongation and increases flavonol accumulation consistent with elevated reactive oxygen species levels. The elevated flavonols are required for the growth effect, because the transparent testa4 mutation reverses the noa1 mutant root elongation phenotype. In addition, noa1 and nia1 nia2 noa1 NO-deficient mutant roots display small root meristems with abnormal divisions. Concomitantly, auxin biosynthesis, transport, and signaling are perturbed. We further show that NO accumulates in cortex/endodermis stem cells and their precursor cells. In endodermal and cortical cells, the noa1 mutant acts synergistically to the effect of the wuschel-related homeobox5 mutation on the proximal meristem, suggesting that NO could play an important role in regulating stem cell decisions, which has been reported in animals.


Assuntos
Arabidopsis/fisiologia , Ácidos Indolacéticos/metabolismo , Óxido Nítrico/metabolismo , Reguladores de Crescimento de Plantas/metabolismo , Nicho de Células-Tronco/fisiologia , Transporte Biológico , Flavonóis/metabolismo , Homeostase , Meristema/fisiologia , Mutação , Nitratos/metabolismo , Raízes de Plantas/fisiologia , Caules de Planta/fisiologia , Espécies Reativas de Oxigênio/metabolismo , Transdução de Sinais
20.
Int J Mol Sci ; 16(8): 17870-84, 2015 Aug 04.
Artigo em Inglês | MEDLINE | ID: mdl-26247940

RESUMO

Strawberry polyphenols have been extensively studied over the last two decades for their beneficial properties. Recently, their possible use in ameliorating skin conditions has also been proposed; however, their role in preventing UVA-induced damage in cosmetic formulation has not yet been investigated. Skin is constantly exposed to several environmental stressors, such as UVA radiation, that induce oxidative stress, inflammation and cell death via the production of reactive oxygen species (ROS). In the present study, we assessed the potential photoprotective capacity of different strawberry-based formulations, enriched with nanoparticles of Coenzyme Q10 and with sun protection factor 10 (SPF10), in human dermal fibroblasts (HuDe) exposed to UVA radiation. We confirmed that strawberries are a very rich source of polyphenols, anthocyanins and vitamins, and possess high total antioxidant capacity. We also showed that strawberry extracts (25 µg/mL-1 mg/mL) exert a noticeable photoprotection in HuDe, increasing cell viability in a dose-dependent way, and that these effects are potentiated by the presence of CoQ10red (100 µg/mL). We have demonstrated for the first time that the topical use of strawberry extract may provide good photoprotection, even if more in-depth studies are strongly encouraged in order to evaluate the cellular and molecular effects of strawberry protection.


Assuntos
Antioxidantes/farmacologia , Fibroblastos/efeitos dos fármacos , Fragaria/química , Extratos Vegetais/farmacologia , Protetores Solares/farmacologia , Antioxidantes/química , Células Cultivadas , Fibroblastos/efeitos da radiação , Humanos , Extratos Vegetais/química , Protetores Solares/química , Raios Ultravioleta/efeitos adversos
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