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1.
J Med Microbiol ; 68(10): 1552-1559, 2019 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-31419210

RESUMO

Introductio n. Pseudomonas aeruginosa is an important Gram-negative pathogen that is intrinsically multidrug-resistant (MDR) and frequently associated with healthcare-associated outbreaks. With increasing resistance to antibiotics and with very few novel drugs under development, clinicians often use combinations to treat critically ill patients.Aim. The aim of this study was to evaluate the ability of epigallocatechin (EGCG) to restore the activity of aztreonam against clinical MDR strains of P. aeruginosa.Methodology. Checkerboard and time-kill kinetic assays were performed to assess synergy in vitro and the Galleria mellonella model of infection was used to test the efficacy of the combination in vivo. Accumulation assays were performed to gain insight into the mechanism of action.Results. The results demonstrate that synergy between aztreonam and EGCG exists [fractional inhibitory concentration indices (FICIs) 0.02-0.5], with the combination affording significantly (P=<0.05) enhanced bacterial killing, with a >3 log10 reduction in colony-forming units ml-1 at 24 h. EGCG was able to restore susceptibility to aztreonam to a level equal to or below the breakpoint set by the European Committee for Antimicrobial Susceptibility Testing. In G. mellonella, the combination was superior to monotherapy, with increased larval survival observed (94 % vs ≤63 %). We also demonstrated the relatively low toxicity of EGCG to human keratinocytes and G. mellonella larvae. Accumulation assay data suggest that the mechanism of synergy may be due to EGCG increasing the uptake of aztreonam.Conclusion. EGCG was able to restore the activity of aztreonam against MDR P. aeruginosa. The data presented support further evaluation of the aztreonam-EGCG combination and highlight its potential for use in clinical medicine.


Assuntos
Antibacterianos/farmacologia , Aztreonam/farmacologia , Catequina/análogos & derivados , Polifenóis/farmacologia , Infecções por Pseudomonas/microbiologia , Pseudomonas aeruginosa/efeitos dos fármacos , Animais , Catequina/farmacologia , Farmacorresistência Bacteriana Múltipla , Sinergismo Farmacológico , Humanos , Larva/efeitos dos fármacos , Testes de Sensibilidade Microbiana , Mariposas/efeitos dos fármacos , Pseudomonas aeruginosa/crescimento & desenvolvimento
2.
Int J Nanomedicine ; 14: 4413-4428, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-31417252

RESUMO

Background: As part of our continuing quest to enhance the efficacy of bioactive phytochemicals in cancer therapy, we report an innovative green nanotechnology approach toward the use of resveratrol for the production of biocompatible resveratrol-conjugated gold nanoparticles (Res-AuNPs). Our overarching aim is to exploit the inherent pro-apoptotic properties of gold nanoparticles (AuNPs) through synergistic anti-tumor characteristics of resveratrol, with the aim of developing a new class of green nanotechnology-based phytochemical-embedded AuNPs for applications in oncology. Method: Resveratrol was used to reduce Au3+ to Au0 for the synthesis of Res-AuNPs at room temperature and gum arabic (GA) was used to further encapsulate the nanoparticulate surface to increase the overall stability of the AuNPs. This comprehensive study involves the synthesis, full characterization and in vitro stability of Res-AuNPs in various biological media for their ultimate applications as anti-cancer agents against human breast (MDAMB-231), pancreatic (PANC-1) and prostate (PC-3) cancers. Results: This strategy to systematically increase the corona of resveratrol on AuNPs, in order to gain insights into the interrelationship of the phytochemical corona on the overall anti-tumor activities of Res-AuNPs, proved successful. The increased resveratrol corona on Res-AuNPs showed superior anti-cancer effects, attributed to an optimal cellular uptake after 24-hour incubation, while GA provided a protein matrix support for enhanced trans-resveratrol loading onto the surface of the AuNPs. Conclusion: The approach described in this study harnesses the benefits of nutraceuticals and nanoparticles toward the development of Res-AuNPs. We provide compelling evidence that the increased corona of resveratrol on AuNPs enhances the bioavailability of resveratrol so that therapeutically active species can be optimally available in vivo for applications in cancer therapy.


Assuntos
Antineoplásicos/farmacologia , Neoplasias da Mama/patologia , Ouro/química , Nanopartículas Metálicas/química , Neoplasias Pancreáticas/patologia , Neoplasias da Próstata/patologia , Resveratrol/farmacologia , Linhagem Celular Tumoral , Forma Celular/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Endocitose , Feminino , Humanos , Concentração Inibidora 50 , Masculino , Nanopartículas Metálicas/ultraestrutura , Tamanho da Partícula , Polifenóis/química , Polifenóis/farmacologia , Resveratrol/química , Espectrofotometria Ultravioleta , Resultado do Tratamento
3.
Fitoterapia ; 137: 104254, 2019 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-31271782

RESUMO

Five new polyphenolic derivatives, sepiumols A-E (1-5), were isolated from the root barks of Periploca sepium. Their structures were elucidated by interpretation of NMR spectroscopic and mass spectrometric data. Compounds 1, 3 and 5 were found to exhibit significant antifungal activity, particularly for 3 with the remarkable activity against Gibberella saubinetii and Alternaria longipes with MIC values of 1.56 and 3.13 µg/mL (ketoconazole: 0.78 µg/mL), respectively. In addition, compounds 1, 3 and 5 also displayed significant antibacterial activity against methicillin-resistant Staphylococcus aureu with MIC values of 12.50-25 µg/mL (ciprofloxacin: 0.78 µg/mL).


Assuntos
Antibacterianos/farmacologia , Antifúngicos/farmacologia , Periploca/química , Polifenóis/farmacologia , Alternaria/efeitos dos fármacos , Antibacterianos/isolamento & purificação , Antifúngicos/isolamento & purificação , Gibberella/efeitos dos fármacos , Staphylococcus aureus Resistente à Meticilina/efeitos dos fármacos , Estrutura Molecular , Compostos Fitoquímicos/isolamento & purificação , Compostos Fitoquímicos/farmacologia , Casca de Planta/química , Raízes de Plantas/química , Polifenóis/isolamento & purificação
4.
Zhongguo Ying Yong Sheng Li Xue Za Zhi ; 35(3): 209-214, 2019 May 28.
Artigo em Chinês | MEDLINE | ID: mdl-31257800

RESUMO

OBJECTIVE: To investigate the effects of apple polyphenols on pulmonary vascular remodeling in rats with pulmonary arterial hypertension and its mechanism. METHODS: Rats were randomly divided into 4 groups:control (Con) group, monocrotaline (MCT) group, apple polyphenol (APP) group,monocrotaline + apple polyphenol (MCT+APP) group. In Con group, rats received a subcutaneous injection of physical saline. In APP group, rats received intraperitoneal injection of 20 mg/kg APP, every other day. In MCT group, rats received a single subcutaneous injection of MCT(60 mg/kg). In MCT+APP group, rats received subcutaneous injection of 60 mg/kg MCT followed by an intraperitoneal injection of 20 mg/kg APP every other day. All the disposal lasted 3 weeks. Then the PAH-relevant indicators, such as mean pulmonary artery pressure(mPAP), pulmonary vascular resistance(PVR), right ventricular hypertrophy index (RVHI) ,wall thickness (WT%) and wall area (WA%) were tested. After that, the inflammatory pathway related indicators, such as interleukin1(IL-1),interleukin1(IL-6), tumor necrosis factor α(TNF-α), cyclooxygenase 2(COX-2) and myeloperoxidase(MPO) in pulmonary tissue and free intracellular Ca2+ in pulmonary smooth muscle cell(PASMC), content of eNOS and NO in endothelial cells were determined. RESULTS: Compared with the control group, the levels of mPAP, PVR, RVHI, WA%, WT%, and IL-1, IL-6, TNF-α, COX-2, MPO in tissue and the expression of Ca2 + in PASMC of MCT group were increased significantly, while the contents of eNOS and NO in endothelial cells were decreased significantly (P<0.05). Compared with the MCT group, the apple polyphenol treatment could improve the above mentioned situation, and the COX-2 and Ca2+ indicators of the apple polyphenol treatment group were decreased significantly (P<0.05). CONCLUSION: MCT can increase COX-2 expression and intracellular Ca2+ in pulmonary artery smooth muscle cells, decrease the contents of eNOS and NO in endothelial cells, while apple polyphenols can significantly inhibit these effects.


Assuntos
Malus/química , Polifenóis/farmacologia , Artéria Pulmonar/efeitos dos fármacos , Remodelação Vascular/efeitos dos fármacos , Animais , Cálcio/metabolismo , Ciclo-Oxigenase 2/metabolismo , Citocinas/metabolismo , Monocrotalina , Óxido Nítrico/metabolismo , Óxido Nítrico Sintase Tipo III/metabolismo , Artéria Pulmonar/patologia , Distribuição Aleatória , Ratos
5.
Food Chem ; 299: 125124, 2019 Nov 30.
Artigo em Inglês | MEDLINE | ID: mdl-31288163

RESUMO

Inflammation plays a key role in diseases such as diabetes, asthma, cardiovascular diseases and cancer. Diet can influence different stages of inflammation and can have an important impact on several inflammatory diseases. Increasing scientific evidence has shown that polyphenolic compounds, such as flavonoids, which are found in fruits, vegetables, legumes, or cocoa, can have anti-inflammatory properties. Recent studies have demonstrated that flavonoids can inhibit regulatory enzymes or transcription factors important for controlling mediators involved in inflammation. Flavonoids are also known as potent antioxidants with the potential to attenuate tissue damage or fibrosis. Consequently, numerous studies in vitro and in animal models have found that flavonoids have the potential to inhibit the onset and development of inflammatory diseases. In the present review, we focused in flavonoids, the most abundant polyphenols in the diet, to give an overview of the most recent scientific knowledge about their impact on different inflammatory diseases.


Assuntos
Anti-Inflamatórios/farmacologia , Antioxidantes/farmacologia , Doenças Cardiovasculares/tratamento farmacológico , Flavonoides/farmacologia , Inflamação/tratamento farmacológico , Neoplasias/tratamento farmacológico , Animais , Anti-Inflamatórios/análise , Antioxidantes/análise , Cacau/química , Doenças Cardiovasculares/patologia , Dieta , Fabaceae/química , Flavonoides/análise , Frutas/química , Humanos , Neoplasias/patologia , Polifenóis/análise , Polifenóis/farmacologia , Verduras/química
6.
J Food Sci ; 84(7): 1692-1702, 2019 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-31206188

RESUMO

Oak wood is used in barrels for wine aging. During aging, polyphenols are transferred from the barrels to the liquid. Although the bioactivity of oak polyphenols in wines has been extensively studied, no investigation exists on their toxicological properties, which limits their use as functional safe ingredients for other products. In this work, the chemical composition of a polyphenolic extract of Quercus crassifolia bark (QCBe) was studied by GC-MS. Its antibacterial properties on probiotic and pathogenic bacteria and its subacute-oral toxicity were determined as a way to understand the potential impact from its addition to fermented food as a functional ingredient. QCBe shows a selective inhibition of Escherichia coli compared with Lactobacillus bulgaricus and Streptococcus thermophylus. According to the toxicity evaluation, the subacute no-observed-adverse-effect-level was achieved at 11 mg/kg bw/day, whereas the subacute lowest-observed-adverse-effect-level for kidney damage was at 33 mg/kg bw/day. These results suggest that, given the fact an adverse effect was observed after subacute administration of this extract, further longer term toxicological studies are needed to provide sufficient safety evidence for its use in humans. PRACTICAL APPLICATION: Mexico's yogurt market is growing which creates opportunities for the development of some yogurt products as functional foods. As a first step to evaluate its potential use in yogurt formulation, the antibacterial effect of a Quercus crassifolia polyphenolic extract (QCBe) on probiotic bacteria and its subacute-oral toxicity in rats were studied. A low inhibition on probiotic bacteria growth was observed after QCBe addition to Lactobacillus bulgaricus and Streptococcus thermophylus cultures. Exposure to QCBe for a subacute duration resulted in renal injury in rats at dosages greater than or equal to 33 mg/kg/bw/day. This adverse effect indicates the importance of performing further long-term toxicological assessments prior to the addition of QCBe to a food like yogurt, which is regularly eaten by consumers.


Assuntos
Antibacterianos/farmacologia , Casca de Planta/química , Extratos Vegetais/farmacologia , Polifenóis/farmacologia , Quercus/química , Animais , Antibacterianos/química , Antibacterianos/toxicidade , Bactérias/efeitos dos fármacos , Aditivos Alimentares/química , Aditivos Alimentares/farmacologia , Aditivos Alimentares/toxicidade , Alimento Funcional/análise , Cromatografia Gasosa-Espectrometria de Massas , Humanos , México , Nível de Efeito Adverso não Observado , Casca de Planta/toxicidade , Extratos Vegetais/química , Extratos Vegetais/toxicidade , Polifenóis/química , Polifenóis/toxicidade , Quercus/toxicidade , Ratos , Vinho/análise , Madeira/efeitos adversos , Madeira/química , Iogurte/análise
7.
Chem Biol Interact ; 310: 108711, 2019 Sep 01.
Artigo em Inglês | MEDLINE | ID: mdl-31207224

RESUMO

Gastrointestinal infections are considered a serious public health problem in view of their high incidence and the increasing antibiotic resistance of the microorganisms involved in their pathogenesis, namely Escherichia coli. Consequently, finding new ways to prevent and/or threat these infections is urgent. In this study we investigated whether a well-characterised polyphenolic red wine extract is able to inhibit the cytotoxic effects induced by a clinical pathogenic Escherichia coli strain (E. coli 270) against HT-29 colon epithelial cells. Firstly, we provide evidences showing that the E. coli strain triggered the death of the intestinal epithelial cells through the production and release of a toxin. Then we support that, in a concentration dependent way, RWE through both, a direct interaction with bacterial exotoxin and the epithelial cells, prevented the action of the toxin on the cells, significantly reducing cell death. This intends to constitute a position paper as detailed mechanisms for the inhibition of E. coli-induced toxicity by polyphenols are yet to be completely unraveled. However, considering that the amount of red wine polyphenols used can be easily achieved in a normal diet, this study suggests that RWE may provide a readily available dietary product with potential benefit for the prevention and/or treatment of intestinal infections induced by intestinal pathogenic bacteria and may open new therapeutic avenues for the development of potential natural antimicrobial agents.


Assuntos
Infecções por Escherichia coli/prevenção & controle , Gastroenteropatias/prevenção & controle , Polifenóis/uso terapêutico , Vinho , Morte Celular/efeitos dos fármacos , Células Epiteliais/patologia , Escherichia coli/efeitos dos fármacos , Escherichia coli/patogenicidade , Infecções por Escherichia coli/tratamento farmacológico , Gastroenteropatias/tratamento farmacológico , Gastroenteropatias/microbiologia , Células HT29 , Humanos , Polifenóis/farmacologia
8.
BMC Complement Altern Med ; 19(1): 145, 2019 Jun 21.
Artigo em Inglês | MEDLINE | ID: mdl-31226983

RESUMO

BACKGROUND: Previous research findings support an antimicrobial effect of polyphenols against a variety of pathogens, but there is no evidence of this effect against periodontal pathogens in complex biofilms. The purpose of this study was to evaluate the antimicrobial activity of red wine and oenological extracts, rich in polyphenols, against the periodontal pathogens Porphyromonas gingivalis, Aggregatibacter actinomycetemcomitans and Fusobacterium nucleatum and total bacteria growing in an in vitro oral biofilm static model. METHODS: A previously validated biofilm model, including Streptococcus oralis, Actinomyces naeslundii, Veillonella parvula, F. nucleatum, P. gingivalis and A. actinomycetemcomitans was developed on sterile hydroxyapatite discs. Red wine (and dealcoholized wine), and two polyphenols-rich extracts (from wine and grape seeds) were applied to 72 h biofilms by dipping the discs during 1 and 5 min in the wine solutions and during 30 s and 1 min in the oenological extracts. Resulting biofilms were analyzed by confocal laser scanning microscopy and viable bacteria (colony forming units/mL) were measured by quantitative polymerase chain reaction combined with propidium monoazide. A generalized linear model was constructed to determine the effect of the tested products on the viable bacterial counts of A. actinomycetemcomitans, P. gingivalis and F. nucleatum, as well on the total number of viable bacteria. RESULTS: The results showed that red wine and dealcoholized red wine caused reduction in viability of total bacteria within the biofilm, with statistically significant reductions in the number of viable P. gingivalis after 1 min (p = 0.008) and in A. actinomycetemcomitans after 5 min of exposure (p = 0.011) with red wine. No evidence of relevant antibacterial effect was observed with the oenological extracts, with statistically significant reductions of F. nucleatum after 30 s of exposure to both oenological extracts (p = 0.001). CONCLUSIONS: Although moderate, the antimicrobial impact observed in the total bacterial counts and counts of A. actinomycetemcomitans, P. gingivalis and F. nucleatum, encourage further investigations on the potential use of these natural products in the prevention and treatment of periodontal diseases.


Assuntos
Antibacterianos/farmacologia , Biofilmes/efeitos dos fármacos , Fusobacterium nucleatum/efeitos dos fármacos , Doenças Periodontais/microbiologia , Extratos Vegetais/farmacologia , Vinho/análise , Aggregatibacter actinomycetemcomitans/efeitos dos fármacos , Aggregatibacter actinomycetemcomitans/fisiologia , Fusobacterium nucleatum/fisiologia , Humanos , Polifenóis/farmacologia , Porphyromonas gingivalis/efeitos dos fármacos , Porphyromonas gingivalis/fisiologia , Sementes/química , Vitis/química
9.
J Agric Food Chem ; 67(25): 7157-7166, 2019 Jun 26.
Artigo em Inglês | MEDLINE | ID: mdl-31146527

RESUMO

Lonicera caerulea berry polyphenols (LCBP) are known to reduce cholesterol accumulation. Currently, it is unknown whether LCBP can activate Sirtuin 1 (SIRT1) to regulate the formation of RAW264.7 macrophage foam cells. In this study, the effect of LCBP on lipid accumulation in macrophages was evaluated. Fluorescently labeled ox-LDL and 25-NBD cholesterol were used to detect the ox-LDL uptake and cholesterol outflow rate from macrophages. Gene silencing was performed using siRNA to detect changes in the expression of the ATP-binding cassette transporter A1 (ABCA1), sterol regulatory element-binding protein 2 (SREBP2), and SIRT1 proteins using Western blotting, and changes in the expression of miR-33 were detected by real-time polymerase chain reaction. The results showed that treatment with 80 µg/mL LCBP significantly inhibited the accumulation of lipids in RAW264.7 macrophages induced by ox-LDL and reduced intracellular cholesterol levels by activating SIRT1 to enhance the expression of ABCA1, a cholesterol efflux gene, but not independent effect. Of the three key LCBP components investigated, chlorogenic acid was found to activate SIRT1 and regulate the expression of the cholesterol-related factors ABCA1, SREBP2, and miR-33; cyanidin-3-glucoside and catechins were effective to a lesser extent. Our results suggest a novel hypolipidemic mechanism of LCBP.


Assuntos
Colesterol/metabolismo , Células Espumosas/efeitos dos fármacos , Lonicera/química , Macrófagos/efeitos dos fármacos , Polifenóis/farmacologia , Sirtuína 1/metabolismo , Transportador 1 de Cassete de Ligação de ATP/genética , Transportador 1 de Cassete de Ligação de ATP/metabolismo , Animais , Transporte Biológico/efeitos dos fármacos , Células Espumosas/metabolismo , Frutas/química , Lipoproteínas LDL/metabolismo , Macrófagos/metabolismo , Camundongos , Células RAW 264.7 , Sirtuína 1/genética , Proteína de Ligação a Elemento Regulador de Esterol 2/genética , Proteína de Ligação a Elemento Regulador de Esterol 2/metabolismo
10.
Life Sci ; 230: 208-217, 2019 Aug 01.
Artigo em Inglês | MEDLINE | ID: mdl-31152815

RESUMO

Mushroom Phellinus linteus ("Sanghuang" in Chinese) is a popular medicinal polypore used to treat several disorders through its various biological functions. Inonotus sanghuang is claimed to produce general immune-potentiating and strengthening, anti-inflammatory, anti-tumor and anti-microbial properties, but its effect on acute lung inflammation and oxidative stress are not clearly understood. To determine the effect and mechanism of the polyphenols-rich ethyl acetate fraction from wild I. sanghuang extract (ISE) on acute lung injury (ALI) induced by bleomycin (BLM), female C57BL/6 mice were fed ISE (0%, 0.15% or 0.6% in diet) for 4 weeks prior to challenge with BLM. Bronchoalveolar lavage fluid (BALF) from lung, spleen and lung tissues were collected on day 3 after BLM challenge for histological, oxidative stress, molecular and biochemical analysis. ISE supplementation improved pathological features in lung injury scores and reduced lung wet-to-dry ratios. Moreover, ISE reduced inflammatory cell infiltration and the pro-inflammatory cytokines including IL-1ß, IL-6 and TNF-α in BALF, decreased the MPO activity and the MDA level and increased the SOD, CAT and GSH-Px activities in lung tissue homogenates. Further mechanism analysis demonstrated that dietary ISE inhibited NF-κB signal. Finally, peripheral immune function analysis showed that ISE had less effect on immune response including splenocyte producing inflammatory cytokines and T cell proliferation except for IL-1ß and IL-2. Our findings indicate the possibility that dietary ISE attenuates ALI induced by BLM through correcting the inflammation and oxidation balance at least in part via inhibiting NF-κB signal in vivo, suggesting that ISE might be a valuable medicinal food effective in improving lung injury.


Assuntos
Lesão Pulmonar Aguda/tratamento farmacológico , Extratos Vegetais/farmacologia , Lesão Pulmonar Aguda/induzido quimicamente , Agaricales/isolamento & purificação , Agaricales/metabolismo , Animais , Antioxidantes/farmacologia , Bleomicina/farmacologia , Líquido da Lavagem Broncoalveolar/citologia , Citocinas/metabolismo , Feminino , Inflamação/patologia , Interleucina-1beta/farmacologia , Pulmão/patologia , Camundongos , Camundongos Endogâmicos C57BL , Fator 2 Relacionado a NF-E2/metabolismo , NF-kappa B/metabolismo , Estresse Oxidativo/efeitos dos fármacos , Polifenóis/isolamento & purificação , Polifenóis/farmacologia , Transdução de Sinais/efeitos dos fármacos , Fator de Necrose Tumoral alfa/farmacologia
11.
Molecules ; 24(9)2019 Apr 27.
Artigo em Inglês | MEDLINE | ID: mdl-31035535

RESUMO

Juçara berry is a potential inflammatory modulator, rich in dietary fiber, fatty acids, and anthocyanins. Considering this, we evaluated the high-fat diet (HFD) intake supplemented with different doses of freeze-dried juçara pulp on the TLR4 pathway. Twenty-seven male Wistar rats with ad libitum access to food and water were divided into four experimental groups: control standard chow group (C); high-fat diet control group (HFC); high-fat diet juçara 0.25% group (HFJ0.25%); and high-fat diet juçara 0.5% group (HFJ0.5%). The inflammatory parameters were analyzed by ELISA and Western blotting in liver and retroperitoneal adipose tissue (RET). The HFJ0.25% group had the energy intake, aspartate transaminase (AST) levels, and liver triacylglycerol accumulation reduced; also, the tumor necrosis factor α (TNF-α) and TNF receptor-associated factor 6 (TRAF6) expression in RET were reduced. However, there were no changes in other protein expressions in liver and adipose tissue. Adiposity and pNFκBp50 had a positive correlation in HFC and HFJ0.5%, but not in the C group and HFJ0.25%. The necrosis hepatic score did not change with treatment; however, the serum (AST) levels and the hepatic triacylglycerol were increased in HFC and HFJ0.5%. These results demonstrated that one week of HFD intake triggered pro-inflammatory mechanisms and liver injury. Additionally, 0.25% juçara prevented inflammatory pathway activation, body weight gain, and liver damage.


Assuntos
Anti-Inflamatórios/farmacologia , Euterpe/química , Frutas/química , Polifenóis/farmacologia , Tecido Adiposo/efeitos dos fármacos , Tecido Adiposo/metabolismo , Animais , Anti-Inflamatórios/química , Biomarcadores , Peso Corporal/efeitos dos fármacos , Citocinas/metabolismo , Dieta Hiperlipídica/efeitos adversos , Inflamação/tratamento farmacológico , Inflamação/etiologia , Inflamação/metabolismo , Inflamação/patologia , Mediadores da Inflamação/metabolismo , Metabolismo dos Lipídeos/efeitos dos fármacos , Fígado/efeitos dos fármacos , Fígado/metabolismo , Fígado/patologia , Masculino , NF-kappa B/metabolismo , Polifenóis/química , Ratos , Transdução de Sinais/efeitos dos fármacos
12.
Plant Physiol Biochem ; 141: 95-104, 2019 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-31136935

RESUMO

Biostimulants improve yield, quality, and stress acclimation in crops. In this work, we tested the possibility of using phenolics-rich extracts from spelt (Triticum dicoccum L.) husks to attenuate the effects of salt stress (100-200 mM NaCl) in maize. Two methanolic extracts were prepared from the soluble-conjugated (SC), and the insoluble-bound (IB) phenolic acid fractions of the spelt husk, and their effects were investigated on several stress-associated biochemical parameters, such as proline, lipid peroxidation, H2O2, GSH levels, and ion content. Results show that SC and IB fractions of husk extracts behaved very differently, no doubt due to their greatly divergent chemical composition, as revealed by both GC-MS and HPLC analyses. The efficacy of treatments in mitigating salt stress was also dose- and timing-dependent. IB, even at the lower concentration tested, was able to recover the performance of stressed plants in terms of growth, photosynthetic pigments content, and levels of salt stress markers. Recovery of shoot growth to control levels and reduction of stress-induced proline accumulation occurred regardless of whether plants were pre-treated or post-treated with IB, whereas only pre-treatment with the higher dose of IB was effective in mitigating oxidative stress. Although in some cases SC and even methanol alone exerted some positive effects, they could also be deleterious whereas IB never was. Overall, results indicate that a polyphenol-containing extract obtained from spelt by-products can behave as biostimulant in maize plants and can mitigate their response to salt stress, by acting on different biochemical targets.


Assuntos
Extratos Vegetais/farmacologia , Polifenóis/farmacologia , Estresse Salino , Triticum/química , Zea mays/química , Antioxidantes/química , Produtos Agrícolas/química , Cromatografia Gasosa-Espectrometria de Massas , Glutationa/química , Peróxido de Hidrogênio/química , Peroxidação de Lipídeos , Estresse Oxidativo , Fotossíntese , Compostos Fitoquímicos/química , Pigmentação , Folhas de Planta/química , Proteínas de Plantas/química , Potássio/química , Prolina/química , Tolerância ao Sal , Sódio/química
13.
BMC Complement Altern Med ; 19(1): 99, 2019 May 07.
Artigo em Inglês | MEDLINE | ID: mdl-31064377

RESUMO

BACKGROUND/OBJECTIVES: Type 2 diabetes (T2D) is a global pandemic, and contributes significantly to the increasing incidence of conditions such as cardiovascular disease (CVD). Postprandial plasma glucose measured 2-h after the start of a meal is a good indicator of the overall status of glucose homeostasis. Clove (Syzygium aromaticum L.) and its essential oils (eugenol and acetyl eugenol) have been shown in preclinical studies to modulate pathways involved in glucose homeostasis. In addition, a water-soluble polyphenolic extract of unopened clove buds was recently shown to benefit liver function and redox status. Therefore, we conducted an open-label pilot study to test whether this polyphenolic clove extract (PCE) could influence glucose metabolism. METHODS: We evaluated the effect of PCE supplementation (250 mg once daily for 30 days) on preprandial glucose levels and 2-h postprandial glucose levels in 13 otherwise healthy volunteers who were stratified into two groups according to their initial preprandial glucose levels: Group I (n = 7) ≤100 mg/dL, Group II (n = 6) - between 101 and 125 mg/dL. In an effort to elucidate the molecular mechanisms of PCE action, we tested in vitro the effects of PCE on glucose uptake, hepatocyte glucose production, and carbohydrate hydrolyzing enzymes. RESULTS: At day 12 of supplementation, we observed statistically significant reductions in mean postprandial glucose levels in both groups [(Group I: Initial - Day 12 PPG = 13.29 mg/dL, 95% CI: 3.329-23.24) (Group II: Initial - Day 12 PPG = 16.67 mg/dL, 95% CI: 4.687-28.65, P = 0.0159)], which continued through study completion at day 30. PCE supplementation significantly decreased mean preprandial glucose levels only in Group II at Days 24 (Initial - Day 24 = 13.00 mg/dL, 95% CI: 1.407-24.59, P = 0.0345) and 30 (Initial - Day 30 = 13.67 mg/dL, 95% CI: 5.766-21.57, P = 0.0067). In cell-based assays, PCE enhanced glucose uptake in L6 myocytes and inhibited hepatocyte glucose production HepG2 cells. In cell-free assays, PCE inhibited α-amylase activity and α-glucosidase activity. CONCLUSIONS: These findings underscore the therapeutic utility of PCE for maintaining healthy glucose metabolism and warrant further larger-scale clinical trials. TRIAL REGISTRATION: This trial was retrospectively registered in the ISRCTN registry on September 29, 2018 ( ISRCTN15680985 ).


Assuntos
Glicemia/efeitos dos fármacos , Extratos Vegetais , Polifenóis , Estado Pré-Diabético/tratamento farmacológico , Syzygium , Adulto , Glicemia/análise , Glicemia/metabolismo , Feminino , Humanos , Masculino , Projetos Piloto , Extratos Vegetais/farmacologia , Extratos Vegetais/uso terapêutico , Polifenóis/farmacologia , Polifenóis/uso terapêutico , Estudos Retrospectivos
14.
Plant Dis ; 103(7): 1674-1684, 2019 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-31095470

RESUMO

A growing world population requires an increase in the quality and quantity of food production. However, field losses due to biotic stresses are currently estimated to be between 10 and 20% worldwide. The risk of resistance and strict pesticide legislation necessitate innovative agronomical practices to adequately protect crops in the future, such as the identification of new substances with novel modes of action. In the present study, liquid chromatography mass spectrometry was used to characterize Rheum rhabarbarum root extracts that were primarily composed of the stilbenes rhaponticin, desoxyrhaponticin, and resveratrol. Minor components were the flavonoids catechin, epicatechin gallate, and procyanidin B1. Specific polyphenolic mixtures inhibited mycelial growth of several phytopathogenic fungi and oomycetes. Foliar spray applications with fractions containing stilbenes and flavonoids inhibited spore germination of powdery mildew in Hordeum vulgare with indications of synergistic interactions. Formulated extracts led to a significant reduction in the incidence of brown rust in Triticum aestivum under field conditions. Arabidopsis thaliana mutant and quantitative reverse-transcription polymerase chain reaction studies suggested that the stilbenes induce salicylic acid-mediated resistance. Thus, the identified substances of Rheum roots represent an excellent source of antifungal agents that can be used in horticulture and agriculture.


Assuntos
Resistência à Doença , Fungos , Oomicetos , Extratos Vegetais , Polifenóis , Rheum , Antifúngicos/farmacologia , Antiparasitários/farmacologia , Resistência à Doença/efeitos dos fármacos , Fungos/efeitos dos fármacos , Oomicetos/efeitos dos fármacos , Extratos Vegetais/farmacologia , Raízes de Plantas/química , Polifenóis/farmacologia , Rheum/química
15.
J Food Sci ; 84(6): 1371-1381, 2019 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-31112298

RESUMO

Industrial processing of raspberries into juice and jam results in the production of with high content of lipophilic and hydrophilic phytochemicals. Usually considered as waste, raspberry pomace is occasionally cold-pressed to recover specialty oil. However, the resulting pomace press-cake (PPC) still contains 30% to 35% of lipophilic compounds, such as essential fatty acids, tocols, phytosterols, and ellagitannins initially present in pomace. In a perspective of sustainable development, we investigate an eco-friendly process using an aqueous enzyme-assisted extraction (AEAE) to simultaneously and effectively recover lipophilic compounds and polyphenols from the PPC. The performance of different combinations of carbohydrases and proteases was compared. After selecting the best enzymatic system, a definitive screening design involving six factors was then implemented to optimize the process. Under optimized conditions, 1.2 units of thermostable alkaline protease/100 g PPC, pH 9, 60 °C, and 2 hr hydrolysis, more than 38% of total PPC lipophilic content were recovered in the aqueous medium. The recovery of polyphenols and antioxidant activity was, respectively, 48% and 25% higher than obtained by extraction with methanol/acetone/water mixture. Such an AEAE extract might prove useful in food and nutraceutical applications. PRACTICAL APPLICATION: Raspberry pomace, a food industrial by-product, is often considered as waste. However, it is a rich source of phytochemicals, such as tocols, polyphenols, and polyunsaturated fatty acids. To overcome the drawbacks of organic solvent use, an enzyme-assisted extraction process was developed as an eco-friendly alternative to recover these bioactive compounds. Definitive screening design experimental design was used to enhance polyphenols and lipophilics extraction yields while reducing process costs. This extract is an oil-in-water emulsion, with high content in antioxidant phytochemicals, which might have potential for use in nutraceutical applications. Therefore, this green process developed for the valorization of raspberry pomace is considered as a perspective of sustainable development.


Assuntos
Antioxidantes/análise , Proteínas de Bactérias , Endopeptidases , Frutas/química , Química Verde , Compostos Fitoquímicos/análise , Extratos Vegetais/química , Rubus/química , Antioxidantes/farmacologia , Emulsões , Ácidos Graxos Essenciais/análise , Indústria Alimentícia , Humanos , Taninos Hidrolisáveis/análise , Taninos Hidrolisáveis/farmacologia , Resíduos Industriais , Compostos Fitoquímicos/farmacologia , Fitosteróis/análise , Extratos Vegetais/farmacologia , Polifenóis/análise , Polifenóis/farmacologia , Tocoferóis/análise
16.
J Med Food ; 22(5): 508-520, 2019 May.
Artigo em Inglês | MEDLINE | ID: mdl-31084540

RESUMO

In this study, we investigated the antioxidant and protective effect of Lindera glauca stem (LGS) extracts against oxidative stress. We compared antioxidant properties of water extract (LGSW) with ethanol extract (LGSE) by determining the contents responsible for antioxidant activities such as polyphenols and flavonoids. Antioxidant properties were also determined by 2,2'-azinobis-(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) radical scavenging activity and ferric reducing antioxidant power (FRAP). Lipid peroxidation was estimated using ferric thiocyanate (FTC) and thiobarbituric acid (TBA) method. Both LGSW and LGSE strongly inhibited lipid peroxidation. Especially, LGSE showed a protective effect through increasing cell viability, decreasing intracellular reactive oxygen species (ROS) against tert-butyl hydroperoxide-induced oxidative stress in Chang cells. Furthermore, LGSE increased antioxidant related enzyme activities such as catalase, glutathione S-transferase, glutathione peroxidase, and superoxide dismutase gene expression against oxidative stress in a zebrafish model. Our findings suggest that LGSE could be useful for developing potential therapeutic agents with protective effects against oxidative stress.


Assuntos
Lindera/química , Estresse Oxidativo/efeitos dos fármacos , Extratos Vegetais/farmacologia , Substâncias Protetoras/química , terc-Butil Hidroperóxido/farmacologia , Catalase/metabolismo , Linhagem Celular , Glutationa Peroxidase/metabolismo , Humanos , Peroxidação de Lipídeos/efeitos dos fármacos , Extratos Vegetais/química , Caules de Planta/química , Polifenóis/química , Polifenóis/farmacologia , Substâncias Protetoras/farmacologia , Espécies Reativas de Oxigênio/metabolismo , Superóxido Dismutase/metabolismo , terc-Butil Hidroperóxido/química
17.
Food Chem Toxicol ; 129: 291-300, 2019 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-31059746

RESUMO

Methylglyoxal (MGO), a cytotoxic factor, reacts irreversibly with the side chains of lysine, cysteine, and arginine residues in proteins to form advanced glycation end products (AGEs) which might be a major pathological factor associated with diabetic complications. Thus, it is necessary to prevent or alleviate such diseases through inhibiting the formation of AGEs or lowering these AGEs-induced cellular damages. Based on our previous work, it was known that phloretin, an apple polyphenol, can inhibit the formation of AGEs under simulated physiological conditions. In this study, we found that phloretin prevented the formation of AGEs through trapping MGO in human umbilical endothelial cells (HUVECs). The phloretin-MGO adducts were analyzed in PBS and HUVECs. Surprisingly, only 1 MGO-phloretin adduct was detected in HUVECs, which was formed within 0.5 h and metabolized eventually within 24 h. The specific phloretin-MGO adduct was synthesized and identified by MS and NMR analysis. Its anti-inflammatory effect against AGEs was further investigated together with the parent compound, phloretin, which was proved to be through RAGE/p38 MAPK/NF-κB signaling pathway. Taken together, our data indicated the positive role of phloretin-MGO adduct on phloretin's protective effects, which might offer a new insight into the action mechanism of polyphenols against AGEs-induced damages.


Assuntos
Endotélio Vascular/efeitos dos fármacos , Produtos Finais de Glicação Avançada/metabolismo , Inflamação/metabolismo , Floretina/farmacologia , Aldeído Pirúvico/farmacologia , Sistema Livre de Células , Endotélio Vascular/citologia , Endotélio Vascular/metabolismo , Células Endoteliais da Veia Umbilical Humana , Humanos , NF-kappa B/metabolismo , Floretina/química , Polifenóis/farmacologia , Aldeído Pirúvico/química , Receptor para Produtos Finais de Glicação Avançada/metabolismo , Proteínas Quinases p38 Ativadas por Mitógeno/metabolismo
18.
Food Chem Toxicol ; 129: 354-364, 2019 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-31071388

RESUMO

The polyphenols profiles of the methanol extracts of bitter apricot [Armeniaca Sibirica (L.)] kernel skins (AKS) were analysed by liquid chromatography-electrospray ionization mass spectrometry. The antioxidan, anticancer effect on HepG2 cell and antibacterial properties of the AKS polyphenol extracts were further characterized in vitro. Polyphenol compounds (35), including nine phenolic acids, thirteen anthocyanins and thirteen flavonoids, were identified in AKS for the first time. The content of apigenin 7-O-glucoside, (cyanidin 3-(4″-acetylrutinoside), 3- (6″-acetylglucoside)-5-glucoside and salicylic acid was relatively high than the others. The AKS polyphenols strongly reduced Fe3+ and exhibited good scavenging activity towards 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid) free radicals, 1,1-diphenyl-1-picrylhydrazyl free radicals, hydroxyl radicals, superoxide anions and hydrogen peroxide. The AKS polyphenols could regulate oxidant stress in HepG2 cells by downregulating reduced glutathione, upregulating oxidative glutathione, malondialdehyde and advanced oxidation protein products, and reduced cell viability to induce apoptosis of HepG2 cells in vitro. The AKS polyphenols showed strong antibacterial activity against Escherichia coli, Staphylococcus aureus, Bacillus subtilis, Acetobacter aceti and Bacillus cereus. Therefore, the antioxidant, inhibitory effect on HepG2 cells and antimicrobial activity of the AKS polyphenols were distinct and worthy of further consideration for medical industry applications.


Assuntos
Antibacterianos/farmacologia , Antioxidantes/farmacologia , Polifenóis/análise , Polifenóis/farmacologia , Prunus armeniaca/química , Antioxidantes/química , Apoptose/efeitos dos fármacos , Bacillus/efeitos dos fármacos , Escherichia coli/efeitos dos fármacos , Células Hep G2 , Humanos , Peróxido de Hidrogênio/química , Testes de Sensibilidade Microbiana , Staphylococcus aureus/efeitos dos fármacos
19.
Int J Mol Sci ; 20(8)2019 Apr 15.
Artigo em Inglês | MEDLINE | ID: mdl-30991717

RESUMO

The recent emergence and re-emergence of viral infections transmitted by vectors, such as the Zika virus (ZIKV) and Dengue virus (DENV), is a cause for international concern. These highly pathogenic arboviruses represent a serious health burden in tropical and subtropical areas of the world. Despite the high morbidity and mortality associated with these viral infections, antiviral therapies are missing. Medicinal plants have been widely used to treat various infectious diseases since millenaries. Several compounds extracted from plants exhibit potent effects against viruses in vitro, calling for further investigations regarding their efficacy as antiviral drugs. Here, we demonstrate that an extract from Psiloxylon mauritianum, an endemic medicinal plant from Reunion Island, inhibits the infection of ZIKV in vitro without exhibiting cytotoxic effects. The extract was active against different ZIKV African and Asian strains, including an epidemic one. Time-of-drug-addition assays revealed that the P. mauritianum extract interfered with the attachment of the viral particles to the host cells. Importantly, the P. mauritianum extract was also able to prevent the infection of human cells by four dengue virus serotypes. Due to its potency and ability to target ZIKV and DENV particles, P. mauritianum may be of value for identifying and characterizing antiviral compounds to fight medically-important flaviviruses.


Assuntos
Antivirais/farmacologia , Vírus da Dengue/efeitos dos fármacos , Dengue/tratamento farmacológico , Magnoliopsida/química , Polifenóis/farmacologia , Infecção por Zika virus/tratamento farmacológico , Zika virus/efeitos dos fármacos , Animais , Antivirais/química , Células Cultivadas , Cercopithecus aethiops , Dengue/epidemiologia , Humanos , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Plantas Medicinais/química , Polifenóis/química , Reunião/epidemiologia , Células Vero , Infecção por Zika virus/epidemiologia
20.
Food Funct ; 10(4): 1856-1869, 2019 Apr 17.
Artigo em Inglês | MEDLINE | ID: mdl-30950465

RESUMO

Grape pomace (GP) is a major byproduct worldwide, and it is well known for its bioactive compounds, such as fibers and phenolic compounds, that are popular for their impact upon human health, including gastrointestinal health. The objective of this work was to evaluate the chemical composition and biological activities of an enzymatic GP extract, as well as to investigate how gastrointestinal digestion (GID) modulates these properties. GP extract was previously produced using an enzymatic cocktail with xylanase activity and was then exposed to simulated conditions of GID, characterized for its chemical composition, and screened for antimicrobial, prebiotic, and antioxidant activities. The safety of this ingredient after GID was also assessed. GP extract presented high contents of dietary fiber and other carbohydrates, including xylooligosaccharides, in addition to minerals and phenolic compounds. In vitro simulated GID revealed that xylobiose was resistant to gastric conditions, unlike phenolic compounds. The use of 2% (w/v) of this ingredient proved to be a potential carbon source that could be fermented by Lactobacillus and Bifidobacterium spp, even after digestion. The extract also exhibited strong antioxidant and antimicrobial activities against Staphylococcus aureus, Escherichia coli, and Pseudomonas aeruginosa; however, after GID, the antioxidant capacity decreased, and the antimicrobial capacity was strongly reduced or lost. Furthermore, the extract safety was also guaranteed on Caco-2 intestinal cells. This novel and green GP extract proved to be composed of relevant bioactive molecules, including xylooligosaccharides, polyphenols, organic acids, and minerals, which provided different biological properties; it has potential applications in the food industry such that it can be used as an ingredient in the development of new functional foods.


Assuntos
Antibacterianos/química , Antibacterianos/farmacologia , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Vitis/química , Resíduos/análise , Antibacterianos/metabolismo , Antioxidantes/química , Antioxidantes/metabolismo , Antioxidantes/farmacologia , Bifidobacterium/metabolismo , Células CACO-2 , Digestão , Escherichia coli/efeitos dos fármacos , Fermentação , Frutas/química , Frutas/metabolismo , Microbioma Gastrointestinal/efeitos dos fármacos , Trato Gastrointestinal/metabolismo , Glucuronatos/química , Glucuronatos/metabolismo , Glucuronatos/farmacologia , Humanos , Lactobacillus/metabolismo , Oligossacarídeos/química , Oligossacarídeos/metabolismo , Oligossacarídeos/farmacologia , Fenóis/química , Fenóis/metabolismo , Fenóis/farmacologia , Extratos Vegetais/metabolismo , Polifenóis/química , Polifenóis/metabolismo , Polifenóis/farmacologia , Staphylococcus aureus/efeitos dos fármacos , Vitis/metabolismo
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