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1.
Adv Food Nutr Res ; 98: 253-280, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-34507644

RESUMO

Phenolic compounds have demonstrated several in vitro beneficial properties by acting as antioxidant and pro-oxidant agents. This chapter approaches the relationship among oxidative stress, cancer, phenolic compounds and antiproliferative activity. Moreover, it discusses in vitro techniques and their biological applications, regarding cell viability and intracellular measure of reactive oxygen assays. The in vitro methods are important tools for screening and understanding the pathways involved on antiproliferative and antioxidant/pro-oxidant effects of phenolic compounds. These findings open avenues for the development of innovative food, chemical structures, technological applications and future perspectives in this research field.

2.
Molecules ; 26(13)2021 Jul 02.
Artigo em Inglês | MEDLINE | ID: mdl-34279398

RESUMO

The aim of this study was to compare the influence of the extraction method, chemical composition, antimicrobial effects, antioxidant activity, and cytotoxicity on human cells of the non-polar extracts of grape (Vitis labrusca) and blackberry (Rubus fruticosus) seeds. The Soxhlet (Sox), Bligh-Dyer (BD), and ultrasound (US) methods were used for extractions. For blackberry non-polar seed extract, extraction via the BD method showed the highest mean values of total phenolic content (TPC), expressed in milligrams of gallic acid equivalent per 100 mL of non-polar seed extracts (102.37 mg GAE/100 mL), and higher antioxidant activity in relation to the 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical, expressed in milligrams of gallic acid equivalent per 100 mL of non-polar seed extracts (11.50 mg AAE/100 mL), if compared with the Sox and US extractions. Similar results were obtained for the non-polar grape seed extracts, where BD extraction obtained the highest values for TPC (28.61 mg GAE/100 mL) and DPPH (35.36 mg AAE/100 mL). The type of extraction method had an impact on the composition of fatty acids. Only the non-polar blackberry and grape seed extracts obtained via the Sox method showed some in vitro inhibitory effect against Escherichia coli (IAL 2064) and Staphylococcus aureus (ATCC 13565). Regardless of the extraction method used, the non-polar blackberry and grape seed extracts did not decrease the cell viability (IC50 >1000 µg/mL) of cancer and normal cell lines, thus indicating the relative safety of the extracts. All the seed extracts decreased the generation of reactive oxygen species in the cell lines. Blackberry and grape seed lipid fractions can be utilized as antioxidants, and the extraction methods used cause significant changes in relation to their bioactivity and chemical composition.


Assuntos
Anti-Infecciosos/química , Antioxidantes/química , Extrato de Sementes de Uva/química , Rubus/química , Anti-Infecciosos/farmacologia , Anti-Infecciosos/toxicidade , Antioxidantes/farmacologia , Antioxidantes/toxicidade , Escherichia coli/efeitos dos fármacos , Ácidos Graxos/análise , Flavonoides/análise , Extrato de Sementes de Uva/farmacologia , Staphylococcus aureus/efeitos dos fármacos
3.
Food Chem Toxicol ; 154: 112287, 2021 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-34058233

RESUMO

Since dietary factors are thought to be responsible for high colon cancer risk, we investigated the chemopreventive effect of jabuticaba seed extract (LJE) by administering yogurt with or without LJE against 1,2 dimethyl hydrazine (DMH)-induced colon carcinogenesis in rats. Results showed that LJE contained a total phenolic content of 57.16 g/100 g of seed extract in which 7.67 and 10.09 g/100 g represented total flavonoids and ellagitannins, respectively. LJE protected DNA and human LDL against induced in vitro oxidation, which was associated with the ellagitannin content and with the free-radical scavenging and reducing capacities. LJE alone had a non-clastogenicity/aneugenicity property, but in combination with cisplatin, it enhanced the chromosome aberrations in cancer cells. In colon cancer-induced rats, yogurt with or without LJE caused a reduction in pro-inflammatory parameters, decreased the RNA expression of antiapoptotic cytokines and increased the expression of proapoptotic cytokines. Moreover, LJE attenuated colon cancer initiation and progression by decreasing aberrant crypt foci and LJE recovered the gut microbiome. Together, this evidence suggests that LJE provides chemopreventive protection against colon cancer development by reducing inflammation and increasing proapoptotic pathways.

4.
Food Chem ; 361: 130078, 2021 Nov 01.
Artigo em Inglês | MEDLINE | ID: mdl-34023692

RESUMO

Ora-pro-nobis (Pereskia aculeata Miller) is a non-conventional food plant common in Brazil. The objective of this study was to optimize the extraction of bioactive phenolic compounds from ora-pro-nobis leaves by employing solvent mixtures. Ten extracts were obtained with water, ethanol, acetone, and their binary and ternary mixtures, evaluating the chemical composition, antioxidant activity and bioactivities in vitro. The response surface methodology was applied to model the results and calculate the optimal solvent composition, which is 60% water, 40% ethanol and 0% acetone. The optimized extract is rich in phenolic compounds (64 mg GAE/g) and proteins (823 mg/g) and presents antioxidant activity (in intracellular media as well) and inhibits lipid peroxidation (32%) along with hypotonic hemolysis (H50 = 0.339%), it does not present toxicity in vitro against cancer and normal cells. This is the first report of chicoric, caffeoyl-hexaric and coumaroyl-hexaric acids and some glycosylate derivatives of flavonols in ora-pro-nobis leaves.


Assuntos
Antioxidantes/química , Cactaceae/química , Extratos Vegetais/química , Antioxidantes/farmacologia , Linhagem Celular , Sobrevivência Celular/efeitos dos fármacos , Humanos , Fenóis/química , Fenóis/farmacologia , Extratos Vegetais/farmacologia , Folhas de Planta/química
5.
Food Chem Toxicol ; 153: 112284, 2021 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-34044082

RESUMO

Aqueous extracts from blackcurrant press cake (BC), Norway spruce bark (NS), Scots pine bark (SP), and sea buckthorn leaves (SB) were obtained using maceration and pressurized hot water and tested for their bioactivities. Maceration provided the extraction of higher dry matter contents, including total phenolics (TPC), anthocyanins, and condensed tannins, which also impacted higher antioxidant activity. NS and SB extracts presented the highest mean values of TPC and antioxidant activity. Individually, NS extract presented high contents of proanthocyanidins, resveratrol, and some phenolic acids. In contrast, SB contained a high concentration of ellagitannins, ellagic acid, and quercetin, explaining the antioxidant activity and antibacterial effects. SP and BC extracts had the lowest TPC and antioxidant activity. However, BC had strong antiviral efficacy, whereas SP can be considered a potential ingredient to inhibit α-amylase. Except for BC, the other extracts decreased reactive oxygen species (ROS) generation in HCT8 and A549 cells. Extracts did not inhibit the production of TNF-alpha in lipopolysaccharide-stimulated THP-1 macrophages but inhibited the ROS generation during the THP-1 cell respiratory burst. The recovery of antioxidant compounds from these by-products is incentivized for high value-added applications.


Assuntos
Anti-Infecciosos/farmacologia , Anti-Inflamatórios/farmacologia , Antioxidantes/farmacologia , Extratos Vegetais/farmacologia , Anti-Infecciosos/isolamento & purificação , Anti-Infecciosos/toxicidade , Anti-Inflamatórios/isolamento & purificação , Anti-Inflamatórios/toxicidade , Antioxidantes/isolamento & purificação , Antioxidantes/toxicidade , Bactérias/efeitos dos fármacos , Candida albicans/efeitos dos fármacos , Linhagem Celular Tumoral , Enterovirus Humano B/efeitos dos fármacos , Química Verde , Hippophae/química , Humanos , Testes de Sensibilidade Microbiana , Picea/química , Pinus sylvestris/química , Casca de Planta/química , Extratos Vegetais/isolamento & purificação , Extratos Vegetais/toxicidade , Folhas de Planta/química , Ribes/química
6.
Molecules ; 26(3)2021 Jan 31.
Artigo em Inglês | MEDLINE | ID: mdl-33572682

RESUMO

The sesquiterpenes selina-1,3,7(11)-trien-8-one and oxidoselina-1,3,7(11)-trien-8-one were isolated from the essential oil of Eugenia uniflora L. leaves. The structures were elucidated using spectrometric methods (UV, GC-MS, NMR, and specific optical rotation). The relationship between antioxidant activity, as determined by DPPH assay, and the cytotoxic effect was evaluated using tumor cells, namely lung adenocarcinoma epithelial cells (A549) and human hepatoma carcinoma cells (HepG2), as well as a model of normal human lung fibroblast cells (IMR90). Both compounds did not show prominent free-radical scavenging activity according to DPPH assay, and did not inhibit lipid peroxidation in Wistar rat brain homogenate. The isolated compounds showed pro-oxidative effects and cytotoxicity in relation to the IMR90 cell line.


Assuntos
Antineoplásicos/farmacologia , Antioxidantes/farmacologia , Eugenia/química , Naftalenos/farmacologia , Óleos Voláteis/química , Folhas de Planta/química , Sesquiterpenos/farmacologia , Linhagem Celular Tumoral , Sobrevivência Celular/efeitos dos fármacos , Humanos
7.
Eur J Med Chem ; 212: 113123, 2021 Feb 15.
Artigo em Inglês | MEDLINE | ID: mdl-33412421

RESUMO

Cyclic nucleotide phosphodiesterases (PDEs) are a superfamily of enzymes known to play a critical role in the indirect regulation of several intracellular metabolism pathways through the selective hydrolysis of the phosphodiester bonds of specific second messenger substrates such as cAMP (3',5'-cyclic adenosine monophosphate) and cGMP (3',5'-cyclic guanosine monophosphate), influencing the hypertrophy, contractility, apoptosis and fibroses in the cardiovascular system. The expression and/or activity of multiple PDEs is altered during heart failure (HF), which leads to changes in levels of cyclic nucleotides and function of cardiac muscle. Within the cardiovascular system, PDEs 1-5, 8 and 9 are expressed and are interesting targets for the HF treatment. In this comprehensive review we will present a briefly description of the biochemical importance of each cardiovascular related PDE to the HF, and cover almost all the "long and winding road" of designing and discovering ligands, hits, lead compounds, clinical candidates and drugs as PDE inhibitors in the last decade.


Assuntos
3',5'-AMP Cíclico Fosfodiesterases/antagonistas & inibidores , Desenho de Fármacos , Insuficiência Cardíaca/tratamento farmacológico , Inibidores de Fosfodiesterase/farmacologia , 3',5'-AMP Cíclico Fosfodiesterases/metabolismo , Animais , Insuficiência Cardíaca/metabolismo , Humanos , Estrutura Molecular , Inibidores de Fosfodiesterase/síntese química , Inibidores de Fosfodiesterase/química
8.
Food Chem ; 334: 127565, 2021 Jan 01.
Artigo em Inglês | MEDLINE | ID: mdl-32717686

RESUMO

The chemical composition, antioxidant activity (AA), cytotoxic activity, antihemolytic effects, and enzyme inhibition (EI) of lyophilized jabuticaba (Myrciaria jaboticaba) seed extract (LJE) was studied. The main compounds found were castalagin, vescalagin, procyanidin A2, and ellagic acid. LJE was more toxic to cancer cells than to normal cells, meaning relative toxicological safety. This cytotoxic effect can be attributed to the pro-oxidant effect observed in the reactive oxygen species (ROS) generation assay. LJE inhibited α-amylase, α-glucosidase, and ACE-I activities and protected human erythrocytes from hemolysis. LJE was incorporated into yogurts at different concentrations and the total phenolic content, AA, and EI increased in a dose-dependent manner. LJE-containing yogurt presented 86% sensory acceptance. The yogurt was administered to Wistar rats bearing cancer and it modulated the gut bacterial microbiota, having a prebiotic effect. LJE is a potential functional ingredient for food companies looking for TPC, AA, and prebiotic effect in vivo.


Assuntos
Neoplasias do Colo/tratamento farmacológico , Microbioma Gastrointestinal/efeitos dos fármacos , Myrtaceae/química , Polifenóis/farmacologia , Iogurte , 1,2-Dimetilidrazina/toxicidade , Inibidores da Enzima Conversora de Angiotensina/química , Inibidores da Enzima Conversora de Angiotensina/farmacologia , Animais , Antioxidantes/química , Antioxidantes/farmacologia , Catequina/análise , Catequina/farmacologia , Neoplasias do Colo/induzido quimicamente , Neoplasias do Colo/microbiologia , Humanos , Taninos Hidrolisáveis/análise , Taninos Hidrolisáveis/farmacologia , Masculino , Fenóis/análise , Extratos Vegetais/análise , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Polifenóis/análise , Proantocianidinas/análise , Proantocianidinas/farmacologia , Ratos Wistar , Sementes/química , alfa-Amilases/antagonistas & inibidores
9.
Mastology (Online) ; 31: 1-5, 2021.
Artigo em Inglês | LILACS-Express | LILACS | ID: biblio-1292860

RESUMO

Adenoid cystic carcinoma (AdCC) of the breast is an uncommon invasive lobular neoplasm whose morphology is similar to the homonymous tumor of salivary glands and with a peculiar behavior toward the "triple-negative" (TN) profile. Tumors belonging to this family do not immunohistochemically express three of the main prognostic biomarkers and tend to show a more aggressive behavior. However, this rare histological pattern of breast cancer is generally associated with good prognosis. In this study, the authors describe the case of a 49-year-old woman diagnosed with this rare malignant tumor and who underwent breast-conserving surgery. Recent studies have aimed to understand the genes, genetic alterations, and etiological aspects related to the still obscure etiopathogenesis of AdCC. Thus, morphological and molecular aspects relevant to AdCC and reported in the literature will be discussed.

10.
Food Res Int ; 137: 109430, 2020 11.
Artigo em Inglês | MEDLINE | ID: mdl-33233112

RESUMO

The aims of this study were to quantify and optimize the extraction of total phenolic content (TPC), total flavonoids (TF) and antioxidant activity (AA) of aqueous pu-erh (Camellia sinensis var. assamica) extracts, as well as to compare the optimized pu-erh tea extract (OPT) with toasted mate (Ilex paraguariensis), black and green (Camellia sinensis) teas. The optimization process increased the TPC and the ferric reducing antioxidant power (FRAP). The results showed that the green tea extract presented the highest values for TPC and antioxidant capacity. The pasteurized OPT showed lower TPC and TF, and higher FRAP, DPPH and Cu2+ chelating ability compared to the non-pasteurized OPT. The lyophilized OPT showed inhibition of lipid peroxidation in Wistar rat brain homogenate and displayed antibiofilm activity against Enterococcus faecalis ATCC 25212 and 19433, and Staphylococcus aureus ATCC 25923. Additionally, lyophilized OPT presented cytotoxic and antiproliferative effects against tumor cell lines (Caco-2, A549 and HepG2), inhibited the production of reactive oxygen species in A549 and IMR90 cells, and presented antihemolytic activity in human erythrocytes. The lyophilized OPT inhibited α-glucosidase (IC50 = 47.0 µg/mL) and α-amylase at 30.0 mg/mL. The main compounds detected in OPT were gallic acid, caffeine and theobromine.


Assuntos
Anti-Infecciosos , Camellia sinensis , Animais , Antioxidantes/análise , Antioxidantes/farmacologia , Células CACO-2 , Humanos , Extratos Vegetais/farmacologia , Ratos , Ratos Wistar , Chá , alfa-Amilases , alfa-Glucosidases
11.
Neurochem Res ; 45(12): 3003-3020, 2020 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-33079324

RESUMO

A new series of ten multifunctional Cinnamoyl-N-acylhydrazone-donepezil hybrids was synthesized and evaluated as multifunctional ligands against neurodegenerative diseases. The molecular hybridization approach was based on the combination of 1-benzyl-4-piperidine fragment from the anti-Alzheimer AChE inhibitor donepezil (1) and the cinnamoyl subunit from curcumin (2), a natural product with remarkable antioxidant, neuroprotective and anti-inflammatory properties, using a N-acylhydrazone fragment as a spacer subunit. Compounds 4a and 4d showed moderate inhibitory activity towards AChE with IC50 values of 13.04 and 9.1 µM, respectively. In addition, compound 4a and 4d showed a similar predicted binding mode to that observed for donepezil in the molecular docking studies. On the other hand, compounds 4a and 4c exhibited significant radical scavenging activity, showing the best effects on the DPPH test and also exhibited a significant protective neuronal cell viability exposed to t-BuOOH and against 6-OHDA insult to prevent the oxidative stress in Parkinson's disease. Similarly, compound 4c was capable to prevent the ROS formation, with indirect antioxidant activity increasing intracellular GSH levels and the ability to counteract the neurotoxicity induced by both OAß1-42 and 3-NP. In addition, ADMET in silico prediction indicated that both compounds 4a and 4c did not show relevant toxic effects. Due to their above-mentioned biological properties, compounds 4a and 4c could be explored as lead compounds in search of more effective and low toxic small molecules with multiple neuroprotective effects for neurodegenerative diseases.

12.
Rev. bras. oftalmol ; 79(5): 309-314, set.-out. 2020. tab, graf
Artigo em Português | LILACS | ID: biblio-1137993

RESUMO

Resumo Introdução: Os rastreamentos visuais realizados nas escolas são, às vezes, a única oportunidade de deteção dos erros de refração não corrigidos (ERN) causadores de baixa visual, prejuízo na aquisição do conhecimento, evasão e repetência escolar, habilidades motoras pobres, dificuldade na interação social e baixa autoestima nos escolares. Objetivos: Comparar a detecção de ERN em escolares do ensino fundamental por meio de rastreamento visual (medida da AV com a tabela de Snellen) e por photoscreener; avaliar a acurácia do SpotTM Vision Screener (Welch Allyn) como autorefrator comparando suas medidas de refração com as do autorrefrator Topcon KR 8000 (Japão) e levantar a proporção de óculos com a tecnologia ready to Clip™ que foram dispensados no momento da avaliação dos escolares. Métodos: Duzentos e noventa e sete escolares foram submetidos à rastreamento visual (ponto de corte: AV monocular ≤ 0,7 e/ou diferença duas linhas de Snellen entre os olhos), photoscreening (ponto de corte: hipermetropia ≥3,00D, miopia ≥0,75D e astigmatismo > 1D) e à mensuração do erro de refração sob cicloplegia com o photoscreener e o autorrefrator. Somente os dados de refração do olho direito foram analisados. Os achados foram convertidos em vetores de magnitude para análise. Resultados: Os valores de sensibilidade e especificidade do método de rastreamento visual foram 67,2% e 63,5% e do photoscreening, foram 76,1% e 79,1%. A diferença da refração do SVS com o autorrefrator foi de +0,154 DE com -0,170 DC no eixo de 6 graus para o olho direito de cada paciente. Conclusões: Na população avaliada o método de rastreamento refrativo por photoscreener foi mais efetivo que o do rastreamento visual. A comparação dos resultados da refração sob cicloplegia com o autorrefrator validou o uso do photoscreener como um método de refração acurado para a mensuração de erros refrativos em escolares. A maioria dos escolares receberam os óculos com a tecnologia ready to Clip™ no momento da prescrição.


Abstract Background: The visual screening performed in schools is sometimes the only opportunity to detect uncorrected refraction errors (URE) causing low visual impairments, prejudice in the acquisition of knowledge, dropout and school repetition, poor motor skills, difficulty in social interaction and low self-esteem in schoolchildren. Objectives: To compare the detection of URE in elementary school children by visual screening (measurement of the AV with the Snellen table) and photoscreening; to evaluate the accuracy of the SpotTM Vision Screener (Welch Allyn) as an autorefractor by comparing its refraction measurements with those of the autorefractor Topcon KR 800 (Japan) and to verify the proportion of glasses with ready to ClipTM technology dispensed at the time of the students' evaluation. Methods: Two hundred ninety-seven students were submitted to visual screening (cutoff point: AV monocular ≤ 0.7 and/or difference two Snellen lines between the eyes), photoscreening (cutoff point: hypermetropia ≥ 3, 00D, myopia ≥ 0, 75D and astigmatism > 1D) and the measurement of the refraction error under cycloplegia with the photoscreener and autorefractor. Only the refraction data of the right eye were analyzed. The findings were converted into vectors of magnitude for analysis. Results: The sensitivity and specificity values of the visual screening method were 67.2% and 63.5% and photo screening were 76.1% and 79.1%. The mean difference between refraction by SVS and autorefractor was of + 0.154 SD combined with -0.170 DC in the 6-degree axis for the right eye of each patient. Conclusions: In the population evaluated the method of refractive screening by photoscreener was more effective than the visual screening. The comparison of the results of refraction under cycloplegia with the autorefractor validated the use of photoscreener as an accurate refraction method for the measurement of refractive errors in schoolchildren. The majority of the students received their glasses with ready to Clip™ technology at the time of prescription.


Assuntos
Humanos , Masculino , Feminino , Criança , Refração Ocular , Serviços de Saúde Escolar , Transtornos da Visão/diagnóstico , Acuidade Visual , Saúde Ocular , Técnicas de Diagnóstico Oftalmológico , Ensino Fundamental e Médio
13.
Food Res Int ; 136: 109334, 2020 10.
Artigo em Inglês | MEDLINE | ID: mdl-32846532

RESUMO

Parasitic diseases have attracted worldwide attention of their consequent impact on mortality and morbidity. Accordingly, several plants have been screened for antiparasitic activity aiming to create new alternatives for treatment. These diseases have been neglected and have not attracted worldwide attention (nowadays), the health concerns are focused in chronic diseases, but it is necessary to focus on parasitic diseases and look for prophylactic alternatives, such as plant extracts. Although camu-camu (Myrciaria dubia) seeds are a rich source of antioxidant antimutagenic, cytotoxic, anti-inflammatory, antimicrobial, antihypertensive and neuroprotective compounds, nothing is known about their antiparasitic effects. Thus, in the present study we aimed to evaluate five extracts of camu-camu seeds (100% water, 100% ethyl alcohol, 50% water + 50% ethyl alcohol, 25% water + 75% ethyl alcohol, and 75% water + 25% ethyl alcohol) in relation to their in vitro antimalarial, antischistosomicidal, leishmanicidal and anti-hemolytic effects. The extracts exhibited antischistosomicidal (ED50 values from 418.4 to >1000.0 µg/mL) and antimalarial activities (IC50 values from 24.2 to 240.8 µg/mL) for both W2 and 3D7 strains in all intra-erythrocytic stages. Correlation analysis showed that the toxic effects may mainly be attributed to methylvescalagin (r = -0.548 to -0.951, p < 0.05) and 2,4-dihydroxybenzoic acid (r = -0.612 to -0.917, p < 0.05) contents. Moreover, the anti-hemolytic effect was associated to methylvescalagin (r = -0.597, p < 0.05). No toxic effects were observed for leishmaniasis and IMR90 normal cells. Herein, methylvescalagin was the bioactive compound of greatest interest once it presented simultaneous relation with antiparasitic and anti-hemolytic activities.


Assuntos
Antimaláricos , Myrtaceae , Antimaláricos/farmacologia , Antioxidantes/farmacologia , Extratos Vegetais/farmacologia , Sementes
14.
Molecules ; 25(14)2020 Jul 10.
Artigo em Inglês | MEDLINE | ID: mdl-32664425

RESUMO

Alzheimer's disease (AD) is a multifactorial neurodegenerative disorder that involves different pathogenic mechanisms. In this regard, the goal of this study was the design and synthesis of new compounds with multifunctional pharmacological activity by molecular hybridization of structural fragments of curcumin and resveratrol connected by an N-acyl-hydrazone function linked to a 1,4-disubstituted triazole system. Among these hybrid compounds, derivative 3e showed the ability to inhibit acetylcholinesterase activity, the intracellular formation of reactive oxygen species as well as the neurotoxicity elicited by Aß42 oligomers in neuronal SH-SY5Y cells. In parallel, compound 3e showed a good profile of safety and ADME parameters. Taken together, these results suggest that 3e could be considered a lead compound for the further development of AD therapeutics.


Assuntos
Doença de Alzheimer/tratamento farmacológico , Triazóis/química , Triazóis/farmacologia , Acetilcolinesterase/metabolismo , Doença de Alzheimer/metabolismo , Peptídeos beta-Amiloides/metabolismo , Células Cultivadas , Inibidores da Colinesterase/química , Inibidores da Colinesterase/farmacocinética , Inibidores da Colinesterase/farmacologia , Curcumina/farmacocinética , Curcumina/farmacologia , Humanos , Neurônios/efeitos dos fármacos , Neurônios/metabolismo , Fármacos Neuroprotetores/química , Fármacos Neuroprotetores/farmacocinética , Fármacos Neuroprotetores/farmacologia , Farmacocinética , Espécies Reativas de Oxigênio/metabolismo , Resveratrol/farmacocinética , Resveratrol/farmacologia , Triazóis/farmacocinética
15.
J Food Sci ; 85(8): 2358-2367, 2020 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-32645216

RESUMO

Food companies should comply with the requirements of a zero-waste concept to adapt to the circular economy requirements. In fruit companies, usually seeds are discarded without proper utilization and extraction of the bioactive compounds. Fruit seeds are sources of chemical compounds that can be extracted, studied, and applied in high value-added products. Thus, in this work the experimental conditions for the water extraction of phenolic compounds from camu-camu (Myrciaria dubia) seed coat were optimized using a central composite design and the desirability function. Total phenolic content (TPC), and condensed tannins (CT), DPPH radical scavenging activity, ferric reducing antioxidant capacity (FRAP), Folin-Ciocalteu reducing capacity (FCRC), and Cu2+ chelating ability were assessed. Seed coat extracted for 51.1 min using a 1:34.1 solid:liquid ratio was the optimal condition to extract 6,242 mg gallic acid equivalent (GAE)/100 g of TPC and 695 mg catechin equivalent (CE)/100 g of CT. The optimized extract displayed free-radical scavenging activity, reducing properties and ability to chelate Cu2+ , and inhibited the growth of Listeria monocytogenes, Pseudomonas aeruginosa, Salmonella Typhimurium, Salmonella Enteritidis, Bacillus cereus, and Staphylococcus aureus. Additionally, the lyophilized water extract inhibited the in vitro activity of α-amylase, α-glucosidase, and angiotensin converting enzyme and showed cytotoxic effects towards Caco-2, A549, and HepG2 cancer cells, but no cytotoxicity towards IMR90 cells. Vescalagin, castalagin, and 3,4-dihydroxybenzoic acid were the major phenolic compounds identified in the optimized extract. In conclusion, the optimized camu-camu seed coat water extract is a rich source of phenolic compounds with antioxidant, antidiabetic, antihypertensive, and antiproliferative effects. PRACTICAL APPLICATION: Camu-camu fruit pulp and seeds have been studied for their phenolic composition and bioactivity. However, seeds are usually discarded and represent an environmental problem in South American countries. We presented a methodological overview on the extraction optimization of the phenolic compounds from camu-camu seed coat and studied the bioactivity of the optimized extract using chemical, enzymatic, and cell-based experiments. Results can be used by camu-camu processors to obtain a phenolic-rich extract for industrial applications, without any further processing.


Assuntos
Myrtaceae/química , Fenóis/química , Fenóis/isolamento & purificação , Extratos Vegetais/química , Sementes/química , Antibacterianos/isolamento & purificação , Anti-Hipertensivos/isolamento & purificação , Antineoplásicos Fitogênicos/isolamento & purificação , Antioxidantes/isolamento & purificação , Células CACO-2 , Humanos , Hipoglicemiantes/isolamento & purificação , Resíduos Industriais/análise , Proantocianidinas/análise , alfa-Amilases/antagonistas & inibidores
16.
Food Chem Toxicol ; 142: 111439, 2020 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-32450285

RESUMO

The aim of this study was to evaluate the effects of different solvents and maximize the extraction of bioactive compounds from jabuticaba (Myrciaria cauliflora) seeds. In general, the solvent system composed of water and propanone (52:48 v/v) modified the extract polarity and increased extraction yield of bioactive compounds. The optimized extract presented antioxidant capacity measured by different chemical and biological assays. The optimized extract exerted antiproliferative and cytotoxic effects against A549 and HCT8 cells, antimicrobial and antihemolytic effects, inhibited α-amylase/α-glucosidase activities and presented in vitro antihypertensive effect. Nonetheless, the optimized extract showed no cytotoxicity in a human cell model (IMR90). Vescalagin, castalagin and ellagic acid were the major phenolic compounds in the optimized extract. Our results show that jabuticaba seed may be a potential ingredient for the development of potentially functional foods.


Assuntos
Myrtaceae/embriologia , Fenóis/análise , Extratos Vegetais/farmacologia , Sementes/química , Inibidores da Enzima Conversora de Angiotensina/farmacologia , Anti-Infecciosos/farmacologia , Anti-Hipertensivos/farmacologia , Antineoplásicos Fitogênicos/farmacologia , Antioxidantes/farmacologia , Linhagem Celular Tumoral , Humanos , Hipoglicemiantes/farmacologia , Peroxidação de Lipídeos/efeitos dos fármacos , Testes de Sensibilidade Microbiana
17.
Food Res Int ; 132: 109090, 2020 06.
Artigo em Inglês | MEDLINE | ID: mdl-32331681

RESUMO

Studies regarding the bioactivity of teas are mainly based on the phenolic composition and in vitro antioxidant activity of the herbal species used in their preparation. The aim of this study was to compare the in vitro and ex vivo antioxidant activity, cytotoxic/antiproliferative activity against cancer cells, the inhibitory activity of α-amylase, α-glucosidase and angiotensin I-converting enzymes, as well as the inhibition of DNA-induced fission of the peroxyl radical, in relation to aqueous extracts of Camellia sinensis var. sinensis (CS), Ilex paraguariensis (IP), Aspalathus linearis (AL) and an optimised extract (OT) containing the three herb species. A bivariate and multivariate statistical approach was employed to associate functional activities with individual phenolic composition. The CS and OT extracts showed the highest levels of hesperidin, quercetin-3-rutinoside, (-)-epigallocatechin-3-gallate and isoquercitrin. The CS and OT extracts showed the highest antioxidant activity, greater ability to inhibit α-amylase and proliferation of HCT8 cells, and greater ability to reduce Folin-Ciocalteu reagent. The AL extract, which is the major source of quercetin-3-rutinoside, hesperidin and isoquercitrin, showed the highest ability to inhibit α-glucosidase, the inhibition of LDL oxidation and protection of human erythrocytes. The IP extract showed the highest inhibition of lipoperoxidation in brain homogenate of Wistar rats, antihypertensive activity, and A549 cell proliferation; chlorogenic acid was its major phenolic compound. In general, the in vitro functionality of each extract was dependent on its chemical composition and the OT extract presented the most varied phenolic composition, and biological activity similar to the CS sample. In conclusion, the mixture of CS, AL, and IP represents a chemical and functional-based strategy to develop functional teas.


Assuntos
Fenóis/química , Fenóis/toxicidade , Compostos Fitoquímicos/química , Compostos Fitoquímicos/toxicidade , Extratos Vegetais/química , Extratos Vegetais/toxicidade , Células A549 , Angiotensinas/efeitos dos fármacos , Animais , Antioxidantes , Aspalathus/química , Camellia sinensis/química , Catequina/análogos & derivados , Linhagem Celular , LDL-Colesterol/efeitos dos fármacos , Clivagem do DNA/efeitos dos fármacos , Hesperidina , Humanos , Hipertensão , Ilex paraguariensis/química , Masculino , Capacidade de Absorbância de Radicais de Oxigênio , Folhas de Planta/química , Quercetina/análogos & derivados , Ratos , Ratos Wistar , Rutina , alfa-Amilases/efeitos dos fármacos
18.
Food Res Int ; 128: 108763, 2020 02.
Artigo em Inglês | MEDLINE | ID: mdl-31955736

RESUMO

The purpose of this study was to use a statistical approach to optimise the experimental conditions regarding the extraction of bioactive compounds, and to analyse the in vitro functional properties of crude lyophilized extracts (CLE) and partially purified (PPE) extracts of Clitoria ternatea petals. The results showed that the factors of temperature and time influenced the extraction of phenolic compounds, antioxidant activity and the physicochemical parameters. Simultaneous optimisation showed that the same levels of bioactive compounds were extracted when using temperatures from 11.7 to 68.3 °C and times from 8.47 to 51.12 min. Principal component analysis revealed the experimental conditions that provided the extraction producing the highest level of phenolic content (40 °C/30 min). The CLE showed antimicrobial activity; protective effect against hemolysis of erythrocytes; inhibition of α-amylase, α-glucosidase and angiotensin-I-converting (ACE-I) enzymes; and inhibition of lipid peroxidation. The CLE and PPE demonstrated oxygen radical absorption capacity; inhibition of DNA strand scission; inhibition of LDL cholesterol oxidation; intracellular antioxidant activity against reactive oxygen species (>100 µg/mL); and no cytotoxicity (IC50, GI50 and LC50 > 900 µg/mL) against A549, HCT8 and IMR90 cell lines.


Assuntos
Anti-Hipertensivos/metabolismo , Antioxidantes/metabolismo , LDL-Colesterol/efeitos dos fármacos , Clitoria/metabolismo , Hemólise/efeitos dos fármacos , alfa-Amilases/metabolismo , alfa-Glucosidases/metabolismo , DNA , Flores , Humanos , Técnicas In Vitro , Oxirredução/efeitos dos fármacos , Extratos Vegetais/metabolismo , Análise de Componente Principal
19.
Food Res Int ; 128: 108782, 2020 02.
Artigo em Inglês | MEDLINE | ID: mdl-31955755

RESUMO

UPLC-QTOF-MSE phenolic profile of kombuchas produced from the fermentation of green tea or black tea at 25 °C for 10 days was investigated along with the determination of their antioxidant capacities, antibacterial and antiproliferative activities. Overall, 127 phenolic compounds (70.2% flavonoids, 18.3% phenolic acids, 8.4% other polyphenols, 2.3% lignans and 0.8% stilbenes) were identified, with 103 phenolic compounds reported for the first time in kombuchas. A greater diversity and abundance of phenolic compounds was detected in black tea kombucha, which resulted in a higher antioxidant capacity. However, the green tea kombucha was the only one that presented antibacterial activity against all the bacteria tested and an increased antiproliferative activity against the cancer cell lines, which was attributed to the presence of catechins among the most abundant phenolic compounds and verbascoside as an exclusive compound. Thus, the type of tea used in the kombucha production interferes in its bioactive composition and properties.


Assuntos
Antibacterianos/farmacologia , Antineoplásicos/farmacologia , Antioxidantes/farmacologia , Chá de Kombucha/análise , Fenóis/química , Antineoplásicos/química , Bactérias/efeitos dos fármacos , Benzotiazóis/química , Linhagem Celular Tumoral , Sobrevivência Celular/efeitos dos fármacos , Humanos , Concentração de Íons de Hidrogênio , Testes de Sensibilidade Microbiana , Ácidos Sulfônicos/química
20.
Food Chem ; 310: 125909, 2020 Apr 25.
Artigo em Inglês | MEDLINE | ID: mdl-31816536

RESUMO

Camu-camu (Myrciaria dubia) seeds are discarded without recovering the bioactive compounds. The main aim of the present work was to optimise the solvent mixture to extract higher total phenolic content and antioxidant capacity of camu-camu seeds. The optimised solvent system increased the extraction of phenolic compounds, in which vescalagin and castalagin were the main compounds. The optimised extract displayed antioxidant capacity measured by different chemical and biological assays, exerted antiproliferative and cytotoxic effects against A549 and HCT8 cancer cells, antimicrobial effects, protected human erythrocytes against hemolysis, inhibited α-amylase and α-glucosidase enzymes and presented in vitro antihypertensive effect. Additionally, the optimized extract inhibited human LDL copper-induced oxidation in vitro and reduced the TNF-α release and NF-κB activation in macrophages cell culture. Thus, the use of camu-camu seed showed to be a sustainable way to recover bioactive compounds with in vitro functional properties.


Assuntos
Myrtaceae/química , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Animais , Anti-Infecciosos/química , Anti-Infecciosos/farmacologia , Anti-Inflamatórios/química , Anti-Inflamatórios/farmacologia , Anti-Hipertensivos/química , Anti-Hipertensivos/farmacologia , Antioxidantes/química , Antioxidantes/farmacologia , Linhagem Celular , Avaliação Pré-Clínica de Medicamentos/métodos , Hemólise/efeitos dos fármacos , Humanos , Taninos Hidrolisáveis/análise , Hipoglicemiantes/química , Hipoglicemiantes/farmacologia , Fenóis/análise , Sementes/química , alfa-Amilases/antagonistas & inibidores
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