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1.
J Sci Food Agric ; 100(2): 672-681, 2020 Jan 30.
Artigo em Inglês | MEDLINE | ID: mdl-31583701

RESUMO

BACKGROUND: Hibiscus sabdariffa is commonly used in daily life and its extract is applied widely in food and cosmetics. However, it has not been evaluated for its anti-aging effects. RESULTS: Hibiscus sabdariffa calyx aqueous extract (HSCAE) has shown potential collagenase activity suppression effects, together with tyrosinase activity inhibition, and anti-oxidation as a free radical scavenger. The current investigation demonstrated that HSCAE was not cytotoxic in skin fibroblasts, and it significantly decreased ultraviolet B (UVB)-induced reactive oxygen species (ROS) on a flow cytometry assay. Moreover, HSCAE reduced matrix metalloproteinase (MMP) expression, increased tissue inhibition of metalloproteinase (TIMP)-1 level, and enhanced collagen content by inhibiting collagenase activity. It also blocked mRNA and protein expressions of melanin production pathway key factors, including the microphthalmia-associated transcription factor (MITF), tyrosinase, tyrosinase-related protein-1 (TRP-1), and dopachrome tautomerase-2 (TRP-2). CONCLUSION: These results demonstrated, for the first time, the potential of HSCAE as a natural antioxidant with the ability to maintain collagen production and to decrease melanin syntheses under UVB radiation, for anti-aging effects. © 2019 Society of Chemical Industry.


Assuntos
Depuradores de Radicais Livres/farmacologia , Hibiscus/química , Extratos Vegetais/farmacologia , Envelhecimento da Pele/efeitos dos fármacos , Animais , Linhagem Celular , Fibroblastos/efeitos dos fármacos , Fibroblastos/metabolismo , Fibroblastos/efeitos da radiação , Humanos , Oxirredutases Intramoleculares/genética , Oxirredutases Intramoleculares/metabolismo , Camundongos , Monofenol Mono-Oxigenase/genética , Monofenol Mono-Oxigenase/metabolismo , Oxirredutases/genética , Oxirredutases/metabolismo , Espécies Reativas de Oxigênio/metabolismo , Envelhecimento da Pele/efeitos da radiação , Raios Ultravioleta/efeitos adversos
2.
J Agric Food Chem ; 67(40): 11089-11098, 2019 Oct 09.
Artigo em Inglês | MEDLINE | ID: mdl-31509411

RESUMO

Reactive oxygen species and subsequent oxidative stress are reported to play important roles in chronic metabolic diseases. Plant-derived polyphenols, especially food-derived phenolics, have attracted a lot of attention due to their potential usage against oxidative stress-related diseases. The leaf of Psidium guajava (known as guava) is regarded as a good resource of polyphenols and its products are commercially available in Japan as functional foods against multiple chronic metabolism disorders. In the course of finding novel polyphenols with antioxidative activities from guava leaf, 11 acylated phenolic glycosides (1-11), including 5 new oleuropeic acid-conjugated phenolic glycosides, named guajanosides A-E (1, 2, and 5-7), along with 17 known meroterpenoides (12-28), were isolated and identified. Their structures were determined by spectroscopic data analysis, chemical degradation, and acid hydrolysis. Compounds 1, 2, and 5-11 displayed potent reactive oxygen species-scavenging activity in lipopolysaccharide-stimulated RAW 264.7 macrophage cells. Western blot revealed that compound 6 markedly increased the expression levels of nuclear factor-erythroid 2-related factor 2 (Nrf2), NAD(P)H quinone dehydrogenase 1 (NQO1), and the glutamate-cysteine ligase catalytic subunit. The current study revealed the presence of oleuropeic acid-derived phenolic glycosides in guava leaf and highlighted the potential usage of this type of phenolics against oxidative stress-related metabolic diseases via activation of the Nrf2 signaling pathway.


Assuntos
Depuradores de Radicais Livres/farmacologia , Glicosídeos/farmacologia , Fenóis/farmacologia , Extratos Vegetais/farmacologia , Psidium/química , Espécies Reativas de Oxigênio/metabolismo , Animais , Depuradores de Radicais Livres/química , Glicosídeos/química , Macrófagos/efeitos dos fármacos , Macrófagos/metabolismo , Camundongos , Fator 2 Relacionado a NF-E2/genética , Fator 2 Relacionado a NF-E2/metabolismo , Estresse Oxidativo/efeitos dos fármacos , Fenóis/química , Extratos Vegetais/química , Folhas de Planta/química , Células RAW 264.7
3.
Chem Biol Interact ; 313: 108826, 2019 Nov 01.
Artigo em Inglês | MEDLINE | ID: mdl-31545954

RESUMO

BACKGROUND: Despite of the most effective surgical removal of malignant tumors, metastasis makes cancer treatment difficult. The studies on natural compounds to inhibit this metastasis have been actively performed until now. However, the effect of tomatidine on metastasis remains unclear. METHOD: The effect of tomatidine on antioxidative activity was measured with DPPH radical assay and reducing power assay. After treatment with tomatidine, the viability of human fibrosarcoma cells (HT1080 cells) was evaluated with MTT assay. The effect of tomatidine on the inhibition of matrix metalloproteinase-2 (MMP-2) and MMP-9, gelatinases related to metastasis, was analyzed using gelatin zymography, western blot and immunofluorescence staining. Cell invasion assay was used to investigate anti-metastasis activity of tomatidine. RESULT: Tomatidine showed no DPPH radical scavenging effect and showed 8% of reduction power at 8 µM. Furthermore, tomatidine below 8 µM showed more than 80% of cell viability in MTT assay. The inhibition of tomatidine on MMP-2 activity and its protein expression levels were observed by gelatin zymography, western blot and immunofluorescence. It was observed that tomatidine inhibited not only p38 and ERK but also cell invasion. CONCLUSION: Above results suggest that tomatidine could use as a potential candidate for cancer prevention and metastasis through the inhibitory effect on gelatinase.


Assuntos
Antineoplásicos Fitogênicos/farmacologia , Tomatina/análogos & derivados , Proteínas Quinases p38 Ativadas por Mitógeno/metabolismo , Linhagem Celular Tumoral , Movimento Celular/efeitos dos fármacos , Núcleo Celular/efeitos dos fármacos , Núcleo Celular/metabolismo , Ativação Enzimática/efeitos dos fármacos , MAP Quinases Reguladas por Sinal Extracelular/metabolismo , Depuradores de Radicais Livres/farmacologia , Humanos , Metaloproteinase 2 da Matriz/metabolismo , Metaloproteinase 9 da Matriz/metabolismo , NF-kappa B/metabolismo , Acetato de Tetradecanoilforbol/farmacologia , Tomatina/farmacologia , Fator de Transcrição AP-1/metabolismo , Fator A de Crescimento do Endotélio Vascular/farmacologia
4.
Chem Biodivers ; 16(10): e1900381, 2019 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-31403756

RESUMO

The variability in the phytochemical concentrations of Capsicum annuum var. glabriusculum has not been extensively analyzed among wild populations and ecologic niches in its phylogeographic area. This study aimed to determine the variations in the phytochemical and antioxidant contents of the wild Piquin chili. The total flavonoid content of hydroalcoholic extracts (0.06 to 0.70 mg equivalent of quercetin per gram of dry weight (mg QE/g DW)), free radical-scavenging capacity for 2,2-diphenyl-1-picrylhydrazyl (DPPH. ) radicals (0.55 to 8.55 mm TE/g DW), amount of 2,2'-azinobis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS+ ) in aqueous extracts (18.13 to 107.6 mm TE/g DW) and pungency (21,760 to 88,476 Scoville heat units) were highly variable. By analyzing the spatial distribution using the first three principal components, correlations between the phytochemical content and the free radical-scavenging capacity (in both extracts) and flavonoid and phenolic contents (in the hydroalcoholic extract) were observed. Consistent with the statistical analysis, the spatial analysis showed intraregional differences in composition patterns, with an emphasis on central and coastal areas. Flavonoid contents, polyphenol contents and free radical-scavenging activity were the phytochemical components that mainly contributed to the diversity of the population.


Assuntos
Compostos de Bifenilo/antagonistas & inibidores , Capsicum/química , Depuradores de Radicais Livres/farmacologia , Compostos Fitoquímicos/farmacologia , Picratos/antagonistas & inibidores , Ácidos Sulfônicos/antagonistas & inibidores , Tiazóis/antagonistas & inibidores , Depuradores de Radicais Livres/química , Depuradores de Radicais Livres/isolamento & purificação , Compostos Fitoquímicos/química , Compostos Fitoquímicos/isolamento & purificação
5.
Acta Crystallogr C Struct Chem ; 75(Pt 8): 1091-1101, 2019 Aug 01.
Artigo em Inglês | MEDLINE | ID: mdl-31380792

RESUMO

A new set of differently hydrated barium and strontium squarates, namely poly[[triaqua(µ-1,2-dioxocyclobut-3-ene-1,2-diolato)barium] monohydrate], {[Ba(C4O4)(H2O)3]·H2O}n (1), poly[[diaqua(µ-1,2-dioxocyclobut-3-ene-1,2-diolato)strontium] monohydrate], {[Sr(C4O4)(H2O)2]·H2O}n (2), and poly[[triaqua(µ-1,2-dioxocyclobut-3-ene-1,2-diolato)barium/strontium(0.85/0.15)] monohydrate], {[Ba0.85Sr0.15(C4O4)(H2O)3]·H2O}n (3), is reported. The study of their crystal structures indicates that all the complexes crystallize in the triclinic space group P-1. Complexes 1 and 3 have a rare combination of squarate units coordinated through monodentate O atoms to two different metal atoms and through two bidentate O atoms to three different metal atoms. Furthermore, they have three coordinated water molecules to give a coordination number of nine. The squarate ligands in complex 2 exhibit two different coordination modes: (i) monodentate O atoms coordinated to four different Sr atoms and (ii) two monodentate O atoms coordinated to two different metal atoms with the other two O atoms bidentate to four different Sr atoms. All the compounds decompose to give the respective carbonates when heated to 800 °C, as evidenced by thermogravimetry/differential thermal analysis (TG-DTA), which are clusters of nanoparticles. Complexes 1 and 3 show additional endothermic peaks at 811 and 820 °C, respectively, indicating the phase transition of BaCO3 from an orthorhombic (α-Pmcn) to a trigonal phase (ß-R3m). All three complexes have significant DNA-binding constants, ranging from 2.45 × 104 to 9.41 × 104 M-1 against EB-CT (ethidium bromide-calf thymus) DNA and protein binding constants ranging from 1.1 × 105 to 8.6 × 105 with bovine serum albumin. The in vitro cytotoxicity of the complexes is indicated by the IC50 values, which range from 128.8 to 261.3 µg ml-1. Complex 3 shows better BSA binding, antioxidant activity against the DPPH radical and cytotoxicity than complexes 1 and 2.


Assuntos
Antineoplásicos/farmacologia , Complexos de Coordenação/farmacologia , Ciclobutanos/farmacologia , Depuradores de Radicais Livres/farmacologia , Substâncias Intercalantes/farmacologia , Animais , Antineoplásicos/síntese química , Antineoplásicos/química , Antineoplásicos/metabolismo , Bário/química , Bovinos , Complexos de Coordenação/síntese química , Complexos de Coordenação/química , Complexos de Coordenação/metabolismo , Cristalografia por Raios X , Ciclobutanos/síntese química , Ciclobutanos/química , Ciclobutanos/metabolismo , DNA/metabolismo , Depuradores de Radicais Livres/síntese química , Depuradores de Radicais Livres/química , Depuradores de Radicais Livres/metabolismo , Humanos , Ligações de Hidrogênio , Substâncias Intercalantes/síntese química , Substâncias Intercalantes/química , Substâncias Intercalantes/metabolismo , Ligantes , Células MCF-7 , Estrutura Molecular , Ligação Proteica , Soroalbumina Bovina/metabolismo , Estrôncio/química , Água/química
6.
Food Chem ; 299: 125119, 2019 Nov 30.
Artigo em Inglês | MEDLINE | ID: mdl-31295638

RESUMO

Of all the active compounds in rosemary extract, carnosic acid (CaA) has the most potent antimicrobial and antioxidant activity; however, its low solubility limits its applications. We developed complexing systems using cycloamylose (CA), branched dextrin (BD), and ß-cyclodextrin (ßCD) to improve the solubility of CaA and compared it to the use of maltodextrin (MD). The complexes formed with CA, BD, ßCD, and MD improved the water solubility of CaA by as much as 2.8-fold, 2.1-fold, 1.75-fold, and 2.06-fold, respectively. The antioxidant capacity of CaA in aqueous solutions was also enhanced in the complexes due to the increased water solubility. Interestingly, the antimicrobial activity was improved more dramatically upon complexation with CA (7.27-fold) compared to the improvement when complexed with BD (4.82-fold), ßCD (2.87-fold), and MD (3.83-fold). This may be due to the improvement of the antimicrobial potential of the functional groups of CaA by complexation with flexible cyclic glucans.


Assuntos
/farmacologia , Anti-Infecciosos/farmacologia , Antioxidantes/farmacologia , Conservantes de Alimentos/farmacologia , Extratos Vegetais/farmacologia , Rosmarinus/química , Ciclodextrinas/química , Aditivos Alimentares , Depuradores de Radicais Livres/farmacologia , Glucanos/química , Extratos Vegetais/isolamento & purificação , Polissacarídeos/química , Solubilidade/efeitos dos fármacos , beta-Ciclodextrinas/química
7.
Int J Nanomedicine ; 14: 4801-4816, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-31308659

RESUMO

Background: Silver nanoparticles (AgNPs) inhibit the proliferation of various fungi; however, their mechanisms of action remain poorly understood. To better understand the inhibitory mechanisms, we focused on the early events elicited by 5 nm AgNPs in pathogenic Candida albicans and non-pathogenic Saccharomyces cerevisiae. Methods: The effect of 5 nm and 100 nm AgNPs on fungus cell proliferation was analyzed by growth kinetics monitoring and spot assay. We examined cell cycle progression, reactive oxygen species (ROS) production, and cell death using flow cytometry. Glucose uptake was assessed using tritium-labeled 2-deoxyglucose. Results: The growth of both C. albicans and S. cerevisiae was suppressed by treatment with 5 nm AgNPs but not with 100 nm AgNPs. In addition, 5 nm AgNPs induced cell cycle arrest and a reduction in glucose uptake in both fungi after 30 minutes of culture in a dose-dependent manner (P<0.05). However, in C. albicans only, an increase in ROS production was detected after exposure to 5 nm AgNPs. Concordantly, an ROS scavenger blocked the effect of 5 nm AgNPs on the cell cycle and glucose uptake in C. albicans only. Furthermore, the growth-inhibition effect of 5 nm AgNPs was not greater in S. cerevisiae mutant strains deficient in oxidative stress response genes than it was in wild type. Finally, 5 nm AgNPs together with a glycolysis inhibitor, 3-bromopyruvate, synergistically enhanced cell death in C. albicans (P<0.05) but not in S. cerevisiae. Conclusion: AgNPs exhibit antifungal activity in a manner that may or may not be ROS dependent, according to the fungal species. The combination of AgNPs with 3-bromopyruvate may be more useful against infection with C. albicans.


Assuntos
Candida albicans/citologia , Ciclo Celular/efeitos dos fármacos , Nanopartículas Metálicas/toxicidade , Piruvatos/farmacologia , Espécies Reativas de Oxigênio/metabolismo , Saccharomyces cerevisiae/citologia , Prata/farmacologia , Antifúngicos/farmacologia , Candida albicans/efeitos dos fármacos , Candida albicans/crescimento & desenvolvimento , Morte Celular/efeitos dos fármacos , Proliferação de Células/efeitos dos fármacos , Parede Celular/efeitos dos fármacos , Parede Celular/genética , Depuradores de Radicais Livres/farmacologia , Fase G1/efeitos dos fármacos , Genes Fúngicos , Glucose/metabolismo , Glicólise/efeitos dos fármacos , Testes de Sensibilidade Microbiana , Mitocôndrias/efeitos dos fármacos , Mitocôndrias/metabolismo , Estresse Oxidativo/efeitos dos fármacos , Estresse Oxidativo/genética , Saccharomyces cerevisiae/efeitos dos fármacos , Saccharomyces cerevisiae/genética , Saccharomyces cerevisiae/crescimento & desenvolvimento
8.
BMC Complement Altern Med ; 19(1): 164, 2019 Jul 08.
Artigo em Inglês | MEDLINE | ID: mdl-31286949

RESUMO

BACKGROUND: Caesalpinia mimosoides, a vegetable consumed in Thailand, has been reported to exhibit in vitro antioxidant properties. The in vivo antioxidant and anti-aging activities have not been investigated. The aim of this research was to study the antioxidant activity of C. mimosoides extracts in Caenorhabditis elegans, a widely used model organism in this context. METHODS: C. elegans were treated with C. mimosoides extracts in a various concentrations. To investigate the protective effects of the extract against oxidative stress, wild-type N2 were used to determine survival rate under oxidative stress and intracellular ROS. To study underlying mechanisms, the mutant strains with GFP reporter gene including TJ356, CF1553, EU1 and LD4 were used to study DAF-16, SOD-3, SKN-1 and GST-4 gene, respectively. Lifespan and aging pigment of the worms were also investigated. RESULTS: A leaf extract of C. mimosoides improved resistance to oxidative stress and reduced intracellular ROS accumulation in nematodes. The antioxidant effects were mediated through the DAF-16/FOXO pathway and SOD-3 expression, whereas the expression of SKN-1 and GST-4 were not altered. The extract also prolonged lifespan and decreased aging pigments, while the body length and brood size of the worms were not affected by the extract, indicating low toxicity and excluding dietary restriction. CONCLUSIONS: The results of this study establish the antioxidant activity of C. mimosoides extract in vivo and suggest its potential as a dietary supplement and alternative medicine to defend against oxidative stress and aging, which should be investigated in intervention studies.


Assuntos
Antioxidantes/farmacologia , Caenorhabditis elegans/efeitos dos fármacos , Caesalpinia/química , Longevidade/efeitos dos fármacos , Extratos Vegetais/farmacologia , Animais , Tamanho Corporal/efeitos dos fármacos , Caenorhabditis elegans/metabolismo , Caenorhabditis elegans/fisiologia , Proteínas de Caenorhabditis elegans/metabolismo , Flavonoides/análise , Depuradores de Radicais Livres/farmacologia , Metanol , Naftoquinonas , Fenóis/análise , Folhas de Planta/química , Espécies Reativas de Oxigênio , Reprodução/efeitos dos fármacos
9.
Food Chem Toxicol ; 131: 110563, 2019 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-31199992

RESUMO

Apple pomace (AP) utilised for analysis of triterpenic acids (TTAs) using HPLC-MS/MS. The methanol, ethanol and ethyl acetate extracts showed high phenolic content with significant antioxidant activity compared to chloroform and n-hexane. AP TTAs; ursolic acid, betulinic acid and maslinic acid showed potent antioxidant and enzyme inhibitory effects. The IC50 values were 13.2-30.8 µg/mL (tyrosinase), 19.6-42.5 µg/mL (xanthine oxidase) and 16.6-38.6 µg/mL (urease) for AP extracts and 8.4-25.8 µg/mL (tyrosinase), 12.6-30.2 µg/mL (xanthine oxidase) and 10.1-28.6 µg/mL (urease) for TTAs, compared to the positive controls; kojic acid (10.4 ±â€¯0.06 µg/mL), allopurinol (9.6 ±â€¯0.04 µg/mL) and thiourea (8.9 ±â€¯0.02 µg/mL) towards respective enzymes. UA showed a competitive type of inhibition for tyrosinase, while BA showed a noncompetitive type of inhibition towards xanthine oxidase. In addition, the AP extracts and TTAs exerted significant cytotoxic effects towards the proliferation of cancer cell lines. AP methanol extract (IC50 of 38.5 ±â€¯4.1, 47.1 ±â€¯3.5, 70.6 ±â€¯2.3, and 50.5 ±â€¯3.9 µg/mL) and ursolic acid (IC50 of 6.5 ±â€¯0.7, 15.5 ±â€¯1.4, 20.8 ±â€¯1.3, and 5.6 ±â€¯0.8 µg/mL) showed prominent anticancer activity on Hela, Skov-3, Caski, and NCL cancer cell lines, respectively. Thus, this study shows that the AP & TTAs could be utilized for functional food development and as a potent antioxidant, anticancer, skin whitening, and anti-urolithic agents.


Assuntos
Antineoplásicos/farmacologia , Inibidores Enzimáticos/farmacologia , Depuradores de Radicais Livres/farmacologia , Frutas/química , Malus/química , Triterpenos/farmacologia , Animais , Antineoplásicos/química , Antineoplásicos/isolamento & purificação , Linhagem Celular Tumoral , Cães , Ensaios Enzimáticos , Inibidores Enzimáticos/química , Inibidores Enzimáticos/isolamento & purificação , Depuradores de Radicais Livres/química , Depuradores de Radicais Livres/isolamento & purificação , Humanos , Células Madin Darby de Rim Canino , Monofenol Mono-Oxigenase/antagonistas & inibidores , Extratos Vegetais/análise , Extratos Vegetais/química , Extração em Fase Sólida , Triterpenos/química , Triterpenos/isolamento & purificação , Urease/antagonistas & inibidores , Xantina Oxidase/antagonistas & inibidores
10.
Carbohydr Polym ; 221: 73-83, 2019 Oct 01.
Artigo em Inglês | MEDLINE | ID: mdl-31227169

RESUMO

A protein-containing polysaccharide, LCP, showing strong antioxidant activity from the rhizome of Ligusticum chuanxiong Hort was fractionated and purified. Its physicochemical properties were characterised by gel permeation chromatography (GPC), gas chromatography-mass spectrometry (GC-MS), UV and IR analysis. The results showed that LCP was proteoglycan containing 85.7% total carbohydrate, 2.79% protein, 5.14% uronic acid, and four kinds of monosaccharides including xylose, glucose, mannose and galactose with molar ratios of 1.2: 7.8: 1: 2.1, respectively. The average molecular weight of LCP was 15.8 × 104 Da. In addition, the results indicated that LCP exhibited good radical scavenging abilities. Furthermore, LCP partially attenuated the incidence of mortalities and pericardial edema in zebrafish embryos exposed to hydrogen peroxide (H2O2). Moreover, LCP provided protection against H2O2-induced ROS generation and cell death in zebrafish embryo. These results indicated that LCP could be a potential approach for oxidative stress damage reversal.


Assuntos
Depuradores de Radicais Livres/farmacologia , Ligusticum/química , Polissacarídeos/farmacologia , Animais , Desenvolvimento Embrionário/efeitos dos fármacos , Depuradores de Radicais Livres/química , Depuradores de Radicais Livres/isolamento & purificação , Depuradores de Radicais Livres/toxicidade , Peróxido de Hidrogênio/farmacologia , Peso Molecular , Estresse Oxidativo/efeitos dos fármacos , Polissacarídeos/química , Polissacarídeos/isolamento & purificação , Polissacarídeos/toxicidade , Espécies Reativas de Oxigênio/metabolismo , Rizoma/química , Peixe-Zebra/embriologia
11.
Food Chem Toxicol ; 131: 110535, 2019 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-31154083

RESUMO

This study endeavours to investigate the phytochemical composition, biological properties and in vivo toxicity of methanol and dichloromethane extracts of Zaleya pentandra (L.) Jeffrey. Total bioactive contents, antioxidant (phosphomolybdenum and metal chelating, DPPH, ABTS, FRAP and CUPRAC) and enzyme inhibition (cholinesterases, tyrosinase α-amylase, and α-glucosidase) potential were assessed utilizing in vitro bioassays. UHPLC-MS phytochemical profiling was carried out to identify the essential compounds. The methanol extract was found to contain highest phenolic (22.60 mg GAE/g) and flavonoid (31.49 mg QE/g) contents which correlate with its most significant radical scavenging, reducing potential and tyrosinase inhibition. The dichloromethane extract was most potent for phosphomolybdenum, ferrous chelation, α-amylase, α-glucosidase, and cholinesterase inhibition assays. UHPLC-MS analysis of methanol extract unveiled to identify 11 secondary metabolites belonging to five sub-groups, i.e., phenolic, alkaloid, carbohydrate, terpenoid, and fatty acid derivatives. Additionally, in vivo toxicity was conducted for 21 days and the methanol extract at different doses (150, 200, 250 and 300 mg/kg) was administered in experimental chicks divided into five groups each containing five individuals. Different physical, haematological and biochemical parameters along with the absolute and relative weight of visceral body organs were studied. Overall, no toxic effect was noted for the extract at tested doses.


Assuntos
Aizoaceae/química , Extratos Vegetais/farmacologia , Extratos Vegetais/toxicidade , Administração Oral , Animais , Galinhas , Inibidores Enzimáticos/administração & dosagem , Inibidores Enzimáticos/química , Inibidores Enzimáticos/farmacologia , Inibidores Enzimáticos/toxicidade , Depuradores de Radicais Livres/administração & dosagem , Depuradores de Radicais Livres/química , Depuradores de Radicais Livres/farmacologia , Depuradores de Radicais Livres/toxicidade , Metanol/química , Extratos Vegetais/administração & dosagem , Extratos Vegetais/química
12.
Expert Opin Investig Drugs ; 28(7): 593-603, 2019 07.
Artigo em Inglês | MEDLINE | ID: mdl-31185180

RESUMO

INTRODUCTION: Oxidative stress toxicity (OST) has been implicated in almost all pathological conditions. Despite the widespread use of natural antioxidants, no pharmaceutical antioxidants have yet been developed or prescribed in medical practise. Antioxidant drugs such as Deferiprone and N-acetylcysteine can target essential pathways of OST in many pathological conditions. The pharmacological parameters required by antioxidant drugs in relation to the OST target characteristics include the determination of the therapeutic index, ADMET and drug interactions. Antioxidant drug development efforts are currently targeting the treatment of severe diseases with no proven effective therapies. AREAS COVERED: This article addresses the damaging effects of OST, prospects for the development of pharmaceutical antioxidants and clinical studies using other drugs with antioxidant potential. EXPERT OPINION: Effective antioxidant therapeutic strategies should include the design of protocols for the inhibition of OST through iron chelation, administration of synthetic and natural antioxidants and enhancement of the antioxidant defences by increasing the production of endogenous antioxidants and activation of antioxidant mechanisms. Different therapeutic strategies apply in the use of antioxidant drugs for one or more targets, for prevention, treatment, or of post-treatment effects and for systematic, long-term or short-term applications. The design of new antioxidant drugs and effective protocols which can include Deferiprone and N-acetylcysteine combinations, could lead to the development of a new class of therapeutics for clinical use.


Assuntos
Antioxidantes/farmacologia , Depuradores de Radicais Livres/farmacologia , Estresse Oxidativo/efeitos dos fármacos , Acetilcisteína/administração & dosagem , Acetilcisteína/farmacologia , Animais , Antioxidantes/administração & dosagem , Deferiprona/administração & dosagem , Deferiprona/farmacologia , Desenho de Drogas , Desenvolvimento de Medicamentos/métodos , Depuradores de Radicais Livres/administração & dosagem , Radicais Livres , Humanos , Quelantes de Ferro/administração & dosagem , Quelantes de Ferro/farmacologia , Terapia de Alvo Molecular
13.
Life Sci ; 231: 116544, 2019 Aug 15.
Artigo em Inglês | MEDLINE | ID: mdl-31181229

RESUMO

AIMS: To investigate the effect of long-term N-acetyl-l-cysteine (NAC) treatment in Wistar rats subjected to renal ischemia and reperfusion (IR) and a chronic high­sodium diet (HSD). MAIN METHODS: Adult male Wistar rats received an HSD (8.0% NaCl) or a normal­sodium diet (NSD; 1.3% NaCl) and NAC (600 mg/L) or normal drinking water starting at 8 weeks of age. At 11 weeks of age, the rats from both diet and NAC or water treatment groups underwent renal IR or Sham surgery and were followed for 10 weeks. The study consisted of six animal groups: NSD + Sham + water; NSD + IR + water; NSD + IR + NAC; HSD + Sham + water; HSD + IR + water; and HSD + IR + NAC. KEY FINDINGS: Tail blood pressure (tBP) increased with IR and NAC treatment in the NSD group but not in the HSD group. The serum creatinine level was higher after NAC treatment in both diet groups, and creatinine clearance was decreased in only the HSD + IR + NAC group. Albuminuria increased in the HSD + IR + water group and decreased in the HSD + IR + NAC group. Kidney mass was increased in the HSD + IR group and decreased with NAC treatment. Renal fibrosis was prevented with NAC treatment and cardiac fibrosis was decreased with NAC treatment in the HSD + IR group. SIGNIFICANCE: NAC treatment promoted structural improvements, such as decreased albuminuria and fibrosis, in the kidney and heart. However, NAC could not recover kidney function or blood pressure from the effects of IR associated with an HSD. Therefore, in general, long-term NAC treatment is not effective and is deleterious to recovery of function after kidney injury.


Assuntos
Acetilcisteína/farmacologia , Isquemia Encefálica/fisiopatologia , Rim/irrigação sanguínea , Traumatismo por Reperfusão/fisiopatologia , Cloreto de Sódio na Dieta/efeitos adversos , Lesão Renal Aguda/prevenção & controle , Animais , Pressão Sanguínea/efeitos dos fármacos , Isquemia Encefálica/metabolismo , Depuradores de Radicais Livres/farmacologia , Isquemia/etiologia , Isquemia/metabolismo , Isquemia/patologia , Isquemia/fisiopatologia , Rim/efeitos dos fármacos , Rim/metabolismo , Masculino , Ratos , Ratos Wistar , Reperfusão/métodos , Traumatismo por Reperfusão/metabolismo , Cloreto de Sódio na Dieta/administração & dosagem
14.
Food Chem Toxicol ; 131: 110539, 2019 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-31158404

RESUMO

The chemical characterization and protective role against ethanol-induced gastric ulcerated rats of a polysaccharide fraction from Bletilla striata (BSP) collected by ultrafiltration membrane approach were evaluated. This BSP faction was consisted of mannose and glucose at a molar ratio of 2.4:1 approximately, with a molecular weight of 146 KDa. FT-IR, NMR and XRD spectra indicated that BSP faction contained α-Man and ß-Glc residues with low overall crystallinity. The polysaccharide exhibited significant scavenging activities of ABTS and FRAP, as well as non-toxicity against human gastric epithelial GES-1 cells. Oral administration with 100 mg/kg of BSP for 3 days continuously could significantly prevent the formation of ethanol-induced gastric mucosal lesion. It could also reduce the levels of pro-inflammatory cytokines, including TNF-α, IL-1ß, IL-6, and IL-18, and MPO activity in gastric tissue. Additionally, the BSP faction exhibited antioxidant activity, increased the content of PEG2 as a defensive factor, and suppressed MAPK/NF-κB signaling pathway in gastric tissue. These results indicated that the gastroprotective activity of BSP faction could be attributed to the reduction of pro-inflammatory cytokines and oxidative stress and the inhibition of MAPK/NF-κB pathways. Our results provided substantial evidence that BSP could be a promising phytomedicine for gastric ulcer prevention.


Assuntos
Fármacos Gastrointestinais/farmacologia , Orchidaceae/química , Polissacarídeos/farmacologia , Úlcera Gástrica/tratamento farmacológico , Animais , Anti-Inflamatórios/isolamento & purificação , Anti-Inflamatórios/farmacologia , Anti-Inflamatórios/toxicidade , Linhagem Celular , Citocinas/metabolismo , Dinoprostona/metabolismo , Etanol , Depuradores de Radicais Livres/isolamento & purificação , Depuradores de Radicais Livres/farmacologia , Depuradores de Radicais Livres/toxicidade , Mucosa Gástrica/patologia , Fármacos Gastrointestinais/isolamento & purificação , Fármacos Gastrointestinais/toxicidade , Humanos , Estresse Oxidativo/efeitos dos fármacos , Peroxidase/metabolismo , Polissacarídeos/isolamento & purificação , Polissacarídeos/toxicidade , Ratos , Transdução de Sinais/efeitos dos fármacos , Úlcera Gástrica/induzido quimicamente , Superóxido Dismutase/metabolismo
15.
Eur J Med Chem ; 177: 414-424, 2019 Sep 01.
Artigo em Inglês | MEDLINE | ID: mdl-31158754

RESUMO

Due to the role of butyrylcholinesterase (BChE) in acetylcholine hydrolysis in the late stages of the Alzheimer's disease (AD), inhibitors of butyrylcholinesterase (BChE) have been recently envisaged, besides acetylcholinesterase (AChE) inhibitors, as candidates for treating mild-to-moderate AD. Herein, synthesis and AChE/BChE inhibition activity of some twenty derivatives of 1,2,3,4,5,6-hexahydroazepino[4,3-b]indole (HHAI) is reported. Most of the newly synthesized HHAI derivatives achieved the inhibition of both ChE isoforms with IC50s in the micromolar range, with a structure-dependent selectivity toward BChE. Apparently, molecular volume and lipophilicity do increase selectivity toward BChE, and indeed the N2-(4-phenylbutyl) HHAI derivative 15d, which behaves as a mixed-type inhibitor, resulted the most potent (IC50 0.17 µM) and selective (>100-fold) inhibitor toward either horse serum and human BChE. Moreover, 15d inhibited in vitro self-induced aggregation of neurotoxic amyloid-ß (Aß) peptide and displayed neuroprotective effects in neuroblastoma SH-SY5Y cell line, significantly recovering (P < 0.001) cell viability when impaired by Aß1-42 and hydrogen peroxide insults. Overall, this study highlighted HHAI as useful and versatile scaffold for developing new small molecules targeting some enzymes and biochemical pathways involved in the pathogenesis of AD.


Assuntos
Azepinas/farmacologia , Inibidores da Colinesterase/farmacologia , Indóis/farmacologia , Fármacos Neuroprotetores/farmacologia , Peptídeos beta-Amiloides/metabolismo , Azepinas/síntese química , Azepinas/química , Azepinas/metabolismo , Butirilcolinesterase/química , Butirilcolinesterase/metabolismo , Domínio Catalítico , Linhagem Celular Tumoral , Inibidores da Colinesterase/síntese química , Inibidores da Colinesterase/química , Inibidores da Colinesterase/metabolismo , Relação Dose-Resposta a Droga , Desenho de Drogas , Depuradores de Radicais Livres/síntese química , Depuradores de Radicais Livres/química , Depuradores de Radicais Livres/metabolismo , Depuradores de Radicais Livres/farmacologia , Humanos , Indóis/síntese química , Indóis/química , Indóis/metabolismo , Simulação de Acoplamento Molecular , Estrutura Molecular , Fármacos Neuroprotetores/síntese química , Fármacos Neuroprotetores/química , Fármacos Neuroprotetores/metabolismo , Fragmentos de Peptídeos/metabolismo , Ligação Proteica/efeitos dos fármacos , Multimerização Proteica/efeitos dos fármacos , Relação Estrutura-Atividade
16.
Molecules ; 24(11)2019 May 30.
Artigo em Inglês | MEDLINE | ID: mdl-31151176

RESUMO

Oxidative stress has been incriminated in the physiopathology of many diseases, such as diabetes, cancer, atherosclerosis, and cardiovascular and neurodegenerative diseases. There is a great interest in developing new antioxidants that could be useful for preventing and treating conditions for which oxidative stress is suggested as the root cause. The thiazolidine-2,4-dione derivatives have been reported to possess various pharmacological activities and the phenol moiety is known as a pharmacophore in many naturally occurring and synthetic antioxidants. Twelve new phenolic derivatives of thiazolidine-2,4-dione were synthesized and physicochemically characterized. The antioxidant capacity of the synthesized compounds was assessed through several in vitro antiradical, electron transfer, and Fe2+ chelation assays. The top polyphenolic compounds 5f and 5l acted as potent antiradical and electron donors, with activity comparable to the reference antioxidants used. The ferrous ion chelation capacity of the newly synthesized compounds was modest. Several quantum descriptors were calculated in order to evaluate their influence on the antioxidant and antiradical properties of the compounds and the chemoselectivity of the radical generation reactions has been evaluated. The correlation with the energetic level of the frontier orbitals partially explained the antioxidant activity, whereas a better correlation was found while evaluating the O-H bond dissociation energy of the phenolic groups.


Assuntos
Antioxidantes/química , Antioxidantes/farmacologia , Depuradores de Radicais Livres/química , Depuradores de Radicais Livres/farmacologia , Tiazolidinedionas/química , Tiazolidinedionas/farmacologia , Antioxidantes/síntese química , Quelantes/síntese química , Quelantes/química , Quelantes/farmacologia , Técnicas de Química Sintética , Transporte de Elétrons , Depuradores de Radicais Livres/síntese química , Radicais Livres/antagonistas & inibidores , Humanos , Estrutura Molecular , Fenóis/química , Teoria Quântica , Tiazolidinedionas/síntese química
17.
ScientificWorldJournal ; 2019: 7549620, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-31223295

RESUMO

Carissa edulis is a plant used in the management of oxidative stress and inflammatory related disorders such as malaria, rheumatism inflammation, and cardiovascular diseases. The present study evaluates the total phenolic content, antioxidant capacity (DPPH, ABTS, and FRAP), and the bioactive compounds present in the various extracts of C. edulis (HEC, MEC, AEC, and PC). An HPLC analysis determined the different compounds present in the extracts. High concentration of total phenolic content was observed in aqueous and methanolic extracts more than in the hydroethanolic extract though not significantly different. Flavonoids were higher in the hydroethanolic and methanolic extracts, respectively, with 14.84 mg RE/g extract and 12.02 mg RE/g extract. Tannins were also found in large amounts in the same two extracts with 26.76 mg TAE/g extract and 34.67 mg TEE/g extract. The percentage radical scavenging activity DPPH ranged between 58.63% and 94.67% for aqueous extract and for ABTS between 51.39% and 94.12% for the methanolic extract. The highest FRAP was obtained in the methanolic extract (6.73 g AAE/100 g extract). HPLC analysis revealed the presence of quercetin, rutin, and gallic acid in the different extracts. C. edulis represents a potential source of bioactive components with antioxidant capacity.


Assuntos
Antioxidantes/farmacologia , Apocynaceae/química , Extratos Vegetais/farmacologia , Folhas de Planta/química , Antioxidantes/química , Cromatografia Líquida de Alta Pressão , Relação Dose-Resposta a Droga , Flavonoides/química , Depuradores de Radicais Livres/química , Depuradores de Radicais Livres/farmacologia , Fenóis/química , Compostos Fitoquímicos/química , Compostos Fitoquímicos/farmacologia , Extratos Vegetais/química , Taninos/química
18.
BMC Res Notes ; 12(1): 269, 2019 May 14.
Artigo em Inglês | MEDLINE | ID: mdl-31088517

RESUMO

OBJECTIVE: The purpose of the study was to generate information on the safety of probiotics, thus the study objectives were to evaluate the effects of Yoba® on basic physiochemical properties. The study assessed male w1118 Drosophila melanogaster which were provided food supplemented with Yoba® at 1%, 3%, 6%, and 12% on motor function, total protein, catalase activity, and hydrogen peroxide scavenging activity and lifespan. RESULTS: Yoba® at high concentration (≥ 6%) increased locomotor activity in Drosophila melanogaster, however, total protein, catalase, and hydrogen peroxide scavenging activity were significantly higher at 1% Yoba® compared to 3%, 6%, and 12% Yoba®. Yoba consumed at 1% was associated with greater physiological benefits in Drosophila melanogaster. Findings in the study offer a rationale for the consumption of Yoba® at 1% in humans as is currently being promoted by the Yoba for Life consortium, however, high concentrations of Yoba® would disrupt physiological function as shown by this study.


Assuntos
Drosophila melanogaster/microbiologia , Lactobacillus rhamnosus/fisiologia , Animais , Catalase/metabolismo , Drosophila melanogaster/efeitos dos fármacos , Drosophila melanogaster/enzimologia , Depuradores de Radicais Livres/farmacologia , Peróxido de Hidrogênio/metabolismo , Longevidade , Masculino , Atividade Motora/efeitos dos fármacos
19.
ScientificWorldJournal ; 2019: 4705140, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-31110468

RESUMO

The variabilities in the phytochemical contents and antioxidant activities of four varieties of two closely related cultivated Capsicum species, C. annuum and C. frutescens, were examined as an additional tool for establishing their phylogenetic relatedness and for breeding purposes. The methodology involved the use of ethanolic and aqueous extractions for the determination of the phytochemical and antioxidant properties. The phytochemical contents including total flavonoid, total phenol, and proanthocyanidins were evaluated spectrophotometrically while the antioxidant activities were determined by 2,2-diphenyl-1-picrylhydrazyl (DPPH), 2,2'-azino-bis(3-ethylbenzothiazoline)-6-sulfonic acid (ABTS), nitric oxide (NO), and phosphomolybdenum assays. To point out the relationship among the varieties, a dendrogram based on the antioxidative phytochemical contents was constructed using the unweighted pair group method with arithmetic mean (UPMGA) cluster analysis. In all, aqueous extracts gave higher yield while ethanolic extracts showed higher phytochemical content across the varieties. Significant variations were observed among the varieties in relation to their phytochemical constituents and antioxidant activities. Dendrogram obtained from multivariate analysis distinguished the two Capsicum species. The first cluster contained only C. frutescens var. baccatum while the second cluster contained the three varieties of C. annuum species in subclusters, signifying the close genetic affinity among the three varieties. It also revealed that the four varieties are of a common progenitor. Information from this study gives additional evidence of chemotaxonomic significance and baseline data for effective selection of suitable parental genotypes in breeding for nutritional and pharmacological purposes.


Assuntos
Antioxidantes/farmacologia , Capsicum/química , Compostos Fitoquímicos/farmacologia , Extratos Vegetais/farmacologia , Antioxidantes/química , Relação Dose-Resposta a Droga , Estudos de Avaliação como Assunto , Depuradores de Radicais Livres/química , Depuradores de Radicais Livres/farmacologia , Óxido Nítrico/química , Fenótipo , Compostos Fitoquímicos/química , Extratos Vegetais/química
20.
J Appl Microbiol ; 127(2): 481-494, 2019 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-31141277

RESUMO

AIM: The aim of present work was to explore the potential of Chlorella sp. SRD3 extracts for antioxidant and antibacterial activity along with the evaluation of minimum inhibitory concentration (MIC) and haemolytic activity to detect RBC cell damage. METHODS AND RESULTS: Screening and isolation of microalgae was performed using bold basal medium under normal illuminance (at 27°C) and microscopic observation. Growth of the microalgae was optimized using a different medium and light source. The isolated microalgae incubated under fluorescent light when cultured in F/2 medium showed a highest dry biomass yield of 3·77 ± 0·1 g l-1 , when compared to the growth under direct sunlight (2·74 ± 0·07 g dwt l-1 ). The quantitative analysis of extracts revealed higher phenols, flavonoids and proanthocyanidins in ethyl acetate and hexane extracts followed by methanol. The antioxidant activity of extracts was tested against 1-diphenyl-2-picrylhydrazyl and ABTS radical, its reducing power assay was performed. From antibacterial activity, the two extracts showed better inhibition against Gram-negative bacteria. Also, they resulted in very low MIC values with effective activity against pathogens. In haemolytic activity, no haemolysis occurred, when the concentration (µg ml-1 ) was below 64 for methanol and 32 for ethyl acetate extract. In addition, Chlorella sp. extracts were characterized by GC-MS analysis to detect the major compounds. CONCLUSION: The polar extracts revealed satisfactory results against the clinical isolates and the compounds responsible were reflected in the GC-MS spectrum. SIGNIFICANCE AND IMPACT OF THE STUDY: The present study revealed significant biological potentials of the green alga, Chlorella sp. such as antioxidant, antibacterial and hemolytic activities. Therefore, this vital source might serve as a cost-effective, alternative choice to the pharmaceutical and food industries in the near future.


Assuntos
Antibacterianos/farmacologia , Chlorella , Depuradores de Radicais Livres/farmacologia , Antibacterianos/química , Chlorella/química , Chlorella/crescimento & desenvolvimento , Flavonoides/análise , Depuradores de Radicais Livres/química , Bactérias Gram-Negativas/efeitos dos fármacos , Hemolíticos/farmacologia , Humanos , Fenóis/análise , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Proantocianidinas/análise
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