Your browser doesn't support javascript.
Mostrar: 20 | 50 | 100
Resultados 1 - 20 de 1.440
Filtrar
1.
J Sci Food Agric ; 100(3): 1185-1194, 2020 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-31680262

RESUMO

BACKGROUND: Ludwigia hyssopifolia (G. Don) Exell, one of the problem weeds in some rice-producing countries, was studied to determine its allelopathic potential based on the effects of aqueous extracts of its tissues (leaves, roots and stem) on seedling growth of selected weeds and rice. The major phenolic compound of its leaves was also isolated and characterized. RESULTS: L. hyssopifolia aqueous leaf extract showed significant inhibition of shoot growth and biomass accumulation of weeds (Amaranthus spinosus L., Dactyloctenium aegyptium L., Cyperus iria L.) while maintaining less adverse effects on rice (crop) compared to other aqueous extracts of roots and stem. Phytochemical screening showed that phenols, tannins, flavonoids, terpenoids, saponins and coumarins are found in its leaf aqueous extract. The Folin-Ciocalteu method revealed that its leaves contain 26.66 ± 0.30 mg GAE g-1 leaf. The extract was then acid-hydrolyzed to liberate the phenolics (25 mg phenolics g-1 leaf). The major compound was isolated via preparative thin-layer chromatography using formic acid-ethyl acetate-n-hexane (0.05:4:6) solvent system. It had maximum UV absorption at 272 nm while its Fourier transform infrared spectrum revealed phenol, carboxylic acid and ether functionalities. This also had similar chromatographic mobility when run together with syringic acid in two-dimensional paper chromatography and thin-layer chromatography. CONCLUSIONS: L. hyssopifolia has potential allelopathic activity and its leaf aqueous extract showed the highest phytotoxic activity (P ≤ 0.05) indicating its potential as a bioherbicide. The most probable identity of the major phenolic compound is syringic acid. © 2019 Society of Chemical Industry.


Assuntos
Herbicidas/química , Onagraceae/química , Extratos Vegetais/química , Amaranthus/efeitos dos fármacos , Amaranthus/crescimento & desenvolvimento , Flavonoides/química , Flavonoides/isolamento & purificação , Flavonoides/farmacologia , Herbicidas/isolamento & purificação , Herbicidas/farmacologia , Fenóis/química , Fenóis/isolamento & purificação , Fenóis/farmacologia , Compostos Fitoquímicos/química , Compostos Fitoquímicos/isolamento & purificação , Compostos Fitoquímicos/farmacologia , Extratos Vegetais/isolamento & purificação , Extratos Vegetais/farmacologia , Folhas de Planta/química , Plantas Daninhas/efeitos dos fármacos , Plantas Daninhas/crescimento & desenvolvimento , Taninos/química , Taninos/farmacologia
2.
J Chem Ecol ; 46(1): 99-113, 2020 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-31845136

RESUMO

Goat herding is an important tool in the ecologically sound management of Mediterranean shrublands and woodlands, although effective levels of woody biomass removal by the goats is neither guaranteed nor easy to predict. Preliminary observations indicated that one reason for this may be poor understanding of plant-herbivore interactions that operate intraspecifically at the local spatial scale. We asked, whether goats show intraspecific preferences among neighboring plants when foraging a small local population of Pistacia lentiscus, a dominant tall shrub. First, we characterized and quantified the profile of stored and emitted volatile organic compounds (VOCs) and the PEG-binding capacity of tannins (a proxy for protein binding capacity) in the foliage of P. lentiscus shrubs, sampled within an area of 0.9 ha. We then tested goat preference between pairs of these shrubs that differed in chemical composition. Almost all sampled P. lentiscus shrubs were allocated to one of two distinct VOC chemotypes: one dominated by germacrene D and limonene (designated chemotype L) and the other by germacrene D and α-pinene (chemotype P). In contrast, continuous moderate variability was found in the binding capacity of tannins in the foliage. Goats showed preference for shrubs of chemotype L over those of chemotype P, and their preference was negatively correlated with the binding capacity of tannins. Possible influences of VOCs on goat preference that may explain the observed patterns are discussed in the light of possible context-dependent interpretation of plant VOC signals by large mammalian herbivores.


Assuntos
Herbivoria/efeitos dos fármacos , Pistacia/química , Taninos/farmacologia , Compostos Orgânicos Voláteis/farmacologia , Animais , Cromatografia Gasosa-Espectrometria de Massas , Cabras/fisiologia , Modelos Lineares , Pistacia/metabolismo , Folhas de Planta/química , Folhas de Planta/metabolismo , Análise de Componente Principal , Taninos/análise , Taninos/química , Compostos Orgânicos Voláteis/análise , Compostos Orgânicos Voláteis/química
3.
Molecules ; 24(17)2019 Aug 26.
Artigo em Inglês | MEDLINE | ID: mdl-31454971

RESUMO

Quercus mongolica Fisch. ex Ledeb. (QM) has been used as an oriental traditional medicine to relieve hemorrhoids, fever, and enteritis. We screened the inhibitory activities of the extracts and compounds (1-6) isolated from QM on the production of inflammatory cytokines and chemokines to evaluate their anti-inflammatory activities. Further, we evaluated the expression levels of cytokines, chemokines, and immune factors on pedunculagin (PC, 1), which was selected from isolated compounds (1-6) because of its potential anti-inflammation effect. Additionally, we evaluated whether the inflammation mitigation effects of PC (1) following UVB exposure in keratinocytes occurred because of nuclear factor (NF)-κB and signal transducer and activator of transcription (STAT)/Janus kinase (JAK) activation. PC (1) remarkably suppressed interleukin (IL)-6, IL-10, IL-13, and monocyte chemoattractant protein-1 (MCP-1) mRNA expression and reduced the mRNA expression level of Cyclooxygenase-2 (COX-2) and also reduced the phosphorylation of p38 mitogen-activated protein kinases (p38), c-Jun N-terminal kinase (JNK), and extracellular signal-regulated kinase (ERK) in a concentration-dependent manner.


Assuntos
Anti-Inflamatórios/farmacologia , Queratinócitos/citologia , Fenóis/farmacologia , Quercus/química , Taninos/farmacologia , Anti-Inflamatórios/química , Linhagem Celular , Células Cultivadas , Citocinas/genética , Citocinas/metabolismo , Avaliação Pré-Clínica de Medicamentos , Regulação da Expressão Gênica/efeitos dos fármacos , Humanos , Queratinócitos/efeitos dos fármacos , Queratinócitos/efeitos da radiação , Lipopolissacarídeos/efeitos adversos , NF-kappa B , Fenóis/química , Fosforilação , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Transdução de Sinais/efeitos dos fármacos , Taninos/química , Raios Ultravioleta/efeitos adversos
4.
Microsc Res Tech ; 82(11): 1928-1940, 2019 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-31423711

RESUMO

Tannic acid (TA) is a phenolic compound that might act directly on osteoblast metabolism. The study was performed to investigate the effects of TA on the proliferation, mineralization, and morphology of human fetal osteoblast cells (hFOB 1.19). The cells were divided into TA-treated, untreated, and pamidronate-treated (control drug) groups. Half maximal effective concentration (EC50 ) values for TA and pamidronate were measured using MTT assay. The EC50 of hFOB 1.19 cells treated with TA was 2.94 M. This concentration was more effective compared to the pamidronate (15.27 M). Cell proliferation assay was performed to compare cell viability from Day 1 until Day 14. The morphology of hFOB 1.19 was observed via inverted microscope and scanning electron microscope. Calcium (Ca) and phosphate (P) were assessed using energy-dispersive X-ray (EDX) analysis. Furthermore, the mineralization of hFOB 1.19 was determined by von Kossa staining (P depositions) and Alizarin Red S staining (Ca depositions). The number of cells treated with TA was significantly higher than the two control groups at Day 10 and Day 14. The morphology of cells treated with TA was uniformly fusiform-shaped with filopodia extensions. Besides, globular-like structures of deposited minerals were observed in the TA-treated group. In line with other findings, EDX spectrum analysis confirmed the presence of Ca and P. The cells treated with TA had significantly higher percentage of both minerals at Day 3 and Day 10 compared to the two control groups. In conclusion, TA enhances cell proliferation and causes cell morphology changes, as well as improved mineralization.


Assuntos
Calcificação Fisiológica/efeitos dos fármacos , Proliferação de Células/efeitos dos fármacos , Feto/citologia , Osteoblastos/metabolismo , Taninos/farmacologia , Cálcio/análise , Diferenciação Celular/efeitos dos fármacos , Linhagem Celular , Sobrevivência Celular/efeitos dos fármacos , Humanos , Microscopia Eletrônica de Varredura , Osteoblastos/citologia , Pamidronato/farmacologia , Fosfatos/análise , Espectrometria por Raios X
5.
Mol Immunol ; 114: 362-368, 2019 10.
Artigo em Inglês | MEDLINE | ID: mdl-31450181

RESUMO

Madi-Ryuk (MDR) is a traditional Korean medicine and it has been widely used in Korea to treat arthritis and we previously reported the anti-allergic inflammatory effect of MDR in vitro model. However, therapeutic evidence of MDR on in vivo model of allergic inflammatory reaction has not yet been demonstrated. The research purpose was to investigate the efficacy of MDR and its active ingredient tannic acid (TA) in ovalbumin (OVA)-induced AR mice model. OVA-challenged AR mice orally medicated MDR or its active ingredient TA daily for ten days. In mice having a AR, MDR and TA prominently diminished number of rubs and levels of histamine, IgE, thymic stromal lymphopoietin, interleukin (IL)-1ß, IL-4, IL-5, IL-13, IL-33, and tumor necrosis factor-α. In addition, protein expression levels and activities of caspase-1 were declined by oral medication of MDR and TA. Decline in levels of macrophage inflammatory protein-2 and intercellular adhesion molecules-1 and reduction in penetrations of inflammatory cells into inflamed tissue were also noted in MDR and TA groups. Taken together, identification of MDR effect in preclinical models suggests that MDR may be a therapeutic drug for the treatment and prevention of AR.


Assuntos
Anti-Inflamatórios/farmacologia , Rinite Alérgica/tratamento farmacológico , Taninos/farmacologia , Animais , Caspase 1/metabolismo , Quimiocina CXCL2/metabolismo , Citocinas/metabolismo , Modelos Animais de Doenças , Eosinófilos/efeitos dos fármacos , Eosinófilos/metabolismo , Histamina/metabolismo , Imunoglobulina E/metabolismo , Inflamação/induzido quimicamente , Inflamação/tratamento farmacológico , Inflamação/metabolismo , Interleucina-1beta/metabolismo , Medicina Tradicional Coreana/métodos , Camundongos , Camundongos Endogâmicos BALB C , Mucosa Nasal/efeitos dos fármacos , Mucosa Nasal/metabolismo , Ovalbumina/farmacologia , Rinite Alérgica/metabolismo , Fator de Necrose Tumoral alfa/metabolismo
6.
Curr Pharm Biotechnol ; 20(11): 964-984, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-31258072

RESUMO

BACKGROUND: The study was conducted to identify the bacterial strain associated with marine sponge Hyrtiosaff. erectus collected from the Red Sea coastal water and to assess the utilization of their secondary metabolites for human benefit as antioxidant, anti-Alzheimer, anti-viral, anticancer and anti-inflammatory agent. METHODS: After biochemical identification of Pesudomance sp. bacterial strain, the total polyphenol contents, cytotoxic, antioxidant, anti-Alzheimer, anti-viral, anticancer and anti-inflammatory activity of the Pesudomance sp. ethyl acetate extract were investigated by applying different biochemical assays. Polyphenol contents were investigated using spectrophotometric techniques. Antioxidant activity was determined by 1,1-diphenyl-2-picrylhydrazyl radical (DPPH), and 2,2/-azino-bis (3-ethylbenzothiazoline-6-sulphonic acid) ABTS radical scavenging activity assays. The cytotoxic effects were investigated by using the human cancerous cell lines. RESULTS: The anti-Alzheimer, anti-viral, anticancer and anti-inflammatory activities were determined using ELISA. Qualitative phytochemical analysis of the Pesudomance sp. extract demonstrated the presence of a large and diverse group of substances such as alkaloids, carbohydrates, flavonoids, phenols, terpenoids, saponins, and tannins. The strong antioxidant activity of the Pesudomance sp. extract was mainly attributed to the protective role of polyphenols against reactive oxygen. It was also observed that Pesudomance sp. extract possessed significant anti-Alzheimer activity with 94% at 1 mg. The extract showed also high antiviral activity (90%) using reverse transcriptase enzymes inhibition assay. The examination of the anticancer activity by applying two experimental models, i.e., PTK and SHKI cleared out high significant percentages of 76.19 and 83.09 %; respectively. CONCLUSION: The anti-inflammatory profiling using TNF, COX1, COX2, IL6 also revealed high antiinflammatory activity with different metabolic pathway of 62.70, 75.444, 79.27 and 54.15 %; respectively. The present study concluded that ethyl acetate extract of Pesudomance sp. possessed strong antioxidant, anti-Alzheimer, and anti-viral, anticancer and anti-inflammatory activities. Further studies are required to purify the bioactive compounds.


Assuntos
Anti-Inflamatórios/farmacologia , Antioxidantes/farmacologia , Produtos Biológicos/farmacologia , Descoberta de Drogas/métodos , Poríferos/microbiologia , Pseudomonas/química , Animais , Anti-Inflamatórios/isolamento & purificação , Antioxidantes/isolamento & purificação , Produtos Biológicos/isolamento & purificação , Flavonoides/isolamento & purificação , Flavonoides/farmacologia , Humanos , Fenóis/isolamento & purificação , Fenóis/farmacologia , Pseudomonas/isolamento & purificação , Taninos/isolamento & purificação , Taninos/farmacologia
7.
Biomed Res Int ; 2019: 5641034, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-31309107

RESUMO

Nutraceuticals present in food are molecules able to exert biological activity for the prevention and treatment of various diseases, in form of pharmaceutical preparations, such as capsules, cream, or pills. Myrtus communis L. is a spontaneous Mediterranean evergreen shrub, widely known for the liqueur obtained from its berries rich in phytochemicals such as tannins and flavonoids. In the present study, we aimed to evaluate the properties of myrtle byproducts, residual of the industrial liqueur processing, in Adipose-derived stem cells (ADSCs) induced at oxidative stress by in vitro H2O2 treatment. Cells were exposed for 12-24 and 48h at treatment with extracts and then senescence-induced. ROS production was then determined. The real-time PCR was performed to evaluate the expression of inflammatory cytokines and sirtuin-dependent epigenetic changes, as well the modifications in terms of stem cell pluripotency. The ß-galactosidase assay was conducted to analyze stem cell senescence after treatment. Our results show that industrial myrtle byproducts retain a high antioxidant and antisenescence activity, protecting cells from oxidative stress damages. The results obtained suggest that residues from myrtle liqueur production could be used as resource in formulation of food supplements or pharmaceutical preparations with antioxidant, antiaging, and anti-inflammatory activity.


Assuntos
Myrtus/química , Estresse Oxidativo/efeitos dos fármacos , Extratos Vegetais/farmacologia , Células-Tronco/efeitos dos fármacos , Anti-Inflamatórios/farmacologia , Antioxidantes/farmacologia , Citocinas/metabolismo , Feminino , Flavonoides/farmacologia , Humanos , Inflamação/tratamento farmacológico , Inflamação/metabolismo , Masculino , Pessoa de Meia-Idade , Espécies Reativas de Oxigênio/metabolismo , Células-Tronco/metabolismo , Taninos/farmacologia , beta-Galactosidase/metabolismo
8.
Hum Exp Toxicol ; 38(11): 1296-1301, 2019 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-31315458

RESUMO

The aim of the study was to determine the relationship between anti-inflammatory effects of the natural polyphenolic compound tannic acid (CAS number: 1401-55-4) and myeloperoxidase (MPO) enzyme activity in paw edema model. Thirty-five female rats were divided into five groups. The paws of rats were injected subcutaneously in the plantar surface with formalin except for the control group. Indomethacin and tannic acid were intraperitoneally administered 1 h after formalin injection. The paws volume was measured by using vernier caliper. MPO enzyme activity was determined using 4-aminoantipyrine-phenol solution as the substrate for MPO-mediated oxidation by H2O2. About 17% and 13% edema inhibition has detected in the indomethacin-applied group, at the measurements run every other hour right after the treatment. An inhibition of 16% was found at the group treated with 25 mg/kg tannic acid. However, in the group treated with 50 mg/kg tannic acid, 15% and 7% of the edema inhibition was observed. Serum and paw tissue MPO activities were decreased in treated groups with indomethacin and tannic acid according to formalin control group. Our study results suggest that tannic acid may contribute to the treatment of inflammation by decreasing MPO enzyme activity, but the molecular mechanism is still not clear.


Assuntos
Anti-Inflamatórios/uso terapêutico , Edema/tratamento farmacológico , Taninos/uso terapêutico , Animais , Anti-Inflamatórios/farmacologia , Modelos Animais de Doenças , Edema/induzido quimicamente , Edema/metabolismo , Feminino , , Formaldeído , Peroxidase/metabolismo , Ratos Sprague-Dawley , Taninos/farmacologia
9.
Respir Res ; 20(1): 168, 2019 Jul 29.
Artigo em Inglês | MEDLINE | ID: mdl-31358001

RESUMO

BACKGROUND: Pulmonary fibrosis is a progressive disease characterized by structural distortion of the lungs. Transforming growth factor-beta (TGF-beta) is a key cytokine implicated in the pathogenesis of pulmonary fibrosis. TGF-beta-induced myofibroblast differentiation characterized by expression of smooth muscle alpha-actin and extracellular matrix proteins is a key process in pathogenesis of fibrotic disease. Tannic acid is a natural polyphenol with diverse applications. In this study, we investigated the effect of tannic acid on myofibroblast differentiation and pulmonary fibrosis in cultured cells and in bleomycin model of the disease. METHODS: Primary cultured human lung fibroblasts (HLF) were used. The relative levels of proteins were determined by Western blotting. HLF contraction was measured by traction microscopy. Bleomycin-induced pulmonary fibrosis in mice was used as the disease model. RESULTS: Tannic acid inhibited TGF-beta-induced expression of collagen-1 and smooth muscle alpha-actin (SMA) as well as force generation by HLF. Tannic acid did not affect initial phosphorylation of Smad2 in response to TGF-beta, but significantly inhibited sustained Smad2 phosphorylation, which we recently described to be critical for TGF-beta-induced myofibroblast differentiation. Accordingly, tannic acid inhibited Smad-dependent gene transcription in response to TGF-beta, as assessed using luciferase reporter for the activity of Smad-binding elements. Finally, in mouse model of bleomycin-induced pulmonary fibrosis, therapeutic application of tannic acid resulted in a significant reduction of lung fibrosis, decrease in collagen-1 content and of Smad2 phosphorylation in the lungs. CONCLUSIONS: This study demonstrates the anti-fibrotic effect of tannic acid in vitro and in vivo through a regulation of sustained Smad2 phosphorylation.


Assuntos
Antifibrinolíticos/farmacologia , Fibroblastos/efeitos dos fármacos , Pulmão/efeitos dos fármacos , Receptores de Fatores de Crescimento Transformadores beta/administração & dosagem , Transdução de Sinais/efeitos dos fármacos , Taninos/farmacologia , Animais , Antifibrinolíticos/uso terapêutico , Células Cultivadas , Fibroblastos/metabolismo , Humanos , Pulmão/citologia , Pulmão/metabolismo , Camundongos , Camundongos Endogâmicos C57BL , Fibrose Pulmonar/tratamento farmacológico , Fibrose Pulmonar/metabolismo , Fibrose Pulmonar/patologia , Receptores de Fatores de Crescimento Transformadores beta/metabolismo , Transdução de Sinais/fisiologia , Taninos/uso terapêutico
10.
Mar Drugs ; 17(6)2019 Jun 16.
Artigo em Inglês | MEDLINE | ID: mdl-31208149

RESUMO

Tyrosinase inhibitors improve skin whitening by inhibiting the formation of melanin precursors in the skin. The inhibitory activity of seven phlorotannins (1-7), triphlorethol A (1), eckol (2), 2-phloroeckol (3), phlorofucofuroeckol A (4), 2-O-(2,4,6-trihydroxyphenyl)-6,6'-bieckol (5), 6,8'-bieckol (6), and 8,8'-bieckol (7), from Ecklonia cava was tested against tyrosinase, which converts tyrosine into dihydroxyphenylalanine. Compounds 3 and 5 had IC50 values of 7.0 ± 0.2 and 8.8 ± 0.1 µM, respectively, in competitive mode, with Ki values of 8.2 ± 1.1 and 5.8 ± 0.8 µM. Both compounds showed the characteristics of slow-binding inhibitors over the time course of the enzyme reaction. Compound 3 had a single-step binding mechanism and compound 5 a two-step-binding mechanism. With stable AutoDock scores of -6.59 and -6.68 kcal/mol, respectively, compounds 3 and 5 both interacted with His85 and Asn260 at the active site.


Assuntos
Dioxinas/química , Inibidores Enzimáticos/farmacologia , Taninos/farmacologia , Melaninas/química , Monofenol Mono-Oxigenase/metabolismo , Feófitas/química , Tirosina/metabolismo
11.
Mar Drugs ; 17(6)2019 Jun 24.
Artigo em Inglês | MEDLINE | ID: mdl-31238535

RESUMO

Modulation of multiple protein targets with a single compound is essential for the effective treatment of central nervous system disorders. In our previous G protein-coupled receptor (GPCR) cell-based study, a selective human monoamine oxidase (hMAO)-A inhibitor, eckol, stimulated activity of dopamine D3 and D4 receptors. This result led to our interest in marine phlorotannin-mediated modulation of hMAO enzymes and related GPCRs in neuronal disorders. Here, we evaluate the multi-target effects of phloroglucinol, phlorofucofuroeckol-A (PFF-A), and dieckol by screening their modulatory activity against hMAO-A and -B and various neuronal GPCRs. Among the tested phlorotannins, PFF-A showed the strongest inhibitory activity against both hMAO isoforms, with higher selectivity toward hMAO-B than hMAO-A. Enzyme kinetics and docking data revealed that PFF-A noncompetitively acts on hMAOs into the alternative binding pocket of enzymes with allosteric functions. In a functional assay for GPCR screening, dieckol and PFF-A exhibited a multi-target combination of D3R/D4R agonism and D1/5HT1A/NK1 antagonism. In particular, they effectively stimulated D3R and D4R, compared to other GPCRs. Docking analysis confirmed that dieckol and PFF-A successfully docked into the conserved active sites of D3R and D4R and interacted with aspartyl and serine residues in the orthosteric binding pockets of the respective receptors. Based on our experimental and computational data, we established the structure-activity relationship between tested phlorotannins and target proteins, including hMAOs and GPCRs. Our current findings suggest that hMAO inhibitors dieckol and PFF-A, major phlorotannins of edible brown algae with multi-action on GPCRs, are potential agents for treatment of psychological disorders and Parkinson's disease.


Assuntos
Antagonistas de Dopamina/farmacologia , Inibidores da Monoaminoxidase/farmacologia , Monoaminoxidase/metabolismo , Doenças do Sistema Nervoso/tratamento farmacológico , Receptores Dopaminérgicos/metabolismo , Taninos/farmacologia , Benzofuranos/farmacologia , Dioxinas/farmacologia , Dopamina/metabolismo , Humanos , Simulação de Acoplamento Molecular/métodos , Doenças do Sistema Nervoso/metabolismo , Feófitas/química , Receptores Acoplados a Proteínas-G/metabolismo , Relação Estrutura-Atividade
12.
Bull Exp Biol Med ; 167(2): 275-278, 2019 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-31243675

RESUMO

We studied the particularities of osteo- and angiogenesis in albino rats after implantation of polycaprolactone scaffolds mineralized with vaterite with adsorbed tannic acid in the femoral bone defect. It was found that the processes of angio- and osteogenesis in the bone tissue after scaffolds implantation depend on their biocompatibility. Implantation of non-biocompatible scaffolds was followed by activation of angio- and osteogenesis aimed at separation of these scaffold from surrounding tissues. Implantation of polycaprolactone/vaterite scaffolds containing tannic acid stimulated angio- and osteogenesis leading to vascularization and bone tissue formation in the matrix. This demonstrate prospects of clinical approbation of these scaffolds for stimulation of bone regeneration in traumatological and orthopedic patients.


Assuntos
Regeneração Óssea/efeitos dos fármacos , Carbonato de Cálcio/química , Poliésteres/química , Taninos/química , Tecidos Suporte/química , Animais , Osso e Ossos/citologia , Masculino , Ratos , Taninos/farmacologia
13.
PLoS One ; 14(5): e0215291, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-31150404

RESUMO

Among neurodegenerative diseases, Alzheimer's disease (AD) is one of the most grievous disease. The oldest cholinergic hypothesis is used to elevate the level of cognitive impairment and acetylcholinesterase (AChE) comprises the major targeted enzyme in AD. Thus, acetylcholinesterase inhibitors (AChEI) constitutes the essential remedy for the treatment of AD. The study aims to evaluate the interactions between natural molecules and AChE by Surface Plasmon Resonance (SPR). The molecules like alkaloids, polyphenols and substrates of AChE have been considered for the study with a major emphasis on affinity and kinetics. To better understand the activity of small molecules, the investigation is supported by both experimental and theoretical approach such as fluorescence, Circular Dichroism (CD) and molecular docking studies. Amongst the screened ones tannic acid showed promising results compared with others. The methodology followed here have highlighted many molecules with a higher affinity towards AChE and these findings may take lead molecules generated in preclinical studies to treat neurodegenerative diseases. Additionally, we suggest a unique signature for the heterogeneous analyte model using competitive experiments for analyzing simultanous interactions of both the analytes.


Assuntos
Acetilcolinesterase/química , Inibidores da Colinesterase/farmacologia , Taninos/farmacologia , Doença de Alzheimer/tratamento farmacológico , Doença de Alzheimer/enzimologia , Inibidores da Colinesterase/química , Dicroísmo Circular , Avaliação Pré-Clínica de Medicamentos , Proteínas Ligadas por GPI/antagonistas & inibidores , Proteínas Ligadas por GPI/química , Humanos , Modelos Moleculares , Simulação de Acoplamento Molecular , Taninos/química
14.
Biol Pharm Bull ; 42(5): 770-777, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-31061319

RESUMO

Previously, we reported that coffee extract and its constituents, caffeic acid (CA) and p-coumaric acid, inhibit infection by the hepatitis C virus (HCV). In the present report, we identified another coffee-related compound, tannic acid (TA), which also inhibits HCV infection. We systematically evaluated which steps of the viral lifecycle were affected by CA and TA. TA substantially inhibits HCV RNA replication and egression, while CA does not. The infectivity of the HCV pretreated with CA or TA was almost lost. Cellular attachment of HCV particles and their interaction with apolipoprotein E, which is essential for HCV infectivity, were significantly reduced by CA. These results indicate that CA inhibits HCV entry via its direct effect on viral particles and TA inhibits HCV RNA replication and particle egression as well as entry into host cells. Taken together, our findings may provide insights into CA and TA as potential anti-HCV strategies.


Assuntos
Antivirais/farmacologia , Ácidos Cafeicos/farmacologia , Hepacivirus/efeitos dos fármacos , Hepatite C/prevenção & controle , Taninos/farmacologia , Apolipoproteínas E/metabolismo , Linhagem Celular Tumoral , Hepacivirus/genética , Hepacivirus/metabolismo , Hepacivirus/patogenicidade , Humanos , RNA Viral/efeitos dos fármacos
15.
Mar Drugs ; 17(5)2019 May 08.
Artigo em Inglês | MEDLINE | ID: mdl-31071969

RESUMO

Blood circulation disorders, such as hyperlipidemia and arteriosclerosis, are not easily cured by dietary supplements, but they can be mitigated. Although Ecklonia cava extract (ECE), as dietary supplements, are associated with improving the conditions, there are not many studies verifying the same. In this study, the beneficial effect of ECE and leaf of Ginkgo biloba extract (GBE), which is a well-known dietary supplement, were first confirmed in a diet induced-obese model. Afterwards, 4 phlorotannins were isolated from ECE, and their inhibitory effects on vascular cell dysfunction were validated. Pyrogallol-phloroglucinol-6,6-bieckol (PPB) was selected to be orally administered in two mice models: the diet induced obese model and diet induced hypertension model. After four weeks of administration, the blood pressure of all mice was measured, after which they were subsequently sacrificed. PPB was found to significantly improve blood circulation, including a reduction of adhesion molecule expression, endothelial cell (EC) death, excessive vascular smooth muscle cell (VSMC) proliferation and migration, blood pressure, and lipoprotein and cholesterol levels. Based on the excellent efficacy in diet-induced mouse models of obese and hypertension, our results demonstrate that PPB is a valuable active compound from among the phlorotannins that were isolated and it has the potential to be used in functional foods for improving the blood circulation.


Assuntos
Circulação Sanguínea/efeitos dos fármacos , Dioxinas/farmacologia , Hipertensão/tratamento farmacológico , Obesidade/tratamento farmacológico , Floroglucinol/farmacologia , Pirogalol/farmacologia , Animais , Proteínas Reguladoras de Apoptose/metabolismo , Pressão Sanguínea , Moléculas de Adesão Celular/efeitos dos fármacos , Moléculas de Adesão Celular/metabolismo , Linhagem Celular , Movimento Celular/efeitos dos fármacos , Proliferação de Células/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Dieta , Hipertensão/induzido quimicamente , Camundongos , Camundongos Endogâmicos C57BL , Modelos Animais , Obesidade/induzido quimicamente , Feófitas/química , Extratos Vegetais/farmacologia , RNA Mensageiro , Transdução de Sinais , Taninos/farmacologia
16.
J Anim Sci ; 97(6): 2468-2478, 2019 May 30.
Artigo em Inglês | MEDLINE | ID: mdl-31073613

RESUMO

The present study investigated the effects of oxidized canola oil and tannic acid (TA) supplementation on nutrient digestibility and microbial metabolites in finishing pigs. Four experimental diets were formulated to include 5% of either fresh canola oil (0 mEq/kg of peroxide value) or oxidized canola oil (180 mEq/kg of peroxide value). An equal portion of each diet was supplemented with 0.1% TA. Eight pigs (initial body weight of 82.89 ± 2.26 kg) were surgically fitted with a T-cannula at the distal ileum. At the beginning of the experiments, all pigs were fed a nitrogen-free diet for 7 d. Then, they were assigned to 4 dietary treatments according to an incomplete replicated 4 × 3 Latin square design with 3 periods to give 6 replicates per treatment. Each experimental period lasted for 9 d, starting with a 5-d adaptation period followed by 2 consecutive 2-d periods for fecal (day 6 and day 7) and ileal digesta (day 8 and day 9) collection. The inclusion of oxidized oil reduced (P < 0.05) the standardized ileal digestibility (SID) of Pro and the apparent ileal digestibility (AID) and apparent total tract digestibility (ATTD) of NDF. Also, pigs fed the oxidized oil tended to have lower (P ≤ 0.10) lactate and ammonia-nitrogen concentrations in the ileum and lower (P ≤ 0.10) acetate and propionate concentrations in the feces than those fed the fresh oil. The supplementation of 0.1% TA reduced (P < 0.05) the AID of NDF and the ATTD of gross energy, crude protein, and NDF. Additionally, the TA-supplemented diet tended to have a lower (P ≤ 0.10) digestible energy content than the nonsupplemented diet. Pigs fed the TA-supplemented diet showed reduced (P < 0.05) AID and SID of His, Cys, and Pro compared with those fed the nonsupplemented diet. There were interactive effects (P < 0.05) of oxidized oil and TA supplementation on acetate, isovalerate, total short chain fatty acids, and pH level in the ileum. In conclusion, the results indicated that the effects of oxidized oil are greater on microbial activities rather than nutrient digestibility. Although negative effects of dietary TA supplementation were observed in relation to nutrient digestibility, TA supplementation was found to ameliorate these negative effects of oxidized oil on microbial metabolites. Therefore, further studies are required to investigate the interaction between dietary oxidized oil and TA in relation with the gut microbiota in pigs.


Assuntos
Ração Animal/análise , Dieta/veterinária , Digestão/efeitos dos fármacos , Óleo de Brassica napus/química , Suínos/fisiologia , Taninos/farmacologia , Aminoácidos/metabolismo , Fenômenos Fisiológicos da Nutrição Animal , Animais , Suplementos Nutricionais , Metabolismo Energético , Ácidos Graxos Voláteis/metabolismo , Fezes/química , Temperatura Alta , Íleo/metabolismo , Taninos/administração & dosagem , Taninos/metabolismo
17.
Appl Biochem Biotechnol ; 189(3): 855-870, 2019 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-31131419

RESUMO

Condensed tannins (CTS) have been isolated and purified from leaves of Acanthus ilicifolius Linn. And their structures were investigated by three methods: 13C nuclear magnetic resonance (13C NMR), reversed-phase high-performance liquid chromatography (RP-HPLC), and matrix-assisted laser desorption/ionization time-of-flight mass spectrometry (MALDI-TOF MS). The results showed that the CTS were a mixture of catechin/epicatechin, galatechin/epicatechin, and amphicin/epigalin, and that the polymer chain lengths were 3-mers to 14-mers. Antityrosinase activities and antioxidant activities of the CTS from A. ilicifolius leaves were further studied. The IC50 of the CTS on mushroom tyrosinase activity was determined to be 19.7 ± 0.13 µg/mL, and inhibition type analyses indicated that the CTS were mixed type inhibitors and their inhibition CTS was reversible. The CTS from A. ilicifolius leaves also exhibited potential antioxidant activity. The IC50 of DPPH and ABTS scavenging activities were 104 ± 0.894 µg/mL and 86 ± 0.616 µg/mL, respectively. And the FRAP value was 758.28 ± 2.42 mg AAE/g. In addition, we found that the CTS from A. ilicifolius leaves had an excellent effect on preserving the quality of fresh-cut apples by preventing apples from browning through reducing polyphenol oxidase activities in apples.


Assuntos
Acanthaceae/química , Antioxidantes/química , Antioxidantes/farmacologia , Malus/efeitos dos fármacos , Taninos/química , Taninos/farmacologia , Agaricales/enzimologia , Antioxidantes/isolamento & purificação , Conservação de Alimentos , Cinética , Malus/metabolismo , Monofenol Mono-Oxigenase/antagonistas & inibidores , Folhas de Planta/química , Polimerização , Taninos/isolamento & purificação
18.
ACS Appl Mater Interfaces ; 11(19): 17157-17166, 2019 May 15.
Artigo em Inglês | MEDLINE | ID: mdl-31017392

RESUMO

Ultrasmall iron oxide nanoparticles (USIONPs) (<4 nm) have recently attracted significant attention because of their potential as positive T1 magnetic resonance imaging (MRI) contrast agent contrary to larger superparamagnetic iron oxide nanoparticles (>6 nm) which act as negative T2 MRI contrast agents. However, studies on the cellular uptake behavior of these nanoparticles are very limited compared to their counterpart, larger-sized superparamagnetic iron oxide nanoparticles. In particular, the effects of specific nanoparticle parameters on the cellular uptake behavior of USIONPs by various cancer cells are not available. Here, we specifically investigated the role of USIONPs' surface functionalities [tannic acid (TA) and quinic acid (QA)] in mediating cellular uptake behavior of cancer cells pertaining to primary (U87 cells) and metastatic (MDA-MB-231Br cells) brain malignancies. Here, we chose TA and QA as representative capping molecules, wherein TA coating provides a general negatively charged nontargeting surface while QA provides a tumor-targeting surface as QA and its derivatives are known to interact with selectin receptors expressed on tumor cells and tumor endothelium. We observed differential cellular uptake in the case of TA- and QA-coated USIONPs by cancer cells. Both the cell types showed significantly higher cellular uptake of QA-coated USIONPs compared to TA-coated USIONPs at 4, 24, and 72 h. Blocking studies indicated that P-selectin cell surface receptors, in part, mediated the cellular uptake of QA-coated USIONPs. Given that P-selectin is overexpressed in cancer cells, tumor microenvironment, and at the metastatic niche, QA-coated USIONPs hold potential to be utilized as a platform for tumor-targeted drug delivery and in imaging and detection of primary and metastatic tumors.


Assuntos
Neoplasias Encefálicas/diagnóstico por imagem , Meios de Contraste/farmacologia , Compostos Férricos/farmacologia , Nanopartículas de Magnetita/química , Neoplasias Encefálicas/tratamento farmacológico , Neoplasias Encefálicas/patologia , Neoplasias Encefálicas/secundário , Linhagem Celular Tumoral , Meios de Contraste/química , Sistemas de Liberação de Medicamentos , Compostos Férricos/química , Regulação Neoplásica da Expressão Gênica/efeitos dos fármacos , Humanos , Imagem por Ressonância Magnética , Nanopartículas de Magnetita/administração & dosagem , Selectina-P/genética , Ácido Quínico/química , Ácido Quínico/farmacologia , Propriedades de Superfície , Taninos/química , Taninos/farmacologia
19.
J Biochem Mol Toxicol ; 33(8): e22340, 2019 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-30974029

RESUMO

Multiple studies have been recorded on the synthesis and design of multi-aim anti-Alzheimer molecules. Using dual butyrylcholinesterase/acetylcholinesterase inhibitor molecules has attracted more interest in the therapy for Alzheimer's disease. In this study, a tannic acid compound showed excellent inhibitory effects against acetylcholine esterase (AChE), α-glycosidase, α-amylase, and butyrylcholinesterase (BChE). IC50 values of tannic acid obtained 11.9 nM against α-glycosidase and 3.3 nM against α-amylase, respectively. In contrast, Ki values were found of 50.96 ± 2.18 µM against AChE and 53.17 ± 4.47 µM against BChE. α-Glycosidase inhibitor compounds can be utilized as a novel group of antidiabetic drugs. By competitively decreasing glycosidase activity, these inhibitor molecules help to hamper the fast breakdown of sugar molecules and thereby control the blood sugar level.


Assuntos
Doença de Alzheimer/tratamento farmacológico , Antioxidantes/farmacologia , Diabetes Mellitus/tratamento farmacológico , Descoberta de Drogas , Inibidores Enzimáticos/uso terapêutico , Taninos/farmacologia , Acetilcolinesterase/efeitos dos fármacos , Amilases/efeitos dos fármacos , Butirilcolinesterase/efeitos dos fármacos , Inibidores Enzimáticos/química , Inibidores Enzimáticos/farmacologia , Humanos , alfa-Glucosidases/efeitos dos fármacos
20.
World J Microbiol Biotechnol ; 35(4): 57, 2019 Mar 21.
Artigo em Inglês | MEDLINE | ID: mdl-30900046

RESUMO

Methicillin-resistant Staphylococcus aureus (MRSA) infections treatment of which is hard and failed, due to being resistant to all types of ß-lactams, have been emerged in hospitals and community. Long-term usage of antibiotics and over doses of antibiotics used in the treatment of infections cause bacteria to develop resistance to antibiotics. ß-lactams combined with tannic acid can be a good alternative to sensitize the resistance of ß-lactams used in the treatment of MRSA, due to their synergistic activities. In this study, after minimal inhibitory concentrations (MICs) and minimal bactericidal concentrations (MBCs) of sole tannic acid and ß-lactam were investigated for each isolate, the synergistic activities of ß-lactams combined with tannic acid against one MRSA ATCC 43300 and four MRSA clinical isolates were investigated with the concentrations starting at four fold of MICs of sole treatments of tannic acid and ß-lactam by using checkerboard assay. To investigate sole and combination activities of tannic acid and ß-lactams, MIC and MBCs were observed. Results of this study showed that the activities of ß-lactams combined with tannic acid were synergistic and partially synergistic against MRSA isolates with FIC indexes ranged from 0.174 to 0.477 and 0.562 to 0.850, respectively. MIC of ß-lactams were decreased 2-16 fold by sub-inhibitory concentrations of tannic acid without toxicity. Alternative treatment options of natural compounds such as tannic acid and ß-lactams must be investigated further and developed to overcome the emergence of ß-lactam resistance and treat MRSA infections by sensitizing the resistance of ß-lactams.


Assuntos
Staphylococcus aureus Resistente à Meticilina/efeitos dos fármacos , Taninos/farmacologia , Resistência beta-Lactâmica/efeitos dos fármacos , beta-Lactamas/farmacologia , Linhagem Celular/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Combinação de Medicamentos , Farmacorresistência Bacteriana Múltipla/efeitos dos fármacos , Sinergismo Farmacológico , Humanos , Staphylococcus aureus Resistente à Meticilina/crescimento & desenvolvimento , Staphylococcus aureus Resistente à Meticilina/patogenicidade , Testes de Sensibilidade Microbiana , Infecções Estafilocócicas/tratamento farmacológico , Infecções Estafilocócicas/microbiologia , Testes de Toxicidade
SELEÇÃO DE REFERÊNCIAS
DETALHE DA PESQUISA