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1.
Int. j. morphol ; 41(1): 79-84, feb. 2023. ilus, graf
Artigo em Inglês | LILACS | ID: biblio-1430536

RESUMO

SUMMARY: Paracetamol (known as acetaminophen, or APAP) poisoning causes acute liver damage that can lead to organ failure and death. We sought to determine that APAP overdose can augment tumor necrosis factor-alpha (TNF-α)/ nuclear factor kappa B (NF-kB)/induced nitic oxide synthase (iNOS) axis-mediated hepatotoxicity in rats, and the anti-inflammatory polyphenolic compounds, quercetin (QUR) plus resveratrol (RES) can ameliorate these parameters. Therefore, we induced acute hepatotoxicity in rats using APAP overdose (2 g/kg, orally) and the protective group of rats were treated with 50 mg/kg QUR plus 30 mg/kg RES for one week before APAP ingestion. Animals were killed at day 8. APAP poisoning caused the induction of hepatic tissue levels of TNF-α, NF-kB, and iNOS, which were significantly (p<0.05) decreased by QUR+RES. QUR+RES, also inhibited liver injury biomarkers, alanine aminotransferase (ALT) and aspartate aminotransferase (AST). Additionally, a link between liver injury and TNF-α /NF-kB / iNOS axis mediated hepatotoxicity was observed. Thus, the presented data backing the conclusion that intoxication by paracetamol increases TNF-α / NF-kB / iNOS axis -mediated hepatotoxicity, and is protected by a combination of quercetin and resveratrol.


El envenenamiento por paracetamol (conocido como acetaminofeno o APAP) causa daño hepático agudo que puede provocar una insuficiencia orgánica y la muerte. El objetivo de este trabajo fue determinar si la sobredosis de APAP puede aumentar la hepatotoxicidad mediada por el eje del factor de necrosis tumoral alfa (TNF-α)/factor nuclear kappa B (NF-kB)/óxido nítico sintasa inducida (iNOS) en ratas, y si el polifenólico antiinflamatorio compuesto por quercetina (QUR) más resveratrol (RES) pueden mejorar estos parámetros. Por lo tanto, inducimos hepatotoxicidad aguda en ratas usando una sobredosis de APAP (2 g/kg, por vía oral). El grupo protector de ratas se trató con 50 mg/ kg de QUR más 30 mg/kg de RES durante una semana antes de la ingestión de APAP. Los animales se sacrificaron el día 8. El envenenamiento con APAP en el tejido hepático provocó la inducción de niveles de TNF-α, NF-kB e iNOS, que se redujeron significativamente (p<0,05) con QUR+RES. QUR+RES, también inhibió los biomarcadores de daño hepático, la alanina aminotransferasa (ALT) y el aspartato aminotransferasa (AST). Además, se observó una relación entre la lesión hepática y la hepatotoxicidad mediada por el eje TNF-α /NF-kB/iNOS. Por lo tanto, los datos presentados respaldan la conclusión de que la intoxicación por paracetamol aumenta la hepatotoxicidad mediada por el eje TNF-α /NF-kB / iNOS, y está protegida por una combinación de quercetina y resveratrol.


Assuntos
Animais , Ratos , Quercetina/administração & dosagem , Doença Hepática Crônica Induzida por Substâncias e Drogas/tratamento farmacológico , Resveratrol/administração & dosagem , Acetaminofen/toxicidade , Doença Aguda , NF-kappa B/antagonistas & inibidores , Fator de Necrose Tumoral alfa/antagonistas & inibidores , Ratos Sprague-Dawley , Óxido Nítrico Sintase/antagonistas & inibidores , Substâncias Protetoras , Quimioterapia Combinada , Overdose de Drogas
2.
Braz. j. biol ; 83: e248746, 2023. graf
Artigo em Inglês | LILACS, VETINDEX | ID: biblio-1339351

RESUMO

Abstract Colorectal cancer (CRC) is one of the most common cancers leading to comorbidities and mortalities globally. The rational of current study was to evaluate the combined epigallocatechin gallate and quercetin as a potent antitumor agent as commentary agent for therapeutic protocol. The present study investigated the effect of epigallocatechin Gallate (EGCG) (150mg) and quercetin (200mg) at different proportions on proliferation and induction of apoptosis in human colon cancer cells (HCT-116). Cell growth, colonogenic, Annexin V in addition cell cycle were detected in response to phytomolecules. Data obtained showed that, the colony formation was inhibited significantly in CRC starting from the lowest concentration tested of 10 µg/mL resulting in no colonies as visualized by a phase-contrast microscope. Data showed a significant elevation in the annexin V at 100 µg/mL EGCG(25.85%) and 150 µg/mL quercetin (48.35%). Moreover, cell cycle analysis showed that this combination caused cell cycle arrest at the G1 phase at concentration of 100 µg/mL (72.7%) and 150 µg/mL (75.25%). The combined effect of epigallocatechin Gallate and quercetin exert antiproliferative activity against CRC, it is promising in alternative conventional chemotherapeutic agent.


Resumo O câncer colorretal (CCR) é um dos cânceres mais comuns, levando a comorbidades e mortalidade em todo o mundo. O racional do presente estudo foi avaliar a combinação de galato de epigalocatequina e quercetina como um agente antitumoral potente como agente de comentário para protocolo terapêutico. O presente estudo investigou o efeito de galato de epigalocatequina (EGCG) (150 mg) e quercetina (200 mg) em diferentes proporções na proliferação e indução de apoptose em células de câncer de cólon humano (HCT-116). O crescimento celular, colonogênico, anexina V, além do ciclo celular foram detectados em resposta a fitomoléculas. Os dados obtidos mostraram que a formação de colônias foi inibida significativamente no CRC a partir da concentração mais baixa testada de 10 µg/mL, resultando em nenhuma colônia conforme visualizado por um microscópio de contraste de fase. Os dados mostraram uma elevação significativa na anexina V a 100 µg/mL de EGCG (25,85%) e 150 µg/mL de quercetina (48,35%). Além disso, a análise do ciclo celular mostrou que essa combinação causou parada do ciclo celular na fase G1 na concentração de 100 µg/mL (72,7%) e 150 µg/mL (75,25%). O efeito combinado da epigalocatequina galato e quercetina exerce atividade antiproliferativa contra o CCR, é promissor como agente quimioterápico alternativo convencional.


Assuntos
Humanos , Neoplasias Colorretais/tratamento farmacológico , Catequina/análogos & derivados , Catequina/farmacologia , Quercetina/farmacologia , Ciclo Celular , Anexina A5 , Linhagem Celular Tumoral , Proliferação de Células
3.
Braz. j. biol ; 83: 1-7, 2023. graf, ilus
Artigo em Inglês | LILACS, VETINDEX | ID: biblio-1468924

RESUMO

Colorectal cancer (CRC) is one of the most common cancers leading to comorbidities and mortalities globally. The rational of current study was to evaluate the combined epigallocatechin gallate and quercetin as a potent antitumor agent as commentary agent for therapeutic protocol. The present study investigated the effect of epigallocatechin Gallate (EGCG) (150mg) and quercetin (200mg) at different proportions on proliferation and induction of apoptosis in human colon cancer cells (HCT-116). Cell growth, colonogenic, Annexin V in addition cell cycle were detected in response to phytomolecules. Data obtained showed that, the colony formation was inhibited significantly in CRC starting from the lowest concentration tested of 10 µg/mL resulting in no colonies as visualized by a phase-contrast microscope. Data showed a significant elevation in the annexin V at 100 µg/mL EGCG(25.85%) and 150 µg/mL quercetin (48.35%). Moreover, cell cycle analysis showed that this combination caused cell cycle arrest at the G1 phase at concentration of 100 µg/mL (72.7%) and 150 µg/mL (75.25%). The combined effect of epigallocatechin Gallate and quercetin exert antiproliferative activity against CRC, it is promising in alternative conventional chemotherapeutic agent.


O câncer colorretal (CCR) é um dos cânceres mais comuns, levando a comorbidades e mortalidade em todo o mundo. O racional do presente estudo foi avaliar a combinação de galato de epigalocatequina e quercetina como um agente antitumoral potente como agente de comentário para protocolo terapêutico. O presente estudo investigou o efeito de galato de epigalocatequina (EGCG) (150 mg) e quercetina (200 mg) em diferentes proporções na proliferação e indução de apoptose em células de câncer de cólon humano (HCT-116). O crescimento celular, colonogênico, anexina V, além do ciclo celular foram detectados em resposta a fitomoléculas. Os dados obtidos mostraram que a formação de colônias foi inibida significativamente no CRC a partir da concentração mais baixa testada de 10 µg/mL, resultando em nenhuma colônia conforme visualizado por um microscópio de contraste de fase. Os dados mostraram uma elevação significativa na anexina V a 100 µg/mL de EGCG (25,85%) e 150 µg/mL de quercetina (48,35%). Além disso, a análise do ciclo celular mostrou que essa combinação causou parada do ciclo celular na fase G1 na concentração de 100 µg/mL (72,7%) e 150 µg/mL (75,25%). O efeito combinado da epigalocatequina galato e quercetina exerce atividade antiproliferativa contra o CCR, é promissor como agente quimioterápico alternativo convencional.


Assuntos
Humanos , /uso terapêutico , Apoptose/efeitos dos fármacos , Catequina/administração & dosagem , Neoplasias Colorretais/tratamento farmacológico , Quercetina/administração & dosagem
4.
Braz. J. Pharm. Sci. (Online) ; 59: e21182, 2023. tab, graf
Artigo em Inglês | LILACS | ID: biblio-1429967

RESUMO

Abstract Suanzaoren Decoction (SZRD) is an ancient prescription used in the treatment of insomnia. This study aimed to investigate the components and targets of SZRD in treating insomnia. First, the compounds of five herbs in SZRD were collected from the Traditional Chinese Medicine Systems Pharmacology Database and Analysis Platform (TCMSP), and the putative targets for treating insomnia were obtained from DrugBank to construct the herb-compound-target- disease network. A protein-protein interaction (PPI) network was constructed in the STRING database, and then Gene Ontology functional enrichment and Kyoto Encyclopedia of Genes and Genomes (KEGG) pathway enrichment analysis were performed to predict the mechanism of action of intersection target. Finally, 30 mice were divided into five groups: control, model, and quercetin groups (100, 50, 25 mg/kg). The sleep latency and duration of pentobarbital-induced sleeping were measured. The production of interleukin-6 (IL-6) and γ-aminobutyric acid (γ-GABA) was detected by using an enzyme-linked immunosorbent assay kit (ELISA), and Gamma-aminobutyric acid type a receptor subunit alpha1 (GABRA1) was tested by Reverse Transcription-Polymerase Chain Reaction (RT-PCR). A total of 152 active ingredients, including 80 putative targets of SZRD, were obtained. The main active compounds included quercetin and kaempferol, and the key targets involved IL-6 and nitric oxide synthase 3 (NOS3). The results of pathway enrichment analysis indicated that the putative targets of SZRD mainly participated in Neuroactive ligand-receptor interaction. The experiment of P-chlorophenylalanine (PCPA)-induced insomnia model showed that quercetin obviously shortened the sleep latency and prolonged the sleep duration of the insomnia model. The production of IL-6, γ-GABA, and GABRA1 mRNA was significantly increased in mice treated with quercetin. This study predicted the active ingredients and potential targets of SZRD on insomnia on the basis of a systematic network pharmacology approach and illustrated that SZRD might exert hypnotic effects via regulating IL-6, γ-GABA, and GABRA1


Assuntos
Animais , Masculino , Feminino , Ratos , Extratos Vegetais/farmacologia , Distúrbios do Início e da Manutenção do Sono/classificação , Pentobarbital/análise , Quercetina/efeitos adversos , Quempferóis/efeitos adversos
5.
Braz. J. Pharm. Sci. (Online) ; 59: e201085, 2023. graf
Artigo em Inglês | LILACS | ID: biblio-1429968

RESUMO

Abstract Nitric oxide (NO) is an abundant mediator which is demonstrated to be involved in pruritus. Assuming that the increased NO also mediates chloroquine-induced pruritus, which is a frequent complication seen in the chronic chloroquine treatment, the current study aimed to investigate the effect of quercetin and the role of NO in chloroquine-induced pruritus in C57BL/6 mice. Model was created with subcutaneous chloroquine (400µg/site) injection to the nape of the mice. Effect of quercetin and role of NO were investigated with administration of quercetin, and co-administration with L-NAME, 7-NI and L-arginine before chloroquine injection. Locomotor activity was assessed by activity cage and number of the scratching bouts after chloroquine injection was recorded for 30 minutes. Our results show that quercetin significantly reduced scratching bouts at the doses of 10, 20, 40 and 80 mg/kg. Locomotor activity was decreased at the 40 and 80 mg/kg doses of quercetin. Additionally, decrease of the number of scratching bouts by quercetin prevented by L-arginine treatment, while L-NAME and 7-NI enhanced the anti-pruritic effect of sub-effective doses of quercetin. Therefore, our study demonstrated that acute injection of quercetin significantly diminished chloroquine-induced scratching behavior, and this effect is partly mediated by inhibition of neuronal nitric oxide synthase enzyme.


Assuntos
Animais , Masculino , Camundongos , Prurido/induzido quimicamente , Quercetina/efeitos adversos , Cloroquina/administração & dosagem , Óxido Nítrico/agonistas , Atividade Motora
6.
Arq. ciências saúde UNIPAR ; 26(3): 1091-1098, set-dez. 2022.
Artigo em Português | LILACS | ID: biblio-1414403

RESUMO

Eugenia pyriformis Cambess (Myrtaceae), conhecida popularmente como uvaia. Em seus frutos são encontrados compostos fenólicos com ação antioxidante e nas folhas foram detectados altos teores de flavonoides e taninos hidrolisados que se mostraram inibidor da protease de 2019 - nCoV e SARS-CoV. Neste sentido, o objetivo deste estudo foi a obtenção do extrato bruto das folhas, a análise da composição química e a possibilidade da ação antiviral frente ao SARS COV-2. O extrato bruto (EB) foi obtido a partir das folhas secas de E. pyriformis, pela técnica de maceração dinâmica com esgotamento do solvente (etanol 90º GL) e concentrado em evaporador rotativo. Seis gramas do EB foram fracionados em cromatografia em coluna, e eluído com hexano, diclorometano, acetato de etila e metanol, as frações foram concentradas em um evaporador rotativo (Tecnal TE-210). O EB e as frações foram identificadas por cromatografia líquida de alta eficiência à espectrometria de massas de alta resolução (CLAE-ESI/qTOF). A identificação química do extrato bruto e frações das folhas de E. pyriformis evidenciou a presença de compostos fenólicos destacando os ácidos fenólicos, flavonoides e taninos. De forma complementar, foi realizado um levantamento bibliográfico sobre a provável ação antiviral dos compostos fenólicos e taninos presentes nas folhas de uvaia. Os resultados evidenciaram que os flavonoides quercetina e kaempferol possuem ação antiviral quando se ligam a glicoproteína do envelope ou capsídeo viral interferindo na ligação e penetração do vírus na célula. Este resultado coloca as folhas de E. pyriformis na lista de plantas com ação antiviral.


Eugenia pyriformis Cambess (Myrtaceae), popularly known as uvaia. In its fruits, phenolic compounds with antioxidant action are found and in the leaves, high levels of flavonoids and hydrolyzed tannins were detected, which proved to be an inhibitor of the 2019 protease - nCoV and SARS-CoV. In this sense, the objective of this study was to obtain the crude extract of the leaves, the analysis of the chemical composition and the possibility of antiviral action against SARS COV-2. The crude extract (EB) was obtained from the dried leaves of E. pyriformis, by the dynamic maceration technique with solvent exhaustion (ethanol 90º GL) and concentrated in a rotary evaporator. Six grams of EB were fractionated in column chromatography, and eluted with hexane, dichloromethane, ethyl acetate and methanol, the fractions were concentrated on a rotary evaporator (Tecnal TE-210). EB and fractions were identified by high performance liquid chromatography using high resolution mass spectrometry (HPLC-ESI/qTOF). The chemical identification of the crude extract and fractions of E. pyriformis leaves evidenced the presence of phenolic compounds, highlighting phenolic acids, flavonoids and tannins. In addition, a bibliographic survey was carried out on the probable antiviral action of phenolic compounds and tannins present in uvaia leaves. The results showed that the flavonoids quercetin and kaempferol have antiviral action when they bind to the envelope glycoprotein or viral capsid, interfering with the binding and penetration of the virus into the cell. This result places E. pyriformis leaves in the list of plants with antiviral action.


Eugenia pyriformis Cambess (Myrtaceae), conocida popularmente como uvaia. En sus frutos se encuentran compuestos fenólicos con acción antioxidante y en las hojas se detectaron altos contenidos de flavonoides y taninos hidrolizados que demostraron inhibir la proteasa de 2019 - nCoV y SARS-CoV. En este sentido, el objetivo de este estudio fue obtener el extracto crudo de las hojas, el análisis de la composición química y la posibilidad de acción antiviral contra el SARS COV-2. El extracto crudo (EB) se obtuvo a partir de las hojas secas de E. pyriformis, mediante la técnica de maceración dinámica con agotamiento del disolvente (etanol 90º GL) y se concentró en evaporador rotatorio. Seis gramos de EB se fraccionaron en cromatografía en columna, y se eluyeron con hexano, diclorometano, acetato de etilo y metanol, las fracciones se concentraron en un evaporador rotatorio (Tecnal TE-210). El EB y las fracciones se identificaron mediante cromatografía líquida de alta resolución a espectrometría de masas de alta resolución (HPLC-ESI/qTOF). La identificación química del extracto crudo y de las fracciones de las hojas de E. pyriformis mostró la presencia de compuestos fenólicos destacando los ácidos fenólicos, los flavonoides y los taninos. De forma complementaria, se realizó un estudio bibliográfico sobre la probable acción antiviral de los compuestos fenólicos y los taninos presentes en las hojas de la uva. Los resultados mostraron que los flavonoides quercetina y kaempferol tienen acción antiviral cuando se unen a la glicoproteína de la envoltura o cápside viral, interfiriendo en la unión y penetración del virus en la célula. Este resultado sitúa a las hojas de E. pyriformis en la lista de plantas con acción antiviral.


Assuntos
Folhas de Planta/química , Coronavírus Relacionado à Síndrome Respiratória Aguda Grave/química , Eugenia/química , Antivirais/farmacologia , Quercetina/farmacologia , Flavonoides/farmacologia , Cromatografia Líquida de Alta Pressão/métodos , Quempferóis/farmacologia , Taninos Hidrolisáveis/farmacologia , Compostos Fenólicos
7.
Acta sci., Health sci ; 44: e55845, Jan. 14, 2022.
Artigo em Inglês | LILACS | ID: biblio-1366721

RESUMO

The effects of the aqueous extract of Ilex paraguariensis (Ip)and the flavonoid quercetin were tested during the induction of in vivomyocardial ischemia/ reperfusion in Rattus norvegicus. The antioxidant power of the extract and quercetin were chemically determined. The experimental groups were: control, ischemia/reperfusion induction, Iporal treatment, Iporal treatment and ischemia /reperfusion, quercetin oral treatment, and quercetin oral treatment and ischemia/reperfusion. Rats were anesthetized with sodium thiopental and xylazine via intraperitoneal injection and subsequently underwent 15 minutes of ischemia followed by 15 minutes of reperfusion. Ischemia was promoted by tying the left anterior descending coronary artery. Areas of risk and infarction were stained by intravenous Evans blue and triphenyl tetrazolium chloride. Reactive oxygen species (ROS), antioxidant capacity against peroxylradicals, and lipid peroxidation of the myocardium were quantified. A significant reduction in areas of risk and infarction was detected in the ischemic myocardium treated with Ipand quercetin; ROS generation and lipid peroxidation were significantly reduced, and the antioxidant capacity was elevated. Oral administration of Ippromoted antioxidant benefits in the myocardium during ischemia and reperfusion, which reduced infarction. We suggest that Mate (a hot drink made from steeped dried leaves of Ip) consumption is a potential cardioprotective habit of indigenous people from southern South American countries, which must be better understood scientifically and ethnographically.


Assuntos
Animais , Ratos , Flavonoides , Ilex paraguariensis/efeitos adversos , Isquemia/tratamento farmacológico , Antioxidantes , Quercetina/análise , Ratos , Reperfusão , Administração Oral , Estresse Oxidativo/efeitos dos fármacos , Chás Medicinais/efeitos adversos , Infarto do Miocárdio/tratamento farmacológico
8.
Araçatuba; s.n; 2022. 66 p. ilus, tab, graf.
Tese em Inglês | LILACS, BBO - Odontologia | ID: biblio-1510576

RESUMO

O objetivo do presente estudo foi investigar o efeito de soluções contendo fluoreto (F), hexametafosfato de sódio (HMP) e quercetina (QC), sozinhos ou em associação, sobre a erosão dentinária e sobre a inibição de metaloproteinases da matriz (MMPs) -2 e -9, em protocolos in vitro. Blocos de dentina radicular bovina (4 × 4 × 2 mm; n = 96), selecionados por dureza superficial, foram aleatoriamente divididos em 8 grupos experimentais (n = 12/grupo) e tratados 2×/dia (um minuto) com as seguintes soluções: (1) água deionizada (controle negativo); (2) 1100 ppm F ("F"); (3) 1,0% HMP ("HMP"); (4) 0,03% QC ("QC"); (5) F+HMP; (6) F+QC; (7) HMP+QC; e (8) F+HMP+QC. Os blocos foram submetidos a desafios erosivos 4×/dia, por 5 dias (exposição dinâmica a ácido cítrico 50 mmol.l-1 , pH 3,2, 90 s). Em seguida, foram analisados quanto à perda dentinária (perfilometria) e à perda de dureza integrada em profundidade (área sob a curva, ∆KHN). O potencial antiproteolítico das soluções contendo F, HMP e/ou QC foi analisado por zimografia. Os dados de perda dentinária (log10) foram submetidos a ANOVA um critério, seguido do teste de Tukey. Os resultados de ∆KHN (dados brutos) foram submetidos a ANOVA dois critérios, medidas repetidas, seguido do teste HolmSidak (p< 0,05). O menor desgaste erosivo foi observado no grupo F+HMP+QC. Nas menores profundidades (5-30 µm), os blocos tratados com a solução contendo F+HMP+QC apresentaram os maiores valores de ∆KHN. A análise zimográfica mostrou que todos os tratamentos promoveram atividade antiproteolítica total da MMP-2, com exceção da QC administrada sozinha (inibição de 77%). Para MMP-9, todas as soluções contendo HMP e a associação de F+QC apresentaram atividade antiproteolítica total. Conclui-se que a adição de HMP e QC a soluções contendo F levou a uma maior proteção contra a erosão dentinária, tanto em superfície (perda dentinária) quanto em relação ao conteúdo mineral do tecido remanescente (∆KHN), além de promover uma completa inibição da atividade de MMPs -2 e -9 in vitro(AU)


The aim of the present study was to investigate the effect of solutions containing fluoride (F), sodium hexametaphosphate (HMP) and quercetin (QC), alone or in association, on dentin erosion and on the inhibition of matrix metalloproteinases (MMPs) - 2 and -9, using in vitro protocols. Bovine root dentin blocks (4 × 4 × 2 mm; n = 96), selected by surface hardness, were randomly divided into 8 experimental groups (n = 12/group) and treated 2×/day (one minute) with the following solutions: (1) deionized water (negative control); (2) 1100 ppm F ("F"); (3) 1.0% HMP ("HMP"); (4) 0.03% QC ("QC"); (5) F+HMP; (6) F+QC; (7) HMP+QC; and (8) F+HMP+QC. Blocks were submitted to erosive challenges 4×/day for 5 days (dynamic exposure to 50 mmol.l-1 citric acid, pH 3.2, 90 s). They were then analyzed for dentin loss (profilometry) and integrated hardness loss in depth (area under the curve, ∆KHN). The antiproteolytic potential of solutions containing F, HMP and/or QC was analyzed by zymography. Dentin loss results (log10 transformed) were submitted to one-way ANOVA, followed by Tukey's test. ∆KHN data (raw) were submitted to two-way, repeated-measures ANOVA, followed by the Holm-Sidak test (p< 0.05). The lowest dentin erosive wear was promoted by F+HMP+QC. At the lowest depths (5-30 µm), blocks treated with F+HMP+QC showed the highest values of ∆KHN. Zymography analysis showed that all treatments completely inhibited MMP-2 activity, except for QC administered alone (77% inhibition). For MMP-9, all the solutions containing HMP or the association of F+QC promoted total antiproteolytic activity. It was concluded that the addition of HMP and QC to F solutions led to greater protection against dentin erosion, both at the surface (dentin loss) and in relation to the mineral content of the remaining tissue (∆KHN), in addition to promoting a complete inhibition of MMPs -2 and -9 activity in vitro(AU)


Assuntos
Fosfatos , Quercetina , Erosão Dentária , Inibidores de Metaloproteinases de Matriz , Flavonoides , Flavonóis
9.
Int. j. morphol ; 40(5): 1174-1180, 2022. ilus, graf
Artigo em Inglês | LILACS | ID: biblio-1405293

RESUMO

SUMMARY: Ingestion of an overdose of paracetamol (also called acetaminophen, or APAP) induces hepatotoxicity that can lead to liver failure. The link between the pro-inflammatory microRNA-155 (miR-155) and leukocyte infiltration (CD45) in APAP- antioxidant depletion and liver toxicity with and without the natural polyphenolic compounds, quercetin (QUR) plus resveratrol (RES) has not been previously studied. Therefore, acute hepatic injury was induced in rats by 2 g/kg APAP (single dose, orally) and another group started QUR (50 mg/kg) plus RES (30 mg/kg) treatment one week prior to APAP ingestion. Animals were culled 24 hours post the paracetamol treatment. APAP overdose induced hepatic and blood levels of miR-155 expression, CD45 (leukocyte common antigen) immunostaining, degenerated hepatocytes, and hepatic injury enzymes; alanine aminotransferase (ALT) and aspartate aminotransferase (AST), which were markedly decreased by QUR+RES. Whereas, APAP intoxication ameliorated liver tissue levels of the antioxidants, glutathione peroxidase and superoxide dismutase that were augmented by QUR+RES. Moreover, a significant (p<0.05) correlation between miR-155/CD45 axis and liver tissue injury was observed. These findings show that paracetamol intoxication augments miR- 155/CD45 axis-mediated modulation of antioxidants and liver injury in rats, and is protected by QUR+RES.


RESUMEN: La ingestión de una sobredosis de paracetamol (también llamado acetaminofeno o APAP) induce hepatotoxicidad que puede provocar insuficiencia hepática. El vínculo entre el microARN-155 proinflamatorio (miR-155) y la infiltración de leucocitos (CD45) en el agotamiento de APAP- antioxidante y la toxicidad hepática con y sin los compuestos polifenólicos naturales, quercetina (QUR) más resveratrol (RES) no ha sido previamente investigado. En este estudio, se indujo daño hepático agudo en ratas con 2 g/kg de APAP (dosis única, por vía oral) y otro grupo comenzó el tratamiento con QUR (50 mg/ kg) más RES (30 mg/kg) una semana antes de la ingestión de APAP. Los animales se sacrificaron 24 horas después del tratamiento con paracetamol. La sobredosis de APAP indujo niveles hepáticos y sanguíneos de expresión de miR-155, inmunotinción de CD45 (antígeno leucocitario común), degeneración de los hepatocitos y daño hepático enzimático; alanina aminotransferasa (ALT) y aspartato aminotransferasa (AST), disminuyeron notablemente con QUR+RES. Mientras que la intoxicación con APAP mejoró los niveles de antioxidantes, glutatión peroxidasa y superóxido dismutasa en el tejido hepático los que aumentaron con QUR+RES. Además, se observó una correlación significativa (p<0,05) entre el eje miR-155/CD45 y la lesión del tejido hepático. Estos hallazgos muestran que la intoxicación por paracetamol aumenta la modulación mediada por el eje miR-155/CD45 de los antioxidantes y la lesión hepática en ratas, y está protegida por QUR+RES.


Assuntos
Animais , Ratos , Quercetina/farmacologia , Doença Hepática Induzida por Substâncias e Drogas , Resveratrol/farmacologia , Acetaminofen/toxicidade , Antioxidantes/farmacologia , Ratos Sprague-Dawley , Antígenos Comuns de Leucócito/efeitos dos fármacos , MicroRNAs/efeitos dos fármacos
10.
Braz. J. Pharm. Sci. (Online) ; 58: e18744, 2022. tab, graf
Artigo em Inglês | LILACS | ID: biblio-1374554

RESUMO

Abstract The continuous prolonged exposures of sun light especially the ultra violet (UV) radiation present in it, cause not only the risk of skin cancer but also it may cause premature skin aging, photodermatoses and actinic keratoses. Flavonoids (including Flavane, Flavanone, Flavone, Flavonol, Isoflavone, Neoflavone etc.) having potent antioxidant activity, used as topical applications for protection against UV induced skin damages as well as for skin care. Most commonly used flavonoid is quercetin (Flavonol), which is present in fruits, vegetables, and herbs. We aim to review the research focused on development of different novel formulations to treat UV radiations induced skin diseases. In this review, several formulations of flavonoid quercetin were discussed and their outcomes were compiled and compared in context to solubility, stability and efficiency of application. On the basis this comparative analysis we have concluded that three formulations, namely glycerosomes, nanostructured lipid carriers and deformable liposomes hold good applications for future aspects for topical delivery of quercetin. These formulations showed enhanced stability, increased quercetin accumulation in different skin layers, facilitated drug permeation in skin and long-lasting drug release.


Assuntos
Quercetina/análise , Pele/lesões , Dermatopatias/tratamento farmacológico , Neoplasias Cutâneas/patologia , Raios Ultravioleta/efeitos adversos , Compostos Fitoquímicos/análise , Flavonoides/efeitos adversos , Preparações Farmacêuticas/análise , Ceratose Actínica/patologia , Fatores de Proteção , Antioxidantes/classificação
11.
Int. braz. j. urol ; 47(4): 796-802, Jul.-Aug. 2021. tab, graf
Artigo em Inglês | LILACS | ID: biblio-1286776

RESUMO

ABSTRACT Purpose: To quantitatively evaluate the possible long-term protective effects of quercetin during renal warm ischemia. Materials and Methods: Male rats were allocated into 4 groups: sham (S), sham quercetin (SQ), ischemia (I), and ischemia quercetin (IQ). Groups SQ and IQ received quercetin (50mg/kg) before and after surgery. Groups I and IQ had their left renal vessels clamped for 60 minutes. All animals were euthanized four weeks after the procedure, and serum urea and creatinine levels were measured. Renal weight and volume, cortex-non-cortex area ratio (C-NC), cortical volume (CV), glomerular volumetric density (Vv[glom]), volume-weighted glomerular volume (VWGV) and number of glomeruli per kidney (N[glom]) were evaluated by stereological methods. Results were considered statistically significant when p <0.05. Results: Serum urea levels in group I increased by 10.4% in relation to group S, but no differences were observed among the other groups. The C-NC of group I was lower than those of all other groups, and group IQ had similar results to sham groups. The Vv[glom] and N[glom] of group I were lower than those of group S (33.7% and 28.3%, respectively) and group IQ had no significant difference compared to the S group. Conclusions: Quercetin was effective as a nephroprotective agent in preventing the glomerular loss observed when the kidney was subjected to warm ischemia. This suggests that this flavonoid may be used preventively in kidney surgery, when warm ischemia is necessary, such as partial nephrectomy.


Assuntos
Animais , Masculino , Ratos , Quercetina/uso terapêutico , Isquemia Quente , Roedores , Rim , Glomérulos Renais , Nefrectomia
12.
Int. j. morphol ; 39(3): 839-847, jun. 2021. ilus, tab, graf
Artigo em Inglês | LILACS | ID: biblio-1385404

RESUMO

SUMMARY: A large body of evidence supports the protective role of the flavonol antioxidant compound quercetin in mammals. We tested the hypothesis that quercetin can protect against the hypothalamus-pituitary-gonadal (HPG) axis defect like a reduction in gonadotropins and testicular hormones and abnormal semen analysis induced by chronic unpredictable stress (CUS), possibly via the downregulation of oxidative stress (ROS) and p53-Bax-caspase-3 pathways. Rats were either exposed to a variety of unpredictable stressors daily before being sacrificed after 3 weeks (model group) or were treated with quercetin (50 mg/kg body weight/day) at the same time the CUS were induced (treated group). Harvested testicular tissues were stained with basic histological staining, and testis homogenates were assayed for the tumor suppressor p53, apoptosis regulator Bax, B-cell lymphoma 2 (Bcl-2), caspase-3, malondialdehyde (MDA), glutathione peroxidase (GPx), and superoxide dismutase (SOD). In addition, harvested epididymis tissues were used to assess semen analysis, and blood samples were assayed for the testicular hormone testosterone, the adrenal cortex hormone corticosterone, and the anterior pituitary gonadotropins, follicular stimulating hormone (FSH) and luteinizing hormone (LH). CUS induced profound testicular damage and significantly (p<0.05) induced p53, Bax, caspase-3, MDA, and corticosterone, which were significantly (p<0.05) inhibited by quercetin except corticosterone. Whereas, quercetin significantly (p<0.05) increased FSH, LH, testosterone, Bcl-2, GPx, and SOD levels that were inhibited by CUS. In addition, CUS induced oligozoospermia, asthenozoospermia, and teratozoospermia, which were significantly (p<0.05) protected by quercetin. Thus, Quercetin protects against CUS-induced HPG defects in rats, which is associated with the inhibition of ROS-p53-Bax-caspase-3 axis.


RESUMEN: El papel protector del compuesto antioxidante flavonol quercetina en los mamíferos ha sido ampliamente reportado. Probamos la hipótesis que la quercetina puede proteger contra el defecto del eje hipotálamo-hipofisiario- gonadal (HHG) como una reducción de gonadotropinas y hormonas testiculares y análisis de semen anormal inducido por estrés crónico impredecible (ECI), posiblemente a través de la regulación reducida del estrés oxidativo (REO) y las vías p53- Bax-caspasa-3. Las ratas fueron expuestas a una variedad de fac- tores estresantes impredecibles diariamente antes de ser sacrificadas después de 3 semanas (grupo modelo) o fueron tratadas con quercetina (50 mg / kg de peso corporal / día) al mismo tiempo que se indujo la ECI (grupo tratado). Los tejidos testiculares fueron teñidos con tinción histológica básica y los homogeneizados de testículo se analizaron para determinar el supresor de tumores p53, el regulador de apoptosis Bax, el linfoma de células B 2 (Bcl-2), la caspasa-3, el malondialdehído (MDA), la glutatión peroxidasa (GPx) y superóxido dismutasa (SOD). Además, se utilizaron tejidos del epidídimo recolectados para evaluar el análisis de semen y se analizaron muestras de sangre para determinar la hormona testicular testosterona, la hormona corticosterona de la corteza suprarrenal y las gonadotropinas de la hipófisis anterior, la hormona estimulante folicular (FSH) y la hormona luteinizante (LH). El ECI indujo daño testicular importante e indujo significativamente niveles de (p <0,05) p53, Bax, caspasa-3, MDA y corticosterona, que fueron inhibidos (p <0,05) por la quercetina. La quercetina aumentó significativamente (p <0,05) los niveles de FSH, LH, testosterona, Bcl-2, GPx y SOD que fueron inhibidos por ECI. Además, ECI indujo oligozoospermia, astenozoospermia y teratozoospermia, protegidos de manera significativa (p <0,05) por la quercetina. Por lo tanto, la quercetina protege contra los defectos de HHG inducidos por ECI en ratas, lo que está asociado con la inhibición del eje ROS-p53-Bax-caspasa-3.


Assuntos
Animais , Masculino , Ratos , Quercetina/administração & dosagem , Estresse Fisiológico , Doenças Testiculares/etiologia , Testículo/efeitos dos fármacos , Antioxidantes/administração & dosagem , Testículo/lesões , Doença Crônica , Proteína Supressora de Tumor p53/antagonistas & inibidores , Espécies Reativas de Oxigênio/antagonistas & inibidores , Ratos Wistar , Apoptose/efeitos dos fármacos , Modelos Animais de Doenças , Proteína X Associada a bcl-2/antagonistas & inibidores , Caspase 3/efeitos dos fármacos , Eixo Hipotalâmico-Hipofisário-Gonadal/efeitos dos fármacos
13.
Araçatuba; s.n; 2021. 55 p. ilus, graf.
Tese em Inglês | LILACS, BBO - Odontologia | ID: biblio-1451254

RESUMO

Objetivo: Avaliar o efeito do consumo de vinho tinto ou de seus polifenóis nos processos de inflamação / reabsorção associados à periodontite periapical (PP) em ratos. Metodologia: Trinta e dois ratos Wistar com 3 meses de idade tiveram a periodontite periapical induzida nos quatro primeiros molares, dispostos em quatro grupos: controle (C) - ratos com periodontite periapical; vinho (W) - ratos com PP recebendo 4,28 mL/kg de vinho tinto; resveratrol + quercetina (R+Q) - ratos com PP recebendo 4,28 mL/kg de solução contendo 1,00 mg/L de quercetina e 0,86 mg/L de resveratrol; e álcool (ALC) - ratos com PP recebendo a mesma dose alcoólica contida no vinho. Os tratamentos por gavagem foram administrados diariamente, do início ao 45º dia. No 15º dia a PP foi induzida e no 45º dia os animais foram eutanasiados. Foram realizadas análises histológicas, imunohistoquímica para RANKL, OPG, TRAP, IL-10, TNF-⍺ e IL-1ß e por microtomografia computadorizada nas mandíbulas. O teste de Kruskal-Wallis com Dunn's foi realizado para dados não paramétricos e o teste ANOVA com Tukey's para dados paramétricos, p < 0,05. Resultados: A mediana do escore do processo inflamatório foi menor no grupo R + Q (1) em comparação aos grupos C (2) e ALC (3), e não diferente do grupo W (1.5). Embora os grupos W e R+Q tenham apresentado menor pontuação para RANKL, TNF-⍺ e IL-1ß, não foram encontradas diferenças em relação aos grupos C e ALC. A marcação imunológica para OPG foi maior no grupo R+Q em comparação com todos os grupos; o mesmo observado para IL-10, sendo diferente dos grupos C e ALC. O grupo R+Q apresentou a menor contagem de células TRAP, seguido pelo grupo W, ambos inferiores aos grupos C e ALC, que apresentaram os piores resultados. O menor valor de reabsorção óssea foi no grupo R+Q (0,50 mm3 ± 0,21 mm3 ), inferior ao grupo C (0,88 mm3 ± 0,10 mm3 ). O grupo W (0,60 mm3 ± 0,25 mm3 ) e o grupo R+Q apresentaram menor reabsorção óssea em comparação com o grupo ALC (0,97 mm3 ± 0,22 mm3 ). Conclusão: A administração de vinho tinto reduziu a inflamação oriunda da PP, a marcação TRAP e a reabsorção óssea periapical em comparação ao ALC; a administração de resveratrol-quercetina reduziu o processo inflamatório da PP, a reabsorção óssea periapical e alterou a expressão de OPG, IL-10 e TRAP em comparação aos grupos C e ALC(AU)


Aim: To evaluate the effect of red wine consumption or its polyphenols on the inflammation/resorption processes associated with periapical periodontitis (PP) in rats. Methodology: Thirty-two 3-month-old Wistar rats had the PP induced in the four first molars, arranged into four groups: control (C) - rats with PP; wine (W) - rats with PP receiving 4.28 mL/kg of red wine; resveratrol+quercetin (R+Q) - rats with PP receiving 4.28 mL/kg of solution containing 1.00 mg/L of quercetin and 0.86 mg/L of resveratrol; and alcohol (ALC) - rats with PP receiving the alcoholic dose contained in the wine. The oral gavage treatments were daily administered, from day 0 to day 45th. At the 15th day the PP was induced, and at the 45th day the animals were euthanized; histological, immunohistochemical (RANKL, OPG, TRAP, IL-10, TNF-⍺ and IL-1ß), and micro-computed tomography analysis were performed in the jaws. The Kruskal-Wallis with Dunn's test was performed for nonparametric data, and the ANOVA with Tukey's test for parametric data, p< 0.05. Results: The median score of inflammatory process was statistically lower in the R+Q group (1) compared to the C (2) and ALC (3) groups, and not different from the W (1.5) group. Although the W and R+Q groups had a lower score for RANKL, TNF-⍺ and IL-1ß, no differences were found compared to C and ALC. The immunolabelling for OPG was higher in the R+Q group compared to all groups; the same observed for IL-10, being different from groups C and ALC. The R+Q group had the lowest TRAP cell count, followed by the W group, both inferior to C and ALC groups, which presented the worst results. The lowest bone resorption value was in the R+Q group (0.50mm3 ±0.21mm3 ), statically lower than the C group (0.88mm3 ±0.10mm3 ). The W group (0.60 mm3 ±0.25 mm3 ) and R+Q group showed less bone resorption compared to the ALC group (0.97mm3 ±0.22mm3 ). Conclusion: Red wine administration led to lowers PP inflammation, TRAP marking, and periapical bone resorption compared to ALC; resveratrol-quercetin administration reduced the PP inflammatory processes, periapical bone resorption, and altered the OPG, IL-10, and TRAP expression compared to C and ALC groups(AU)


Assuntos
Animais , Ratos , Quercetina
14.
Araçatuba; s.n; 2021. 52 p. ilus, graf.
Tese em Português | BBO - Odontologia, LILACS | ID: biblio-1381565

RESUMO

A perda óssea dentária e a formação de lesões periapicais surgem como uma consequênc ia do desequilíbrio da homeostase óssea. Os osteoblastos, juntamente com os osteoclastos e osteócitos, atuam na formação e na reabsorção óssea. Vários marcadores de formação óssea são produzidos por osteoblastos ativos e refletem diferentes aspectos da dif erenciação osteoblástica e da remodelação óssea. Com isso, muitos autores têm explorado o uso de fitoterápicos, visando obter novos compostos que apresentem propriedades terapêuticas, como os flavonoides, e que estimulem a neoformação óssea e o reparo da r egião periapical. O objetivo deste estudo foi avaliar in vitro a citotoxicidade e efeito indutor de mineralização de flavonoides sobre células osteoblásticas humanas. Para isso, células osteoblásticas da linhagem Saos expostas aos seguintes flavono2 foram ides: quercetina, miricetina e seus derivados taxifolina, isoquercitrina, rutina, ampelopsina e EGCG, além de pinocembrina, crisina e canferol, de forma isolada e combinada. Foi avaliado o efeito citotóxico, a atividade de fosfatase alcalina e indução de n mé todo de Shapiroódulos de mineralização. Os resultados foram analisados p elo Wilk, e as variáveis foram submetidas à análise de ANOVA seguida pelo teste de Tukey para comparar entre os grupos e/ou concentrações ou teste de Dunnett para comparar entre cada grupo e o controle, com nível de significância de 5%. A viabilidade da cultura de osteoblastos não teve uma redução estatisticamente significativa na presença da maioria dos compostos, exceto crisina a 100µM. Taxifolina, isoquercitrina, rutina, ampelopsina e EGCG foram os compostos que estimularam significativamente a atividade da fosfatase alcalina, juntamente com as combinações taxifolina+isoquercitrina, taxifolina+ampelopsina e taxifolina+rutina a 25/25 µM. Quanto a formação de nódulos de mine ralização, ampelopsina, isoquercitrina, rutina, pinocembrina e miricetina isolados e taxifolina+isoquercitrina, taxifolina+ampelopsina e taxifolina+rutina combinados obtiveram os melhores resultados, variando de acordo com as concentrações. Concluise que a taxifolina, isoquercitrina, rutina e ampelopsina e combinações de taxifolina com esses flavonoides são citocompatíveis e apresentam efeito indutor de mineralização em osteoblastos Saos-2(AU)


Dental bone loss and the formation of periapical lesions arise as a consequence of imbalance of bone homeostasis. Osteoblasts, together with osteoclasts and osteocytes, act in bone formation and resorption. Several markers of bone formation are produced by active osteoblasts and reflect different aspects of osteoblastic differentiation and bone remodeling. Thus, many authors have explored the use of phytotherapics in order to obtain new compounds with therapeutic properties, such as flavonoids, and also stimulate bone neoformation and periapical region repair. The objective of this study was to evaluate in vitro the cytotoxicity and inducing effect of flavonoid mineralization on human osteoblastic cells. For this, osteoblastic cells of the Saos-2 lineage were exposed to the following flavonoids: quercetin, myricetin and its derivatives taxifoline, isoquercitrin, rutin, ampelopsin and EGCG, in addition to pinocembrin, chrysin and kaempferol, in an isolated and combined manner. The cytotoxic effect, the activity of alkaline phosphatase and the induction of mineralization nodules were evaluated. The results were analyzed using the Shapiro-Wilk method, and the variables were submitted to ANOVA analysis followed by the Tukey test to compare between groups and/or concentrations or Dunnett's test to compare between each group and the control, with a level of 5% significance. The viability of the osteoblast culture did not have a statistically significant reduction in the presence of most compounds, except 100 µM chrysin. Taxifoline, isoquercitrin, rutin, ampelopsin and EGCG were the compounds that significantly stimulated the activity of alkaline phosphatase, together with the combinations taxifoline+isoquercitrin, taxifoline+ampelopsin and taxifoline+rutin at 25/25 µM. As for the formation of mineralization nodules, ampelopsin, isoquercitrin, rutin, pinocembrin and myricetin alone and taxifoline+isoquercitrin, taxifoline+ampelopsin and taxifoline+rutin combined obtained the best results, varying according to the concentrations. It is concluded that taxifoline, isoquercitrin, rutin and ampelopsin and combinations of taxifolin with these flavonoids are cytocompatible and have a mineralization-inducing effect on Saos-2 osteoblasts(AU)


Assuntos
Osteoblastos , Periodontite Periapical , Flavonoides , Reabsorção Óssea , Osteoclastos , Osteócitos , Quercetina , Rutina , Flavonoides/toxicidade , Flavonoides/uso terapêutico , Osso e Ossos , Calcificação Fisiológica , Remodelação Óssea , Flavanonas , Homeostase
15.
Int. j. morphol ; 38(4): 876-881, Aug. 2020. graf
Artigo em Inglês | LILACS | ID: biblio-1124869

RESUMO

Acetaminophen (also called paracetamol, or APAP) causes acute kidney injury after accidental or intentional ingestion of a toxic dose of the drug. We tested whether the antioxidant and anti-inflammatory agent, quercetin (QUR) given alone can protect against acute nephrotoxicity induced by APAP overdose in a rat model of APAP-induced acute kidney injury. Rats were either given a single dose of APAP (2 g/kg) before being sacrificed after 24 hours or were pre-treated for 7 days with QUR (50 mg/kg) before being given a single dose of APAP and then sacrificed 24 hours post APAP ingestion. Kidneys were examined by light microscopy after staining with hematoxylin and eosin (H&E) and collected blood samples were assayed for biomarkers of oxidative stress, inflammation, and kidney injury. H&E stained sections of kidney from the model group of rats (APAP) showed substantial damage to the kidney architecture as demonstrated by widening of Bowman's space, tubular dilatation, vacuolization of tubular epithelium, and congested dilated blood vessels, which were partially protected by QUR. In addition, APAP significantly (p<0.05) increased blood levels of urea, creatinine, malondialdehyde (MDA), tumor necrosis factor-alpha (TNF-a), and interleukin-6 (IL-6), which were significantly (p<0.05) reduced by QUR. These results indicate that quercetin partially protects against APAP-induced acute kidney injury in rats, which is associated with the inhibition of biomarkers of oxidative stress and inflammation and kidney injury.


El acetaminofeno (también llamado paracetamol o DCI) causa daño renal agudo después de la ingestión accidental o intencional de una dosis tóxica del medicamento. En el estudio analizamos si el agente antioxidante y antiinflamatorio, la quercetina (QUR) administrada sola, puede proteger contra la nefrotoxicidad aguda inducida por sobredosis de DCI en un modelo de rata. Las ratas recibieron una dosis única de DCI (2 g / kg) antes de ser sacrificadas después de 24 horas o fueron pretratadas durante 7 días con QUR (50 mg / kg) antes de recibir una dosis única de DCI y luego sacrificadas 24 horas post ingestión. Los riñones se examinaron mediante microscopía óptica después de la tinción con hematoxilina y eosina (H&E) y las muestras de sangre recolectadas se analizaron para detectar biomarcadores de estrés oxidativo, inflamación y daño renal. Las secciones de riñón teñidas con H&E del grupo modelo de ratas (DCI) mostraron un daño sustancial a la arquitectura del riñón, como lo demuestra la ampliación del espacio de Bowman, la dilatación tubular, la vacuolización del epitelio tubular y los vasos sanguíneos dilatados congestionados, que estaban parcialmente protegidos por QUR. Además, DCI aumentó significativamente (p <0,05) los niveles sanguíneos de la urea, creatinina, malondialdehído (MDA), factor de necrosis tumoral alfa (TNF-a) e interleucina-6 (IL-6), los que fueron reducidos significativamente (p < 0,05) por QUR. Estos resultados indican que la quercetina protege parcialmente contra la lesión renal aguda inducida por DCI en ratas, asociada con la inhibición de biomarcadores de estrés oxidativo, inflamación y lesión renal.


Assuntos
Animais , Ratos , Quercetina/administração & dosagem , Injúria Renal Aguda/induzido quimicamente , Acetaminofen/toxicidade , Antioxidantes/administração & dosagem , Quercetina/farmacologia , Biomarcadores/análise , Estresse Oxidativo/efeitos dos fármacos , Substâncias Protetoras , Creatinina , Modelos Animais de Doenças , Inflamação , Rim/efeitos dos fármacos , Antioxidantes/farmacologia
17.
Arq. bras. cardiol ; 115(1): 102-108, jul. 2020. tab, graf
Artigo em Inglês, Português | LILACS, Sec. Est. Saúde SP | ID: biblio-1131269

RESUMO

Resumo Fundamento Os glicocorticóides (GCs) são amplamente prescritos para o tratamento de numerosos distúrbios clínicos devido às suas propriedades anti-inflamatórias e imunomoduladoras, e um dos efeitos indesejáveis mais comuns desses medicamentos é a dislipidemia. Objetivo Avaliar o efeito da quercetina, um flavonoide derivado de plantas, no perfil lipídico de ratos tratados com glicocorticóides em altas doses. Métodos Um total de 32 ratos Sprague-Dawley foram distribuídos aleatoriamente entre quatro grupos (8 ratos por grupo) e tratados por 6 semanas com uma das seguintes opções : (i) solução salina normal; (ii) 40 mg/kg de succinato sódico de metilprednisolona (MP); (iii) MP + 50 mg/kg de quercetina; (iv) MP + 150 mg/kg de quercetina. O MP foi injetado por via subcutânea e a quercetina foi administrada por gavagem oral 3 dias por semana. No final do estudo, o perfil lipídico dos animais foi medido através de kits enzimáticos. Os dados foram analisados e a significância estatística foi estabelecida em p <0,05. Resultados Os níveis séricos médios de colesterol total (CT), triglicerídeos (TG) e LDL aumentaram drasticamente em animais tratados com GC em comparação com o grupo controle. Ambas as doses de quercetina (50 e 150 mg/kg) melhoraram o CT (43% e 45%), LDL (56% e 56%) e TG (46% e 55%, respectivamente). A razão Apo B/A1 diminuiu mais de 20% após a ingestão de Anti-Inflamatory Agents. Conclusões Esses dados sugerem que a ingestão de quercetina Quercetin; induzida por glicocorticóides. (Arq Bras Cardiol. 2020; 115(1):102-108)


Abstract Background Glucocorticoids (GCs) are widely prescribed for the treatment of numerous clinical disorders due to their anti-inflammatory and immune-modulatory properties and one of the most common untoward effects of these drugs is dyslipidemia. Objective To evaluate the effect of quercetin, a plant-derived flavonoid, on the lipid profile of high-dose glucocorticoid treated rats. Methods A total of 32 Sprague-Dawley rats, were randomly distributed among four groups (8 rats per group) and treated for 6 weeks with one of the following: (i) normal saline; (ii) 40 mg/kg methylprednisolone sodium succinate (MP); (iii) MP + 50 mg/kg quercetin; (iv) MP + 150 mg/kg quercetin. MP was injected subcutaneously, and quercetin was administered by oral gavage 3 days a week. At the end of the study, the animals' lipid profile was measured by enzymatic kits. Data were analyzed and statistical significance was set at p<0.05. Results The mean serum total cholesterol (TC), triglyceride (TG) and LDL levels were drastically increased in GC-treated animals compared with the control group. Both doses of quercetin (50 and 150 mg/kg) ameliorated TC (43% and 45%), LDL (56% and 56%) and TG (46% and 55% respectively). Apo B/A1 ratio decreased more than 20% following quercetin intake and the decline in TC/HDL, TG/HL, LDL/HDL ratios were significant. Conclusions These data suggest that quercetin intake with both doses of 50 and 150 mg/kg could be considered as a protective agent for glucocorticoid-induced dyslipidemia. (Arq Bras Cardiol. 2020; 115(1):102-108.)


Assuntos
Animais , Ratos , Quercetina/farmacologia , Glucocorticoides , Apolipoproteínas , Triglicerídeos , Ratos Sprague-Dawley , Lipídeos
18.
Int. j. morphol ; 38(3): 585-591, June 2020. graf
Artigo em Inglês | LILACS | ID: biblio-1098291

RESUMO

Acetaminophen (also called paracetamol, or APAP) induced nephrotoxicity is reported after accidental or intentional ingestion of an overdose of the drug. Renal tubular ultrastructural alterations induced by APAP overdose associated with the induction of biomarkers of kidney injury have not been investigated before. Also, we investigated whether the combined polyphenolic anti-inflammatory and antioxidants agents, resveratrol (RES) and quercetin (QUR) can protect against APAP-induced acute kidney injury. The model group of rats received a single dose of APAP (2 g/kg), whereas the protective group of rats was pre-treated for 7 days with combined doses of RES (30 mg/kg) and QUR (50 mg/kg) before being given a single dose of APAP. All rats were then sacrificed one day post APAP ingestion. Harvested kidney tissues were prepared for transmission electron microscopy (TEM) staining and blood samples were assayed for urea, creatinine, and biomarkers of inflammation and oxidative stress. TEM images and blood chemistry analysis showed that APAP overdose induced kidney damage as demonstrated by substantial alterations to the proximal convoluted tubule ultrastructure, and a significant (p<0.05) increase in urea, creatinine, tumor necrosis factor-alpha (TNF-a), and malondialdehyde (MDA) blood levels, which were protected by RES+QUR. These findings indicate that APAP induces alterations to the renal tubular ultrastructure, which is inhibited by resveratrol plus quercetin, which also decreases blood levels of kidney injury biomarkers.


El objetivo de este trabajo fue estudiar la nefrotoxicidad inducida por acetaminofeno (también llamado paracetamol o APAP) después de la ingestión accidental o intencional de una sobredosis de la droga. Las alteraciones ultraestructurales tubulares renales inducidas por sobredosis de APAP asociadas con la inducción de biomarcadores de daño renal no se han investigado. Además, estudiamos si los agentes combinados antiinflamatorios y antioxidantes polifenólicos, el resveratrol (RES) y la quercetina (QUR) pueden proteger contra la lesión renal aguda inducida por APAP. El grupo modelo de ratas recibió una dosis única de APAP (2 g / kg), mientras que el grupo protector de ratas se trató previamente durante 7 días con dosis combinadas de RES (30 mg / kg) y QUR (50 mg / kg) antes de recibir una dosis única de APAP. Todas las ratas se sacrificaron un día después de la ingestión de APAP. Los tejidos renales fueron preparados para el análisis a través de la microscopía electrónica de transmisión (MET). En las muestras de sangre se determinaron la urea, creatinina y los biomarcadores de inflamación y estrés oxidativo. Las imágenes MET y el análisis químico de la sangre mostraron que la sobredosis de APAP inducía daño renal, como lo demuestran las alteraciones sustanciales en la ultraestructura del túbulo contorneado proximal, y además, de un aumento significativo (p <0,05) de la urea, creatinina, factor de necrosis tumoral alfa y niveles sanguíneos de malondialdehído, protegidos por RES + QUR. Estos hallazgos indican que APAP induce alteraciones en la ultraestructura tubular renal, inhibida por el resveratrol más quercetina, que también disminuye los niveles sanguíneos de biomarcadores de daño renal.


Assuntos
Animais , Ratos , Quercetina/administração & dosagem , Resveratrol/administração & dosagem , Túbulos Renais/efeitos dos fármacos , Acetaminofen/toxicidade , Quercetina/farmacologia , Ureia/sangue , Ratos Sprague-Dawley , Creatinina/sangue , Microscopia Eletrônica de Transmissão , Modelos Animais de Doenças , Overdose de Drogas , Resveratrol/farmacologia , Túbulos Renais/patologia , Anti-Inflamatórios/administração & dosagem , Antioxidantes/administração & dosagem
19.
Int. j. morphol ; 38(1): 83-90, Feb. 2020. tab, graf
Artigo em Inglês | LILACS | ID: biblio-1056402

RESUMO

We sought to determine whether the combined polyphenolic compounds, resveratrol and quercetin can substantially protect against modulation of hepatic biomarkers of apoptosis and survival, p53-Bax axis and B-cell lymphoma 2 (Bcl-2) in an animal model of acetaminophen-induced acute liver injury via the association of oxidative stress and interleukin-11 (IL-11). The model group of rats received a single dose of acetaminophen (2 g/kg), whereas the protective group of rats was pre-treated for 7 days with combined doses of resveratrol (30 mg/kg) and quercetin (50 mg/kg) before being given a single dose of acetaminophen. All rats were then sacrificed 24 hours post acetaminophen ingestion. Acetaminophen overdose induced acute liver injury as demonstrated by profound liver parenchymal damage and increased levels of the liver injury enzymes, alanine aminotransferase (ALT) and aspartate aminotransferase (AST). Acetaminophen significantly (p<0.05) modulated malondialdehyde (MDA), p53, apoptosis regulator Bax, Bcl-2, IL-11, interleukin-6 (IL-6), ALT, AST, superoxide dismutase (SOD), and glutathione peroxidase (GPx), which were significantly protected by resveratrol plus quercetin. We further demonstrated a significant (p<0.01) correlation between IL-11 scoring and the levels of p53, Bax, Bcl-2, and MDA. Thus, resveratrol plus quercetin effectively protect against acetaminophen-induced apoptosis, which is associated with the inhibition of oxidative stress and IL-11.


En el estudio se intentó determinar si los compuestos polifenólicos combinados, el resveratrol y la quercetina pueden proteger sustancialmente contra la modulación de los biomarcadores hepáticos de apoptosis y supervivencia, el eje p53-Bax y el linfoma de células B 2 (Bcl-2) en un modelo animal de lesión hepática aguda inducida por acetaminofén, a través de la asociación del estrés oxidativo y la interleucina-11 (IL-11). El grupo modelo de ratas recibió una dosis única de acetaminofén (2 g / kg), mientras que el grupo protector de ratas fue tratado durante 7 días con dosis combinadas de resveratrol (30 mg / kg) y quercetina (50 mg / kg) antes de recibir una dosis única de acetaminofén. Todas los animales fueron sacrificados 24 horas después de la ingestión de acetaminofén. La sobredosis de acetaminofén indujo una lesión hepática aguda, como se observó en el daño profundo del parénquima hepático y el aumento de los niveles de las enzimas en la lesión hepática, alanina aminotransferasa (ALT) y aspartato aminotransferasa (AST). Acetaminofén moduló significativamente (p <0.05) malondialdehído (MDA), p53, regulador de apoptosis Bax, Bcl2, IL-11, interleucina-6 (IL-6), ALT, AST, superóxido dismutasa (SOD) y glutatión peroxidasa ( GPx), los que se encontraron significativamente protegidos por el resveratrol y quercetina. Además se determinó una correlación significativa (p <0.01) entre la puntuación de IL-11 y los niveles de p53, Bax, Bcl-2 y MDA. En conclusión, el resveratrol más la quercetina protegen de manera efectiva contra la apoptosis inducida por acetaminofén, asociada con la inhibición del estrés oxidativo y la IL-11.


Assuntos
Animais , Ratos , Quercetina/administração & dosagem , Apoptose/efeitos dos fármacos , Doença Hepática Crônica Induzida por Substâncias e Drogas/patologia , Resveratrol/administração & dosagem , Acetaminofen/toxicidade , Antioxidantes/administração & dosagem , Quercetina/farmacologia , Aspartato Aminotransferases/análise , Biomarcadores , Interleucina-1 , Estresse Oxidativo , Alanina Transaminase/análise , Modelos Animais de Doenças , Doença Hepática Induzida por Substâncias e Drogas/enzimologia , Resveratrol/farmacologia , Antioxidantes/farmacologia
20.
Acta cir. bras ; 35(6): e202000602, 2020. tab, graf
Artigo em Inglês | LILACS | ID: biblio-1130655

RESUMO

Abstract Purpose To examine the effects of quercetin on healing of experimental colon anastomosis injury in early and late period. Methods Eighty male Wistar-Albino rats were divided into 8 groups. For all groups, left colons of the rats were resected and for the rest end-to-end anastomosis was performed. Two of the groups for which the experiment protocol was ended on the 3rd and 7th day following the anastomosis were not administered with either quercetin or dimethylsulfoxide DMSO, whereas two other groups were administered with DMSO only, and four other groups were administered with quercetin dissolved in DMSO in doses of 20 and 100 mg/kg during the protocol. At the end of the study, anastomosis line was resected, histopathological evaluation was performed and bursting pressure, malondialdehyde, superoxide dismutase, catalase, and hydroxyproline levels were measured. Results Quercetin significantly increased hydroxyproline, superoxide dismutase, catalase levels, histopathological healing score, bursting pressure values and decreased malondialdehyde level in early period. It also significantly increased superoxide dismutase, catalase, and hydroxyproline levels and decreased malondialdehyde level in late period. Conclusion It was seen that quercetin speeds up the injury healing process and reveals an antioxidant effect, specifically in early period.


Assuntos
Animais , Masculino , Ratos , Colo , Quercetina , Anastomose Cirúrgica , Dimetil Sulfóxido , Ratos Wistar , Hidroxiprolina
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