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1.
Biomed Pharmacother ; 158: 114175, 2023 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-36587556

RESUMO

Gout is a metabolic disease affected by monosodium urate (MSU) deposition, which is directly related to hyperuricemia. Recent reports on the prevalence and incidence of gout have been widely circulated worldwide. Currently, the anti-gout drugs in clinical practice are mainly small-molecule synthetic drugs, and the effectiveness and safety are limited. Reducing uric acid and inhibiting inflammation are the focused areas of drug research and development on gout. Rutin, a natural flavonoid, has been reported to alleviate inflammation in various diseases. However, whether rutin exerts protective effects on gout remains to be elucidated. This study used quails without urate oxidase as experimental animals to induce endogenous gout models through a high purine diet. We confirmed that quail in the model group developed gout symptoms at 30 days of the experiment. And the targets of uric acid metabolism, oxidative stress level, and NLRP3 inflammasome were dysregulated in quails. Rutin treatment improves gout and reduces inflammatory expression in quail. We further confirmed that rutin treatment reduced XOD activity and uric acid levels in quail. And rutin inhibited ROS production, restored oxidative stress balance, inhibited NLRP3 inflammasome activation, and exerted anti-inflammatory effects. We extracted and identified the fibroblast-like synoviocytes (FLS) for the first time. The results showed that rutin could reduce ROS production and NLRP3 inflammasome activation of FLS after uric acid stimulation. In conclusion, our findings underscore that rutin may be a gout protective agent by reducing XOD activity, inhibiting ROS production and NLRP3 inflammasome activation. Meanwhile, this study also provides an available animal model for the research drugs of gout.


Assuntos
Gota , Inflamassomos , Espécies Reativas de Oxigênio , Rutina , Animais , Gota/tratamento farmacológico , Gota/metabolismo , Inflamassomos/metabolismo , Inflamação/tratamento farmacológico , Proteína 3 que Contém Domínio de Pirina da Família NLR/metabolismo , Espécies Reativas de Oxigênio/metabolismo , Rutina/farmacologia , Ácido Úrico/farmacologia , Codorniz
2.
Molecules ; 28(2)2023 Jan 16.
Artigo em Inglês | MEDLINE | ID: mdl-36677937

RESUMO

The rising prevalence of non-alcoholic fatty liver disease NAFLD has strained the healthcare system. Natural products could solve this problem, so the current study focused on the impact of G. thunbergia Thunb. against this ailment. LC-ESI-MS/MS revealed the phytochemical profile of the methanol extract from Gardenia thunbergia leaves (GME). Forty-eight compounds were tentatively identified, and stigmasterol, fucosterol, ursolic acid, and rutin were isolated. The separation of the last three compounds from this plant had not before been achieved. The anti-NAFLD effect of the methanol extract of the leaves of G. thunbergia, and its major metabolite, rutin, was assessed in mice against high-fructose diet (HFD)-induced obesity. Male mice were allocated into nine groups: (1) saline (control), (2) 30% fructose (diseased group), (3) HFD, and 10 mg/kg of simvastatin. Groups 4-6 were administered HFD and rutin 50, 75, and 100 mg/kg. Groups (7-9) were administered HFD and methanol extract of leaves 100, 200, and 300 mg/kg. Methanol extract of G. thunbergia leaves at 200 mg/kg, and rutin at 75 mg/kg significantly reduced HFD-induced increments in mice weight and hepatic damage indicators (AST and ALT), steatosis, and hypertrophy. The levels of total cholesterol, LDL-C, and triglycerides in the blood decreased. In addition, the expressions of CYP2E1, JNK1, and iNOS in the diseased mice were downregulated. This study found that GME and rutin could ameliorate NAFLD in HFD-fed mice, with results comparable to simvastatin, validating G. thunbergia's hepatoprotective effects.


Assuntos
Gardenia , Hepatopatia Gordurosa não Alcoólica , Extratos Vegetais , Animais , Camundongos , Dieta Hiperlipídica/efeitos adversos , Gardenia/química , Fígado , Metanol , Camundongos Endogâmicos C57BL , Hepatopatia Gordurosa não Alcoólica/tratamento farmacológico , Hepatopatia Gordurosa não Alcoólica/etiologia , Rutina/farmacologia , Espectrometria de Massas em Tandem , Extratos Vegetais/farmacologia
3.
J Environ Sci (China) ; 127: 158-168, 2023 May.
Artigo em Inglês | MEDLINE | ID: mdl-36522050

RESUMO

The wastewater discharge from the process of chrome plating, which contains 6:2 chlorinated polyfluorinated ether sulfonate (F-53B) and chromium (Cr), may be toxic to biofilm. In this study we found that the biofilm formed by Pseudomonas aeruginosa PAO1 was inhibited by exposure to a combination of F-53B and Cr(VI). The combined pollution damaged the cell membranes and the structure of the biofilm, and inhibited the production of the Pseudomonas quinolone-based signal, which affected biofilm formation. Moreover, the secretion of extracellular polymeric substances decreased as a result of this combined exposure. Exposure to F-53B and Cr(VI) individually or in combination could induce the excessive accumulation of intracellular reactive oxygen species (ROS), and the ROS positive rate of the bacteria increased under the treatment with 0.2 mmol/L of Cr(VI) and 250 nmol/L of F-53B, respectively. In addition, the activities of superoxide dismutase (SOD) and catalase (CAT) were enhanced for scavenging ROS in the bacteria that were exposed to Cr(VI) and F-53B. As an antioxidant, rutin was used to repair the toxicity of Cr(VI) and F-53B towards the biofilm formed by the bacteria. When rutin was added to the bacteria medium, with either Cr(VI) or F-53B as pollutant, or with the combined pollutants, the extracellular protein content of the bacteria recovered to 0.84, 0.94, and 0.85 times that of the control, respectively. Meanwhile, the accumulation of ROS and the activities of SOD and CAT decreased, which indicated that the addition of rutin can alleviate the oxidative stress and promote the antioxidant stress system.


Assuntos
Ácidos Alcanossulfônicos , Fluorcarbonetos , Poluentes Químicos da Água , Animais , Ácidos Alcanossulfônicos/toxicidade , Fluorcarbonetos/química , Pseudomonas aeruginosa , Peixe-Zebra/metabolismo , Rutina/farmacologia , Rutina/metabolismo , Antioxidantes/metabolismo , Espécies Reativas de Oxigênio/metabolismo , Poluentes Químicos da Água/análise , Cromo/toxicidade , Cromo/metabolismo , Superóxido Dismutase/metabolismo , Biofilmes
4.
Pestic Biochem Physiol ; 189: 105294, 2023 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-36549820

RESUMO

Thiram is a fungicide that is used to prevent fungal diseases in seeds and crops and also as an animal repellent. The pro-oxidant activity of thiram is well established. Rutin is a flavonoid glycoside present in many fruits and plants and has several beneficial properties, including antioxidant effects. We have previously shown that thiram causes oxidative damage in human erythrocytes. The present study was designed to evaluate the protective effect of rutin against thiram-induced damage in human erythrocytes. Treatment of erythrocytes with 0.5 mM thiram for 4 h increased the level of oxidative stress markers, decreased antioxidant power and lowered the activity of antioxidant and membrane bound enzymes. It also enhanced the generation of reactive oxygen and nitrogen species (ROS and RNS) and altered the morphology of erythrocytes. However, prior treatment of erythrocytes with rutin (0.5, 1 and 2 mM) for 2 h, followed by 4 h incubation with 0.5 mM thiram, led to a decrease in the level of oxidative stress markers in a rutin concentration-dependent manner. A significant restoration in the antioxidant power and activity of antioxidant enzymes was observed upon the treatment of erythrocytes with 1 and 2 mM rutin. Pre-incubation with rutin lowered the generation of ROS and RNS which will reduce oxidative damage in erythrocytes. The thiram-induced changes in cell morphology and activity of membrane-bound enzymes were also attenuated by rutin. These results suggest that rutin can be used to mitigate thiram-induced oxidative damage in human erythrocytes.


Assuntos
Antioxidantes , Rutina , Animais , Humanos , Antioxidantes/farmacologia , Antioxidantes/metabolismo , Espécies Reativas de Oxigênio/metabolismo , Rutina/farmacologia , Rutina/metabolismo , Tiram , Glutationa/metabolismo , Estresse Oxidativo , Eritrócitos
5.
Int J Mol Sci ; 23(23)2022 Nov 26.
Artigo em Inglês | MEDLINE | ID: mdl-36499113

RESUMO

Quercetin and its glycosides, such as isoquercitrin or rutin, are among the most ubiquitous flavonoids present in plants. They possess numerous health-promoting properties, whose applicability is, however, limited by poor water solubility and absorption issues. Enzymatically modified isoquercitrin (EMIQ) is an isoquercitrin derivative obtained from rutin via enzymatic transformations that greatly enhance its bioavailability. Due to advantageous reports on its safety and bioactivity, EMIQ is currently gaining importance as a food additive and a constituent of dietary supplements. This review summarizes the thus-far-conducted investigations into the metabolism, toxicity, biological properties, and molecular mechanisms of EMIQ and presents a comprehensive characterization of this valuable substance, which might represent the future of flavonoid supplementation.


Assuntos
Quercetina , Rutina , Quercetina/farmacologia , Disponibilidade Biológica , Rutina/farmacologia , Glicosídeos , Solubilidade
6.
J Microencapsul ; 39(7-8): 668-679, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-36476253

RESUMO

Solid lipid nanoparticles (SLNs) containing rutin were prepared to enhance their photochemopreventive effect on the skin. SLNs were produced by the hot melt microemulsion technique. Two 3D skin models: ex vivo skin explants and 3D tissue engineering skin were used to evaluate the photochemopreventive effect of topical formulations containing rutin SLNs, against ultraviolet B (UVB) radiation, inducing sunburn cells, caspase-3, cyclobutane pyrimidine dimers, lipid peroxidation, and metalloproteinase formation. The rutin SLNs presented average size of 74.22 ± 2.77 nm, polydispersion index of 0.16 ± 0.04, encapsulation efficiency of 98.90 ± 0.25%, and zeta potential of -53.0 ± 1.61 mV. The rutin SLNs were able to efficiently protect against UVB induced in the analysed parameters in both skin models. Furthermore, the rutin SLNs inhibited lipid peroxidation and metalloproteinase formation. These results support the use of rutin SLNs as skin photochemopreventive agents for topical application to the skin.


Assuntos
Nanopartículas , Rutina , Rutina/farmacologia , Pele , Lipossomos , Raios Ultravioleta/efeitos adversos
7.
Molecules ; 27(21)2022 Oct 27.
Artigo em Inglês | MEDLINE | ID: mdl-36364141

RESUMO

Mental disorders have a poor clinical prognosis and account for approximately 8% of the global burden of disease. Some examples of mental disorders are anxiety and depression. Conventional antidepressants have limited efficacy in patients because their pharmacological effects wear off, and side effects increase with prolonged use. It is claimed that herbal medicine's antioxidant capacity helps regulate people's mood and provide a more substantial pharmacological effect. With this background, the purpose of this study is to investigate the effect of rutin on reserpine-induced anxiety and depression in rats. The animals were divided into groups of six rats each: normal control (water), a depression model, a rutin-treated rat model, and an amitriptyline-treated rat model. According to the results, 14 days of treatment with rutin, once daily, showed a modest antidepressant effect. This effect was mediated by increased serotonin, norepinephrine, and dopamine levels in cortical and hippocampal regions. The antioxidant and vasodilator properties of rutin may contribute to its antidepressant properties. According to this study, rutin has shown antidepressant effects by reducing antioxidant activity and acetylcholinesterase.


Assuntos
Depressão , Reserpina , Animais , Ratos , Depressão/induzido quimicamente , Depressão/tratamento farmacológico , Rutina/farmacologia , Serotonina , Acetilcolinesterase , Antioxidantes/farmacologia , Antidepressivos/farmacologia , Antidepressivos/uso terapêutico , Ansiedade/induzido quimicamente , Ansiedade/tratamento farmacológico
8.
Nutrients ; 14(19)2022 Sep 21.
Artigo em Inglês | MEDLINE | ID: mdl-36235552

RESUMO

The presented research evaluates the medical use potential of Lonicera caerulea leaves, which are waste plants in cultivating berries. The study's screening activity included the leaves of five varieties of Lonicera caerulea: Atut, Duet, Wojtek, Zojka, and Jugana. The microbiological analysis confirmed the safety of using Lonicera caerulea leaves without significant stabilization. Lonicera caerulea leaves standardization was carried out based on the results of the chromatographic analysis, and it showed differences in the contents of active compounds (loganic, chlorogenic and caffeic acids, and rutin), which are attributed to biological activity. For the Lonicera caerulea leaves varieties tested, the differences in the content of total polyphenol content, chlorophylls, and carotenoids were also confirmed. The screening of biological activity of five Lonicera caerulea leaf varieties was carried out concerning the possibility of inhibiting the activity of α-glucosidase, lipase, and hyaluronidase as well, and the antioxidant potential was determined. The defined profile of the biological activity of Lonicera caerulea leaves makes it possible to indicate this raw material as an essential material supporting the prevention and treatment of type II diabetes. However, this research showed that tested enzymes were strongly inhibited by the variety Jugana. The health-promoting potential of Lonicera caerulea leaves was correlated with the highest chlorogenic acid and rutin content in the variety Jugana.


Assuntos
Diabetes Mellitus Tipo 2 , Lonicera , Antioxidantes/análise , Antioxidantes/farmacologia , Ácidos Cafeicos/análise , Carotenoides/análise , Carotenoides/farmacologia , Ácido Clorogênico/análise , Ácido Clorogênico/farmacologia , Frutas/química , Hialuronoglucosaminidase/análise , Lipase , Lonicera/química , Folhas de Planta/química , Polifenóis/análise , Polifenóis/farmacologia , Rutina/análise , Rutina/farmacologia , alfa-Glucosidases
9.
Arch Razi Inst ; 77(2): 835-841, 2022 04.
Artigo em Inglês | MEDLINE | ID: mdl-36284937

RESUMO

Rutin is a citrus flavonoid that exists in different types of food, such as fruits, tea, as well as vegetables, and is considered a natural antioxidant. This study aimed to investigate the therapeutic role of Rutin in oxidative stress-induced in Wistar rats exposed to Ciprofloxacin (CPX). The study included 36 healthy adult Wistar rats, which were randomly divided into six groups (n=6). The control group (C) received normal drinking water for 20 days. The first treatment group (T1) received Rutin at a dose of 50 mg/kg of b.w for 20 days. The second treatment group (T2) received CPX antibiotic at a dose of 14 mg/kg of b.w for 20 days. The third treatment group (T3) received Rutin at a dose of 50 mg/kg of b.w for 20 days, and afterward, they received CPX antibiotic at a dose of 14 mg/kg of b.w for 20 days. The fourth treatment group (T4) received CPX antibiotic at a dose of 14 mg/kg of b.w for 20 days, and then, they received Rutin at a dose of 50 mg/kg of b.w for 20 days. The fifth treatment group (T5) received CPX antibiotic at a dose of 14 mg/ kg of b.w and Rutin at a dose of 50 mg/ kg of b.w together for 20 days. All the treatments were administrated by oral gavage. Analysis of the recorded data showed a significant increase (P<0.05) in the concentration of Methylenedioxyamphetamine (MDA) in the T2 group, compared to the other groups. The MDA level significantly (P<0.05) increased in the T3 group (2.29±0.04), compared to the C (1.71±0.01), T1 (1.54±0.04), T4 (1.18±0.02), and T5 (1.29±0.03) groups. However, there were no significant differences (P<0.05) between the C (1.71±0.01) and T1 (1.54±0.04) groups, as well as the T4 (1.18±0.02) and T5 (1.29±0.03) groups with regards to the MDA. The results clarified a significant increase (P<0.05) in the antioxidant activity, Glutathione (GSH), Superoxide dismutase (SOD), and Catalase (CAT) contents in the T1 group, determined at 5.91±0.26, 5.78±0.02, and 1.98±0.05, respectively, compared to the other groups. The lowest antioxidant activity, GSH, SOD, and CAT contents were recorded in the T2 group, in comparison with the other groups (P<0.05). The findings revealed that the level of SOD, GSH, and CAT in the T4 and T5 groups significantly (P<0.05) increased, compared to the T2 and T3 groups. Histological examination of the slides obtained from the brain demonstrated that in the T2 group, some histopathological changes were observed, compared to the C, T1, T4, and T5 groups. These changes were as follows: 1) damaged and clear blood vessel congestion with the deposition of fibrous networks, 2) brain edema, 3) multiple necrotic foci, 4) accumulation of neutrophils, and 5) simple histopathological changes in the brain of animals in the T2 group, compared to the other groups. It is, therefore, concluded that Rutin supplementation at a dose of 50 mg/kg b.w can be the most appropriate dose in protecting brain tissue against tissue damages caused by CPX.


Assuntos
Água Potável , Rutina , Animais , Ratos , Antibacterianos , Antioxidantes , Catalase , Ciprofloxacina/análise , Água Potável/análise , Flavonoides/análise , Flavonoides/farmacologia , Glutationa/análise , Ratos Wistar , Rutina/farmacologia , Rutina/análise , Superóxido Dismutase , Chá
10.
Int J Mol Sci ; 23(19)2022 Oct 04.
Artigo em Inglês | MEDLINE | ID: mdl-36233071

RESUMO

Rutin, also called quercetin-3-rhamnosyl glucoside, is a natural flavonol glycoside present in many plants. Rutin is used to treat various diseases, such as inflammation, diabetes, and cancer. For polymeric biomaterials, triethylene glycol dimethacrylate (TEGDMA) is the most commonly used monomer and serves as a restorative resin, a dentin bonding agent and sealant, and a bone cement component. Overall, TEGDMA induces various toxic effects in macrophages, including cytotoxicity, apoptosis, and genotoxicity. The aim of this study was to investigate the protective mechanism of rutin in alleviating TEGDMA-induced toxicity in RAW264.7 macrophages. After treatment with rutin, we assessed the cell viability and apoptosis of TEGDMA-induced RAW264.7 macrophages using an methylthiazol tetrazolium (MTT) assay and Annexin V-FITC/propidium iodide assay, respectively. Subsequently, we assessed the level of genotoxicity using comet and micronucleus assays, assessed the cysteinyla aspartate specific proteinases (caspases) and antioxidant enzyme (AOE) activity using commercial kits, and evaluated the generation of reactive oxygen species (ROS) using a dichlorodihydrofluorescein diacetate (DCFH-DA) assay. We evaluated the expression of heme oxygenase (HO)-1, the expression of nuclear factor erythroid 2 related factor (Nrf-2), and phosphorylation of AMP activated protein kinase (AMPK) using the Western blot assay. The results indicated that rutin substantially reduced the level of cytotoxicity, apoptosis, and genotoxicity of TEGDMA-induced RAW264.7 macrophages. Rutin also blocked the activity of caspase-3, caspase-8, and caspase-9 in TEGDMA-stimulated RAW264.7 macrophages. In addition, it decreased TEGDMA-induced ROS generation and AOE deactivation in macrophages. Finally, we found that TEGDMA-inhibited slightly the HO-1 expression, Nrf-2 expression, and AMPK phosphorylation would be revered by rutin. In addition, the HO-1 expression, Nrf-2 expression, and AMPK phosphorylation was enhanced by rutin. These findings indicate that rutin suppresses TEGDMA-induced caspase-mediated toxic effects through ROS generation and antioxidative system deactivation through the Nrf-2/AMPK pathway. Therefore, rutin has the potential to serve as a novel antitoxicity agent for TEGDMA in RAW264.7 macrophages.


Assuntos
Proteínas Quinases Ativadas por AMP , Rutina , Proteínas Quinases Ativadas por AMP/metabolismo , Antioxidantes/farmacologia , Apoptose , Ácido Aspártico , Materiais Biocompatíveis/farmacologia , Cimentos Ósseos/farmacologia , Caspase 3/metabolismo , Caspase 8/metabolismo , Caspase 9/metabolismo , Caspases/metabolismo , Adesivos Dentinários , Glucosídeos/farmacologia , Glicosídeos/farmacologia , Macrófagos/metabolismo , Polietilenoglicóis , Ácidos Polimetacrílicos , Propídio , Quercetina/farmacologia , Espécies Reativas de Oxigênio/metabolismo , Rutina/farmacologia
11.
Molecules ; 27(19)2022 Sep 27.
Artigo em Inglês | MEDLINE | ID: mdl-36234917

RESUMO

Flavonols are found in plants as aglycones and as glycosides. Antioxidant activity of flavonols may occur via several mechanisms within the cell, and mitochondria as a target may play an important role. There is a lack of information about the influence of the sugar moiety on biological activity of flavonoid glycosides. The aims of study were to investigate the effects of quercetin and its glycosides on mitochondrial respiration rates at various metabolic states, and to evaluate their antioxidant potential using chemical and biological approaches. Mitochondrial function was measured using an oxygraphic method, cytochrome c reduction spectrophotometrically, H2O2 generation in mitochondria fluorimetrically, and antioxidant activity of flavonoids using an HPLC-post column system. Our data revealed that quercetin and its glycosides isoquercitrin, rutin, and hyperoside uncouple kidney mitochondrial respiration (increasing the State 2 respiration rate) and significantly reduce cytochrome c. Moreover, quercetin, and its glycosides decrease the production of mitochondrial H2O2 and possess radical scavenging and ferric reducing capacities. The highest activity was characteristic for quercetin, showing that the sugar moiety significantly diminishes its activity. In conclusion, our results show the efficient radical scavenging, ferric and cytochrome c reducing capacities, and uncoupling properties of quercetin and its glycosides, as well as the importance of the sugar residue and its structure in the regulation of kidney mitochondrial function.


Assuntos
Antioxidantes , Quercetina , Antioxidantes/química , Citocromos c/metabolismo , Flavonoides/química , Flavonóis/química , Glicosídeos/química , Peróxido de Hidrogênio/metabolismo , Rim/metabolismo , Mitocôndrias/metabolismo , Quercetina/química , Rutina/metabolismo , Rutina/farmacologia , Açúcares/metabolismo
12.
Eur J Pharmacol ; 933: 175289, 2022 Oct 15.
Artigo em Inglês | MEDLINE | ID: mdl-36122758

RESUMO

Diabetic nephropathy (DN) is a renal complication of diabetic hyperglycemia. The Signal transducer and activator of transcription 3 (Stat3) is a center molecule of the chronic inflammation causing DN progression. Therefore, the study investigated the possible inhibitory effects of Rutin (Ru) and Selenium (Se), formulated as nanoparticles (SeNPs), on Stat3 pathway in streptozotocin (STZ)-induced DN in Sprague-Dawley rats. Ru (100 mg/kg/orally) and SeNPs (equivalent to 5 mg of Se/kg/orally) were given as treatment for eight weeks. An assessment of fasting blood glucose, renal function biomarkers, GSH, and MDA was carried out spectrophotometrically. ELISA assessment of renal IL-6, NF-κB, TNF-α, Jak-2, and p-Stat3 was performed. Sirt-1, Nrf-2, and HO-1 were assessed immunohistochemically. DN group receiving Ru + SeNPs showed a decrease in fasting blood glucose, serum creatinine, and urea (163.8 ± 22.8, 0.54 ± 0.1, and 53.6 ± 25.7 mg/dl, respectively), compared to the DN group (443.8 ± 42.72, 1.58 ± 0.4, and 281.8 ± 47.35 mg/dl, respectively). In addition, it exhibited elevation in the levels of Sirt-1, Nrf-2 and HO-1 compared to the DN group. Finally, Ru + SeNPs exhibited a significant reduction in IL-6, NF-κB, TNF-α, Jak-2, and p-Stat3 (42.8 ± 10.3, 1.2 ± 0.1, 53.4 ± 3.87, 0.8 ± 0.06 and 1.1 ± 0.2 U/g tissue, respectively) when compared to the DN group (155.3 ± 13.97, 2.8 ± 0.3, 105.5 ± 32.84, 2.03 ± 0.2 and 2.56 ± 0.15 U/g tissue, respectively). Therefore, combining Ru with SeNPs has a potential renoprotective effect against DN by upregulating Nrf-2/HO-1 and downregulating Jak-2/Stat3 Pathways.


Assuntos
Diabetes Mellitus Experimental , Nefropatias Diabéticas , Nanopartículas , Selênio , Sirtuínas , Animais , Biomarcadores , Glicemia/análise , Creatinina , Diabetes Mellitus Experimental/induzido quimicamente , Diabetes Mellitus Experimental/complicações , Diabetes Mellitus Experimental/tratamento farmacológico , Nefropatias Diabéticas/complicações , Nefropatias Diabéticas/tratamento farmacológico , Nefropatias Diabéticas/prevenção & controle , Interleucina-6/metabolismo , NF-kappa B/metabolismo , Ratos , Ratos Sprague-Dawley , Rutina/farmacologia , Rutina/uso terapêutico , Fator de Transcrição STAT3/metabolismo , Selênio/farmacologia , Selênio/uso terapêutico , Transdução de Sinais , Sirtuínas/metabolismo , Estreptozocina/efeitos adversos , Fator de Necrose Tumoral alfa/metabolismo
13.
Molecules ; 27(18)2022 Sep 07.
Artigo em Inglês | MEDLINE | ID: mdl-36144513

RESUMO

Bee products are known for their beneficial properties widely used in complementary medicine. This study aims to unveil the physicochemical, nutritional value, and phenolic profile of bee pollen and honey collected from Boulemane-Morocco, and to evaluate their antioxidant and antihyperglycemic activity. The results indicate that Citrus aurantium pollen grains were the majority pollen in both samples. Bee pollen was richer in proteins than honey while the inverse was observed for carbohydrate content. Potassium and calcium were the predominant minerals in the studied samples. Seven similar phenolic compounds were found in honey and bee pollen. Three phenolic compounds were identified only in honey (catechin, caffeic acid, vanillic acid) and six phenolic compounds were identified only in bee pollen (hesperidin, cinnamic acid, apigenin, rutin, chlorogenic acid, kaempferol). Naringin is the predominant phenolic in honey while hesperidin is predominant in bee pollen. The results of bioactivities revealed that bee pollen exhibited stronger antioxidant activity and effective α-amylase and α-glycosidase inhibitory action. These bee products show interesting nutritional and bioactive capabilities due to their chemical constituents. These features may allow these bee products to be used in food formulation, as functional and bioactive ingredients, as well as the potential for the nutraceutical sector.


Assuntos
Catequina , Hesperidina , Mel , Animais , Antioxidantes/química , Apigenina/análise , Abelhas , Cálcio/análise , Catequina/análise , Ácido Clorogênico/análise , Glicosídeo Hidrolases/análise , Hesperidina/análise , Mel/análise , Hipoglicemiantes/análise , Quempferóis/análise , Minerais/análise , Marrocos , Fenóis/química , Pólen/química , Potássio/análise , Rutina/análise , Rutina/farmacologia , Ácido Vanílico , alfa-Amilases
14.
Molecules ; 27(18)2022 Sep 08.
Artigo em Inglês | MEDLINE | ID: mdl-36144568

RESUMO

Phytocosmetic is an important aspect of traditional medicine in several cultures. Researchers are now focusing to find new and effective ingredients of natural origin. Propolis is a natural beehive product extensively used in traditional medicine. We aimed in the present study to investigate the potential use of propolis as an aesthetic and phytotherapeutic constituent in phytocosmetics. Propolis was extracted using 80% ethanol. Total phenolic and flavonoid contents were determined calorimetrically. Free radical scavenging ability and reducing capacity were evaluated using four assays and expressed as IC50 values. Antibacterial activity was evaluated by the determination of minimum inhibitory concentration (MIC) on 11 Gram-positive and Gram-negative bacteria. The wound healing activity of 30% ethanolic extract and propolis ointment was studied using excision wounds in the anterio-dorsal side of the rats. The phenolic acid composition of the tested propolis was investigated using UFLC/MS-MS analysis. The tested propolis was rich in phenolic and flavonoid content and demonstrated an interesting antibacterial and antioxidant activity. Wounds treated with propolis appear to display a lesser degree of inflammation. Chemical analysis led to the identification of 11 phenolics. Among them, five are considered as main compounds: Chlorogenic acid (48.79 ± 5.01 ng/mL), Gallic acid (44.25 ± 6.40 ng/mL), Rutin (21.12 ± 3.57 ng/mL), Caffeic acid (28.19 ± 4.95 ng/mL), and trans-cinnamic acid (20.10 ± 6.51 ng/mL). Our results indicated that propolis can not only be used as a cosmetic ingredient but also be used as a preventative and curative constituent, which might be used as a barrier when applied externally on infected and non-infected skin.


Assuntos
Própole , Animais , Antibacterianos/farmacologia , Antibacterianos/uso terapêutico , Antioxidantes/química , Ácido Clorogênico/farmacologia , Etanol/farmacologia , Flavonoides/análise , Flavonoides/farmacologia , Radicais Livres/farmacologia , Ácido Gálico/farmacologia , Bactérias Gram-Negativas , Bactérias Gram-Positivas , Pomadas/farmacologia , Fenóis/química , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Própole/química , Ratos , Rutina/farmacologia
15.
Molecules ; 27(18)2022 Sep 12.
Artigo em Inglês | MEDLINE | ID: mdl-36144661

RESUMO

This present study aimed to delineate Rumex hastatus D. Don crude extract (Rh.Cr), n-Hexane, ethyl acetate, aqueous fractions (Rh.n-Hex, Rh.ETAC, Rh.Aq) and rutin for antidiarrheal, antisecretory effects, anti-spasmodic, gastrointestinal transient time, anti H. pylori, antiulcer effects, and toxicology. The preliminary phytochemical analysis of Rumex hastatus showed different phytoconstituents and shows different peaks in GC-MC chromatogram. Rumex hastatus crude extract (Rh.Cr), fractions, and rutin attributed dose-dependent (50-300 mg/kg) protection (0-100%) against castor oil-induced diarrhea and dose-dependently inhibited intestinal fluid secretions in mice. They decreased the distance traversed by charcoal in the gastrointestinal transit model in rats. In rabbit jejunum preparations, Rh.Cr and Rh.ETAC caused a concentration-dependent relaxation of both spontaneous and K+ (80 mM)-induced contractions at a similar concentration range, whereas Rh.n-Hex, rutin, and verapamil were relatively potent against K+-induced contractions and shifted the Ca2+ concentration-response curves (CRCs) to the right, Rh.Cr (0.3-1 mg/mL) and Rh.ETAC (0.1-0.3 mg/mL) shifted the isoprenaline-induced inhibitory CRCs to the left. Rh.n-Hex, Rh.ETAC and rutin showed anti-H. pylori effect, also shows an inhibitory effect against H+/K+-ATPase. Rumex hastatus showed gastroprotective and antioxidant effects. Histopathological evaluation showed improvement in cellular architecture and a decrease in the expression of inflammatory markers such as, cyclooxygenase (COX-2), tumor necrosis factor (TN,F-α) and phosphorylated nuclear factor kappa B (p-NFƙB), validated through immunohistochemistry and ELISA techniques. In RT-PCR it decreases H+/K+-ATPase mRNA levels. Rumex hastatus was found to be safe to consume up to a dose of 2000 mg/kg in a comprehensive toxicity profile. Docking studies revealed that rutin against H+/K+-ATPase pump and voltage-gated L-type calcium channel showed E-values of -8.7 and -9.4 Kcal/mol, respectively. MD simulations Molecular Mechanics Poisson Boltzmann surface area and molecular mechanics Generalized Born surface area (MMPBSA/GBSA) findings are consistent with the in-vitro, in-vivo and docking results.


Assuntos
Gastroenteropatias , Rumex , Adenosina Trifosfatases , Animais , Antidiarreicos/química , Antioxidantes/farmacologia , Canais de Cálcio Tipo L , Hidróxido de Cálcio , Óleo de Rícino , Carvão Vegetal/farmacologia , Ciclo-Oxigenase 2 , Gastroenteropatias/tratamento farmacológico , Isoproterenol/farmacologia , Jejuno , Camundongos , NF-kappa B/farmacologia , Parassimpatolíticos/farmacologia , Compostos Fitoquímicos/farmacologia , Extratos Vegetais/química , Extratos Vegetais/farmacologia , RNA Mensageiro , Coelhos , Ratos , Rumex/química , Rutina/farmacologia , Fatores de Necrose Tumoral , Verapamil/farmacologia , Óxido de Zinco
16.
Food Funct ; 13(20): 10401-10414, 2022 Oct 17.
Artigo em Inglês | MEDLINE | ID: mdl-36148811

RESUMO

Rutin, a naturally derived flavonoid molecule with known neuroprotective properties, has been demonstrated to have anticonvulsive potential, but the mechanism of this effect is still unclear. The current study aimed to investigate the probable antiseizure mechanisms of rutin in rats using the kainic acid (KA) seizure model. Rutin (50 and 100 mg kg-1) and carbamazepine (100 mg kg-1) were administered daily by oral gavage for 7 days before KA (15 mg kg-1) intraperitoneal (i.p.) injection. Seizure behavior, neuronal cell death, glutamate concentration, excitatory amino acid transporters (EAATs), glutamine synthetase (GS), glutaminase, α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor subunits GluA1 and GluA2, N-methyl-D-aspartate (NMDA) receptor subunits GluN2A and GluN2B, activated astrocytes, and inflammatory and anti-inflammatory molecules in the hippocampus were evaluated. Supplementation with rutin attenuated seizure severity in KA-treated rats and reversed KA-induced neuronal loss and glutamate elevation in the hippocampus. Decreased glutaminase and GluN2B, and increased EAATs, GS, GluA1, GluA2 and GluN2A were observed with rutin administration. Rutin pretreatment also suppressed activated astrocytes, downregulated the protein levels of inflammatory molecules [interleukin-1ß (IL-1ß), interleukin-6 (IL-6), tumor necrosis factor-α (TNF-α), high mobility group Box 1 (HMGB1), interleukin-1 receptor 1 (IL-1R1), and Toll-like receptor-4 (TLR-4)] and upregulated anti-inflammatory molecule interleukin-10 (IL-10) protein expression. Taken together, the results indicate that the preventive treatment of rats with rutin attenuated KA-induced seizures and neuronal loss by decreasing glutamatergic hyperactivity and suppressing the IL-1R1/TLR4-related neuroinflammatory cascade.


Assuntos
Proteína HMGB1 , Ácido Caínico , Sistemas de Transporte de Aminoácidos , Animais , Anti-Inflamatórios/farmacologia , Carbamazepina , Glutamato-Amônia Ligase/metabolismo , Glutamato-Amônia Ligase/farmacologia , Ácido Glutâmico/metabolismo , Glutaminase/genética , Glutaminase/metabolismo , Glutaminase/farmacologia , Proteína HMGB1/genética , Proteína HMGB1/metabolismo , Hipocampo/metabolismo , Inflamação/induzido quimicamente , Inflamação/tratamento farmacológico , Inflamação/metabolismo , Interleucina-10/metabolismo , Interleucina-1beta/genética , Interleucina-1beta/metabolismo , Interleucina-6/metabolismo , Ácido Caínico/efeitos adversos , N-Metilaspartato/efeitos adversos , N-Metilaspartato/metabolismo , Ratos , Receptores de Interleucina-1/metabolismo , Receptores de Interleucina-1/uso terapêutico , Rutina/metabolismo , Rutina/farmacologia , Convulsões/induzido quimicamente , Convulsões/tratamento farmacológico , Convulsões/metabolismo , Receptor 4 Toll-Like/genética , Receptor 4 Toll-Like/metabolismo , Fator de Necrose Tumoral alfa/metabolismo , Ácido alfa-Amino-3-hidroxi-5-metil-4-isoxazol Propiônico/efeitos adversos , Ácido alfa-Amino-3-hidroxi-5-metil-4-isoxazol Propiônico/metabolismo
17.
Int J Mol Sci ; 23(18)2022 Sep 16.
Artigo em Inglês | MEDLINE | ID: mdl-36142712

RESUMO

Chemical investigation of the crude extract of the aerial part of Zygophyllum album L. (Z. album) led to the isolation of a new saponin, Zygo-albuside A (7), together with seven known compounds, one of them (caffeic acid, compound 4) is reported in the genus for the first time. NMR (1D and 2D) and mass spectrometric analysis, including high-resolution mass spectrometry (HRMS), were utilized to set up the chemical structures of these compounds. The present biological study aimed to investigate the protective antioxidant, anti-inflammatory, and antiapoptotic activities of the crude extract from the aerial part of Z. album and two of its isolated compounds, rutin and the new saponin zygo-albuside A, against methotrexate (MTX)-induced testicular injury, considering the role of miRNA-29a. In all groups except for the normal control group, which received a mixture of distilled water and DMSO (2:1) as vehicle orally every day for ten days, testicular damage was induced on the fifth day by intraperitoneal administration of MTX at a single dose of 20 mg/kg. Histopathological examination showed that pre-treatment with the crude extract of Z. album, zygo-albuside A, or rutin reversed the testicular damage induced by MTX. In addition, biochemical analysis in the protected groups showed a decrease in malondialdehyde (MDA), interleukin-6 (IL-6) and IL-1ß, Bcl-2-associated-protein (Bax), and an increase in B-cell lymphoma 2 (Bcl-2) protein, catalase (CAT), superoxide dismutase (SOD) in the testis, along with an increase in serum testosterone levels compared with the unprotected (positive control) group. The mRNA expression levels of nuclear factor-kappa B (NF-κB), tumor necrosis factor-α (TNF-α), p53, and miRNA-29a were downregulated in the testicular tissues of the protected groups compared with the unprotected group. In conclusion, the study provides sufficient evidence that Z. album extract, and its isolated compounds, zygo-albuside A and rutin, could alleviate testicular damage caused by the chemotherapeutic agent MTX.


Assuntos
MicroRNAs , Saponinas , Zygophyllum , Animais , Anti-Inflamatórios/farmacologia , Antioxidantes/metabolismo , Antioxidantes/farmacologia , Catalase/metabolismo , Dimetil Sulfóxido/farmacologia , Interleucina-6/metabolismo , Malondialdeído/metabolismo , Metotrexato/farmacologia , MicroRNAs/metabolismo , NF-kappa B/metabolismo , Estresse Oxidativo , Extratos Vegetais/química , RNA Mensageiro/metabolismo , Rutina/metabolismo , Rutina/farmacologia , Saponinas/metabolismo , Saponinas/farmacologia , Superóxido Dismutase/metabolismo , Testículo/metabolismo , Testosterona/metabolismo , Fator de Necrose Tumoral alfa/metabolismo , Proteína Supressora de Tumor p53/metabolismo , Água/metabolismo , Proteína X Associada a bcl-2/metabolismo
18.
Molecules ; 27(17)2022 Aug 25.
Artigo em Inglês | MEDLINE | ID: mdl-36080207

RESUMO

We focused on the functional components, antioxidant activity, skin-whitening, and anti-wrinkle properties of subcritical and supercritical water (SCW)-treated rutin. Rutin treatments were performed at the following temperature and pressure conditions: 200 °C/15 bar, 300 °C/100 bar, and 400 °C/250 bar. ABTS and DPPH radical scavenging activities and reducing power presented their highest values (1193.72 mg AAE/g, 728.73 mg AAE/g, and 0.65, respectively) at 300 °C/100 bar. The tyrosinase inhibitory activity of SCW-treated rutin was 21.72-60.05% at 1 mg/mL. The ethyl acetate fraction showed 14.91% melanin inhibitory activity at a concentration of 10 µg/mL compared to the α-MSH treatment group. The protein expression inhibition rates of MITF, tyrosinase, TRP-1, and TRP-2 in the ethyl acetate fractions were 14.05%, 72%, 93.05%, and 53.44%, respectively, at a concentration of 10 µg/mL, compared to the control. These results indicate that SCW treatment could be used to develop cosmetic materials and functional food with physiological activity, and that SCW-treated rutin can be used as a skin-whitening cosmetic material.


Assuntos
Antioxidantes , Monofenol Mono-Oxigenase , Antioxidantes/química , Melaninas/metabolismo , Extratos Vegetais/química , Rutina/farmacologia , Água
19.
Molecules ; 27(17)2022 Aug 30.
Artigo em Inglês | MEDLINE | ID: mdl-36080352

RESUMO

Tartary buckwheat (Fagopyrum tataricum (L.) Gaertn.) and common buckwheat (Fagopyrum esculentum Moench) are adapted to growing in harsh conditions of high altitudes. Ultraviolet radiation at high altitudes strongly impacts plant growth and development. Under the influence of ultraviolet radiation, protecting substances are synthesized in plants. The synthesis of UV-B defense metabolites is genetically conditioned, and their quantity depends on the intensity of the ultraviolet radiation to which the plants and plant parts are exposed. These substances include flavonoids, and especially rutin. Other substances with aromatic rings of six carbon atoms have a similar function, including fagopyrin, the metabolite specific for buckwheat. Defensive substances are formed in the leaves and flowers of common and Tartary buckwheat, up to about the same concentration in both species. In comparison, the concentration of rutin in the grain of Tartary buckwheat is much higher than in common buckwheat. Flavonoids also have other functions in plants so that they can protect them from pests and diseases. After crushing the grains, rutin is exposed to contact with the molecules of rutin-degrading enzymes. In an environment with the necessary humidity, rutin is turned into bitter quercetin under the action of rutin-degrading enzymes. This bitterness has a deterrent effect against pests. Moreover, flavonoids have important functions in human nutrition to prevent several chronic diseases, including obesity, cardiovascular diseases, gallstone formation, and hypertension.


Assuntos
Fagopyrum , Fagopyrum/metabolismo , Flavonoides/metabolismo , Humanos , Quercetina , Rutina/metabolismo , Rutina/farmacologia , Raios Ultravioleta/efeitos adversos
20.
Molecules ; 27(17)2022 Aug 30.
Artigo em Inglês | MEDLINE | ID: mdl-36080355

RESUMO

Several species within the genera Cassia or Senna have a treasure of traditional medicines worldwide and can be a promising source of bioactive molecules. The objective of the present study was to evaluate the phenolic content and antioxidant and enzyme inhibition activities of leaf methanolic extracts of C. fistula L., C. grandis L., S. alexandrina Mill., and S. italica Mill. The two Cassia spp. contained higher total polyphenolic content (42.23-49.75 mg GAE/g) than the two Senna spp., and C. fistula had significantly (p ˂ 0.05) the highest concentration. On the other hand, the Senna spp. showed higher total flavonoid content (41.47-59.24 mg rutin equivalent per g of extract) than that found in the two Cassia spp., and S. alexandrina significantly (p ˂ 0.05) accumulated the highest amount. HPLC-MS/MS analysis of 38 selected bioactive compounds showed that the majority of compounds were identified in the four species, but with sharp variations in their concentrations. C. fistula was dominated by epicatechin (8928.75 µg/g), C. grandis by kaempferol-3-glucoside (47,360.04 µg/g), while rutin was the major compound in S. italica (17,285.02 µg/g) and S. alexandrina (6381.85). The methanolic extracts of the two Cassia species exerted significantly (p ˂ 0.05) higher antiradical activity, metal reducing capacity, and total antioxidant activity than that recorded from the two Senna species' methanolic extracts, and C. fistula displayed significantly (p ˂ 0.05) the highest values. C. grandis significantly (p ˂ 0.05) exhibited the highest metal chelating power. The results of the enzyme inhibition activity showed that the four species possessed anti-AChE activity, and the highest value, but not significantly (p ≥ 0.05) different from those obtained by the two Cassia spp., was exerted by S. alexandrina. The Cassia spp. exhibited significantly (p ˂ 0.05) higher anti-BChE and anti-Tyr properties than the Senna spp., and C. grandise revealed significantly (p ˂ 0.05) the highest values. C. grandise revealed significantly (p ˂ 0.05) the highest α- amylase inhibition, while the four species had more or less the same effect against the α-glucosidase enzyme. Multivariate analysis and in silico studies showed that many of the identified phenols may play key roles as antioxidant and enzyme inhibitory properties. Thus, these Cassia and Senna species could be a promising source of natural bioactive agents with beneficial effects for human health.


Assuntos
Cassia , Senna (Planta) , Antioxidantes/farmacologia , Metanol , Fenóis , Extratos Vegetais/farmacologia , Folhas de Planta , Rutina/farmacologia , Espectrometria de Massas em Tandem , alfa-Amilases
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