RESUMO
The aim of this research was the synthesis of silver nanoparticles (SPA- and SPR-AgNPs) using the aqueous extracts of the aerial (SPA) and the root (SPR) parts of the plant Salvia pratensis L., their characterization, reaction condition optimization, and evaluation of their biological and catalytic activity. UV-Vis spectroscopy, X-ray powder diffraction (XRPD), scanning electron microscopy with EDS analysis (SEM/EDS), and dynamic light scattering (DLS) analysis were utilized to characterize the nanoparticles, while Fourier transform infrared (FTIR) spectroscopy was used to detect some functional groups of compounds present in the plant extracts and nanoparticles. The phenolic and flavonoid contents, as well as the antioxidant activity of the extracts, were determined spectrophotometrically. The synthesized nanoparticles showed twice-higher activity in neutralizing 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS+) compared with the respective extracts. SPR-AgNPs exhibited strong antimicrobial activity against almost all of the tested bacteria (<0.0039 mg/mL) and fungal strains, especially against the genus Penicillium (<0.0391 mg/mL). Moreover, they were fully biocompatible on all the tested eukaryotic cells, while the hemolysis of erythrocytes was not observed at the highest tested concentration of 150 µg/mL. The catalytic activity of nanoparticles toward Congo Red and 4-nitrophenol was also demonstrated. The obtained results confirm the possibility of the safe application of the synthesized nanoparticles in medicine and as a catalyst in various processes.
Assuntos
Antibacterianos , Nanopartículas Metálicas , Antibacterianos/farmacologia , Antibacterianos/química , Prata/farmacologia , Prata/química , Nanopartículas Metálicas/química , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Espectroscopia de Infravermelho com Transformada de Fourier , Componentes Aéreos da PlantaRESUMO
The study's objective was to obtain silver nanoparticles (SVAgNP and FUAgNP) using aqueous extracts of Salvia verticillata and Filipendula ulmaria. The optimal conditions for nanoparticle synthesis were determined and obtained; nanoparticles were then characterized using UV-Vis, Fourier-transform infrared spectroscopy (FTIR), X-ray powder diffraction (XRD), Dynamic Light Scattering (DLS), Scanning Electron Microscopy with Energy Dispersive Spectroscopy (SEM/EDS). SVAgNP and FUAgNP possessed a crystalline structure with 48.42% and 60.41% silver weight, respectively. The highest percentage of nanoparticles in the solution had a diameter between 40 and 70 nm. In DPPHË and ABTSË+ methods, FUAgNP (IC50 15.82 and 59.85 µg/mL, respectively) demonstrated a higher antioxidant capacity than SVAgNP (IC50 73.47 and 79.49 µg/mL, respectively). Obtained nanoparticles also showed pronounced antibacterial activity (MIC Ë 39.1 µg/mL for most of the tested bacteria), as well as high biocompatibility with the human fibroblast cell line MRC-5 and significant cytotoxicity on some cancer cell lines, especially on the human colon cancer HCT-116 cells (IC50 31.50 and 66.51 µg/mL for SVAgNP and FUAgNP, respectively). The nanoparticles demonstrated high catalytic effectiveness in degrading Congo red dye with NaBH4. The results showed a rapid and low-cost methodology for the synthesis of AgNPs using S. verticillata and F. ulmaria with promising biological potential.
Assuntos
Filipendula , Nanopartículas Metálicas , Salvia , Humanos , Prata/química , Nanopartículas Metálicas/química , Antibacterianos/química , Extratos Vegetais/farmacologia , Extratos Vegetais/química , Espectroscopia de Infravermelho com Transformada de FourierRESUMO
Nanoparticles (NPs) are used in many products and materials for humans such as electronics, in medicine for drug delivery, as biosensors, in biotechnology, and in agriculture, as ingredients in cosmetics and food supplements. Besides that, NPs may display potentially hazardous properties on human health and the environment as a consequence of their abundant use in life nowadays. Hence, there is increased interest of researchers to provide possible therapeutic agents or dietary supplements for the amelioration of NP-induced toxicity. This review summarizes the new findings in the research of the use of antioxidants as supplements for the prevention and alleviation of harmful effects caused by exposure of organisms to NPs. Also, mechanisms involved in the formation of NP-induced oxidative stress and protective mechanisms using different antioxidant substances have also been elaborated. This review also highlights the potential of naturally occurring antioxidants for the enhancement of the antioxidant defense systems in the prevention and mitigation of organism damage caused by NP-induced oxidative stress. Based on the presented results of the most recent studies, it may be concluded that the role of antioxidants in the prevention and treatment of nanoparticle-induced toxicity is unimpeachable. This is particularly important in terms of oxidative stress suppression.
Assuntos
Antioxidantes/farmacologia , Nanopartículas/toxicidade , Estresse Oxidativo/efeitos dos fármacos , Animais , HumanosRESUMO
Mineral components of dental composites are used in many medical and dental applications, including preventive, restorative, and regenerative dentistry. To evaluate the behavioural alterations induced by nanosized particles of novel dental composites, by means of depressive level and cognitive functions, experimental groups of rats were chronically administered with nanosized hydroxyapatite (HA), tricalcium phosphate (TCP), and amorphous calcium phosphate (ACP) with or without simultaneous application of Filipendula ulmaria L. (FU) methanolic extract. The significant prodepressant action was observed in groups solely treated with HA and ACP. Besides, prolonged treatment with ACP also resulted in a significant decline in cognitive functions estimated in the novel object recognition test. The adverse impact of calcium phosphates on estimated behavioural functions was accompanied by increased oxidative damage and apoptotic markers in the prefrontal cortex, as well as diminished specific neurotrophin (BDNF) and gabaergic expression. The results of our investigation showed that simultaneous antioxidant supplementation with FU extract prevented calcium phosphate-induced behavioural disturbances, as well as prooxidative and apoptotic actions, with the simultaneous restoration of BDNF and GABA-A receptors in the prefrontal cortex. These findings suggest that FU may be useful in the prevention of prodepressant impact and cognitive decline as early as the manifestation of calcium phosphate-induced neurotoxicity.
Assuntos
Fosfatos de Cálcio/toxicidade , Disfunção Cognitiva/tratamento farmacológico , Disfunção Cognitiva/prevenção & controle , Depressão/tratamento farmacológico , Depressão/prevenção & controle , Filipendula/química , Nanopartículas/toxicidade , Extratos Vegetais/uso terapêutico , Animais , Apoptose/efeitos dos fármacos , Apoptose/genética , Fator Neurotrófico Derivado do Encéfalo/metabolismo , Disfunção Cognitiva/complicações , Disfunção Cognitiva/genética , Depressão/complicações , Depressão/genética , Regulação da Expressão Gênica/efeitos dos fármacos , Elevação dos Membros Posteriores , Masculino , Teste de Campo Aberto , Estresse Oxidativo/efeitos dos fármacos , Estresse Oxidativo/genética , Extratos Vegetais/farmacologia , Ratos Wistar , Ácido gama-Aminobutírico/metabolismoRESUMO
We evaluated the influence of an antioxidant-rich extract of Filipendula ulmaria L. on anxiety levels induced by nano-sized particles of different calcium phosphates. Rats in experimental groups were administered with either nano-sized hydroxyapatite, tricalcium phosphate, or amorphous calcium phosphate in the presence of Filipendula ulmaria extract. Appropriate behavioral tests were performed to assess anxiety levels, while oxidative status and apoptosis parameters were determined in the hippocampus samples. The applied calcium phosphates increased oxidative stress markers in hippocampal tissue, accompanied by an enhanced pro-apoptotic mechanism. Moreover, the hippocampal immunoreactivity for brain-derived neurotrophic factor and GABAergic-A receptors was significantly lower following calcium phosphate nanoparticles intake. The observed functional and morphological alterations in the rat hippocampus occurred simultaneously with the anxiogenic response estimated in behavioral testing. The neuroprotective effect of Filipendula ulmaria was markedly manifested by the attenuation of oxidative damage induced by amorphous calcium phosphate and enhanced anti-apoptotic action in the rat hippocampus. The increased hippocampal immunoreactivity for brain-derived neurotrophic factor, GABAergic-A receptors and significant anxiolytic-like effects of Filipendula ulmaria may suggest a beneficial role of antioxidant supplementation in preventing anxiogenic response to nano-sized calcium phosphates.
Assuntos
Antioxidantes/farmacologia , Ansiedade/tratamento farmacológico , Apoptose/efeitos dos fármacos , Filipendula , Hipocampo/efeitos dos fármacos , Estresse Oxidativo/efeitos dos fármacos , Extratos Vegetais/farmacologia , Animais , Ansiedade/induzido quimicamente , Comportamento Animal/efeitos dos fármacos , Fosfatos de Cálcio/administração & dosagem , Masculino , Nanopartículas/administração & dosagem , Ratos , Ratos WistarRESUMO
Cancer represents one of the most pernicious public health problems with a high mortality rate among patients worldwide. Chemotherapy is one of the major therapeutic approaches for the treatment of various malignancies. Platinum-based drugs (cisplatin, oxaliplatin, carboplatin, etc.) are highly effective chemotherapeutic drugs used for the treatment of several types of malignancies, but their application and dosage are limited by their toxic effects on various systems, including neurotoxicity. Simultaneously, researchers have tried to improve the survival rate and quality of life of cancer patients and decrease the toxicity of platinum-containing drugs by combining them with non-chemotherapy-based drugs, dietary supplements and/or antioxidants. Additionally, recent studies have shown that the root cause for the many side effects of platinum chemotherapeutics involves the production of reactive oxygen species (ROS) in naive cells. Therefore, suppression of ROS generation and their inactivation with antioxidants represents an appropriate approach for platinum drug-induced toxicities. The aim of this paper is to present an updated review of the protective effects of different antioxidant agents (vitamins, dietary antioxidants and supplements, medicaments, medicinal plants and their bioactive compounds) against the neurotoxicity induced by platinum-based chemotherapeutics. This review highlights the high potential of plant antioxidants as adjuvant strategies in chemotherapy with platinum drugs.
Assuntos
Protocolos de Quimioterapia Combinada Antineoplásica/efeitos adversos , Antioxidantes/uso terapêutico , Suplementos Nutricionais , Neoplasias/tratamento farmacológico , Síndromes Neurotóxicas/prevenção & controle , Protocolos de Quimioterapia Combinada Antineoplásica/uso terapêutico , Antioxidantes/administração & dosagem , Carboplatina/administração & dosagem , Carboplatina/efeitos adversos , Cisplatino/administração & dosagem , Cisplatino/efeitos adversos , Humanos , Neoplasias/metabolismo , Síndromes Neurotóxicas/etiologia , Oxaliplatina/administração & dosagem , Oxaliplatina/efeitos adversos , Espécies Reativas de Oxigênio/antagonistas & inibidores , Espécies Reativas de Oxigênio/metabolismoRESUMO
Since cisplatin therapy is usually accompanied with numerous toxicities, including neurotoxicity, that involve tissue oxidative damage, the aim of this study was to evaluate the possible protective effect of N-acetylcysteine (NAC) on the anxiogenic response to cisplatin (CIS). Thirty-two male Wistar albino rats divided into four groups (control, cisplatin, NAC, and CIS + NAC). All treatments were delivered intraperitoneally. On day one, the control and cisplatin groups received saline while the NAC and CIS + NAC groups were administered with NAC (500 mg/kg). On the fifth day, the control group received saline while the CIS group was treated with cisplatin (7.5 mg/kg), the NAC group again received NAC (500 mg/kg), and the CIS + NAC group was simultaneously treated with cisplatin and NAC (7.5 and 500 mg/kg, respectively). Behavioral testing, performed on the tenth day in the open field (OF) and elevated plus maze (EPM) tests, revealed the anxiogenic effect of cisplatin that was significantly attenuated by NAC. The hippocampal sections evaluation showed increased oxidative stress (increased lipid peroxidation and decline in antioxidant enzymes activity) and proapoptotic action (predominantly by diminished antiapoptotic gene expression) following a single dose of cisplatin. NAC supplementation along with cisplatin administration reversed the prooxidative and proapoptotic effects of cisplatin. In conclusion, the results obtained in this study confirmed that antioxidant supplementation with NAC may attenuate the cisplatin-induced anxiety. The mechanism of anxiolytic effect achieved by NAC may include the decline in oxidative damage that down regulates increased apoptosis and reverses the anxiogenic action of cisplatin.
Assuntos
Acetilcisteína/farmacologia , Ansiolíticos/farmacologia , Ansiedade/induzido quimicamente , Ansiedade/tratamento farmacológico , Cisplatino/efeitos adversos , Substâncias Protetoras/farmacologia , Acetilcisteína/administração & dosagem , Acetilcisteína/química , Animais , Ansiolíticos/administração & dosagem , Ansiolíticos/química , Antineoplásicos/administração & dosagem , Antioxidantes/administração & dosagem , Comportamento Animal/efeitos dos fármacos , Cisplatino/administração & dosagem , Masculino , Estresse Oxidativo/efeitos dos fármacos , Substâncias Protetoras/administração & dosagem , Substâncias Protetoras/química , Ratos , Ratos WistarRESUMO
Numerous adverse effects of cisplatin-based therapy are usually accompanied by enhanced oxidative damage and cell apoptosis in various tissues. Even neurotoxic manifestations of cisplatin administration, such as the anxiogenic effect, appear along with the increased oxidative stress and apoptotic indicators in certain brain regions. Thirty-five Wistar albino male rats were divided into seven groups: control, cisplatin (received a single dose of cisplatin: 7.5 mg/kg), three groups with oral administration of Satureja hortensis L. methanolic extract (SH) (low: 50 mg/kg, middle: 100 mg/kg, and high dose: 200 mg/kg) along with cisplatin application, a group with the extract in high dose alone, and a silymarin group (cisplatin and silymarin: 100 mg/kg), in order to evaluate the antioxidant effects of SH on cisplatin-induced increase in the anxiety level. After completing 10-day pretreatments, behavioral testing was performed in the open field and the elevated plus maze, followed by an investigation of oxidative stress and apoptosis parameters in hippocampal tissue samples. Cisplatin administration resulted in anxiogenic-like behavior, increased lipid peroxidation, and proapoptotic markers accompanied by the decline in antioxidant and antiapoptotic defense. The administration of extract alone did not significantly alter any of the estimated parameters. When applied along with cisplatin, SH in a dose of 100 mg/kg induced the significant anxiolytic effect with concomitant recovery of antioxidant and antiapoptotic activity indicators, while both lower and higher doses of the extract failed to improve the adverse effects of cisplatin administration. The beneficial effects of the middle dose of SH were equivalent to the same dose of silymarin, as a "golden standard." Our results indicate that the antioxidant supplementation with SH in an optimal dose significantly improved the oxidative status and it had antiapoptotic effect in the rat hippocampus disturbed by cisplatin administration, which was accompanied with attenuation of cisplatin-induced anxiogenic effect.
Assuntos
Antioxidantes/uso terapêutico , Cisplatino/uso terapêutico , Plantas/química , Satureja/química , Animais , Antioxidantes/farmacologia , Cisplatino/farmacologia , Masculino , Ratos , Ratos WistarRESUMO
A simple and efficient ultrasonic-assisted extraction (UAE) technique was developed in order to find optimal conditions for the extraction of total phenolic compounds, flavonoids and anthocyanins in wild raspberry (Rubus idaeus L.) fruits. Several extraction variables, including methanol composition (v/v, %), solid-solvent ratio (g/mL), time (min) and extraction temperature (°C) were optimized using response surface methodology (RSM). Under optimal conditions for extraction, the total phenolics were found in the concentration of 383 mg GAE/100 g of fresh fruit weight, while HPLC-PDA analysis of the optimized extract showed the presence of cyanidin-3-glucoside, cyanidin-3-sophoroside, catechin, gallic and ellagic acid. The experimental values of DPPH and ABTS radical scavenging activities were 29.0 and 39.5 µmol Trolox/g of fresh fruit weight, respectively. In vitro simulated gastrointestinal digestion showed great raspberry phenolics stability. Our study assessed the bioaccessible phenolics in wild raspberry fruits and showed optimal conditions for the effective extraction of bioactive compounds for their analysis.
Assuntos
Flavonoides/análise , Frutas/química , Fenóis/isolamento & purificação , Compostos Fitoquímicos/isolamento & purificação , Rubus/química , Antocianinas/análise , Antocianinas/isolamento & purificação , Cromatografia Líquida de Alta Pressão , Flavonoides/isolamento & purificação , Fenóis/análise , Compostos Fitoquímicos/análise , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , SonicaçãoRESUMO
Filipendula vulgaris Moench (dropwort) is used in traditional medicine for relieving various inflammation-related diseases. In the present study, the phytochemical profile of F. vulgaris aerial part (FVA) and root (FVR) methanolic extracts was evaluated by LC-DAD-HRMS analysis. Furthermore, their in vitro and in vivo anti-inflammatory effects, as well as their potential cytotoxicity, were assessed. Results showed that the extracts mainly contain phenolics like flavonoids, hydrolyzable tannins, procyanidins, and phenolic acid derivatives, including gaultherin. No in vitro cytotoxicity was found at the highest concentration (50⯵g/mL). FVA extract (50⯵g/mL) significantly inhibited cyclooxygenase-1 and -2 (COX-1 and COX-2) activities in vitro (>50% inhibition), and FVR extract considerably inhibited COX-2 activity (52.5⯱â¯2.7%) without affecting COX-2 gene expression in LPS-stimulated THP-1â¯cells. The extracts demonstrated prominent in vivo anti-inflammatory potential upon oral administration in rats. Especially FVA extract at 100 and 200â¯mg/kg significantly inhibited carrageenan-induced edema formation. From these results, it can be concluded that F. vulgaris extracts possess interesting anti-inflammatory properties.
Assuntos
Anti-Inflamatórios/farmacologia , Filipendula/química , Compostos Fitoquímicos/química , Extratos Vegetais/farmacologia , Animais , Anti-Inflamatórios/administração & dosagem , Linhagem Celular , Linhagem Celular Tumoral , Cromatografia Líquida/métodos , Ciclo-Oxigenase 1/efeitos dos fármacos , Ciclo-Oxigenase 1/genética , Ciclo-Oxigenase 1/metabolismo , Ciclo-Oxigenase 2/efeitos dos fármacos , Ciclo-Oxigenase 2/genética , Ciclo-Oxigenase 2/metabolismo , Inibidores de Ciclo-Oxigenase/farmacologia , Relação Dose-Resposta a Droga , Sequestradores de Radicais Livres/farmacologia , Expressão Gênica , Humanos , Concentração Inibidora 50 , Masculino , Espectrometria de Massas/métodos , Metanol/química , Óxido Nítrico/metabolismo , Compostos Fitoquímicos/farmacologia , Componentes Aéreos da Planta/química , Extratos Vegetais/química , Raízes de Plantas/química , Ratos WistarRESUMO
The aim of our study was to examine the potential ameliorating effect of the methanolic extract of Satureja hortensis L. (summer savory) aerial parts against cisplatin-induced oxidative damage in renal, hepatic, and testicular tissues. S. hortensis methanol extract at the doses of 50, 100 and 200â¯mg/kg of body weight were orally administered to Wistar rats once daily for 10 days. Toxicity was induced by intraperitoneal injection of a single dose of cisplatin (7.5â¯mg/kg of body weight) on the 5th day of the experiment. Applied treatment with S. hortensis extract restored tissue morphology, ameliorated levels of serum parameters for liver, renal and testes function, tissue oxidative stress parameters, and increased Bcl-2/Bax ratio as an indicator of apoptosis in experimental animals caused by application of cisplatin. UHPLC/DAD/HESI-MS/MS analysis revealed that S. hortensis extract was rich in phenolic compounds with rosmarinic acid (24.9â¯mg/g) as the main compound, followed by caffeic acid (1.28â¯mg/g) and naringenin (1.06â¯mg/g). Our findings suggest that S. hortensis may be a valuable source of dietary and pharmacologically important phenolic compounds, especially rosmarinic acid, in pharmaceutical and functional food formulations in order to maintain normal health conditions or as a remedy in various diseases caused by oxidative damage.
Assuntos
Antineoplásicos/toxicidade , Cisplatino/toxicidade , Rim/efeitos dos fármacos , Fígado/efeitos dos fármacos , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Satureja/química , Testículo/efeitos dos fármacos , Animais , Cromatografia Líquida de Alta Pressão , Masculino , Estresse Oxidativo/efeitos dos fármacos , Ratos Wistar , Espectrometria de Massas por Ionização por Electrospray , Espectrometria de Massas em TandemRESUMO
Liver damage is a serious medical problem worldwide and is caused by primary or secondary metabolic, microbiological, toxicological, immunological and circulatory etiological factors. The objective of this paper is to analyze the hepatoprotective effect of various plants, their biologically active compounds and extracts and the possibility of these compounds to attenuate complex pathophysiology processes during chronic inflammation and the development of liver cirrhosis. This review summarizes several plants whose hepatoprotective effects have been demonstrated and partially describes the mechanisms of inflammation inhibition. It is known that fibrosis includes an oxidative damage, inflammatory and immune response and star-shaped cells and their activation in hepatocytes. Effects of particular phytocompounds and their anti-inflammatory mechanisms have been studied in several cell lines in vitro, in vivo in different animal models, as well as in some clinical studies. Results suggest that mechanisms include reduction of oxidative stress, suppression of the inflammatory and immune response, as well as the inhibition of the activation of hepatic stellate cells (HSCs), decreasing extracellular matrix (ECM) deposition and induction of apoptosis, protection of hepatocytes from apoptosis and creating apoptotic bodies, which are phagocytic and activate HSCs. Medical herbs are abundant, economical and versatile and thus are potential alternative agents with anti-inflammatory mechanism. They can be a source of bioactive compounds, and with the aim of preventing the formation and progression of fibrosis, they can find wide applications in medical practice. The obtained results should promote further research in order to identify safe and effective protective and therapeutic resources.
Assuntos
Medicina Herbária/métodos , Cirrose Hepática/tratamento farmacológico , Hepatopatias/tratamento farmacológico , Fígado/patologia , HumanosRESUMO
Methanolic extracts of Moltkia aurea Boiss. (MA) and Moltkia coerulea (Willd.) Lehm. (MC) were investigated for their antioxidant capacity and enzymatic inhibitory potential against acetylcholinesterase, butyrylcholinesterase, α-amylase, α-glucosidase, and tyrosinase in vitro. MA and MC were also explored for their antimicrobial effect, as well as for their possible genotoxic/antigenotoxic potential on Drosophila melanogaster in vivo. The total bioactive components (phenolic (TPC) and flavonoid contents (TFC)) were determined and liquid chromatography-tandem mass spectrometry (LC-MS/MS) metabolite profiling of MA and MC appraised. The plausible docking poses of bioactive compounds to key enzymes were further studied using molecular modelling approach. MA proved to be a better antioxidant with higher TPC and TFC compared to MC. Protocatechuic acid, rutin, hesperidin and malic acid were the most abundant in these extracts. Both MA and MC exhibited antigenotoxic potential with a %R in DNA damage of 60.90 and 53.14% respectively. The docking studies revealed that rutin, hesperidin, and rosmarinic acid have the best scores for all the enzymes tested. MA and MC were found to be rich in phytochemicals with potent antioxidant, antimicrobial, and antigenotoxic activities that can be further studied for the management of neurodegenerative complications, diabetes, and hyperpigmentation.
Assuntos
Boraginaceae/química , Suplementos Nutricionais/análise , Extratos Vegetais/química , Animais , Antioxidantes/química , Antioxidantes/farmacologia , Drosophila melanogaster/efeitos dos fármacos , Drosophila melanogaster/genética , Compostos Fitoquímicos/química , Compostos Fitoquímicos/farmacologia , Extratos Vegetais/farmacologia , Espectrometria de Massas em TandemRESUMO
Filipendula ulmaria, known as meadowsweet, is a perennial herb found in wild and cultivated habitats in Europe and Asia. Usage of F. ulmaria in traditional medicine is based on diuretic, astringent, antirheumatic, and anti-inflammatory properties of this plant. Exposure to cisplatin at a dose of 7.5 mg/kg caused significant increase in serum parameters of liver and kidneys function and tissue oxidative stress markers along with some histopathological changes in liver and kidney tissues of experimental rats, as well as high level of genotoxicity. Administration of F. ulmaria extracts in three different concentrations (100, 200, and 400 mg/kg/day) for 10 days resulted in a reduction of oxidative stress in tissues and decrease of serum parameters. Moreover, tested extracts attenuated the genotoxicity of cisplatin in reverse dose-dependent manner. F. ulmaria extracts had no in vitro cytotoxic activity at all applied concentrations (IC50 > 50 µg/mL). Tested extracts, rich in polyphenolic compounds, attenuate cisplatin-induced liver and kidney oxidative stress, reduce tissue damage, and enhance the antioxidative status of experimental animals during cisplatin application. Therefore, F. ulmaria extracts may be used as supportive agent for the prevention and amelioration of cisplatin side effects.
Assuntos
Doença Hepática Induzida por Substâncias e Drogas/prevenção & controle , Cisplatino/toxicidade , Filipendula/química , Nefropatias/prevenção & controle , Rim/efeitos dos fármacos , Fígado/efeitos dos fármacos , Estresse Oxidativo/efeitos dos fármacos , Extratos Vegetais/farmacologia , Animais , Antineoplásicos/toxicidade , Sobrevivência Celular/efeitos dos fármacos , Doença Hepática Induzida por Substâncias e Drogas/etiologia , Cromatografia Líquida/métodos , Dano ao DNA/efeitos dos fármacos , Rim/metabolismo , Nefropatias/induzido quimicamente , Fígado/metabolismo , Espectrometria de Massas/métodos , Ratos , Ratos WistarRESUMO
ETHNOPHARMACOLOGICAL RELEVANCE: Meadowsweet (Filipendula ulmaria (L.) Maxim, Rosaceae) has been traditionally used in most European countries for the treatment of inflammatory diseases due to its antipyretic, analgesic, astringent, and anti-rheumatic properties. However, there is little scientific evidence on F. ulmaria anti-inflammatory effects regarding its impact on cyclooxygenases enzymatic activity and in vivo assessment of anti-inflammatory potential. This study aims to reveal the anti-inflammatory activity of methanolic extracts from the aerial parts (FUA) and roots (FUR) of F. ulmaria, both in in vitro and in vivo conditions. MATERIALS AND METHODS: The characteristic phenolic compounds in F. ulmaria extracts were monitored via high performance thin layer chromatography (HPTLC). The in vitro anti-inflammatory activity of F. ulmaria extracts was evaluated using cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2) enzyme assays, and an assay for determining COX-2 gene expression. The in vivo anti-inflammatory effect of F. ulmaria extracts was determined in two doses (100 and 200 mg/kg b.w.) with hot plate test and carrageenan-induced paw edema test in rats. Inflammation was also evaluated by histopathological and immunohistochemical analysis. RESULTS: FUA extract showed the presence of rutoside, spiraeoside, and isoquercitrin. Both F. ulmaria extracts at a concentration of 50µg/mL were able to inhibit COX-1 and -2 enzyme activities, whereby FUA extract (62.84% and 46.43% inhibition, respectively) was double as effective as the root extract (32.11% and 20.20%, respectively). Extracts hardly inhibited the level of COX-2 gene expression in THP-1 cells at a concentration of 25µg/mL (10.19% inhibition by FUA and 8.54% by FUR). In the hot plate test, both extracts in two doses (100 and 200mg/kg b.w.), exhibited an increase in latency time when compared with the control group (p<0.05). In the carrageenan-induced acute inflammation test, FUA at doses of 100 and 200mg/kg b.w., and FUR at 200mg/kg, were able to significantly reduce the mean maximal swelling of rat paw until 6h of treatment. Indomethacin, FUA, and FUR extracts significantly decreased inflammation score and this effect was more pronounced after 24h, compared to the control group (p<0.05). CONCLUSIONS: The observed results of in vitro and, for the first time, in vivo anti-inflammatory activity of meadowsweet extracts, provide support of the traditional use of this plant in the treatment of different inflammatory conditions. Further investigation of the anti-inflammatory compounds could reveal the mechanism of anti-inflammatory action of these extracts.
Assuntos
Anti-Inflamatórios/farmacologia , Etnofarmacologia , Filipendula/química , Extratos Vegetais/farmacologia , Animais , Anti-Inflamatórios/isolamento & purificação , Anti-Inflamatórios/uso terapêutico , Linhagem Celular Tumoral , Ciclo-Oxigenase 1/genética , Ciclo-Oxigenase 1/metabolismo , Ciclo-Oxigenase 2/genética , Ciclo-Oxigenase 2/metabolismo , Inibidores de Ciclo-Oxigenase/isolamento & purificação , Inibidores de Ciclo-Oxigenase/farmacologia , Inibidores de Ciclo-Oxigenase/uso terapêutico , Relação Dose-Resposta a Droga , Edema/tratamento farmacológico , Expressão Gênica/efeitos dos fármacos , Humanos , Masculino , Dor Nociceptiva/tratamento farmacológico , Componentes Aéreos da Planta/química , Extratos Vegetais/isolamento & purificação , Extratos Vegetais/uso terapêutico , Raízes de Plantas/química , Ratos WistarRESUMO
ETHNOPHARMACOLOGICAL RELEVANCE: The two species of Filipendula genus, Filipendula hexapetala Gilib. and Filipendula ulmaria (L.) Maxim are a traditional herbal medicine widely used to treat haemorrhoids, diarrhoea, fever, rheumatism and arthritic pain, kidney problems, to stop bleeding, and the common cold, as well as food supplements. However, no scientific study has been performed to validate genotoxic and/or antigenotoxic potentials of these two Filipendula species. AIM OF THE STUDY: The aim of the present study was to examine the genotoxic and possible in vitro and in vivo DNA protection potential of methanol extracts of F. hexapetala and F. ulmaria. MATERIALS AND METHODS: The genotoxicity of different concentrations of F. hexapetala and F. ulmaria methanol extracts from roots and aerial parts (20, 40 and 80 mg/ml), mixed with standard food for Drosophila, was evaluated in vivo in the anterior midgut of Drosophila melanogaster using a modified alkaline comet assay. The protective effects of the highest dose of extracts were observed in somatic cells of third-instar larvae against ethyl methanesulphonate (EMS)-induced genotoxicity. Also, DNA protection activity of methanol extracts from F. hexapetala and F. ulmaria (100, 200, and 400 µg/ml) against hydroxyl radical-induced DNA damage was determined under in vitro conditions. RESULTS: The results showed that methanol extracts from the root and aerial part of F. hexapetala at a concentration of 20mg/ml indicated the absence of genotoxicity. Also, there were no statistically significant differences in total scores between any of the groups treated with F. ulmaria root extract and the negative control group, while F. ulmaria aerial part extract possess weak genotoxic effects depending on the concentrations. The percentage reduction in DNA damage was more evident in the group of larvae simultaneously treated with EMS and the highest dose of F. hexapetala root or aerial part extracts and F. ulmaria root extract (91.02, 80.21, and 87.5%, respectively) and less expressive in the group simultaneously treated with F. ulmaria aerial part extract (54.7%). F. hexapetala root and aerial part extracts and F. ulmaria root extract possess strong capabilities to protect DNA from being damaged by hydroxyl radicals. CONCLUSIONS: It can be concluded that F. hexapetala root and aerial part extracts and F. ulmaria root extract demonstrated the absence of genotoxic activity. The extracts appeared to have antigenotoxic effect, reducing the levels of DNA damage induced by EMS by more than 80%. Also, F. hexapetala root and aerial part extracts and F. ulmaria root extracts could effectively protect against hydroxyl radical-induced DNA damage.
Assuntos
Filipendula , Metanol/toxicidade , Componentes Aéreos da Planta/toxicidade , Extratos Vegetais/toxicidade , Raízes de Plantas/toxicidade , Animais , Dano ao DNA/efeitos dos fármacos , Dano ao DNA/fisiologia , Drosophila melanogaster , Testes de Mutagenicidade/métodos , Extratos Vegetais/isolamento & purificaçãoRESUMO
The purpose of the present study was to evaluate the antioxidant and antimicrobial potential of Filipendula ulmaria (L.) Maxim. methanolic extracts, their stabilities under different pH and thermal conditions and in vitro digestibility. The results showed a considerable content of phenolic compounds in the extracts, especially total phenolic acids (47.47 mg CAE g(-1)) and flavonoids (45.47 mg RUE g(-1)) in aerial parts. HPLC analysis indicated the presence of spiraeoside in the aerial part extract. The extracts revealed an interesting antimicrobial effect against the tested microorganisms, especially bacteria E. coli and E. faecalis (MIC 0.156-0.625 mg mL(-1)), and fungi P. cyclopium and F. oxysporum (MIC 2.5-5 mg mL(-1)). The extracts exerted high antioxidant activities, particularly the root extract, paralleled by their considerable activities against the lipid oxidation process. The results of this study suggest that both extracts potentially could be functional food ingredients considering their good antioxidant and antimicrobial activities, and stability under different conditions.
Assuntos
Anti-Infecciosos/química , Antioxidantes/química , Filipendula/química , Fenóis/química , Extratos Vegetais/química , Anti-Infecciosos/farmacologia , Antioxidantes/farmacologia , Cromatografia Líquida de Alta Pressão , Enterococcus faecalis/efeitos dos fármacos , Escherichia coli/efeitos dos fármacos , Flavonoides/química , Flavonoides/farmacologia , Fusarium/efeitos dos fármacos , Concentração de Íons de Hidrogênio , Taninos Hidrolisáveis/química , Peroxidação de Lipídeos/efeitos dos fármacos , Testes de Sensibilidade Microbiana , Modelos Biológicos , Penicillium/efeitos dos fármacos , Fenóis/farmacologia , Extratos Vegetais/farmacologia , TemperaturaRESUMO
The objective of this work was to investigate the effects of the methanol extracts of Gentiana cruciata L. aerial parts (GCA) and roots (GCR) against carbon tetrachloride-induced liver injury in rats. Pretreatment with GCA and GCR, containing sweroside, swertiamarin and gentiopicrin in high concentrations, dose-dependently and significantly decreased the levels of serum transaminases, alkaline phosphatase and total bilirubin, whereas an increase in the level of total protein was found compared with the CCl4-treated group. Moreover, oral administration of extracts significantly enhanced antioxidant enzyme activities (superoxide dismutase and catalase), increased the content of glutathione and decreased the content of TBARS. Microscopic evaluations of the liver revealed CCl4-induced lesions and related toxic manifestations that were minimal in the liver of rats pretreated with extracts at the dose of 400 mg per kg b.w. The results suggest that the use of G. cruciata extracts has a merit as a potent candidate in protecting the liver against chemical induced toxicity.