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To better use the Lecythis pisonis Cambess. biomass, this study investigates whether Sapucaia seed coats present wound healing properties. We analyzed the antibacterial, antioxidant, and wound healing-promoting potentials, plus cytotoxicity and stimulation of vascular endothelial growth factor-A. The chemical composition was analyzed by positive ion mode electrospray ionization Fourier transform ion cyclotron resonance mass spectrometry. A total of 19 compounds were identified, such as proanthocyanidin A1, procyanidins A1, B2, and C1, epigallocatechin, and kaempferol (p-coumaroyl) glycoside. Potent antioxidant strength/index was verified for 2,2-diphenyl-1-picrylhydrazyl radical (IC50 = 0.99 µg/mL) and ferric reducing antioxidant power (IC50 = 1.09 µg/mL). The extract did not present cytotoxicity and promoted significant cell migration and/or proliferation of fibroblasts (p < 0.05). Vascular endothelial growth factor-A was stimulated dose-dependently at 6 µg/mL (167.13 ± 8.30 pg/mL), 12.5 µg/mL (210.3 ± 14.2 pg/mL), and 25 µg/mL (411.6 ± 29.4 pg/mL). Platelet-derived growth factor (PDGF) (0.002 µg/mL) was stimulated at 215.98 pg/mL. Staphylococcus aureus was susceptible to the extract, with a minimum inhibitory concentration of 31.25 µg/mL. The identified compounds benefit the antioxidant activity, promoting hemostasis for the wound healing process, indicating that this extract has the potential for use in dermatological cosmetics.
Assuntos
Antioxidantes , Polifenóis , Antioxidantes/química , Polifenóis/farmacologia , Polifenóis/análise , Fator A de Crescimento do Endotélio Vascular/análise , Sementes/química , Cicatrização , Extratos Vegetais/químicaRESUMO
The control of weeds in agriculture is mainly conducted with the use of synthetic herbicides. However, environmental and human health concerns and increased resistance of weeds to existing herbicides have increased the pressure on researchers to find new active ingredients for weed control which present low toxicity to non-target organisms, are environmentally safe, and can be applied at low concentrations. It is herein described the synthesis of glycerol-fluorinated triazole derivatives and evaluation of their phytotoxic and cytogenotoxic activities. Starting from glycerol, ten fluorinated triazole derivatives were prepared in four steps. The assessment of them on Lactuca sativa revealed that they present effects on phytotoxic and cytogenotoxic parameters with different degrees of efficiency. The compounds 4a, 4b, 4d, 4e, 4i, and 4j have pre-emergent inhibition behavior, while all the investigated compounds showed post emergent effect. Mechanism of action as clastogenic, aneugenic, and epigenetic were observed in the lettuce root meristematic cells, with alterations as stick chromosome, bridge, delay, c-metaphase, and loss. It is believed that glycerol-fluorinated triazole derivatives possess a scaffold that can be explored towards the development of new chemicals for the control of weed species.
Assuntos
Alcaloides , Herbicidas , Humanos , Glicerol/toxicidade , Álcoois de Trioses de Açúcar , Triazóis/toxicidade , Meristema , Alcaloides/farmacologia , Herbicidas/toxicidade , Herbicidas/química , Plantas Daninhas , LactucaRESUMO
The study aimed to investigate the chemical composition and the anti-inflammatory activity of the hydroethanolic rhizomes, stems, and leaf extracts of Renealmia petasites using in vitro and in vivo assays. The chemical composition of the extracts was characterized in a linear iron trap mass spectrometer. Total phenolic, flavonoid, and tannin content were determined by spectrophotometry analyses. In vitro anti-inflammatory activity was investigated in lipopolysaccharide-stimulated macrophages evaluating the influence on the production of superoxide anion (O2-), nitric oxide (NO), and the pro-inflammatory cytokines tumor necrosis factor (TNF-α) and interleukin-6 (IL-6). In vivo effects were determined using the air pouch model in which were inoculated carrageenan and thereafter treated with 50 mg/kg of the hydroethanolic extracts of R. petasites. After 4 and 24 h, the cellular influx, protein exudation, cytokines, and nitric oxide were evaluated. Eight compounds were tentatively identified in the R. petasites extracts, suggesting five diarylheptanoids, one flavonoid, and two fatty alcohols. The in vitro results showed that the extracts were capable of blocking free radicals and/or inhibiting their intracellular actions by inhibiting the production of important mediators of the inflammatory process, such as NO, O2-, TNF-α, and IL-6. In vivo, R. petasites significantly decrease the influx of leukocytes, mainly neutrophils, protein exudation, NO, TNF-α, and IL-6 concentration in the air pouch model. The results evidenced that R. petasites can be considered a promising alternative therapy for the treatment and management of osteoarthritis and other inflammatory diseases.
Assuntos
Anti-Inflamatórios/farmacologia , Inflamação/tratamento farmacológico , Extratos Vegetais/farmacologia , Zingiberaceae/química , Animais , Anti-Inflamatórios/isolamento & purificação , Carragenina , Citocinas/metabolismo , Modelos Animais de Doenças , Inflamação/patologia , Lipopolissacarídeos , Macrófagos/efeitos dos fármacos , Macrófagos/patologia , Masculino , Camundongos , Óxido Nítrico/metabolismo , Células RAW 264.7 , Fatores de TempoRESUMO
BACKGROUND AND AIMS: Terpenes are considered the main components of essential oils and an important source for the identification of novel lead molecules. This study aimed to investigate the in vitro anti-inflammatory activity of L-carveol, L-carvone, and m-cimene (monoterpenes) and of valencene and guaiene (sesquiterpenes). METHODS: The influence on intracellular nitric oxide (NO) and pro- and anti-inflammatory cytokine (TNF-α, IL-1α and IL-10) production and on nuclear factor kappa B (NF-κB) activity was determined using Griess reagent, immunoenzymatic assay kits (ELISA) and chemiluminescence measurements in cell-based assays, respectively. Antioxidant activity was assayed through the protective effect against cellular oxidative damage produced by superoxide anion production (O 2 ·- ) and hydrogen peroxide on macrophages and by the quenching activity of the NO radical. RESULTS AND DISCUSSION: Terpenes reduced the pro-inflammatory cytokines TNF-α and IL-1α and increased the production of IL-10. In addition, the terpenes, especially guaiene (53.3 ± 2.4%) and m-cymene (38.1 ± 0.6%), significantly inhibited NO production in a macrophage cell culture-based assay, whereas no effect was observed in the scavenging activity of this radical. L-carveol and m-cymene significantly inhibited O 2 ·- production with reductions of approximately 68.6 ± 2.2% and 48.2 ± 4.2%, respectively, at a concentration of 10 µM. Moreover, these terpenes were verified to suppress NF-κB activity. The results indicate that these terpenes have therapeutic potential and may be used to suppress inflammatory diseases or as a leading compounds.
Assuntos
Anti-Inflamatórios/farmacologia , Inflamação/tratamento farmacológico , NF-kappa B/metabolismo , Óxido Nítrico/metabolismo , Transdução de Sinais/efeitos dos fármacos , Superóxidos/metabolismo , Terpenos/farmacologia , Células 3T3 , Animais , Antioxidantes/metabolismo , Linhagem Celular , Linhagem Celular Tumoral , Monoterpenos Cicloexânicos , Citocinas/metabolismo , Humanos , Inflamação/metabolismo , Macrófagos/efeitos dos fármacos , Macrófagos/metabolismo , Camundongos , Monoterpenos/farmacologia , Células RAW 264.7RESUMO
Background: The antimicrobial activity of essential oils has been reported in hundreds of studies, however, the great majority of these studies attribute the activity to the most prevalent compounds without analyzing them independently. Therefore, the aim was to investigate the antibacterial activity of 33 free terpenes commonly found in essential oils and evaluate the cellular ultrastructure to verify possible damage to the cellular membrane. Methods: Screening was performed to select substances with possible antimicrobial activity, then the minimal inhibitory concentrations, bactericidal activity and 24-h time-kill curve studies were evaluated by standard protocols. In addition, the ultrastructure of control and death bacteria were evaluated by scanning electron microscopy. Results: Only 16 of the 33 compounds had antimicrobial activity at the initial screening. Eugenol exhibited rapid bactericidal action against Salmonella enterica serovar Typhimurium (2 h). Terpineol showed excellent bactericidal activity against S. aureus strains. Carveol, citronellol and geraniol presented a rapid bactericidal effect against E. coli. Conclusions: The higher antimicrobial activity was related to the presence of hydroxyl groups (phenolic and alcohol compounds), whereas hydrocarbons resulted in less activity. The first group, such as carvacrol, l-carveol, eugenol, trans-geraniol, and thymol, showed higher activity when compared to sulfanilamide. Images obtained by scanning electron microscopy indicate that the mechanism causing the cell death of the evaluated bacteria is based on the loss of cellular membrane integrity of function. The present study brings detailed knowledge about the antimicrobial activity of the individual compounds present in essential oils, that can provide a greater understanding for the future researches.
Assuntos
Antibacterianos/farmacologia , Óleos Voláteis/química , Terpenos/farmacologia , Escherichia coli/efeitos dos fármacos , Escherichia coli/ultraestrutura , Testes de Sensibilidade Microbiana , Salmonella typhimurium/efeitos dos fármacos , Salmonella typhimurium/ultraestrutura , Staphylococcus aureus/efeitos dos fármacos , Staphylococcus aureus/ultraestruturaRESUMO
This study was undertaken to investigate the in vitro wound healing effects and the anti-inflammatory and antioxidant activities of terpinolene and α-phellandrene. The in vitro stimulatory effects on the proliferation and migration of fibroblasts were assessed using the scratch assay. The anti-inflammatory activity was evaluated using cell-based assays by investigating their influence on nitric oxide (NO), superoxide anion (O2â¢-), tumour necrosis factor-alpha (TNF-α) and interleukin 6 (IL-6) production and using the TNF-α-induced nuclear factor kappa (NF-κB) assay. Antioxidant activity was determined by the ABTS cation radical scavenging capacity, ferric reducing/antioxidant potential (FRAP), and NO free radical scavenging assays. Terpinolene and α-phellandrene significantly increased the migration and proliferation of fibroblasts and suppressed the pro-inflammatory cytokines IL-6 and TNF-α in a dose-dependent manner. Terpinolene and α-phellandrene at a concentration of 100⯵M significantly inhibited NO production (41.3 and 63.8%, respectively) in a macrophage cell-culture-based assay, and resulted in reductions in O2â¢- production of 82.1⯱â¯3.5% and 70.6⯱â¯4.3%, respectively. Moreover, these monoterpenes were verified to suppress NF-κB activity. In summary, terpinolene and α-phellandrene may contribute to broadening clinical options in the treatment of wounds by attenuating inflammation and oxidative stress in vitro.
Assuntos
Inflamação/fisiopatologia , Monoterpenos/metabolismo , Terpenos/metabolismo , Cicatrização/fisiologia , Análise de Variância , Monoterpenos Cicloexânicos , Humanos , Inflamação/metabolismo , Monoterpenos/análise , Estresse Oxidativo/fisiologia , Terpenos/análiseRESUMO
In the present work, we report the antioxidant, antimicrobial and cytotoxic activities of quercetin-capped gold nanoparticles (AuNPsQct). The synthesis of AuNPsQct was confirmed by UV-Vis spectroscopy, FTIR and transmission electron microscopy (TEM) analyses. The FTIR spectrum showed the integrity of the quercetin molecules on the nanoparticle surface. The TEM images showed sizes less than 100â¯nm and a slight spherical shape. The electrostatic stability was confirmed by the zeta potential method. The antioxidant activity of quercetin, evaluated by DPPH, ABTS and nitric oxide free radical scavenging methods, was preserved in the gold nanoparticles, furthermore quercetin-capped gold nanoparticles (IR50 0.37⯵g/mL) demonstrated a higher antioxidant activity than free quercetin (IR50 0.57⯵g/mL) by nitric oxide free radical scavenging method. Strong antifungal activity was observed for Aspergillus fumigatus with concentrations ranging from 0.1 to 0.5â¯mg/mL. The nanoparticles with quercetin did not exhibit cytotoxicity to human fibroblasts (L929 cells). In conclusion, these results suggest that AuNPsQct, produced by cost-effective method, can act as a promising candidate for different medical applications.
RESUMO
Considering the high number of accidents with diesel oil spills occurring in the marine ecosystem, toxicity tests aimed at assessing the effects of this pollutant on biota are necessary and urgent. Thus, the present study aimed to evaluate the toxicity of the soluble fraction of diesel oil (WSD) in the fertilization success of gametes and pluteu larvae of the sea urchin Echinometra lucunter. To do this, gametes and embryos were exposed to concentrations of 0% (control group), 0.5%, 1.5% and 2.5% of WSD. The fertilization success of exposed gametes and embryos were reduced significantly when compared to the control group in all tested concentrations. With this finding, it is evident that diesel oil can be significantly promoted in the early and adult life stages of a particular organism, and a better way of evaluating this toxicity is through the analysis of contaminant effects throughout the reproductive cycle of a species.
Assuntos
Gasolina/toxicidade , Ouriços-do-Mar/efeitos dos fármacos , Poluentes Químicos da Água/toxicidade , Animais , Fertilização/efeitos dos fármacos , Larva/efeitos dos fármacos , Ouriços-do-Mar/embriologia , Ouriços-do-Mar/crescimento & desenvolvimento , Água/químicaRESUMO
Toranja 'Burarama', Citrus maxima (Burm.) Merr. (Citrus grandis), is a new citrus discovered in the State of Espírito Santo, Brazil. As several varieties of citrus are known to possess antioxidant and cancer chemopreventive properties, the aim of the study was to evaluate in vitro if this Toranja possess these properties. The antioxidant activity, the potential to induce quinone reductase 1, and the influence on cell viability were measured. ESI(-)FT-ICR MS analysis was also performed and identified flavonoids, coumarins, and fatty acids in the extract. The ethyl acetate and methanolic extracts of the peels presented the highest antioxidant activity in vitro by DPPH (IC50 = 298.3 ± 2.6 µg/ml and 303.8 ± 0.4 µg/ml), ABTS assay (IC50 = 298.2 ± 6.4 µg/ml and 296.4 ± 2.5 µg/ml), and FRAP (IC50 = 234.6 ± 1.8 µg/ml and 398.1 ± 3.8 µg/ml). The ethyl acetate extract of the peel induced quinone reductase 1 activity in Hepa1c1c7 cells, indicating that C. maxima exhibited cancer chemopreventive properties.
Assuntos
Antineoplásicos Fitogênicos/farmacologia , Antioxidantes/farmacologia , Citrus/química , NAD(P)H Desidrogenase (Quinona)/metabolismo , Extratos Vegetais/farmacologia , Animais , Brasil , Linhagem Celular Tumoral , Sobrevivência Celular/efeitos dos fármacos , Cumarínicos/química , Cumarínicos/isolamento & purificação , Ácidos Graxos/química , Ácidos Graxos/isolamento & purificação , Flavonoides/química , Flavonoides/isolamento & purificação , Frutas/química , Camundongos , OxirreduçãoRESUMO
BACKGROUND: Pineapple is the fruit of Ananas comosus var. comosus plant, being cultivated in tropical areas and has high energy content and nutritional value. Herein, 30 samples of pineapple cv. Vitória were analyzed as a function of the maturation stage (0-5) and their physico-chemical parameters monitored. In addition, negative-ion mode electrospray ionization mass spectrometry [ESI(-)FT-ICR MS] was used to identify and semi-quantify primary and secondary metabolites present in the crude and phenolic extracts of pineapple, respectively. RESULTS: Physico-chemical tests show an increase in the total soluble solids (TSS) values and in the TSS/total titratable acidity ratio as a function of the maturity stage, where a maximum value was observed in stage 3 (¾ of the fruit is yellow, which corresponds to the color of the fruit peel). ESI(-)FT-ICR MS analysis for crude extracts showed the presence mainly of sugars as primary metabolites present in deprotonated molecule form ([M - H]- and [2 M - H]- ions) whereas, for phenolic fractions, 11 compounds were detected, being the most abundant in the third stage of maturation. This behavior was confirmed by quantitative analysis of total polyphenols. CONCLUSION: ESI-FT-ICR MS was efficient in identifying primary (carbohydrates and organic acids) and secondary metabolites (13 phenolic compounds) presents in the crude and phenolic extract of the samples, respectively. © 2017 Society of Chemical Industry.
Assuntos
Ananas/crescimento & desenvolvimento , Aromatizantes/química , Frutas/química , Extratos Vegetais/química , Espectrometria de Massas por Ionização por Electrospray/métodos , Ananas/química , Carboidratos/química , Cor , Frutas/crescimento & desenvolvimento , Polifenóis/químicaRESUMO
The juçara fruits (Euterpe edulis Martius), native to the Atlantic Forest, are rich in anthocyanins. To preserve the anthocyanins in juçara fruit pulp, this study aimed to evaluate the effectiveness of microencapsulation by spray drying and freeze drying with maltodextrin (dextrose equivalent 16.5 to 19.5) and gum arabic in different proportions. The obtained microparticles were characterized by quantifying the total polyphenol and anthocyanin contents, by performing differential scanning calorimetry, thermogravimetry, and infrared spectroscopy and by using scanning electron microscopy to analyze the morphology of the particles. The total amount of polyphenols in the fruit pulp was 750 ± 16.7 mg GAE/100 g of the freeze-dried sample. The total anthocyanins in the fruit pulp was 181.25 ± 5.36 (mg/100 g). The microparticles were formed by employing maltodextrin and gum arabic in a 1:1 proportion as the polymeric matrix; the mixtures of pulp and polymeric matrix were prepared in proportions of 2:3 and 2:1, preserving up to 83.69% of the anthocyanin content. Lyophilization of the 2:1 mixture resulted in an anthocyanin content of 116.89 ± 4.43 (mg/100 g), whereas lyophilization of the 2:3 mixture resulted in 151.68 ± 1.39 (mg/100 g) anthocyanin content, which did not differ from the value obtained by spray drying the 2:3 mixture (150.76 ± 5.79 (mg/100 g)). Thermal analyses showed that the microparticles obtained by freeze drying at a ratio of 2:3 presented greater resistance to degradation with increasing temperature. The incorporation of the pulp in the polymeric matrix was demonstrated by IR analyses. Microparticles obtained by freeze drying showed the formation of various-sized flakes, whereas those obtained by spray drying were spherical in shape. Microencapsulation is a possible alternative for improving the stability of the anthocyanins in this fruit.
Assuntos
Antocianinas/análise , Composição de Medicamentos , Euterpe/química , Goma Arábica/química , Polifenóis/análise , Polissacarídeos/química , Dessecação , Estabilidade de Medicamentos , Liofilização , Frutas/químicaRESUMO
Struthanthus vulgaris is probably the most common medicinal mistletoe plant in Brazil, and has been used in folk medicine as an anti-inflammatory agent and for cleaning skin wounds. Our proposal was to evaluate the anti-inflammatory activity of S. vulgaris ethanol leaf extract and provide further insights of how this biological action could be explained using in vitro and in vivo assays. In vitro anti-inflammatory activity was preliminarily investigated in lipopolysaccharide/interferon gamma-stimulated macrophages based on their ability to inhibit nitric oxide production and tumor necrosis factor-alpha. In vivo anti-inflammatory activity of S. vulgaris ethanol leaf extract was investigated in the mice carrageenan-induced inflammation air pouch model. The air pouches were inoculated with carrageenan and then treated with 50 and 100 mg/kg of S. vulgaris ethanol leaf extract or 1 mg/kg of dexamethasone. Effects on the immune cell infiltrates, pro- and anti-inflammatory mediators such as tumor necrosis factor-alpha, interleukin 1, interleukin 10, and nitric oxide, were evaluated. The chemical composition of S. vulgaris ethanol leaf extract was characterized by LC-MS/MS. In vitro S. vulgaris ethanol leaf extract significantly decreased the production of nitric oxide and tumor necrosis factor-alpha in macrophages and did not reveal any cytotoxicity. In vivo, S. vulgaris ethanol leaf extract significantly suppressed the influx of leukocytes, mainly neutrophils, protein exudation, nitric oxide, tumor necrosis factor-alpha, and interleukin 1 concentrations in the carrageenan-induced inflammation air pouch. In conclusion, S. vulgaris ethanol leaf extract exhibited prominent anti-inflammatory effects, thereby endorsing its usefulness as a medicinal therapy against inflammatory diseases, and suggesting that S. vulgaris ethanol leaf extract may be a source for the discovery of novel anti-inflammatory agents.
Assuntos
Anti-Inflamatórios/isolamento & purificação , Inflamação/tratamento farmacológico , Erva-de-Passarinho/química , Extratos Vegetais/uso terapêutico , Animais , Anti-Inflamatórios/uso terapêutico , Brasil , Carragenina , Linhagem Celular , Linhagem Celular Tumoral , Inflamação/induzido quimicamente , Ativação de Macrófagos , Macrófagos/efeitos dos fármacos , Macrófagos/imunologia , Masculino , Camundongos , Camundongos Endogâmicos C57BL , Fitoterapia , Extratos Vegetais/farmacologia , Extratos Vegetais/toxicidade , Folhas de Planta/química , Plantas MedicinaisRESUMO
Petroleum hydrocarbons are one of the primary organic chemicals found in water bodies, and the water-soluble fraction of petroleum (WSFP) may be responsible for much of the toxic effects. In the present study, genotoxicity assays and histopathological analysis of the gills were analyzed for two experimental protocols: 1) Juvenile Centropomus parallelus were exposed to different concentrations of WFSP (0%, 25%, 50% and 75%) for 96h; 2) A second fish group was exposed to 50% WFSP for 168h followed by a post-exposure period for 168h in clean water (recovery). The total benzene, toluene, ethyl benzene and xylene (BTEX) and polycyclic aromatic hydrocarbon (PAH) concentrations at time 0 were 254µgL-1 and 4.72µgL-1 in 25%; 552.9µgL-1 and 9.36µgL-1 in 50%; and 842.4µgL-1 and 9.97µgL-1 in 75% WSFP, respectively. Based on the alkaline comet assay, the damage index (DI) values of fish exposed to 25% WSFP for 96h were significantly higher than those in the control group, and in the micronucleus test, the higher damage values were found in fish exposed to 75% WSFP. Furthermore, this last genotoxic test showed recovery after 168h. At all concentrations of WSFP, several histopathological changes were observed, and overall, most of these changes observed in the gills were classified as proliferative changes and represented a protective mechanism against pollutant uptake. Based on the recovery experiment, the damage was also significantly reduced after recovery. Our results showed that short-term exposure to WSFP compounds triggered cellular alterations in C. parallelus, but total recovery did not occur with time. Additionally, the different periods of exposure were not sufficient to induce severe gill damage in C. parallelus. Moreover, this fish demonstrated its usefulness as a sentinel species.
Assuntos
Dano ao DNA , Perciformes/genética , Petróleo/toxicidade , Hidrocarbonetos Policíclicos Aromáticos/toxicidade , Poluentes Químicos da Água/toxicidade , Animais , Ensaio Cometa , Brânquias/efeitos dos fármacos , Brânquias/patologia , Testes para Micronúcleos , Testes de Mutagenicidade , SolubilidadeRESUMO
CONTEXT: Sambucus australis Cham. & Schltdl. (Adoxaceae) is used in Brazilian folk medicine to treat inflammatory disorders. OBJECTIVE: To evaluate the in vitro anti-inflammatory, antioxidant and antimicrobial properties of S. australis. MATERIALS AND METHODS: The anti-inï¬ammatory activity of ethanol extracts of the leaf and bark of S. australis (1-100 µg/mL) were studied in lipopolysaccharide/interferon γ stimulated murine macrophages RAW 264.7 cells (24 h incubation) by investigating the release of nitric oxide (NO) and tumour necrosis factor-alpha (TNF-α) and in the TNF-α-induced nuclear factor kappa (NF-κB) assay. Minimum inhibitory concentration (MIC) was determined by the microdilution test (24 h incubation). Antioxidant activity was determined by 2,2-diphenyl-1-picrylhydrazyl (DPPH), ferric reducing antioxidant power (FRAP) and the NO scavenging assays. Chemical composition was assessed by LC-MS/MS. RESULTS: Antioxidant activities in the DPPH (IC50 43.5 and 66.2 µg/mL), FRAP (IC50 312.6 and 568.3 µg/mL) and NO radical scavenging assays (IC50 285.0 and 972.6 µg/mL) were observed in the leaf and bark ethanol extracts, respectively. Solely the leaf extract showed significant inhibition of NO and TNF-α production in RAW264.7 cells at concentrations of 2 and 100 µg/mL, respectively, and suppression of TNF-α inhibition of NF-κB by 12.8 and 20.4% at concentrations of 50 and 100 µg/mL, respectively. The extract also exhibited antibacterial activity against Salmonella typhimurium (MIC 250 µg/mL) and Klebsiella pneumoniae (MIC 250 µg/mL). LC-MS/MS revealed the presence of chlorogenic acid and rutin as major compounds. DISCUSSION AND CONCLUSION: The results indicate that the ethanol leaf extract of S. australis exhibit prominent anti-inï¬ammatory effects.
Assuntos
Anti-Infecciosos/farmacologia , Anti-Inflamatórios/farmacologia , Antioxidantes/farmacologia , Klebsiella pneumoniae/efeitos dos fármacos , Macrófagos/efeitos dos fármacos , Extratos Vegetais/farmacologia , Salmonella typhimurium/efeitos dos fármacos , Sambucus/química , Animais , Anti-Infecciosos/química , Anti-Infecciosos/isolamento & purificação , Anti-Inflamatórios/química , Anti-Inflamatórios/isolamento & purificação , Antioxidantes/química , Antioxidantes/isolamento & purificação , Compostos de Bifenilo/química , Cloretos/química , Ácido Clorogênico/isolamento & purificação , Ácido Clorogênico/farmacologia , Relação Dose-Resposta a Droga , Etanol/química , Compostos Férricos/química , Células HEK293 , Humanos , Mediadores da Inflamação/metabolismo , Klebsiella pneumoniae/crescimento & desenvolvimento , Lipopolissacarídeos/farmacologia , Macrófagos/metabolismo , Camundongos , Testes de Sensibilidade Microbiana , NF-kappa B/genética , NF-kappa B/metabolismo , Óxido Nítrico/metabolismo , Oxirredução , Fitoterapia , Picratos/química , Casca de Planta , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Folhas de Planta , Plantas Medicinais , Células RAW 264.7 , Rutina/isolamento & purificação , Rutina/farmacologia , Salmonella typhimurium/crescimento & desenvolvimento , Solventes/química , Células Swiss 3T3 , Transfecção , Fator de Necrose Tumoral alfa/metabolismoRESUMO
CONTEXT: The resin from the trunk wood of Virola oleifera (Schott) A. C. Smith (Myristicaceae) is used in folk medicine to hasten wound repair and to treat pain and inflammatory conditions, and our previous report indicated the anti-oxidative properties in other oxidative stress model. OBJECTIVE: To investigate the protective effects of resin from V. oleifera in two experimental models of gastric ulcer oxidative-stress dependent. MATERIALS AND METHODS: Plant material was collected and the resin was subjected to partitioning with organic solvents. The buthanol fraction was subjected to chromatographic and spectrometric methods for isolation and structural elucidation. The resin was quantified for polyphenols and flavonoids by colorimetric methods. Furthermore, the antioxidant activity of resin was determined by three different methods. The ulcers were induced acutely in Swiss male mice with ethanol/HCl and indomethacin using single-doses of 10 and 100 mg/kg. The gastroprotection of the experimental groups was comparable to reference control lansoprazole (3 mg/kg). RESULTS: The high content of polyphenols (â¼82%) and the presence of epicatechin and eriodictyol were determined. The LD50 was estimated at 2500 mg/kg. At minimum (10 mg/kg) and maximum (100 mg/kg) dosage of resin, both in ethanol/HCl as indomethacin ulcer induction models demonstrate reduction of lesions (minimum: â¼97% and â¼66%; maximum: â¼95% and â¼59%). DISCUSSION: The gastroprotection might be related to tannins, phenolic acids and flavonoids present in the resin by antioxidant properties. CONCLUSIONS: The results indicate that this resin has gastroprotective activity probably associated with the presence of phenolic antioxidant substances.
Assuntos
Antioxidantes/farmacologia , Mucosa Gástrica/efeitos dos fármacos , Myristicaceae/química , Extratos Vegetais/farmacologia , Resinas Vegetais/farmacologia , Úlcera Gástrica/prevenção & controle , Animais , Antiulcerosos/química , Antiulcerosos/isolamento & purificação , Antiulcerosos/farmacologia , Antiulcerosos/toxicidade , Antioxidantes/química , Antioxidantes/isolamento & purificação , Antioxidantes/toxicidade , Benzotiazóis/química , Cromatografia em Camada Fina , Modelos Animais de Doenças , Etanol , Flavonoides/isolamento & purificação , Flavonoides/farmacologia , Mucosa Gástrica/patologia , Ácido Clorídrico , Indometacina , Dose Letal Mediana , Masculino , Camundongos , Fitoterapia , Casca de Planta , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Extratos Vegetais/toxicidade , Plantas Medicinais , Polifenóis/isolamento & purificação , Polifenóis/farmacologia , Resinas Vegetais/química , Resinas Vegetais/isolamento & purificação , Resinas Vegetais/toxicidade , Solventes/química , Espectrometria de Massas por Ionização por Electrospray , Úlcera Gástrica/induzido quimicamente , Úlcera Gástrica/patologia , Ácidos Sulfônicos/química , Espectrometria de Massas em TandemRESUMO
CONTEXT: Orange Jessamine [Murraya paniculata L. (Rutaceae)] has been used worldwide in folk medicine as an anti-inflammatory, antibiotic and analgesic. OBJECTIVE: The objective of this study is to investigate the in vitro antioxidant, cytotoxic, antibacterial and antifungal activity and the time-kill curve studies of orange jessamine essential oil and ß-caryophyllene, as well as the chemical composition of the essential oil. MATERIAL AND METHODS: The cytotoxic activity of M. paniculata and ß-caryophyllene (7.8-500 µg/mL) was evaluated using the MTT assay on normal fibroblasts and hepatoma cells. The minimal inhibitory concentration and time-kill curves (24 h) were evaluated against those of Staphylococcus aureus, Escherichia coli, Salmonella typhimurium, Enterococcus faecallis, Aspergillus (niger, fumigates and parasiticum) and F. solani by the broth microdilution method. The antioxidant activity was measured by the DPPH and ABTS assays. Chemical composition was evaluated by GC/MS analyses. RESULTS: GC/MS analyses identified 13 compounds, with ß-caryophyllene as the major compound. The oil exhibited moderate antibacterial activity (MIC <1.0 mg/mL) and strong antifungal activity. Time-kill curve studies showed that either the essential oil or ß-caryophyllene presented rapid bacterial killing (4 h for S. aureus) and fungicidal effect (2-4 h for F. solani); however, both displayed weak free radical scavenger capacity. The cytotoxic activity exhibited a prominent selective effect against hepatoma cancer cells (IC50 value =63.7 µg/mL) compared with normal fibroblasts (IC50 value =195.0 µg/mL), whereas the ß-caryophyllene showed low cytotoxicity. DISCUSSION AND CONCLUSION: The experimental data suggest that the activities of M. paniculata essential oil are due to the synergistic action among its components.
Assuntos
Antibacterianos/farmacologia , Antifúngicos/farmacologia , Antineoplásicos Fitogênicos/farmacologia , Carcinoma Hepatocelular/tratamento farmacológico , Fusarium/efeitos dos fármacos , Neoplasias Hepáticas/tratamento farmacológico , Murraya/química , Óleos Voláteis/farmacologia , Extratos Vegetais/farmacologia , Óleos de Plantas/farmacologia , Sesquiterpenos/farmacologia , Staphylococcus aureus/efeitos dos fármacos , Animais , Antibacterianos/isolamento & purificação , Antifúngicos/isolamento & purificação , Antineoplásicos Fitogênicos/isolamento & purificação , Antioxidantes/isolamento & purificação , Antioxidantes/farmacologia , Carcinoma Hepatocelular/patologia , Linhagem Celular Tumoral , Sobrevivência Celular/efeitos dos fármacos , Relação Dose-Resposta a Droga , Fibroblastos/efeitos dos fármacos , Fibroblastos/patologia , Fusarium/crescimento & desenvolvimento , Cromatografia Gasosa-Espectrometria de Massas , Concentração Inibidora 50 , Neoplasias Hepáticas/patologia , Camundongos , Testes de Sensibilidade Microbiana , Óleos Voláteis/isolamento & purificação , Fitoterapia , Extratos Vegetais/isolamento & purificação , Folhas de Planta , Óleos de Plantas/isolamento & purificação , Plantas Medicinais , Sesquiterpenos Policíclicos , Sesquiterpenos/isolamento & purificação , Staphylococcus aureus/crescimento & desenvolvimento , Células Swiss 3T3 , Fatores de TempoRESUMO
Searches related to global warming have provided important insights into the response of terrestrial ecosystems, but few have examined the impacts on agricultural crops, particularly those associated with the monitoring of agrotoxin residues. In this context, the agriclimatological zoning is an important tool in the planning and consolidation of crops and should be considered in any initiative that involves such planning. This tool is particularly important in the analysis of agrotoxin residues and may be applied by the Program Analysis of Agrotoxin Residues in Food (PARA) created by the National Health Vigilance Agency of Brazil (ANVISA), which enables greater food security and contributes to the improvement of human health. The aim of this study was to elaborate the current and future agriclimatological zoning for the tomato crop, relating it with the monitoring of samples collected by PARA in Espírito Santo State, Brazil. The results indicate that a temperature increase of 5 °C creates a decrease in apt areas from 37.3% to 4.3%, for a total reduction of 33 percentage points (-88.5%). It is noted that of the 41 producing municipalities, only 26 have apt areas greater than 50%, highlighting the municipalities with apt areas greater than 90%, represented by Mantenópolis (100%), Guaçuí (98.5%), São José do Calçado (97.8%), Irupi (94.4%), Santa Teresa (92.3%), and Marechal Floriano (91.4%). The veracity of agriclimatological zoning is proved by a Kendall rank correlation coefficient of 0.876, indicating that the distribution of the variables of apt areas and productivity are similar at the significance level of 0.05 with a confidence interval 95%. After validation of the agriclimatological zoning for the tomato crop, it is recommended that the PARA should monitor 36 municipalities rather than the current 18, representing an increase of 100%. The methodology can be adjusted to agricultural crops of other countries.
Assuntos
Produtos Agrícolas , Contaminação de Alimentos/análise , Sistemas de Informação Geográfica , Solanum lycopersicum , Brasil , Ecossistema , Monitoramento Ambiental , Análise de Alimentos/métodos , Aquecimento GlobalRESUMO
CONTEXT: Struthanthus vulgaris (Vell.) Mart. (Loranthaceae) has been widely used in traditional medicine in Brazil to bathe wounds. OBJECTIVE: The objective of this study is to investigate the in vitro wound healing effects, together with the antioxidant and antimicrobial activities of S. vulgaris leaf and branch extracts. MATERIAL AND METHODS: Ethanol leaf and branch extracts of S. vulgaris were investigated at 1-100 µg/ml concentrations in the scratch assay after 14 h. Antioxidant activity was investigated using the 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical-scavenging assay, and the antibacterial activity was tested at concentrations up to 1000 µg/ml against Gram-positive and Gram-negative bacteria by the microdilution test after 24 h. The total phenolic and flavonoid contents were determined by colorimetric methods. RESULTS: Struthanthus vulgaris leaf and branch extracts at 100 µg/ml concentration stimulated migration and proliferation of fibroblasts and enhanced cell numbers by 56.2% and 18.6%, respectively. Antioxidant activity exhibited IC50 values of 24.3 and 18.9 µg/ml for the leaf and branch extracts, respectively. The ethanol leaf extract showed antimicrobial activity against the Gram-positive Staphylococcus mutans and Staphylococcus aureus bacteria, exhibiting minimum inhibitory concentration values of 125 and 500 µg/ml, respectively. An appreciable total phenolic content in the leaves (813.6 ± 2.7 mg/g) and branches (462.8 ± 9.6 mg/g), and relatively low concentration of flavonoids in the leaves (13.3 ± 4.3 mg/g) and branches (1.9 ± 0.2 mg/g), was detected. DISCUSSION AND CONCLUSION: The antioxidant and antibacterial activities, together with the strong ability to stimulate proliferation and migration of fibroblasts, provide some support for the traditional use of S. vulgaris.
Assuntos
Antibacterianos/farmacologia , Antioxidantes/farmacologia , Loranthaceae/química , Extratos Vegetais/farmacologia , Cicatrização/efeitos dos fármacos , Animais , Antibacterianos/isolamento & purificação , Antioxidantes/isolamento & purificação , Compostos de Bifenilo/química , Linhagem Celular , Movimento Celular/efeitos dos fármacos , Proliferação de Células/efeitos dos fármacos , Sobrevivência Celular/efeitos dos fármacos , Fibroblastos/efeitos dos fármacos , Bactérias Gram-Negativas/efeitos dos fármacos , Bactérias Gram-Positivas/efeitos dos fármacos , Humanos , Testes de Sensibilidade Microbiana , Picratos/química , Extratos Vegetais/isolamento & purificação , Folhas de Planta/química , Caules de Planta/químicaRESUMO
Pharmaceuticals are emerging contaminants and it must be noted that approximately 70 % of them are excreted via urine. Therefore, urine usage implies the risk of transfer of pharmaceutical residues to agricultural fields and environment contamination. Thus, this study aimed on the development and validation of a LC-MS/MS method for D-norgestrel (D-NOR) and progesterone (PRO) determination in human urine, as well as the evaluation of the removal efficiency of two methods (storage and evaporation), and the effects of acidification with sulfuric acid. The storage process was evaluated for 6 weeks, while the evaporation was assessed at three different temperatures (50, 75, and 100 °C). All experiments were done with normal urine (pH = 6.0) and acidified urine (pH = 2.0, with sulfuric acid). The results of validation showed good method efficiency. In the second week of storage, higher hormone degradation was observed. In the evaporation method, both D-NOR and PRO were almost completely degraded when the volume was reduced to the lowermost level. Results also indicate that acidification did not affect degradation. Overall, the results showed that combination of two methods can be employed for more efficient hormone removal in urine.
Assuntos
Monitoramento Ambiental/métodos , Levanogestrel/isolamento & purificação , Progesterona/isolamento & purificação , Urina/química , Adulto , Cromatografia Líquida , Voluntários Saudáveis , Humanos , Levanogestrel/urina , Limite de Detecção , Masculino , Progesterona/urina , Reprodutibilidade dos Testes , Manejo de Espécimes , Espectrometria de Massas em Tandem/métodos , Temperatura , Volatilização , Adulto JovemRESUMO
The aims of this study were to evaluate the antihypertensive effects of the standardised methanolic extract of Carica papaya, its angiotensin converting enzyme inhibitory effects in vivo, its effect on the baroreflex and serum angiotensin converting enzyme activity, and its chemical composition. The chemical composition of the methanolic extract of C. papaya was evaluated by liquid chromatography-mass/mass and mass/mass spectrometry. The angiotensin converting enzyme inhibitory effect was evaluated in vivo by Ang I administration. The antihypertensive assay was performed in spontaneously hypertensive rats and Wistar rats that were treated with enalapril (10 mg/kg), the methanolic extract of C. papaya (100 mg/kg; twice a day), or vehicle for 30 days. The baroreflex was evaluated through the use of sodium nitroprusside and phenylephrine. Angiotensin converting enzyme activity was measured by ELISA, and cardiac hypertrophy was evaluated by morphometric analysis. The methanolic extract of C. papaya was standardised in ferulic acid (203.41 ± 0.02 µg/g), caffeic acid (172.60 ± 0.02 µg/g), gallic acid (145.70 ± 0.02 µg/g), and quercetin (47.11 ± 0.03 µg/g). The flavonoids quercetin, rutin, nicotiflorin, clitorin, and manghaslin were identified in a fraction of the extract. The methanolic extract of C. papaya elicited angiotensin converting enzyme inhibitory activity. The antihypertensive effects elicited by the methanolic extract of C. papaya were similar to those of enalapril, and the baroreflex sensitivity was normalised in treated spontaneously hypertensive rats. Plasma angiotensin converting enzyme activity and cardiac hypertrophy were also reduced to levels comparable to the enalapril-treated group. These results may be associated with the chemical composition of the methanolic extract of C. papaya, and are the first step into the development of a new phytotherapic product which could be used in the treatment of hypertension.