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2.
Braz J Biol ; 83: e275046, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-37851774

RESUMO

Sugarcane is one of the largest agricultural commodities when considering the export volume and the number of jobs generated. Sugarcane production in the Brazilian Northeast region is generally low due to several factors, including the irregular rainfall distribution, which highlights the importance of studies aimed at mitigating the deleterious effects of water stress. In this scenario, this study aimed to evaluate calcium pyruvate as a water deficit attenuator on the agro-industrial quality of sugarcane in the second cycle of cultivation. The experiment was conducted out under greenhouse conditions of the Federal University of Campina Grande, where five sugarcane commercial genotypes tested (G1- RB863129, G2- RB92579, G3- RB962962, G4- RB021754, and G5- RB041443) and three irrigation management strategies (E1- full irrigation, E2- water deficit with application of 30 mM of calcium pyruvate, and E3- water deficit without calcium pyruvate application), distributed in randomized blocks in 5 × 3 factorial arrangement with three replications. The RB021754 genotype under water deficit and without foliar application of calcium pyruvate increased the fiber content (13.2%) and the sugarcane moist cake weight (143.5 g). The effects of water deficit in sugarcane genotypes are attenuated by the exogenous application of 30 mM of calcium pyruvate, with benefits on the polarized sucrose content, apparent sucrose content of the juice, soluble solids content, purity, corrected cane POL, total recoverable sugars, and stem mass in relation to plants under water deficit without calcium pyruvate application.


Assuntos
Saccharum , Saccharum/genética , Cálcio , Genótipo , Grão Comestível , Sacarose , Piruvatos
3.
Braz J Biol ; 83: e272853, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-37672435

RESUMO

The aim of this study was to determine the acute toxicity of the essential oils (EOs) of Aloysia triphylla, Lippia gracilis and Piper aduncum in juvenile tambaqui (Colossoma macropomum), and evaluate the possible histopathological alterations in their gills. For the acute toxicity tests, juvenile tambaqui (n=24/treatment) were distributed in six treatments with three replicates, which comprised the control and five EO concentrations of A. triphylla (60, 80, 100, 120 and 140 mg L-1), L. gracilis (35, 40, 45, 50 and 55 mg L-1) and P. aduncum (42.5, 45, 47.5, 50 and 52.5 mg L-1), with an exposure period of 4 h. The mortality rate and severity of damage to the tambaqui gills were proportional to the increase in the concentration of the EO, with LC50-4 h values estimated at 109.57 mg L -1 for A. triphylla, 41.63 mg L -1 for L. gracilis and 48.17 mg L -1 for P. aduncum. The main morphological damages observed in the gills of the tambaqui exposed to the three EOs, were Grade I: hypertrophy and hyperplasia of lamellar epithelial cells, lamellar fusion, epithelial detachment, capillary dilation and constriction, proliferation of chloride cells and mucosal cells and edema; in low frequency Grade II damage as epithelial rupture and lamellar aneurysm. Necrosis (Grade III damage) was observed only in gill lamellae exposed to P. aduncum EO (47.5, 50.0 and 52.5 mg L-1). Concentrations of EOs below LC50-4 h can be used sparingly, for short periods of exposure for the treatment of diseases in tambaqui breeding.


Assuntos
Caraciformes , Lippia , Óleos Voláteis , Verbenaceae , Animais , Óleos Voláteis/toxicidade , Melhoramento Vegetal
4.
Rev. chil. nutr ; 50(3)jun. 2023.
Artigo em Espanhol | LILACS-Express | LILACS | ID: biblio-1515180

RESUMO

La composición química del aceite de oliva extra virgen (AOEV) se compone principalmente de triglicéridos, ácidos grasos insaturados como ácido oleico, ácido linoleico y el α-linolénico. También se destacan compuestos fenólicos de tres clases químicas: simples, secoiridoides y lignanos. En la presente revisión se analizó el consumo del AOEV en enfermedades crónicas, ciertos tipos de cáncer y en enfermedades neurodegenerativas. La evidencia muestra que el consumo de entre 8 y 40 g de AOEV diario tiene efectos protectores en enfermedades cardiovasculares, puede evitar la aparición de diabetes tipo 2 y aumentar los niveles de colesterol HDL. Respecto al cáncer, entre los efectos evaluados se destacan los encontrados a partir de los compuestos fenólicos hidroxitirosol (HT) y oleocantal, los que han demostrado un efecto protector en algunos tipos de cáncer como cáncer de piel y de mama. En las enfermedades neurodegenerativas, se observó que el consumo diario de 50 g de AOEV, tiene un efecto inhibidor en la degeneración neuronal atribuido a sus compuestos fenólicos como oleuropeina e HT. Investigaciones a futuro debieran enfocarse en determinar los efectos a largo plazo del consumo de AOEV en las diferentes enfermedades analizadas, para así poder ir estableciendo la "dosis" de AOEV que permita obtener resultados protectores sobre la salud. Además de explorar los efectos de las diferentes variedades de aceitunas (con sus componentes bioactivos particulares) con el fin de establecer los efectos en la salud y enfermedad asociados a variedades específicas.


The chemical composition of extra virgin olive oil (EVOO) is mainly composed of triglycerides, unsaturated fatty acids such as oleic acid, linoleic acid, and α-linolenic acid. Phenolic compounds of three chemical classes are also relevant, such as simple, secoiridoids, and lignans. Here, we review the association between EVOO consumption and chronic diseases, certain types of cancer, and neurodegenerative diseases. Evidence shows that consuming between 8 and 40 g of EVOO / day has protective effects on cardiovascular diseases, can prevent the onset of type 2 diabetes, and increases HDL cholesterol levels. Regarding cancer, phenolic compounds hydroxytyrosol (HT) and oleocanthal have protective effects on some types of cancer, such as skin and breast cancer. Regarding neurodegenerative diseases, daily consumption of phenolic compounds such as oleuperin and hydroxytyrosol and 50 g of EVOO has an inhibitory effect on neuronal degeneration and a protective effect on neuroprotective capacity. Future research should focus on determining the long-term impact of EVOO consumption on different diseases to establish the "dose" of EVOO that will allow health-protective results. It is also necessary to establish the effects of the specific olives (with their particular bioactive components) to establish the different impacts on health and disease associated with olives varieties.

5.
Vet Parasitol ; 290: 109362, 2021 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-33524780

RESUMO

Nematicide combinations may be a valid strategy to achieve effective nematode control in the presence of drug resistance. The goal of the current trial was to evaluate the pharmaco-parasitological performance of the moxidectin (MOX) and levamisole (LEV) combination after four years of continuous use in lambs naturally parasitized with multi-resistant gastrointestinal nematodes. At the beginning of the trial, 40 lambs were divided into four groups (n = 10), which were untreated (control) or subcutaneously treated with MOX (0.2 mg/kg), LEV (8 mg/kg) or with the combination MOX + LEV (administered separately at 0.2 and 8 mg/kg, respectively). Blood samples were collected at different times post-treatment and LEV and MOX plasma concentrations were measured by HPLC. The clinical efficacy of the continuous use of MOX + LEV combination was assessed with the controlled efficacy test (CET), performed at the beginning and end of the study, and with the faecal egg count reduction (FECR) test, performed over the four-year study period. No significant adverse pharmacokinetic changes were observed either for MOX or LEV after their co-administration to infected lambs. The CET (first year) showed efficacies of 84.3 % (Haemonchus contortus), 100 % (Teladorsagia circumcincta and Trichostrongylus axei), and 97.4 % (T. colubriformis). After the repetitive use of the combined treatment for four years, those efficacies remained high (100 %) and only decreased to 58 % against T. colubriformis. The evaluation of the FECR over the study period showed fluctuations in the performance of the combined administration. The initial FECR (2014) was 99 % (MOX), 85 % (LEV) and 100 % (MOX + LEV). The co-administration of MOX + LEV during the four-year experimental period resulted in a significantly higher anthelmintic effect (87 %) than that of MOX (42 %) or LEV (69 %) given alone. The combined use of MOX + LEV to control resistant gastrointestinal nematodes appears to be a valid strategy under specific management conditions. A high initial therapeutic response to the combination would be a relevant feature for the success of this tool.


Assuntos
Levamisol/uso terapêutico , Macrolídeos/uso terapêutico , Nematoides/efeitos dos fármacos , Infecções por Nematoides/veterinária , Doenças dos Ovinos/tratamento farmacológico , Animais , Anti-Helmínticos/administração & dosagem , Anti-Helmínticos/uso terapêutico , Área Sob a Curva , Esquema de Medicação , Combinação de Medicamentos , Resistência a Múltiplos Medicamentos , Feminino , Meia-Vida , Levamisol/administração & dosagem , Levamisol/farmacocinética , Macrolídeos/administração & dosagem , Macrolídeos/farmacocinética , Masculino , Infecções por Nematoides/tratamento farmacológico , Infecções por Nematoides/parasitologia , Ovinos , Doenças dos Ovinos/parasitologia
6.
J Public Health (Oxf) ; 43(3): 493-498, 2021 Sep 22.
Artigo em Inglês | MEDLINE | ID: mdl-33501982

RESUMO

BACKGROUND: To design better measures to contain the Covid-19 epidemics, it is relevant to know whether socioeconomic factors are associated with a higher risk of death by Covid-19. This work estimates the effects of individual socioeconomic characteristics on the risk of death by Covid-19. METHODS: Logistic models were estimated to assess the effect of socioeconomic characteristics (income, race/ethnicity, schooling, occupation and economic activity) on the risk of death from Covid-19. For this purpose, Covid-19 individual death records in Rio de Janeiro state, Brazil were combined with the Annual Register of Social Information, which contains socioeconomic information about formal workers. FINDINGS: Workers employed in establishments in the health and public safety sectors present a risk of dying 2.46 and 2.25 times higher than those employed in other activities. Non-white people, men, and those who work in the Metropolitan Region are also more likely to die from Covid-19. People with higher education are 44% less likely to die from the disease. CONCLUSIONS: Some population groups are more vulnerable to the Covid-19 pandemic and individual socioeconomic conditions play a relevant role in the probability of death by the disease. That should be considered in the design of prevention policies to be adopted.


Assuntos
COVID-19 , Pandemias , Brasil/epidemiologia , Humanos , Modelos Logísticos , Masculino , SARS-CoV-2 , Fatores Socioeconômicos
7.
Neurobiol Learn Mem ; 166: 107101, 2019 12.
Artigo em Inglês | MEDLINE | ID: mdl-31629785

RESUMO

Extinction is the learned inhibition of retrieval of a previously acquired memory and is a major component of exposure therapy, which has attracted much attention because of the use in the treatment of drug addiction, phobias and particularly fear disorders such as post-traumatic stress disorder (PTSD). Exposure to a novel environment before or after extinction training can enhance the extinction of contextual fear conditioning, however the cellular and molecular substrates are still unclear. Here, we investigated the participation of H2-histaminergic, ß-adrenergic and 5-HT1A-serotonergic receptors of the hippocampus on the enhancement of extinction memory caused by novelty. The infusion into the CA1 region of the serotonin 5-HT1A-receptor agonist, 8-OH-DPAT and the ß-adrenergic blocker, Timolol, after the exposure to the novelty hindered the enhancement of extinction by novelty, while Timolol also hindered the extinction consolidation when infused post-extinction. These impairments were abolished by the coinfusion of 8-OH-DPAT plus the 5-HT1A receptor antagonist, NAN-190 and Timolol plus ß-adrenergic agonist, Isoproterenol. However, Dimaprit and Ranitidine blocked the retrieval of CFC, but did not prevented the extinction learning. Here we elucidated some of the molecular mechanisms that are involved on the enhancement of extinction by novelty, demonstrating that the ß-adrenoreceptors and 5-HT1A serotonergic receptors participate on this process alongside with dopaminergic D1 receptors previously described, while histamine H2 receptors, so ubiquitous in learning-related functions in hippocampus are not involved.


Assuntos
Agonistas Adrenérgicos beta/farmacologia , Antagonistas Adrenérgicos beta/farmacologia , Aprendizagem por Associação/efeitos dos fármacos , Extinção Psicológica/efeitos dos fármacos , Medo/efeitos dos fármacos , Hipocampo/efeitos dos fármacos , Agonistas do Receptor de Serotonina/farmacologia , 8-Hidroxi-2-(di-n-propilamino)tetralina/farmacologia , Animais , Condicionamento Clássico/efeitos dos fármacos , Isoproterenol/farmacologia , Masculino , Ratos Wistar , Timolol/farmacologia
8.
Arq. bras. med. vet. zootec. (Online) ; 71(2): 577-583, mar.-abr. 2019. tab, ilus
Artigo em Português | LILACS, VETINDEX | ID: biblio-1011252

RESUMO

O objetivo do presente estudo foi correlacionar os valores de reticulócitos pontilhados e agregados obtidos por metodologia manual com a metodologia automática de contagem de reticulócitos totais em amostras de sangue de gatos anêmicos, analisados em um contador hematológico com citometria de fluxo. Para isso, 40 amostras de sangue de pacientes felinos anêmicos, independentemente de idade e sexo, foram utilizadas para a determinação das contagens absolutas de reticulócitos totais pela metodologia automatizada por citometria de fluxo fluorescente e pela técnica manual com corante supravital, em duplicata. Na contagem manual, houve a discriminação entre reticulócitos pontilhados e agregados. Para a correlação entre os métodos, foi realizada a análise de regressão de Passing-Bablok. A média do hematócrito dos gatos foi de 15,25%, tendo a maioria dos gatos (32,5%) apresentado anemia moderada (hematócrito = 17,81%). Como resultados, a análise de regressão demonstrou que a correlação entre a contagem absoluta total automática foi superior à contagem manual de reticulócitos agregados (rho= 0,71; P<0,001) do que a contagem absoluta de reticulócitos pontilhados (rho= 0,68; P<0,001). Os resultados apresentados sugerem que a contagem de reticulócitos total absoluta realizada pelo analisador hematológico ProCyte Dx em gatos anêmicos se refere à contagem absoluta de reticulócitos. Dessa maneira, recomenda-se que os valores possam ser utilizados para a avaliação imediata da condição hematológica de gatos anêmicos.(AU)


The aim of this study was to correlate the punctate and aggregated reticulocytes values obtained by manual methodology and the automatic reticulocyte count in 40 blood samples from anemic cats. Total reticulocyte absolute counts were determined by automated fluorescence flow cytometry and manual methods in 40 blood samples obtained from anemic cats. The manual count was obtained by supravital stain in duplicate to each sample and the reticulocyte morphology were discriminated between punctate and aggregates reticulocytes. Passing-Bablok regression analysis was utilized to compare the methods. Most samples were from anemic cat (15,25%) and the hematocrit mean was 17,81%. Regression analysis showed that the correlation between the absolute total automatic counts is higher with aggregated reticulocytes (rho= 0,71; P< 0,001) than with absolute punctate reticulocytes counts (rho= 0, 68, P< 0.001). Results suggest that the ProCyte Dx reticulocytes count in anemic cats is correlated with aggregate reticulocyte count. Thus, the greater amount of RNA and organelles in aggregate reticulocytes generates a cellular complexity and, therefore, greater impregnation of the dye in an automatic count. Thus, the values obtained by the hematologic instrument can be used for the immediate evaluation of the hematological condition in anemic cats.(AU)


Assuntos
Animais , Gatos , Doenças do Gato/sangue , Anemia/veterinária , Leucemia Felina/sangue , Contagem de Reticulócitos/veterinária , Citometria de Fluxo/veterinária
9.
Purinergic Signal ; 14(2): 167-176, 2018 06.
Artigo em Inglês | MEDLINE | ID: mdl-29541926

RESUMO

Diabetes mellitus is characterized by increased levels of reactive oxygen species (ROS), leading to high levels of adenosine triphosphate (ATP) and the activation of purinergic receptors (P2X7), which results in cell death. Klotho was recently described as a modulator of oxidative stress and as having anti-apoptotic properties, among others. However, the roles of P2X7 and klotho in the progression of diabetic nephropathy are still unclear. In this context, the aim of the present study was to characterize P2X7 and klotho in several stages of diabetes in rats. Diabetes was induced in Wistar rats by streptozotocin, while the control group rats received the drug vehicle. From the 1st to 8th weeks after the diabetes induction, the animals were placed in metabolic cages on the 1st day of each week for 24 h to analyze metabolic parameters and for the urine collection. Then, blood samples and the kidneys were collected for biochemical analysis, including Western blotting and qPCR for P2X7 and klotho. Diabetic rats presented a progressive loss of renal function, with reduced nitric oxide and increased lipid peroxidation. The P2X7 and klotho expressions were similar up to the 4th week; then, P2X7 expression increased in diabetes mellitus (DM), but klotho expression presented an opposite behavior, until the 8th week. Our data show an inverse correlation between P2X7 and klotho expressions through the development of DM, which suggests that the management of these molecules could be useful for controlling the progression of this disease and diabetic nephropathy.


Assuntos
Diabetes Mellitus Experimental/metabolismo , Nefropatias Diabéticas/metabolismo , Glucuronidase/metabolismo , Receptores Purinérgicos P2X7/metabolismo , Animais , Progressão da Doença , Proteínas Klotho , Masculino , Ratos , Ratos Wistar
10.
J Vet Pharmacol Ther ; 41(1): 83-91, 2018 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-28695609

RESUMO

The goals of the current study were to evaluate the potential pharmacokinetic (PK) interactions and the clinical efficacy occurring after the subcutaneous (s.c.) administration of ricobendazole (RBZ) and levamisole (LEV) given both separately and co-administered to calves naturally infected with susceptible gastrointestinal nematodes. The clinical efficacy was shown in two seasons, winter and spring, with predominance of different nematode populations. Groups of 15 calves were treated with RBZ alone, LEV alone and RBZ + LEV combination, and an untreated group was kept as a Control. RBZ and LEV plasma concentrations were quantified by HPLC. The clinical efficacy was determined by the faecal egg count reduction test. RBZ and LEV have similar plasma persistence, being detected in plasma over 24 hr post-treatment. No PK interactions were observed after the combined treatment, with similar PK parameters (p > .05) obtained for the single-drug and the combination-based strategy. In winter, the observed clinical efficacies were 96%, 99% and 100% for groups treated with RBZ, LEV and RBZ + LEV, respectively; however, in spring, the efficacies were 95%, 93% and 96% for the same groups. Remarkably, the combination was the only treatment that achieved 100% clinical efficacy against both Haemonchus spp and Ostertagia spp in winter; but the increased presence of Ostertagia spp. in spring (28% in untreated group) determined a tendency to reduced efficacies compared to winter time (only 10% of Ostertagia spp. in untreated group), even for the combined treatment. Overall, in a scenario where the nematode population is susceptible, the RBZ + LEV treatment may be a valid combination in cattle to delay the development of resistance, especially in winter when this combination achieved 100% of efficacy. Thus, selection of anthelmintic resistance will never occur. In fact, this is one of the greatest challenges for the whole cattle production system: to be one step ahead of anthelmintic resistance.


Assuntos
Albendazol/análogos & derivados , Antinematódeos/uso terapêutico , Levamisol/uso terapêutico , Albendazol/administração & dosagem , Albendazol/sangue , Albendazol/uso terapêutico , Animais , Antinematódeos/administração & dosagem , Bovinos , Doenças dos Bovinos/tratamento farmacológico , Doenças dos Bovinos/parasitologia , Quimioterapia Combinada/veterinária , Hemoncose/tratamento farmacológico , Hemoncose/veterinária , Haemonchus/efeitos dos fármacos , Injeções Subcutâneas/veterinária , Levamisol/administração & dosagem , Levamisol/sangue , Masculino , Ostertagia/efeitos dos fármacos , Ostertagíase , Contagem de Ovos de Parasitas/veterinária , Estações do Ano
11.
Mar Pollut Bull ; 123(1-2): 291-303, 2017 Oct 15.
Artigo em Inglês | MEDLINE | ID: mdl-28847632

RESUMO

References areas are sites that have undergone little or no anthropogenic impact and therefore represent the natural state of an environment. The objective of this study was to test if the Camamu Bay (CB), Bahia, can be used as a reference area for tropical coastal environments. Trace and major elements, polycyclic aromatic hydrocarbons (PAH), and the structure of the benthic macrofauna were determined. To compare the studied sites and identify the possible occurrence of anomalous concentrations, trace elements were normalized by Al and linear regressions were also performed. For all trace elements (except Cu), regressions showed a significant correlation (p<0.05) and few outliers (<3% of cases), showing that the concentrations found represent natural values for this bay. In the case of Cu, the highest concentrations were found near small municipalities, which may be associated with domestic sewage. About 60% of the organic compounds occurred at levels below the limit of quantification (<0.26ngg-1). The sum of PAHs was low for all stations, ranging from 1.17 to 313ngg-1. The benthic assemblages also indicated that the CB is a healthy, well-preserved ecosystem that deserves conservation efforts. The integrated use of geochemical and biotic data supported the use of CB as a reference area. Capsule: Organic and inorganic contaminants together with macrobenthic assemblages indicated that Camamu Bay is a pristine, tropical reference area.


Assuntos
Monitoramento Ambiental/normas , Poluentes Químicos da Água/análise , Animais , Organismos Aquáticos , Baías , Brasil , Ecossistema , Monitoramento Ambiental/métodos , Metais/análise , Compostos Orgânicos/análise , Hidrocarbonetos Policíclicos Aromáticos/análise , Esgotos , Clima Tropical
12.
Ultrasonics ; 73: 1-8, 2017 01.
Artigo em Inglês | MEDLINE | ID: mdl-27592203

RESUMO

This work studies methods for efficient extraction and selection of features in the context of a decision support system based on neural networks. The data comes from ultrasonic testing of steel welded joints, in which are found three types of flaws. The discrete Fourier, wavelet and cosine transforms are applied for feature extraction. Statistical techniques such as principal component analysis and the Wilcoxon-Mann-Whitney test are used for optimal feature selection. Two different artificial neural network architectures are used for automatic classification. Through the proposed approach, it is achieved a high discrimination efficiency by using only 20 features to feed the classifier, instead of the original 2500 A-scan sample points.

13.
Arq. bras. med. vet. zootec ; 68(4): 967-976, jul.-ago. 2016. tab
Artigo em Português | LILACS, VETINDEX | ID: lil-792479

RESUMO

A urolitíase obstrutiva em pequenos ruminantes é uma doença metabólica de etiologia multifatorial com distribuição mundial. A elevação da concentração urinária de solutos, minerais ionizados (cristaloides) que formam cristais insolúveis é citada por alguns autores como o fator mais importante. Assim, o conhecimento do perfil mineral dos animais submetidos a dietas calculogênicas e a composição química dos urólitos tornam-se ferramentas eficazes na prevenção da doença. Neste estudo, foram utilizados 14 ovinos hígidos, machos (não castrados), da raça Santa Inês, com idade aproximada de 90 dias, distribuídos em dois grupos (G1 - sem vitamina C e G2 - com vitamina C) e alimentados com dieta calculogênica. A análise dos perfis minerais, séricos e urinários revelou completo desbalanceamento na relação entre concentrações de cálcio, fósforo e magnésio, havendo elevação expressiva do fósforo e do magnésio e diminuição substancial do cálcio. Com isso, a análise bioquímica dos urólitos demonstrou que o cálcio esteve presente em 50% das amostras analisadas.(AU)


Urolithiasis in small ruminants is a metabolic disease of multifactorial etiology with worldwide distribution. Increased urinary concentration of solutes, ionized minerals (crystalloid) that form insoluble crystals is cited by some authors as the most important factor. Thus, knowledge of mineral profile of the animals fed calculogenic diets and chemical composition of uroliths becomes an effective tool in preventing the disease. In this study, we used 14 healthy, male, non-neutered sheep, of the Santa Ines breed, aged approximately 90 days, divided into two groups (G1-without vitamin C and G2-with vitamin C) fed calculogenic diet. Analysis of mineral profiles in serum and urine revealed complete imbalance in the relationship between concentrations of calcium, phosphorus and magnesium, with significant increase of phosphorus and magnesium and substantial reduction of calcium. Thus, biochemical analysis of uroliths showed that calcium was present in 50% of samples.(AU)


Assuntos
Animais , Masculino , Ovinos , Urolitíase/veterinária , Coleta de Amostras Sanguíneas/veterinária , Testes Hematológicos/veterinária , Coleta de Urina/veterinária
14.
BMC Cancer ; 15: 807, 2015 Oct 27.
Artigo em Inglês | MEDLINE | ID: mdl-26503030

RESUMO

BACKGROUND: Malignant melanoma is an aggressive type of skin cancer, and despite recent advances in treatment, the survival rate of the metastatic form remains low. Nifuroxazide analogues are drugs based on the substitution of the nitrofuran group by benzofuroxan, in view of the pharmacophore similarity of the nitro group, improving bioavailability, with higher intrinsic activity and less toxicity. Benzofuroxan activity involves the intracellular production of free-radical species. In the present work, we evaluated the antitumor effects of different benzofuroxan derivatives in a murine melanoma model. METHODS: B16F10-Nex2 melanoma cells were used to investigate the antitumor effects of Benzofuroxan derivatives in vitro and in a syngeneic melanoma model in C57Bl/6 mice. Cytotoxicity, morphological changes and reactive oxygen species (ROS) were assessed by a diphenyltetrasolium reagent, optical and fluorescence microscopy, respectively. Annexin-V binding and mitochondrial integrity were analyzed by flow cytometry. Western blotting and colorimetry identified cell signaling proteins. RESULTS: Benzofuroxan N-Br and N-I derivatives were active against murine and human tumor cell lines, exerting significant protection against metastatic melanoma in a syngeneic model. N-Br and N-I induce apoptosis in melanoma cells, evidenced by specific morphological changes, DNA condensation and degradation, and phosphatidylserine translocation in the plasma membrane. The intrinsic mitochondrial pathway in B16F10-Nex2 cells is suggested owing to reduced outer membrane potential in mitochondria, followed by caspase -9, -3 activation and cleavage of PARP. The cytotoxicity of N-Br and N-I in B16F10-Nex2 cells is mediated by the generation of ROS, inhibited by pre-incubation of the cells with N-acetylcysteine (NAC). The induction of ROS by N-Br and N-I resulted in the inhibition of AKT activation, an important molecule related to tumor cell survival, followed by upregulation of BIM. CONCLUSION: We conclude that N-Br and N-I are promising agents aiming at cancer treatment. They may be useful in melanoma therapy as inducers of intrinsic apoptosis and by exerting significant antitumor activity against metastatic melanoma, as presently shown in syngeneic mice.


Assuntos
Proteínas Reguladoras de Apoptose/metabolismo , Apoptose/efeitos dos fármacos , Benzoxazóis/química , Benzoxazóis/uso terapêutico , Melanoma Experimental/metabolismo , Proteínas de Membrana/metabolismo , Proteína Oncogênica v-akt/metabolismo , Proteínas Proto-Oncogênicas/metabolismo , Animais , Antineoplásicos/química , Antineoplásicos/farmacologia , Antineoplásicos/uso terapêutico , Apoptose/fisiologia , Proteínas Reguladoras de Apoptose/antagonistas & inibidores , Proteína 11 Semelhante a Bcl-2 , Benzoxazóis/farmacologia , Linhagem Celular Tumoral , Células HeLa , Humanos , Masculino , Melanoma Experimental/tratamento farmacológico , Proteínas de Membrana/antagonistas & inibidores , Camundongos , Camundongos Endogâmicos C57BL , Proteína Oncogênica v-akt/antagonistas & inibidores , Proteínas Proto-Oncogênicas/antagonistas & inibidores , Transdução de Sinais/efeitos dos fármacos , Transdução de Sinais/fisiologia
15.
J Endocrinol Invest ; 38(10): 1065-74, 2015 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-25894865

RESUMO

PURPOSE: To analyze the impact of selenium supplementation on serum antiTPO levels and thyroid echogenicity in patients with CAT, evaluating the response in subgroups with different GPx1 genotypes. METHODS: CAT patients (n = 55) with positive antiTPO were randomized to selenomethionine (SeMet) 200 µg daily (n = 28) or placebo (n = 27) for 3 months. Assessments included GPx1 genotyping at baseline and serum levels of plasma selenium, erythrocyte GPx1 activity, antiTPO and thyroid echogenicity at baseline, and 3 and 6 months. RESULTS: In the SeMet group, the increase in plasma levels of selenium and erythrocyte GPx1 activity was similar among patients with different GPx1 genotypes. In the overall cohort, patients randomized to SeMet showed a 5 % decrease in antiTPO levels at 3 months (p = non-significant) and 20 % at 6 months (p < 0.001 versus 3 months). In contrast, patients in the placebo group did not show significant changes in antiTPO levels at any time point. Subgroup analysis showed that patients with different GPx1 genotypes presented comparable responses in antiTPO levels and echogenicity index to SeMet. CONCLUSIONS: Selenium supplementation decreased serum antiTPO levels in CAT patients, with similar response among patients with different GPx1 genotypes.


Assuntos
Autoimunidade/efeitos dos fármacos , Suplementos Nutricionais , Glutationa Peroxidase/genética , Iodeto Peroxidase/imunologia , Selenometionina/uso terapêutico , Glândula Tireoide/efeitos dos fármacos , Tireoidite Autoimune/tratamento farmacológico , Adulto , Método Duplo-Cego , Feminino , Genótipo , Humanos , Inflamação/tratamento farmacológico , Inflamação/genética , Inflamação/imunologia , Masculino , Pessoa de Meia-Idade , Selenometionina/administração & dosagem , Glândula Tireoide/imunologia , Tireoidite Autoimune/genética , Tireoidite Autoimune/imunologia , Resultado do Tratamento , Adulto Jovem , Glutationa Peroxidase GPX1
16.
J Sports Med Phys Fitness ; 55(12): 1488-96, 2015 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-25781214

RESUMO

AIM: The purpose of this investigation was to determine the effects of 3 d of creatine supplementation on thermoregulation and isokinetic muscular performance. METHODS: Fourteen males performed two exercise bouts following 3 d of creatine supplementation and placebo. Subjects exercised for 60 min at 60-65% of VO2max in the heat followed by isokinetic muscular performance at 60, 180, and 300°·s(-1). Dependent variables for pre- and postexercise included nude body weight, urine specific gravity, and serum creatinine levels. Total body water, extracellular water and intracellular water were measured pre-exercise. Core temperature was assessed every 5 min during exercise. Peak torque and Fatigue Index were used to assess isokinetic muscular performance. RESULTS: Core temperature increased during the run for both conditions. Total body water and extracellular water were significantly greater (P<0.05) following creatine supplementation. No significant difference (P>0.05) was found between conditions for intracellular water, nude body weight, urine specific gravity, and serum creatinine. Pre-exercise scores for urine specific gravity and serum creatinine were significantly less (P<0.05) versus post-exercise. No significant differences (P>0.05) were found in peak torque values or Fatigue Index between conditions for each velocity. A significant (P<0.05) overall velocity effect was found for both flexion and extension. As velocity increased, mean peak torque values decreased. CONCLUSION: Three d of creatine supplementation does not affect thermoregulation during submaximal exercise in the heat and is not enough to elicit an ergogenic effect for isokinetic muscle performance following endurance activity.


Assuntos
Creatina/administração & dosagem , Desidratação/fisiopatologia , Exercício Físico/fisiologia , Contração Muscular/fisiologia , Músculo Esquelético/fisiologia , Esforço Físico/fisiologia , Adulto , Regulação da Temperatura Corporal , Peso Corporal , Creatina/metabolismo , Suplementos Nutricionais , Método Duplo-Cego , Teste de Esforço , Frequência Cardíaca , Humanos , Masculino , Contração Muscular/efeitos dos fármacos , Músculo Esquelético/efeitos dos fármacos , Esforço Físico/efeitos dos fármacos , Torque
17.
N Z Vet J ; 62(5): 279-85, 2014 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-24861276

RESUMO

AIMS: To assess the comparative drug systemic exposure of a reference (RF) and four test (Test I, Test II, Test III and Test IV) formulations of triclabendazole (TCBZ) in heifers. METHODS: Thirty Holstein heifers were randomly distributed into five groups (n=6 per group). Animals in the RF group received the reference formulation (Fasinex), and those in the other groups received different commercially available TCBZ formulations (Test I, Test II, Test III and Test IV). All treatments were orally administered at 12 mg/kg bodyweight. The concentrations of TCBZ metabolites in plasma between 0 and 168 hours after treatment were quantified by high-performance liquid chromatography (HPLC). RESULTS: Triclabendazole sulphoxide (TCBZ.SO) and TCBZ-sulphone (TCBZ.SO2) were the only analytes recovered in plasma. Only the Test I formulation did not differ from the RF for all pharmacokinetic parameters measured for either metabolite (p>0.8). The TCBZ.SO area under the concentration vs. time curve for Test II formulation (268.9 µg.h/mL) was lower, and for Test III (619.9 µg.h/mL) and Test IV (683.4 µg.h/mL) was higher, than the RF (418.1 µg.h/mL) (p<0.005). CONCLUSION: Based on the currently available bioequivalence criteria, the only test formulation under evaluation that could be considered equivalent to the RF was the Test I formulation, which demonstrated an equivalent systemic exposure for the active TCBZ.SO metabolite. This comparison of TCBZ pioneer and test formulations in cattle raises awareness of the need for further quality control for drug approval in the veterinary pharmaceutical field in many regions of the world.


Assuntos
Anti-Helmínticos/farmacocinética , Benzimidazóis/farmacocinética , Bovinos/metabolismo , Animais , Anti-Helmínticos/sangue , Anti-Helmínticos/metabolismo , Área Sob a Curva , Benzimidazóis/sangue , Benzimidazóis/metabolismo , Bovinos/sangue , Química Farmacêutica , Feminino , Meia-Vida , Triclabendazol
18.
Rev Med Chil ; 141(4): 419-27, 2013 Apr.
Artigo em Espanhol | MEDLINE | ID: mdl-23900361

RESUMO

BACKGROUND: Up to 70% of hospitalized older people experience a deterioration of their functional capacity during the course of hospital stay. This change has a dismal effect of quality of life and prognosis. AIM: To assess the change in functional status of older people during the course of hospitalization in a geriatric unit. MATERIAL AND METHODS: Review of medical records of 83 patients with a mean age of 79 years (70% women), hospitalized in an acute geriatric unit of a clinical hospital, between 2007 and 2009. Functional capacity was assessed using Barthel and Lawthon scales in a basal period, on admission and on discharge. RESULTS: Mean hospital stay was nine days. Median scores of Barthel scale on the basal period, on admission and on discharge were 90, 50 and 80, respectively. The figures for Lawthon scale were 4,2 and 3 respectively. Seventy eight percent of patients lost functional capacity during hospital stay and 72% recovered their functional status on discharge. CONCLUSIONS: A great proportion of older people experience a loss of functional capacity during hospitalization. This deterioration can be reverted with an adequate geriatric management.


Assuntos
Atividades Cotidianas/psicologia , Avaliação Geriátrica/métodos , Hospitalização , Qualidade de Vida/psicologia , Idoso , Feminino , Humanos , Tempo de Internação , Masculino , Equipe de Assistência ao Paciente , Prognóstico , Estudos Retrospectivos
19.
Rev. méd. Chile ; 141(4): 419-427, abr. 2013. tab
Artigo em Espanhol | LILACS | ID: lil-680463

RESUMO

Background: Up to 70% of hospitalized older people experience a deterioration of their functional capacity during the course of hospital stay. This change has a dismal effect of quality oflife and prognosis. Aim: To assess the change in functional status of older people during the course of hospitalization in a geriatric unit. Material and Methods: Review of medical records of83 patients with a mean age of79years (70% women), hospitalized in an acute geriatric unit of a clinical hospital, between 2007 and 2009. Functional capacity was assessed using Barthel and Lawthon scales in a basal period, on admission and on discharge. Results: Mean hospital stay was nine days. Median scores of Barthel scale on the basal period, on admission and on discharge were 90, 50 and 80, respectively. The figures for Lawthon scale were 4,2 and 3 respectively. Seventy eight percent of patients lost functional capacity during hospital stay and 72% recovered their functional status on discharge. Conclusions: A great proportion of older people experience a loss of functional capacity during hospitalization. This deterioration can be reverted with an adequate geriatric management.


Assuntos
Idoso , Feminino , Humanos , Masculino , Atividades Cotidianas/psicologia , Avaliação Geriátrica/métodos , Hospitalização , Qualidade de Vida/psicologia , Tempo de Internação , Equipe de Assistência ao Paciente , Prognóstico , Estudos Retrospectivos
20.
Food Chem Toxicol ; 50(10): 3819-25, 2012 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-22841955

RESUMO

Oxfendazole (OFZ) is efficacious for porcine cysticercosis at 30 mg/kg. OFZ is not registered to be used at this dose. The assessment of the OFZ and metabolites [(fenbendazole sulphone (FBZSO2), fenbendazole (FBZ)] plasma pharmacokinetic and tissue residue profiles after its oral administration to pigs and the withdrawal period for human consumption were reported. Forty-eight pigs allocated into two groups received OFZ (30 mg/kg) orally as a commercial (CF) or as experimental formulation (SMF). Samples (blood, muscle, liver, kidney and fat) were collected over 30 days post-treatment and analyzed by HPLC. OFZ was the main compound recovered in plasma, followed by FBZSO2 and low FBZ concentrations. OFZ AUC0-LOQ (209.9±33.9 µg·h/ml) and Cmax (5.40±0.65 µg/ml) parameters for the CF tended to be higher than those for the SMF (AUC0-LOQ: 159.4±18.3 µg h/ml, Cmax: 3.80±0.35 µg/ml). The highest total residue (OFZ+FBZSO2+FBZ) concentrations were quantified in liver, followed by kidney, muscle and fat tissue. FBZSO2 residue levels were the highest found in muscle (0.68±0.39 µg/g) and fat (0.69±0.39 µg/g). In liver and kidney the highest residues corresponded to FBZ (5.29±4.36 µg/g) and OFZ (2.86±0.75 µg/g), respectively. A withdrawal time of 17 days post-treatment was established before tissues are delivered for human consumption.


Assuntos
Anti-Helmínticos/uso terapêutico , Benzimidazóis/uso terapêutico , Cisticercose/veterinária , Resíduos de Drogas/análise , Doenças dos Suínos/tratamento farmacológico , Tecido Adiposo/química , Animais , Anti-Helmínticos/administração & dosagem , Anti-Helmínticos/farmacocinética , Área Sob a Curva , Benzimidazóis/administração & dosagem , Benzimidazóis/farmacocinética , Cisticercose/tratamento farmacológico , Cisticercose/patologia , Relação Dose-Resposta a Droga , Feminino , Meia-Vida , Rim/química , Masculino , Músculo Esquelético/química , Suínos , Doenças dos Suínos/parasitologia
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