Concerned about weed infestation, a major threat to food production and herbicide resistance that interferes in the mechanism of action of the main herbicides, we have synthesized eight isatin derivatives using the "Click Chemistry" approach through copper-catalyzed azide-alkyne cycloadditions (CuAAC). Sixteen isatin derivatives were evaluated for their phytotoxic activity against the seed culture of the model plants, and . Six of them showed phytotoxic activity similar to the positive control, trifluralin.
View Article and Find Full Text PDFDiabetes is a metabolic disorder that presents hyperglycemia and vascular complications due to the non-production of insulin or its inappropriate use by the body. One of the strategies to treat diabetes is the inhibition of dipeptidyl peptidase-4 (DPP-4) and it is interesting to conduct virtual screening studies to search for new inhibitors of the DPP-4 enzyme. This study involves a virtual screening using the crystallographic structure of DPP-4 and a compound subset from the ZINC database.
View Article and Find Full Text PDFProtein kinases (in this case, HER-2 and EGFR) are involved in cancer-related diseases. Some reports have shown unique CoMFA models using the sum of activities expressed as pIC (-log IC), as the classical CoMFA technique would not be the best strategy to construct models for multitarget therapy considering that the molecular alignment will not be the same for different targets. An alternative for this problem is the use of Topomer-CoMFA, a variation of CoMFA, which does not require the alignment step in the generation of 3D models.
View Article and Find Full Text PDFBackground: Natural products have been universally approached in the research of novel trends useful to detail the essential paths of the life sciences and as a strategy for pharmacotherapeutics.
Objective: This work focuses on further modification to the 6-hydroxy-flavanone building block aiming to obtain improved BCR-ABL kinase inhibitors.
Methods: Ether derivatives were obtained from Williamson synthesis and triazole from Microwave- assisted click reaction.
This study aimed to investigate the risk factors for depressive symptoms among rural residents in Brazil. A representative sample of two hundred eighty-eight volunteers aged from 18 to 65 years was included and determining factors for high BDI-II score were investigated through a multivariate logistic model. Sadness, loss of pleasure, crying, worthlessness and loss of interest in sex are more likely to be observed in females, and risk factors to this high depression score among rural residents were shown to be: female gender, tobacco use, pesticide application, poor self-perceived health and presence of chronic disease.
View Article and Find Full Text PDFThe authors regret that Philipp E Scherer's name was spelt incorrectly in the author list. The name of the author is now corrected above.
View Article and Find Full Text PDFThe underlying pathogenic mechanisms of cardiomyopathy in Chagas disease are still unsolved. In order to better clarify the role of fat on the evolution of cardiomyopathy, the present study employed three murine models of chronic Trypanosoma cruzi infection: (1) aP2-RIDα/β transgenic mice (RID mice; an adipose tissue model which express a gain-of-function potent anti-inflammatory activity), (2) allograft inflammatory factor-1 knockout mice (Aif1), and (3) a Swiss outbred mice. RID mice and non-transgenic mice (wild type, WT) were infected with blood trypomastigotes of Brazil strain.
View Article and Find Full Text PDFBackground: Glycogen synthase kinase-3 (GSK-3) is involved in the phosphorylation and inactivation of glycogen synthase. GSK-3 inhibitors have been associated with a variety of diseases, including Alzheimer´s disease (AD), diabetes type II, neurologic disorders, and cancer. The inhibition of GSK-3β isoforms is likely to represent an effective strategy against AD.
View Article and Find Full Text PDFHER-2 and EGFR are biological targets related to the development of cancer and the discovery and/or development of a dual inhibitor could be a good strategy to design an effective drug candidate. In this study, analyses of the chemical properties of a group of substances having affinity for both HER-2 and EGFR were carried out with the aim of understanding the main factors involved in the interaction between these inhibitors and the biological targets. Comparative analysis of molecular interaction fields (CoMFA) and comparative molecular similarity index analysis (CoMSIA) techniques were applied on 63 compounds.
View Article and Find Full Text PDFObjective: To assess the association between indicators of psychosocial stress and central adiposity in adult users of the Unified Health System (SUS) from Southeast of Brazil.
Methods: This cross-sectional study was conducted with 384 adults (20 to 59 years old) from the city of Alegre, Southeastern Brazil. The simple random sample represented the population using the public health system of the municipality.
The discovery of the importance of kinase activity and its relationship to the emergence and proliferation of cancer cells, due to changes in normal physiology, opened a remarkable pathway for the treatment of chronic myelogenous leukemia through intense search of drug candidates. Six Abl kinase inhibitors have received the US FDA approval as chronic myelogenous leukemia treatment, and continuous efforts in obtaining new, more effective and selective molecules are being carried out. Herein we discuss the mechanisms of Abl inhibition, structural features and ligand/protein interactions that are important for the design of new Abl kinase inhibitors.
View Article and Find Full Text PDFBackground: Flaxseed is a promising alternative to reduce the risk of diseases associated with body weight excess because it is rich in a-linolenic acid, lignans, and dietary fiber. Flaxseed (Linum usitatissimum) can be found in brown and golden varieties; however, questions have arisen as to whether the variety may influence the health effects.
Objective: The objective of this study was to compare the effects of brown and golden flaxseeds on lipid profile, glycemia, blood pressure, inflammatory status,body weight, and body composition in overweight adolescents.
Objective: The aim of this study was to evaluate the effect of yacon flour on iron and zinc nutritional status and immune response biomarkers in preschool children.
Methods: Preschool children ages 2 to 5 y were selected from two nurseries and were placed into a control group (n = 58) or a yacon group (n = 59). The yacon group received yacon flour in preparations for 18 wk at a quantity to provide 0.
Background: Metabolic syndrome (MS) is suggested to be associated with a low grade inflammation state, but the relationship between inflammation biomarkers and the components of metabolic syndrome in adolescents are still lacking.
Objective: To investigate the association between C-reactive protein (CRP) serum concentrations and metabolic syndrome components in adolescents.
Methods: A cross-sectional population based study was conducted.
Nutritional and biochemical properties of noncommercial whey protein have been described since 1950. However, comparisons between commercial whey protein for human consumption and casein are rarely found. The aim of this study was to compare biological quality of a commercial whey protein with casein and its effect on biochemical parameters of rats.
View Article and Find Full Text PDFThe objective of this study was to investigate the effect of iron overload with a hyperlipidemic diet on the histologic feature of hepatic tissue, the lipid and glycemic serum profiles, and the markers of oxidative damage and stress in a rat model. Twenty-four male Fischer rats, purchased from Experimental Nutrition Laboratory, Federal University of Ouro Preto, were assigned to 4 equal groups, 2 were fed a standard cholesterol-free diet (group C or control and CI or control with iron) containing 8.0% soybean oil and 2 were fed a hyperlipidemic diet (group H or hyperlipidemic and HI or hyperlipidemic with iron) containing 1.
View Article and Find Full Text PDFCad Saude Publica
September 2007
Epidemiologic and experimental data suggest that excess iron may contribute to the development of cardiovascular diseases (CVD). Because increased LDL cholesterol, decreased HDL cholesterol and alteration of systolic blood pressure (SBP) have all been implicated as risk factors for atherosclerosis and related CVD, the present study was designed to determine whether excess iron alters serum lipids and SBP in control and hypercholesterolemic rats. Female Fischer rats were divided into four groups.
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