Radiosynthesis and in vivo evaluation of a 18F-labelled styryl-benzoxazole derivative for β-amyloid targeting

The formation of β-amyloid deposits is considered a histopathological feature of Alzheimer′s disease (AD). In vivo molecular imaging by means of amyloid-avid radiotracers will allow for an early and conclusive diagnostic of AD. Herein, we describe the radiosynthesis of the radiofluorinated styryl benzoxazole derivative [18F]-[2-[N-methyl-N-(2′-fluoroethyl)-4′-aminostyryl]benzoxazole] ([18F]-1) and its pre-clinical evaluation, including metabolic and biodistribution studies in male Wistar rats. The in vivo biological evaluation of [18F]-1 showed that this new radiotracer has a moderate brain uptake with a slow brain washout and a poor in vivo stability

A Streamlined Approach by a Combination of Bioindication and Geostatistical Methods for Assessing Air Contaminants and Their Effects on Human Health in Industrialized Areas: A Case Study in Southern Brazil

Industrialization in developing countries associated with urban growth results in a number of economic benefits, especially in small or medium-sized cities, but leads to a number of environmental and public health consequences. This problem is further aggravated when adequate infrastructure is lacking to monitor the environmental impacts left by industries and refineries. In this study, a new protocol was designed combining biomonitoring and geostatistics to evaluate the possible effects of shale industry emissions on human health and wellbeing. Futhermore, the traditional and expensive air quality method based on PM2.5 measuring was also used to validate the low-cost geostatistical approach. Chemical analysis was performed using Energy Dispersive X-ray Fluorescence Spectrometer (EDXRF) to measure inorganic elements in tree bark and shale retorted samples in São Mateus do Sul city, Southern Brazil. Fe, S, and Si were considered potential pollutants in the study area. Distribution maps of element concentrations were generated from the dataset and used to estimate the spatial behavior of Fe, S, and Si and the range from their hot spot(s), highlighting the regions sorrounding the shale refinery. This evidence was also demonstrated in the measurements of PM2.5 concentrations, which are in agreement with the information obtained from the biomonitoring and geostatistical model. Factor and descriptive analyses performed on the concentrations of tree bark contaminants suggest that Fe, S, and Si might be used as indicators of industrial emissions. The number of cases of respiratory diseases obtained from local basic health unit were used to assess a possible correlation between shale refinery emissions and cases of repiratory disease. These data are public and may be accessed on the website of the the Brazilian Ministry of Health. Significant associations were found between the health data and refinery activities. The combination of the spatial characterization of air pollution and clinical health data revealed that adverse effects were significant for individuals over 38 years of age. These results also suggest that a protocol designed to monitor urban air quality may be an effective and low-cost strategy in environmentally contaminated cities, especially in low- and middle-income countries

A streamlined approach by a combination of bioindication and geostatistical methods for assessing air contaminants and their effects on human health in industrialized areas: A case study in Southern Brazil

© 2017 Ferreira, Ribeiro, Ferreira, Kniess, Quaresma, Lafortezza, Santos, Saiki and Saldiva. Industrialization in developing countries associated with urban growth results in a number of economic benefits, especially in small or medium-sized cities, but leads to a number of environmental and public health consequences. This problem is further aggravated when adequate infrastructure is lacking to monitor the environmental impacts left by industries and refineries. In this study, a new protocol was designed combining biomonitoring and geostatistics to evaluate the possible effects of shale industry emissions on human health and wellbeing. Futhermore, the traditional and expensive air quality method based on PM2.5 measuring was also used to validate the low-cost geostatistical approach. Chemical analysis was performed using Energy Dispersive X-ray Fluorescence Spectrometer (EDXRF) to measure inorganic elements in tree bark and shale retorted samples in São Mateus do Sul city, Southern Brazil. Fe, S, and Si were considered potential pollutants in the study area. Distribution maps of element concentrations were generated from the dataset and used to estimate the spatial behavior of Fe, S, and Si and the range from their hot spot(s), highlighting the regions sorrounding the shale refinery. This evidence was also demonstrated in the measurements of PM2.5 concentrations, which are in agreement with the information obtained from the biomonitoring and geostatistical model. Factor and descriptive analyses performed on the concentrations of tree bark contaminants suggest that Fe, S, and Si might be used as indicators of industrial emissions. The number of cases of respiratory diseases obtained from local basic health unit were used to assess a possible correlation between shale refinery emissions and cases of repiratory disease. These data are public and may be accessed on the website of the the Brazilian Ministry of Health. Significant associations were found between the health data and refinery activities. The combination of the spatial characterization of air pollution and clinical health data revealed that adverse effects were significant for individuals over 38 years of age. These results also suggest that a protocol designed to monitor urban air quality may be an effective and low-cost strategy in environmentally contaminated cities, especially in low- and middle-income countries.Link_to_subscribed_fulltex

On security evaluation of fingerprint recognition systems

This paper discusses the methodology for evaluating the security of fingerprint recognition systems. For keeping track of the multitude of potential vulnerabilities an attack tree is used. Only potential vulnerabilities specific to fingerprint verification systems are considered. The attack tree is truncated where the efforts required for a successful attack (the attack potential) can be estimated. The attack potential of the parent nodes is the aggregation of the attack potentials of the child nodes

Study of differences in the VEGFR2 inhibitory activities between semaxanib and SU5205 using 3D-QSAR, docking, and molecular dynamics simulations

Caballero, J (reprint author), Univ Talca, Ctr Bioinformat & Simulac Mol, 2 Norte 685,Casilla 721, Talca, Chile.Semaxanib (SU5416) and 3[4'-fluorobenzylidene]indolin-2-one (SU5205) are structurally similar drugs that are able to inhibit vascular endothelial growth factor receptor-2 (VEGFR2), but the former is 87 times more effective than the latter. Previously, SU5205 was used as a radiolabelled inhibitor (as surrogate for SU5416) and a radiotracer for positron emission tomography (PET) imaging, but the compound exhibited poor stability and only a moderate IC50 toward VEGFR2. In the current work, the relationship between the structure and activity of these drugs as VEGFR2 inhibitors was studied using 3D-QSAR, docking and molecular dynamics (MD) simulations. First, comparative molecular field analysis (CoMFA) was performed using 48 2-indolinone derivatives and their VEGFR2 inhibitory activities. The best CoMFA model was carried out over a training set including 40 compounds, and it included steric and electrostatic fields. In addition, this model gave satisfactory cross-validation results and adequately predicted 8 compounds contained in the test set. The plots of the CoMFA fields could explain the structural differences between semaxanib and SU5205. Docking and molecular dynamics simulations showed that both molecules have the same orientation and dynamics inside the VEGFR2 active site. However, the hydrophobic pocket of VEGFR2 was more exposed to the solvent media when it was complexed with SU5205. An energetic analysis, including Embrace and MM-GBSA calculations, revealed that the potency of ligand binding is governed by van der Waals contacts. (C) 2011 Elsevier Inc. All rights reserved

Radiosynthesis and radiopharmacological evaluation of [n-methyl-11c]org 34850 as a glucocorticoid receptor (gr)-binding radiotracer

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