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71.
Emilay B.T. Diogo Gleiston G. Dias Bernardo L. Rodrigues Tiago T. Guimarães Wagner O. Valença Celso A. Camara Ronaldo N. de Oliveira Mauro G. da Silva Vitor F. Ferreira Yen Galdino de Paiva Marilia O.F. Goulart Rubem F.S. Menna-Barreto Solange L. de Castro Eufrânio N. da Silva Júnior 《Bioorganic & medicinal chemistry》2013,21(21):6337-6348
In our continued search for novel trypanocidal compounds, twenty-six derivatives of para- and ortho-naphthoquinones coupled to 1,2,3-triazoles were synthesized. These compounds were evaluated against the infective bloodstream form of Trypanosoma cruzi, the etiological agent of Chagas disease. Compounds 17–24, 28–30 and 36–38 are described herein for the first time. Three of these novel compounds (28–30) were found to be more potent than the standard drug benznidazole, with IC50/24 h values between 6.8 and 80.8 μM. Analysis of the toxicity to heart muscle cells led to LC50/24 h of <125, 63.1 and 281.6 μM for 28, 29 and 30, respectively. Displaying a selectivity index of 34.3, compound 30 will be further evaluated in vivo. The electrochemical properties of selected compounds were evaluated in an attempt to find correlations with trypanocidal activity, and it was observed that more electrophilic quinones were generally more potent. 相似文献
72.
《Animal : an international journal of animal bioscience》2013,7(10):1576-1582
The aim of this study was to develop a method for scoring osteochondrosis (OC) by using information from computed tomography (CT), as well as to estimate the heritability for OC scored by means of CT (OCwCT) of the medial and lateral condyles at the distal end of the humerus or the femur of the right and left leg and the sum of these scores (OCT). In addition, we were aiming at revealing the genetic relationship between OCwCT traits and growth in different periods (days from birth to 30 kg (D30), days from 30 to 50 kg (D30_50), days from 50 to 70 kg (D50_70), days from 70 to 90 kg (D70_90), days from 90 to 100 kg (D90_100) and days from birth to 100 kg (D100)). The OCwCT was assessed for 1449 boars, and growth data were collected for these 1449 boars and additional 3779 boars tested in the same time period. All boars were tested as part of the Norsvin Landrace boar test and in the same test station. Heritabilities for OCwCT on anatomical locations varied from 0.21 (s.e. = 0.08) on the medial condyle of the right humerus to 0.06 (s.e. = 0.06) on the lateral condyle of the left femur, whereas OCT exhibited the highest heritability (h2 = 0.31, s.e. = 0.09). Genetic correlations between OCT and OCwCT for the anatomical locations ranged from 0.94 (s.e. = 0.07) for OCT and OCwCT score for the medial condyle of the humerus right side to 0.26 (s.e. = 0.39) for OCT and the lateral condyle of the femur left side. Genetic correlations between D30 and OCT were medium high and unfavourable (rg = −0.74). As the boar gain weight, the relationship between growth rate – expressed as number of days spent growing from one interval to the next – and OCT decreased to 0.12 (s.e. = 0.19, i.e. not significantly different from zero) for the trait D90_100 kg. These changes of genetic correlation coefficients coincide with the maturing of the joint cartilage and skeletal structures. In this study, we demonstrate that CT could be used for selection against OC in breeding programmes in pigs and that the genetic correlations between growth periods and OC are decreasing over time. 相似文献
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Water quality and phytoplankton community structure in mangrove streams under different logging regimes in Cameroon 下载免费PDF全文
Ambo Beatrice Fonge Pascal Tabi Tabot Coleen Mumbang Chop Adeline Mange 《African Journal of Ecology》2016,54(1):39-48
Mangrove logging is rampant, and its effects on phytoplankton dynamics have not been investigated. Phytoplankton are valuable in biomonitoring pollution in mangrove ecosystems. This study assessed the relationship between physico‐chemical characteristics of the water and observed phytoplankton community structure, in relation to anthropogenic activities. Water samples were collected from seven sites within the mangrove ecosystem that differed in wood harvesting age and proximity to human settlements. Characterization of samples followed standard methods. pH of all water samples indicated acidity. Phytoplankton species richness and soluble P were positively correlated (r = 0.822, P ≤ 0.023), but no correlations existed with logging age (r = ?0.273, P = 0553). The site with highest soluble phosphorus concentration (Site 4) had highest phytoplankton abundance, diversity and richness. A total of 127 species were identified in 58 families. Euglenaceae was the most abundant family (13 species) and Anacystis sp. the most frequent species (100%). The most common genera were Microcystis and Anacystis, bioindicators of pollution. The site at which harvesting was most recently performed had more eutrophic species, while site harvested earliest (Site 5) had the least. These results are discussed with respect to how anthropogenic activities influence water quality, phytoplankton community structure, mangrove conservation and management. 相似文献
77.
Tomasz Krzeszowski Krzysztof Przednowek Krzysztof Wiktorowicz Janusz Iskra 《Computer methods in biomechanics and biomedical engineering》2016,19(12):1319-1329
This paper presents a method of monocular human motion tracking for estimation of hurdle clearance kinematic parameters. The analysis involved 10 image sequences of five hurdlers at various training levels. Recording of the sequences was carried out under simulated starting conditions of a 110 m hurdle race. The parameters were estimated using the particle swarm optimization algorithm and they are based on analysis of the images recorded with a 100 Hz camera. The proposed method does not involve using any special clothes, markers, inertial sensors, etc. As the quality criteria, the mean absolute error and mean relative error were used. The level of computed errors justifies the use of this method to estimate hurdle clearance parameters. 相似文献
78.
Massimo Dal Monte Maurizio Cammalleri Valeria Pecci Monica Carmosino Giuseppe Procino Alessandro Pini Mario De Rosa Vincenzo Pavone Maria Svelto Paola Bagnoli 《Journal of cellular and molecular medicine》2019,23(2):1034-1049
The urokinase‐type plasminogen activator (uPA) receptor (uPAR) participates to the mechanisms causing renal damage in response to hyperglycaemia. The main function of uPAR in podocytes (as well as soluble uPAR ‐(s)uPAR‐ from circulation) is to regulate podocyte function through αvβ3 integrin/Rac‐1. We addressed the question of whether blocking the uPAR pathway with the small peptide UPARANT, which inhibits uPAR binding to the formyl peptide receptors (FPRs) can improve kidney lesions in a rat model of streptozotocin (STZ)‐induced diabetes. The concentration of systemically administered UPARANT was measured in the plasma, in kidney and liver extracts and UPARANT effects on dysregulated uPAR pathway, αvβ3 integrin/Rac‐1 activity, renal fibrosis and kidney morphology were determined. UPARANT was found to revert STZ‐induced up‐regulation of uPA levels and activity, while uPAR on podocytes and (s)uPAR were unaffected. In glomeruli, UPARANT inhibited FPR2 expression suggesting that the drug may act downstream uPAR, and recovered the increased activity of the αvβ3 integrin/Rac‐1 pathway indicating a major role of uPAR in regulating podocyte function. At the functional level, UPARANT was shown to ameliorate: (a) the standard renal parameters, (b) the vascular permeability, (c) the renal inflammation, (d) the renal fibrosis including dysregulated plasminogen‐plasmin system, extracellular matrix accumulation and glomerular fibrotic areas and (e) morphological alterations of the glomerulus including diseased filtration barrier. These results provide the first demonstration that blocking the uPAR pathway can improve diabetic kidney lesion in the STZ model, thus suggesting the uPA/uPAR system as a promising target for the development of novel uPAR‐targeting approaches. 相似文献
79.
The study of animal acoustic signals is a central tool for many fields in ecology and evolution, but the diversity of analytical methods and sources of animal sound recordings poses important challenges for carrying out robust acoustic analyses. Sound file compression and background noise may both affect acoustic analysis, although little attention has been paid to their respective effects. We evaluated the effect of these factors by assessing the systematic deviation (i.e. bias) and measurement error (i.e. precision) that they generate on spectrographic parameters and two (dis)similarity methods (dynamic time warping on frequency contours and cross-correlation), which represent the most common methods currently used for quantitative characterization of acoustic signals. Measurements were taken across a wide range of signals from a diverse group of bird species, and compared between uncompressed files and decompressed files obtained from mp3-encoded files generated using the two most common mp3 encoders (Fraunhofer and LAME). Measurements were also compared across a range of synthetically-generated background noise levels. Compression did not significantly bias any of the acoustic or similarity measurements. However, the precision of acoustic parameters representing single extreme values (e.g. peak frequency) as well as dynamic time warping distances, was strongly affected by compression. High background noise biased most energy distribution-related parameters (e.g. spectral entropy) and affected the precision of most acoustic parameters and dynamic time warping. Overall, compression and background noise did have considerable effects on acoustic analyses. We provide recommendations to avoid potential pitfalls and maximize the information that can be reliably obtained. 相似文献
80.
Albina Dolores Resende Sandra Leal Carla Batista‐Pinto Fernanda Garcez Susana Isabel S 《Journal of biochemical and molecular toxicology》2019,33(5)
The metabolic implications of tamoxifen (TAM) used as preventive therapy of young premenopausal women with high risk of breast cancer is unknown. To unravel this problem, an animal model of long‐term TAM administration to cycling young adult female rats was used to evaluate its effects in the liver. Body weight and food consumption were monitored, and at the end of the study, both parameters were lower in TAM‐treated rats. Biochemical measurements showed that the TAM administration induced alterations in serum levels of liver enzymes when compared with control rats at different stages of the estrous cycle. In TAM‐treated rats, lower glycogen storage was observed in hepatocytes close to the portal areas and pericentrolobular cells had a higher concentration of glycogen. Liver sections of TAM‐treated rats presented mild steatosis—a high percentage of area occupied by lipid droplets in the hepatocytes. These results point to metabolic changes upon long‐term TAM therapy. 相似文献