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101.
Activity of Fluorine‐Containing Analogues of WC‐9 and Structurally Related Analogues against Two Intracellular Parasites: Trypanosoma cruzi and Toxoplasma gondii 下载免费PDF全文
María N. Chao Catherine Li Melissa Storey Dr. Bruno N. Falcone Dr. Sergio H. Szajnman Prof. Dr. Sergio M. Bonesi Prof. Dr. Roberto Docampo Prof. Dr. Silvia N. J. Moreno Prof. Dr. Juan B. Rodriguez 《ChemMedChem》2016,11(24):2690-2702
Two obligate intracellular parasites, Trypanosoma cruzi, the agent of Chagas disease, and Toxoplasma gondii, an agent of toxoplasmosis, upregulate the mevalonate pathway of their host cells upon infection, which suggests that this host pathway could be a potential drug target. In this work, a number of compounds structurally related to WC‐9 (4‐phenoxyphenoxyethyl thiocyanate), a known squalene synthase inhibitor, were designed, synthesized, and evaluated for their effect on T. cruzi and T. gondii growth in tissue culture cells. Two fluorine‐containing derivatives, the 3‐(3‐fluorophenoxy)‐ and 3‐(4‐fluorophenoxy)phenoxyethyl thiocyanates, exhibited half‐maximal effective concentration (EC50) values of 1.6 and 4.9 μm , respectively, against tachyzoites of T. gondii, whereas they showed similar potency to WC‐9 against intracellular T. cruzi (EC50 values of 5.4 and 5.7 μm , respectively). In addition, 2‐[3‐ (phenoxy)phenoxyethylthio]ethyl‐1,1‐bisphosphonate, which is a hybrid inhibitor containing 3‐phenoxyphenoxy and bisphosphonate groups, has activity against T. gondii proliferation at sub‐micromolar levels (EC50=0.7 μm ), which suggests a combined inhibitory effect of the two functional groups. 相似文献
102.
Matthew J. Bauer Catherine S. Snyder Christopher C. Bowland Amanda M. Uhl Maeve A. K. Budi Maria Villancio‐Wolter Henry A. Sodano Jennifer S. Andrew 《Journal of the American Ceramic Society》2016,99(12):3902-3908
Barium titanate nanofibers were uniaxially aligned by electrospinning onto a rotating copper wire drum and alignment was maintained during calcination of the fibers. Two methods for maintaining alignment during calcination were tested, by either using carbon tape or a peeling off method to remove the aligned fibers from the mandrel followed by calcination. The carbon tape removal method led to the formation of shorter aligned nanowires while the peeling off method resulted in longer nanofibers. Additionally, the effects of calcination temperature and time on crystal structure were also examined. The degree of tetragonality in the barium titanate nanofibers increased at higher calcination temperatures and times. Piezoelectricity was confirmed in the nanofibers calcined using piezoeresponse force microscopy, yielding a d33 value of 15.5 pm/V. Using the methods presented here, large quantities of aligned piezoelectric barium titanate and other ceramic fibers or wires can be produced to fulfill their demand in novel microelectronics. 相似文献
103.
Ikbal Zarguili Zoulikha Maache-Rezzoug Catherine Loisel & Jean-Louis Doublier 《International Journal of Food Science & Technology》2009,44(1):10-17
Instantaneous Controlled Pressure Drop, ' Détente Instantanée Contrôlée ' (DIC) was performed on standard maize starch at residual moisture content (∼12%). Changes in moisture distribution were observed during the treatment and modelled through a phenomenological model based on gravimetric data. The model proposes an exponential variation in the moisture content with processing time at various pressures. The predicted data were found to be in good agreement with experimental data. The values of water activity coefficient ( γ ) obtained from the model decrease, when processing pressure increases; 5.86, 3.71 and 3.36 (dry basis)−1 for 1, 2 and 3 bar, respectively. The mass transfer coefficient decreases, when the pressure increases. Its value ranged from 5.89 × 10−5 m s−1 for 1 bar down to 0.92 × 10−5 m s−1 for 2 bar and 0.77 × 10−5 m s−1 for 3 bar. This coefficient is not only controlled by a simple resistance to the mass transfer, but also by gelatinisation phenomenon that progresses when temperature increases. 相似文献
104.
Sylvie Bureau David Ruiz Maryse Reich Barbara Gouble Dominique Bertrand Jean-Marc Audergon Catherine M.G.C. Renard 《Food chemistry》2009
A non-destructive optical method based on near-infrared spectroscopy has been used for the evaluation of apricot fruit quality. Diffuse reflectance measurements (800–2500 nm), physical, physiological and biochemical measurements were performed individually on 877 apricot fruits from eight contrasted cultivars harvested at different ripening stages. Relationships between spectral wavelengths and quality attributes were evaluated by application of chemometric techniques based on partial least squares (PLS) on fruit set divided randomly into two groups: 598 fruits for calibration and 279 for validation. Good prediction performance was obtained for soluble solids and titratable acidity with correlation coefficients of 0.92 and 0.89 respectively and root mean square errors of prediction of 0.98% Brix and 3.62 meq 100 g−1 FW respectively. For the other quality traits such as firmness, ethylene, individual sugars and organic acids, the prediction models were not satisfactorily accurate due to the high error of calibration and prediction. 相似文献
105.
Catherine Drosou Alberto Coz Nikolaos P. Xekoukoulotakis Armando Moya Yolanda Vergara Dionissios Mantzavinos 《Journal of chemical technology and biotechnology (Oxford, Oxfordshire : 1986)》2010,85(8):1049-1053
BACKGROUND: Although chlorination is an effective and widely employed method of water disinfection, it suffers serious drawbacks such as the formation of toxic chlorinated by‐products. Therefore, other disinfection technologies have been researched and developed, including advanced oxidation. RESULTS: The efficacy of heterogeneous photocatalysis and sonophotocatalysis induced by UV‐A irradiation and low frequency (24–80 kHz) ultrasound irradiation in the presence of TiO2 as the photocatalyst and peracetic acid (PAA) as an additional disinfectant to inactivate E. coli in sterile water was evaluated. PAA‐assisted UV‐A/TiO2 photocatalysis generally leads to nearly complete E. coli inactivation in 10–20 min of contact time with the extent of inactivation depending on the photocatalyst type and loading (in the range 100–500 mg L?1) and PAA concentration (in the range 0.5–2 mg L?1). The simultaneous application of ultrasound and UV‐A irradiation in the presence of TiO2 and PAA prompted further E. coli inactivation. CONCLUSIONS: The proposed advanced disinfection technology offers complete E. coli inactivation at short treatment times and low PAA doses. Copyright © 2010 Society of Chemical Industry 相似文献
106.
Kirsti Rouvinen-Watt Anne-Mari Mustonen Rebecca Conway Catherine Pal Lora Harris Seppo Saarela Ursula Strandberg Petteri Nieminen 《Lipids》2010,45(2):111-128
Hepatic lipidosis is a common pathological finding in the American mink (Neovison vison) and can be caused by nutritional imbalance due to obesity or rapid body weight loss. The objectives of the present study were to investigate the timeline and characterize the development of hepatic lipidosis in mink in response to 0–7 days of food deprivation and liver recovery after 28 days of re-feeding. We report here the effects on hematological and endocrine variables, body fat mobilization, the development of hepatic lipidosis and the alterations in the liver lipid classes and tissue fatty acid (FA) sums. Food deprivation resulted in the rapid mobilization of body fat, most notably visceral, causing elevated hepatosomatic index and increased liver triacylglycerol content. The increased absolute amounts of liver total phospholipids and phosphatidylcholine suggested endoplasmic reticulum stress. The hepatic lipid infiltration and the altered liver lipid profiles were associated with a significantly reduced proportion of n-3 polyunsaturated FA (PUFA) in the livers and the decrease was more evident in the females. Likewise, re-feeding of the female mink resulted in a more pronounced recovery of the liver n-3 PUFA. The rapid decrease in the n-3/n-6 PUFA ratio in response to food deprivation could trigger an inflammatory response in the liver. This could be a key contributor to the pathophysiology of fatty liver disease in mink influencing disease progression. 相似文献
107.
The oxidation products formed at 500 and 700°C on an amorphous Ta-44.5 at% Ir alloy in an Ar-0.1% O2 gas mixture were characterized using SEM, XRD, EPMA, TEM, STEM, AES, and XPS. Initially, a thin (3–4 nm) layer of Ta2O5 formed at the surface of the alloy. Continued growth of the Ta2O5, which occurred very rapidly, involved diffusion of oxygen anions from the Ta2O5/gas interface to the alloy/Ta2O5 interface, where tantalum was selectively oxidized. Because the oxide grew more quickly than iridium could diffuse back into the alloy, the iridium coalesced into platelets of crystalline iridium-rich alloy that were oriented approximately parallel to the oxide/alloy interface, and which became embedded in a matrix of Ta2O5. The unoxidized core remained in the glassy state. The oxidation process and/or the dissolution of oxygen into the unoxidized alloy caused the alloy to become embrittled. 相似文献
108.
Catherine J. Watson 《Nutrient Cycling in Agroecosystems》1990,24(1):1-10
Urea can be an inefficient N source due to rapid hydrolysis by soil urease leading to NH3 volatilization. The current study investigated the effect of the urease inhibitor phenylphosphorodiamidate (PPD) incorporated at two concentrations (0.5% and 1% w/w) within the fertilizer granule on NH3 volatilization from surface applied urea. The daily rates of NH3 loss from 20 soils of widely differing properties from Northern Ireland were measured over 14 days using ventilated enclosures under simulated spring conditions. Cumulative loss rates were calculated and fitted to a logistic model from which total NH3 loss (Amax) and the time to maximum rate of loss (Tmax) were determined. Stepwise multiple linear regression analysis related the effectiveness of PPD in reducing NH3 volatilization from urea to soil properties.The total cumulative loss of ammonia from unamended urea varied from 0.37 to 29.2% depending on soil type. Ammonia volatilization appeared to be greatest on a soil with a high pH (R2 = 0.65), a low titratable acidity (TA) (R2 = 0.63) and a soil that was drying out (R2 = 0.50). Soil pH was negatively correlated with TA (r = –0.826, P < 0.001) suggesting that soils with a low TA may have received recent lime. Including cation exchange capacity (CEC) and % N as well as pH-KCl in the multiple linear regression equation explained 86% of the variance.The effectiveness of PPD in reducing Amax varied between 0% to 91% depending on soil type, the average over all 20 soils being 30 and 36% for 0.5% and 1% PPD respectively. The most important soil properties influencing the effectiveness of the urease inhibitor were soil pH-H2O and TA accounting for 33% and 29% of the variance respectively. PPD was less effective on a soil with a high pH and low TA. These were the soil conditions that led to high NH3 volatilization from unamended urea and may explain why PPD had limited success in reducing ammonia loss on these soils. Multiple linear regression analysis indicated that 75% of the variation in the % inhibition of NH3 loss by PPD could be significantly accounted for by pH-H2O, initial soil NO
3
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-N concentration, % moisture content and % moisture loss.The delay in Tmax by PPD ranged from 0.19 to 7.93 days, the average over all 20 soils being 2.5 and 2.8 days for 0.5% and 1% PPD respectively. TA, % moisture content, urease activity and CEC were soil properties that significantly explained 83% of the variation in the % delay in Tmax by PPD in multiple linear regression analysis. However, none of these soil properties were significant on their own. As urea hydrolysis occurs rapidly in soil, delaying Tmax under field conditions would increase the chance of rain falling to move the urea below the soil surface and reduce NH3 volatilization. A urease inhibitor should be more effective than PPD on soils with a high pH and low TA to be successful in reducing high NH3 losses. 相似文献
109.
Catherine A. Fromen Tammy W. Shen Abigail E. Larus Peter Mack Benjamin W. Maynor J. Christopher Luft Joseph M. DeSimone 《American Institute of Chemical Engineers》2013,59(9):3184-3194
The top‐down, micromolding technique, referred to as Particle Replication in Nonwetting Templates (PRINT®), affords a new opportunity for the generation of inhalation therapeutics. Powders were fabricated with predetermined particle size and shape; when dispersed with a collision jet nebulizer, these particles resulted in monodisperse aerosols with geometric standard deviations well below 1.2. Dynamic shape factors for this novel set of uniformly shaped particles were determined by correcting the drag of nonspherical particles in the ultra‐Stokesian flow conditions of the aerodynamic particle sizer (APS). This convenient approach for shape factor determination agreed well with current literature approaches and allowed for the correction of APS results for particles with known volumes. Determined shape factor values of PRINT geometries were used to estimate the theoretical median aerodynamic diameters of individual aerosols, which were then compared to actual inhalation powders. © 2013 American Institute of Chemical Engineers AIChE J, 59: 3184–3194, 2013 相似文献
110.
Majid Soleimani Lope G. Tabil Catherine Niu 《American Institute of Chemical Engineers》2015,61(6):1783-1791
The kinetics of acid‐catalyzed hemicellulose removal and also alkaline delignification of oat hull biomass were investigated. All three operational parameters namely, catalyst concentration (0.10–0.55 N H2SO4), temperature (110–130°C), and residence time (up to 150 min) affected the efficiency of hemicellulose removal, with 100% of hemicellulose removed by appropriate selection of process parameters. Analysis of delignification kinetics (in the temperature range of 30–100°C) indicated that it can be expressed very well by a two‐phase model for the crude biomass and also for the hemicellulose‐prehydrolyzed material. The application of acid‐catalyzed prehydrolysis improved the capacity of lignin dissolution especially at lower temperatures (30 and 65°C) and accelerated the dissolution of lignin. This acceleration of delignification by prehydrolysis was possible at all levels of temperature in the bulk phase; however, results were more significant at the lower temperatures in the terminal phase. © 2015 American Institute of Chemical Engineers AIChE J, 61: 1783–1791, 2015 相似文献