bluuebunny/crossref_metadata_2025_split huggingface dataset:
Absorption of CH330331, a novel 4‐anilinoquinazoline inhibitor of epidermal growth factor receptor tyrosine kinase: comparative studies using in vitro, in situ and in vivo models
Authors: Sun Haiyan , Bi Huichang , Huang Min , Liu Dong , Qin Zhenyu 
Published: October 2010

AbstractCH330331 is a prototype of a new class of synthetic small molecule tyrosine kinase inhibitors (TKIs). In vitro Caco‐2 cell monolayers, the in situ single‐pass rat intestinal perfusion (SPIP) technique with mesenteric vein cannulated and an in vivo animal model were employed to investigate its permeability and transepithelial transport mechanisms. The Caco‐2 model showed that the transport of CH330331 across the monolayers from the apical (AP) to basolateral (BL) side was 6‐ to 10‐fold higher than that from the BL to AP side. The apparent permeability coefficient (Papp) values of CH330331 at 5–20 µg/ml from the AP to BL and from BL to AP side were 5.30–2.21 × 10−6 cm/s, with a decrease in Papp values from the AP to BL side at increased CH330331 concentrations. In the perfused rat intestinal model, a concentration dependent change in permeability was detected where Pblood at 5 µg/ml (1.66 ± 0.69 × 10−6 cm/s) and 10 µg/ml (1.80 ± 0.45 × 10−6 cm/s) was significantly different from Pblood at 20 µg/ml (0.98 ± 0.31 × 10−6 cm/s, p<0.05). Some inhibitors could also change the transepithelial transport of CH330331. Moreover, the in vivo study showed that the oral bioavailability of CH330331 was 82.7% in the rat. All the results confirmed that the transepithelial transport of CH330331 was rapid and saturable, which might involve an active mechanism. The oral bioavailability of CH330331 was relatively high in vivo. Copyright © 2010 John Wiley & Sons, Ltd.
The effect of drugs with ion channel‐blocking activity on the early embryonic rat heart
Authors: Abela Dominique , Ritchie Helen , Ababneh Deena , Gavin Caroline , Nilsson Mats F. , Khan Muhammad Khalid , Carlsson Kristin , Webster William S. 
Published: October 2010

AbstractThis study investigated the effects of a range of pharmaceutical drugs with ion channel‐blocking activity on the heart of gestation day 13 rat embryos in vitro. The general hypothesis was that the blockade of theIKr/hERG channel, that is highly important for the normal functioning of the embryonic rat heart, would cause bradycardia and arrhythmia. Concomitant blockade of other channels was expected to modify the effects of hERG blockade. Fourteen drugs with varying degrees of specificity and affinity toward potassium, sodium, and calcium channels were tested over a range of concentrations. The rat embryos were maintained for 2 hr in culture, 1 hr to acclimatize, and 1 hr to test the effect of the drug. All the drugs caused a concentration‐dependent bradycardia except nifedipine, which primarily caused a negative inotropic effect eventually stopping the heart. A number of drugs induced arrhythmias and these appeared to be related to either sodium channel blockade, which resulted in a double atrial beat for each ventricular beat, orIKr/hERG blockade, which caused irregular atrial and ventricular beats. However, it is difficult to make a precise prediction of the effect of a drug on the embryonic heart just by looking at the polypharmacological action on ion channels. The results indicate that the use of the tested drugs during pregnancy could potentially damage the embryo by causing periods of hypoxia. In general, the effects on the embryonic heart were only seen at concentrations greater than those likely to occur with normal therapeutic dosing.Birth Defects Res (Part B)89:429–440, 2010. © 2010 Wiley‐Liss, Inc.
Thalidomide Derivatives for the Treatment of Neuroinflammation
Authors: Contino‐Pépin Christiane , Parat Audrey , Patinote Cindy , Roscoe Wendi A. , Karlik Stephen J. , Pucci Bernard 
Published: October 2010

AbstractThe precise mechanism‐of‐action of thalidomide remains uncertain and might differ between diseases and under different clinical condition. With implications in the treatment of a variety of inflammatory and autoimmune diseases, as well as for use as an anticancer agent, alone or in combination with established therapeutics, it is clear that thalidomide and its derivatives deserve further scrutiny. In particular, thalidomide was shown to be effective in a mouse model of multiple sclerosis (MS), an autoimmune inflammatory disorder, called experimental autoimmune encephalomyelitis (EAE). Herein, we describe the synthesis and preliminary biological evaluation of new macromolecular prodrugs of thalidomide bearing an aminoalkyl group on the phthalimide ring. The effectiveness of these compounds to limit EAE was investigated, and it was shown that, at 100 mg kg−1 thalidomide‐equivalent dose, they abrogated the clinical and pathological features of EAE.
Hydrolysis of Cellulose by Using Catalytic Amounts of FeCl2 in Ionic Liquids
Authors: Tao Furong , Song Huanling , Chou Lingjun 
Published: October 2010

AbstractMicrocrystalline cellulose (MCC) is hydrolyzed to an appreciable extent (70 %) by using 1‐(4‐sulfonic acid) butyl‐3‐methylimidazolium hydrogen sulfate (IL‐1) as effective catalyst. Valuable chemicals, such as 5‐hydroxymethyl furfural (HMF) and furfural, are obtained in relatively high yields (15 % and 7 %, respectively). Interestingly, the introduction of FeCl2 as catalyst into IL‐1 further enhances the catalytic activity, as proved by the higher conversion of MCC (84 %) and higher yields of HMF and furfural (34 % and 19 %, respectively) under the same experimental conditions, although small amounts of levulinic acid (LA) and total reducing sugars (TRS) were also found. The hydrolysis of MCC scarcely proceeded, or showed a lower efficiency, in the absence of catalyst (4 %) or with Al2O3 (7 %), inorganic acids (≤65 %), or several other ionic liquids (≤24 %) as catalyst. Dimers of furan compounds were detected as the main byproducts, as analyzed by HPLC–MS; from the mass spectrometry analysis, the components of the gas‐phase products were determined to be methane, ethane, CO, CO2, and H2. A mechanism to explain the high activity of FeCl2 in the IL‐1 system is proposed. Recycling of the IL‐1 catalyst showed an almost constant activity during five successive trials. The simple and effective catalyst system may prove valuable in facilitating the energy‐efficient and cost‐effective conversion of biomass into biofuels and platform chemicals.
Wnt/calcium signaling mediates axon growth and guidance in the developing corpus callosum
Authors: Hutchins B. Ian , Li Li , Kalil Katherine 
Published: October 2010

AbstractIt has been shown in vivo that Wnt5a gradients surround the corpus callosum and guide callosal axons after the midline (postcrossing) by Wnt5a‐induced repulsion via Ryk receptors. In dissociated cortical cultures we showed that Wnt5a simultaneously promotes axon outgrowth and repulsion by calcium signaling. Here to test the role of Wnt5a/calcium signaling in a complex in vivo environment we used sensorimotor cortical slices containing the developing corpus callosum. Plasmids encoding the cytoplasmic marker DsRed and the genetically encoded calcium indicator GCaMP2 were electroporated into one cortical hemisphere. Postcrossing callosal axons grew 50% faster than pre‐crossing axons and higher frequencies of calcium transients in axons and growth cones correlated well with outgrowth. Application of pharmacological inhibitors to the slices showed that signaling pathways involving calcium release through IP3 receptors and calcium entry through TRP channels regulate post‐crossing axon outgrowth and guidance. Co‐electroporation of Ryk siRNA and DsRed revealed that knock down of the Ryk receptor reduced outgrowth rates of postcrossing but not precrossing axons by 50% and caused axon misrouting. Guidance errors in axons with Ryk knockdown resulted from reduced calcium activity. In the corpus callosum CaMKII inhibition reduced the outgrowth rate of postcrossing (but not precrossing) axons and caused severe guidance errors which resulted from reduced CaMKII‐dependent repulsion downstream of Wnt/calcium. We show for the first time that Wnt/Ryk calcium signaling mechanisms regulating axon outgrowth and repulsion in cortical cultures are also essential for the proper growth and guidance of postcrossing callosal axons which involve axon repulsion through CaMKII. © 2010 Wiley Periodicals, Inc. Develop Neurobiol 71: 269–283, 2011.
The reasons why eating disorder patients drink
Authors: Hart Susan , Abraham Suzanne , Franklin Richard C. , Russell Janice 
Published: October 2010

AbstractObjectiveTo explore the reasons why eating disorder patients consume non‐alcoholic fluids and to examine variables associated with poor and excessive drinking.MethodsA sample of 115 patients admitted for inpatient treatment to a specialist eating disorder facility completed a semi‐standardised retrospective fluid intake history of type and amount of fluid and of reasons for drinking. ANOVA, chi‐square and factor analysis were performed.ResultsThe main reasons for consuming fluids were for fullness and appetite suppression; for feelings of control including feeling empty; to assist with purging; and for physiological reasons such as drinking when thirsty, after exercising and to increase energy levels via caffeine ingestion.DiscussionAn eating disorder needs to be considered a disorder of fluid intake, as much as a disorder of food intake. Factors affecting the fluid intake of eating disorder patients are related to the presence of eating disorder behaviours. Copyright © 2010 John Wiley & Sons, Ltd and Eating Disorders Association.
River channel and bar patterns explained and predicted by an empirical and a physics‐based method
Authors: Kleinhans Maarten G. , van den Berg Jan H. 
Published: October 2010

AbstractOur objective is to understand general causes of different river channel patterns. In this paper we compare an empirical stream power‐based classification and a physics‐based bar pattern predictor. We present a careful selection of data from the literature that contains rivers with discharge and median bed particle size ranging over several orders of magnitude with various channel patterns and bar types, but no obvious eroding or aggrading tendency. Empirically a continuum is found for increasing specific stream power, here calculated with pattern‐independent variables: mean annual flood, valley gradient and channel width predicted with a hydraulic geometry relation. ‘Thresholds’, above which certain patterns emerge, were identified as a function of bed sediment size. Bar theory predicts nature and presence of bars and bar mode, here converted to active braiding index (Bi). The most important variables are actual width–depth ratio and nonlinearity of bed sediment transport. Results agree reasonably well with data. Empirical predictions are somewhat better than bar theory predictions, because the bank strength is indirectly included in the empirical prediction. In combination, empirical and theoretical prediction provide partial explanations for bar and channel patterns. Increasing potential‐specific stream power implies more energy to erode banks and indeed correlates to channels with high width–depth ratio. Bar theory predicts that such rivers develop more bars across the width (higher Bi). At the transition from meandering to braiding, weakly braided rivers and meandering rivers with chutes are found. Rivers with extremely low stream power and width–depth ratios hardly develop bars or dynamic meandering and may be straight or sinuous or, in case of disequilibrium sediment feed, anastomosing. Copyright © 2010 John Wiley & Sons, Ltd.
Terrestrial laser scanning soil surfaces: a field methodology to examine soil surface roughness and overland flow hydraulics
Authors: Smith Mark W. , Cox Nicholas J. , Bracken Louise J. 
Published: October 2010

AbstractConventional roughness–resistance relationships developed for pipe and open‐channel flows cannot accurately describe shallow overland flows over natural rough surfaces. This paper develops a new field methodology combining terrestrial laser scanning (TLS) and overland flow simulation to provide a high‐resolution dataset of surface roughness and overland flow hydraulics as simulated on natural bare soil surfaces. This method permits a close examination of the factors controlling flow velocity and a re‐evaluation of the relationship between surface roughness and flow resistance. The aggregate effect of flow dynamics, infiltration and depression storage on retarding the passage of water over a surface is important where runoff‐generating areas are distant from well‐defined channels. Experiments to separate these effects show that this ‘effective resistance’ is dominated by surface roughness. Eight measurements of surface roughness are found to be related to flow resistance: standard deviation of elevations, inundation ratio, pit density (measured both perpendicular and parallel to the flow direction), slope, median depth, skewness of the depth distribution and frontal area. Hillslope position is found to affect the significant roughness measures. In contrast, infiltration rate has little effect on the velocity of water fronts advancing over the soil surfaces examined here and the effect of depression storage is limited. Overland flow resistance is depth dependent where complex microtopographic structures are progressively inundated. Copyright © 2010 John Wiley & Sons, Ltd.
Development and application of a physically based landscape water balance in the SWAT model
Authors: White Eric D. , Easton Zachary M. , Fuka Daniel R. , Collick Amy S. , Adgo Enyew , McCartney Matthew , Awulachew Seleshi B. , Selassie Yihenew G. , Steenhuis Tammo S. 
Published: October 2010

AbstractWatershed scale hydrological and biogeochemical models rely on the correct spatial‐temporal prediction of processes governing water and contaminant movement. The Soil and Water Assessment Tool (SWAT) model, one of the most commonly used watershed scale models, uses the popular curve number (CN) method to determine the respective amounts of infiltration and surface runoff. Although appropriate for flood forecasting in temperate climates, the CN method has been shown to be less than ideal in many situations (e.g. monsoonal climates and areas dominated by variable source area hydrology). The CN model is based on the assumption that there is a unique relationship between the average moisture content and the CN for all hydrologic response units (HRUs), and that the moisture content distribution is similar for each runoff event, which is not the case in many regions. Presented here is a physically based water balance that was coded in the SWAT model to replace the CN method of runoff generation. To compare this new water balance SWAT (SWAT‐WB) to the original CN‐based SWAT (SWAT‐CN), two watersheds were initialized; one in the headwaters of the Blue Nile in Ethiopia and one in the Catskill Mountains of New York. In the Ethiopian watershed, streamflow predictions were better using SWAT‐WB than SWAT‐CN [Nash–Sutcliffe efficiencies (NSE) of 0·79 and 0·67, respectively]. In the temperate Catskills, SWAT‐WB and SWAT‐CN predictions were approximately equivalent (NSE > 0·70). The spatial distribution of runoff‐generating areas differed greatly between the two models, with SWAT‐WB reflecting the topographical controls imposed on the model. Results show that a water balance provides results equal to or better than the CN, but with a more physically based approach. Copyright © 2010 John Wiley & Sons, Ltd.
Pan evaporation and potential evapotranspiration trends in South Florida
Authors: Abtew Wossenu , Obeysekera Jayantha , Iricanin Nenad 
Published: October 2010

AbstractDeclining trends in pan and lake evaporation have been reported. It is important to study this trend in every region to evaluate the validity of the trend and water management implications. Data from nine pan evaporation sites in South Florida were evaluated to see if there is a trend and if the quality of the data is sufficient for such analysis. The conclusion is that pan evaporation measurements are prone to too many sources of errors to be used for trend analysis. This condition is demonstrated in South Florida and in other regions by differences in magnitude and direction between spatially related pan stations and unexplainable observations. Also, potential evapotranspiration (ETp) was estimated with the Simple (Abtew equation) and the Penman–Monteith method. Both cases indicated no decline in evapotranspiration for the period of analysis. Based on the decline in humidity and the increasing trend in vapor pressure deficit for the short period of analysis, 1992–2009, it appears that South Florida is experiencing increase in evaporation and evapotranspiration at this time assuming no systematic error in the weather stations' observations. Copyright © 2010 John Wiley & Sons, Ltd.
Testicular development evaluation in rats exposed to 60 Hz and 1 mT electromagnetic field
Authors: Tenorio Bruno Mendes , Jimenez George Chaves , Morais Rosana Nogueira , Torres Sandra Maria , Albuquerque Nogueira Romildo , Silva Junior Valdemiro Amaro 
Published: October 2010

AbstractSociety has been increasingly exposed to low‐frequency electromagnetic fields (EMF), mainly from electricity distribution networks and electro‐electronic devices. Aiming to clarify the extension of possible interactions between EMF and testicular development, this study evaluated the effects of exposure to 60 Hz and 1 mT EMF in the maturation of testicular components. Wistar rats were exposed to EMF three times per day for 30 min, between the 13th day of gestation and the 21st postnatal day. Results showed a decrease in the following parameters: tubular diameter and seminiferous tubules area; seminiferous epithelium height; total volume of seminiferous tubule; tubular lumen; seminiferous epithelium; and Leydig cells. On the other hand, an increase was observed in connective tissue cells and blood vessels volume. Plasma testosterone, Sertoli cells population, tubular length and gonadosomatic index did not change when exposed to EMF. Histomorphometric analysis showed that exposure to EMF can promote a delay in testicular development. Copyright © 2010 John Wiley & Sons, Ltd.
High‐resolution imaging and nano‐manipulation of biological structures on surface
Authors: Zhang Yi , Hu Xiaofang , Sun Jielin , Shen Yi , Hu Jun , Xu Xuemin , Shao Zhifeng 
Published: October 2010

AbstractIn this mini‐review we discuss our recent findings on imaging and manipulation of biological macromolecular structures by atomic force microscopy (AFM). In the first part of this review, we focus on high‐resolution imaging of selected biological samples. AFM images of membrane proteins have revealed detailed conformational features related to identifiable biological functions. Different self‐assembling behaviors of short peptides into supramolecular structures on various substrates under controlled environmental conditions have been systematically studied with AFM imaging. In the second part, we present a novel nano‐manipulation technique for manipulating, isolating, amplifying, and sequencing of individual DNA molecules, which may find unique applications in the analysis of difficult sequence structures. Finally, we discuss how to characterize the elasticity of individual biomolecules and live cells. These results demonstrate that not only the high resolution capacity of the AFM is suited to resolve certain biological questions, but can also be applied to single molecule isolation and biomechanical analysis with its unique advantages. Microsc. Res. Tech., 2011. © 2010 Wiley‐Liss, Inc.
Effect of arsenic absorption on the water‐refilling speed of Pteris cretica
Authors: Lee Sang Joon , Lee Jin Pyung 
Published: October 2010

AbstractHeavy metals are largely responsible for soil and water pollution. Recently, phytoremediation is receiving a large attention as a plant‐based technology for removing metals from contaminated soil and water in an environment‐friendly and cost‐effective way. In such context, some species of ferns such as Pteris cretica were found to be a hyper‐accumulator of arsenic (As). In this study, we first explored the validity of measuring the water‐refilling process in xylem vessels of Pteris cretica using the synchrotron X‐ray microimaging technique. Then we investigated the effects of arsenic concentration on the water‐refilling speed inside the xylem vessel. The methodology to measure the water‐refilling speed was consistent within five repetitions and 3 hours after the stem sample was cut from the plant. The water‐refilling speed in the xylem vessels of the Pteris grown in arsenic solution was faster than that in normal water. Arsenic concentration of 0–1,000 μM was tested and the maximum speed was obtained at 500 μM. Conclusively, the experimental methodology developed in this study allowed to obtain some interesting results for understanding how arsenic affect the xylem sap flow transport and the mechanism by which growth is enhanced in the presence of heavy metal. Microsc. Res. Tech., 2010. © 2010 Wiley‐Liss, Inc.
p120 catenin/αN‐catenin are molecular targets in the neuroprotection and neuronal plasticity mediated by atorvastatin after focal cerebral ischemia
Authors: Céspedes‐Rubio Angel , Jurado Francisco Wandosell , Cardona‐Gómez Gloria Patricia 
Published: October 2010

AbstractAtorvastatin (ATV), a 3‐hydroxy 3‐methylglutaryl coenzyme A (HMG‐CoA) reductase inhibitor, exerts beneficial effects on stroke through several pleiotropic mechanisms. However, its role following cerebral ischemia is not completely understood yet. We evaluated the effect of ATV treatment on the synaptic adhesion proteins after a transient middle cerebral artery occlusion (t‐MCAO) model in rats. Ischemic male Wistar rats were treated with 10 mg/kg ATV. The first dose was 6 hr after reperfusion, then every 24 hr for 3days. Our findings showed that ATV treatment produced an increase in pAkt ser473 and a decrease in pMAPK 44/42 protein levels 12 and 24 hr postischemia in the cerebral cortex and the hippocampus. However, p120 catenin and αN‐catenin became drastically increased throughout the temporal course of postischemia treatment (12–72 hr), mainly in the hippocampus. Neurological recovery was observed at 48 and 72 hr, supported by a significant reduction of infarct volume, neuronal loss, and glial hyperreactivity after 72 hr of postischemia treatment with ATV. ATV treatment also up‐regulated the association of p120ctn, αN‐catenin to PSD‐95, accompanied by a reduction of RhoA activation and the recovery of MAP2 immunoreactivity, these being significantly affected by the focal cerebral ischemia. Our findings suggested that p120ctnand αN‐catenin synaptic adhesion proteins are crucial molecular targets in ATV‐mediated neuroprotection and neuronal plasticity after focal cerebral ischemia. © 2010 Wiley‐Liss, Inc.