UK PubMed Central (United Kingdom)

BackgroundFinasteride, a 5 alpha reductase inhibitor, is an established treatment for benign prostatic hyperplasia. The recommended dosage is 5 mg a day, however case reports have...Full Text Available

Science.gov (United States)

Calcium-activated chloride channels (CaCCs) are widely expressed in mammalian tissues, including intestinal epithelia, where they facilitate fluid secretion. Potent, selective CaCC inhibitors have not been available. We established a high-throughput screen for identification of inhibitors of a human intestinal CaCC based on inhibition of ATP/carbachol-stimulated iodide influx in HT-29 cells after lentiviral infection with the yellow fluorescent halide-sensing protein YFP-H148Q/I152L. Screening of 50,000 diverse, drug-like compounds yielded six classes of putative CaCC inhibitors, two of which, 3-acyl-2-aminothiophenes and 5-aryl-2-aminothiazoles, inhibited by >95% iodide influx in HT-29 cells in response to multiple calcium-elevating agonists, including thapsigargin, without inhibition of calcium elevation, calcium-calmodulin kinase II activation, or cystic fibrosis transmembrane conductance regulator chloride channels. ...

Science.gov (United States)

Spectrophotometric method, using a ratio-recording ultraviolet-absorption spectrophotometer, permits analysis of NaMBT in ethylene glycol-water solutions with high accuracy. It reduces analysis time, requires smaller samples, and is able to detect extremely small concentrations of mercaptobenzothiazole.

Energy Technology Data Exchange (ETDEWEB)

To evaluate the effect of porosity on superplasticity behavior, it is essential to use materials of similar initial grain sizes. This can be achieved by HIPing, which provides an effective way of reducing initial porosity while avoiding appreciable grain growth; various levels of porosity can be achieved for similar grain sizes. This note is concerned with the influence of porosity on superplasticity tensile deformation of a fine grained high-purity alumina doped with copper oxide and containing a grain growth inhibitor. Specimens were prepared by slip casting to net-shape and sintering; some presintered specimens were HIPed to reduce porosity. The subsequent superplasticity behavior is related to porosity in the material.

Science.gov (United States)

1. Choline, and the choline analogues monoethylcholine (MEC) and N-aminodeanol (NAD) were examined for prophylactic activity in acute acetylcholinesterase inhibitor toxicity in mice. The rank order of potency of the compounds was MEC greater than NAD greater than choline. 2. Simultaneous administration of MEC (60 mg kg-1) or NAD (200 mg kg-1) with physostigmine reduced lethality to 17 and 13% respectively. MEC (60 mg kg-1) completely protected against disopropylfluorophosphate (DFP) and diazinon toxicity, and NAD reduced lethality to 17% for both agents. Choline (200 mg kg-1) exhibited only negligible antidotal activity against the inhibitors. 3. In vitro concentrations of choline, MEC, and NAD, similar to the estimated concentration obtained in vivo in the acute toxicity study, produced mixed inhibition of mouse brain acetylcholinesterase. The inhibition was dose-related and was additive to the ...

Wastenet

... Corrosion Inhibitors Equipment on Environmental Expert Find and compare a variety of corrosion inhibitors equipment on the world's largest environmental industry portal. View ...

International Nuclear Information System (INIS)

Those materials that can be extracted from pine or oak by ether, ethanol, methyl methacrylate (MMA), or benzene--alcohol all act as inhibitors in the #gamma# polymerization of MMA--wood composites. It was found that preirradiation of either the wood or of the wood--monomer combination reduces or eliminates the inhibitory effect. The most practical industrial solution to this problem is to increase the dose, thereby achieving high molecular polymer in the composite. However, the presence of a maximum in the molecular weight--dose curves means that each wood--monomer pair may have a different optimum dose.

Science.gov (United States)

The transcriptional silencing of some cell cycle inhibitors and tumor suppressors, such as p16 and retinoic acid receptor beta(2), by DNA hypermethylation at CpG islands is commonly found in human oral squamous carcinoma cells. We examined the effects of the DNA methyltransferase inhibitor 5-Aza-2'-deoxycytidine (5-Aza; 0.25 mg/kg body weight), all-trans retinoic acid (RA; given at 100 microg/kg body weight and 1 mg/kg body weight), and the combination of 5-Aza and the low-dose RA on murine oral cavity carcinogenesis induced by the carcinogen 4-nitroquinoline 1-oxide (4-NQO) in a mouse model. All the drug treatments were done for 15 weeks after a 10-week 4-NQO treatment. Mice in all drug treatment groups showed decreases in the average numbers of neoplastic tongue lesions. The combination of 5-Aza and RA effectively attenuated tongue lesion severity. Although all drug treatments limited the increase in the percentage of proliferating cell ...

British Library Electronic Table of Contents (United Kingdom)

Cyclothiazomycin B1 (CTB1) is an antifungal cyclic thiopeptide isolated from the culture broth of Streptomyces sp. HA 125-40. CTB1 inhibited the growth of several filamentous fungi including plant pathogens along with swelling of hyphae and spores. The antifungal activity of CTB1 was weakened by hyperosmotic conditions, and hyphae treated with CTB1 burst under hypoosmotic conditions, indicating increased cell wall fragility. CTB1-sensitive fungal species contain high levels of cell wall chitin and/or chitosan. Unlike nikkomycin Z, a competitive inhibitor of chitin synthase (CHS), CTB1 did not inhibit CHS activity. Although CTB1 inhibited CHS biosynthesis, the same result was also obtained with a non-specific proteins inhibitor, cycloheximide, which did not reduce cell wall rigidity. These ...

Energy Technology Data Exchange (ETDEWEB)

Niobium carbide can be used to inhibit WC grain growth in hardmetal. The performance of a NbC powder produced at low temperature by solid-gas reaction (an experimental powder) as WC grain growth inhibitor is compared with that of a commercial NbC powder. It is verified that NbC effectively inhibits heterogeneous WC coarsening. This results in an increase in hardness. The commercial and experimental NbC powders exhibit a comparable performance in inhibiting the WC grain coarsening, in spite of a significant difference in particle size and shape. The commercial NbC powder is very fine while the experimental one is coarse and porous, but its crystallites are finer than those of the commercial product. The milling procedure used to prepare the alloys is able to reduce the particle size of the experimental NbC, and thus guarantee a dispersion of the particles with a quality level comparable to that found for the alloy prepared with the commercial ...

UK PubMed Central (United Kingdom)

Background and purpose:Diphenyleneiodonium (DPI) is often used as an NADPH oxidase inhibitor, but is increasingly being found to have unrelated side effects. We investigated its...Full Text Available

UK PubMed Central (United Kingdom)

Chemical genetics is an emerging approach to investigate the biology of host-pathogen interactions. We screened several inhibitors of ATP-dependent DNA motors and detected the gyrase B inhibitor coumermycin...Full Text Available

International Science & Technology Center (ISTC)

The Production of Highly Active Human Blood Plasma Butyrylcholinesterase Preparation by Gene Engineering Methods to Create Protective Means against Poisoning by Organophosphorous Cholinesterase Inhibitors

International Nuclear Information System (INIS)

Under operational conditions in nuclear power plants, the carbon steel components of the primary and secondary circuits react with high temperature cooling agent forming several iron oxides and oxyhydroxides. These deposits can result in tubes' constrictions, pitting and intergranular corrosion and finally to heat transfer reducing and increasing of radiation fields around the circuits, as well. The descaling process involves the chemical dissolution of the corrosion deposits by means of diluted organic acidic solutions containing usually a carboxylic acid, a reductant and one or more corrosion inhibitors. To evaluate the removing rates of these superficial films two types of methods were used, the gravimetric and potentiodynamic techniques. By correlating the experimental results, we established the chemical composition of descaling solution and two models of mechanisms applicable to our specific conditions. (authors)

International Nuclear Information System (INIS)

This report discusses the work done on EPRI program S149-1. In this program the feasibility of cleaning steam generators off line with organic chelants as a means of arresting denting corrosion was investigated. The rationale behind this program is to make use of those periods during which nuclear steam generators are in cold shutdown or wet layup to carry out a low-temperature soak with a combined chelant-inhibitor solution in order to dissolve some of the magnetite which has built up in crevices and to concomitantly remove entrained corrodents such as chloride ion. It was hoped that these soaks would be effective in reducing carbon steel support plate corrosion which produces tube denting.

International Nuclear Information System (INIS)

Air flow rates and carbon dioxide concentrations of air entering and exiting eight H-Area waste tanks were monitored for a period of one year. The average instanteous concentration of carbon dioxide in air is within the range reported offsite, and therefore is not affect by operation of the coal-fired power plant adjacent to the tank farm. Waste solutions in each of the tanks were observed to be continuously absorbing carbon dioxide. The rate of absorption of carbon dioxide decreased linearly with the pH of the solution. Personnel exposure associated with the routine sampling and analysis of radioactive wastes stored at SRP to determine the levels of corrosion inhibitors in solution could be reduced by monitoring the absorption of carbon dioxide and using the relationship between pH and carbon dioxide absorption to determine the free hydroxide concentration in solution.

KoreaScience (Korea)

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Science.gov (United States)

Treatment Induced Hypertension

DEFF Research Database (Denmark)

Udgivelsesdato: 2008-Jul-15

British Library Electronic Table of Contents (United Kingdom)

The acid corrosion inhibition process of mild steel in 1M HCl by 1-butyl-3-methylimidazolium chlorides (BMIC) and 1-butyl-3-methylimidazolium hydrogen sulfate ([BMIM]HSO4) has been investigated using electrochemical impedance, potentiodynamic polarization and weight loss measurements. Potentiodynamic polarization studies indicate the studied inhibitors are mixed type inhibitors. For both inhibitors, the inhibition efficiency increased with increase in the concentration of the inhibitor and the effectiveness of the two inhibitors are in the order [BMIM]HSO4>BMIC. The adsorption of the inhibitors on mild steel surface obeyed the Langmuirs adsorption isotherm. The effect of temperature on the corrosion behavior in the presence of 5x10-3M of inhibitors was studied in the temperature range of 3...

British Library Electronic Table of Contents (United Kingdom)

Abstract Common single nucleotide polymorphisms (SNPs) in SMAD7 (18q21) have been linked to colorectal cancer (CRC) risk in genome-wide association studies, but little is known about their effects on survival. SMAD7 regulates gastrointestinal inflammation by inhibiting transforming growth factor- (TGFB), which can act as both a tumor suppressor and a promoter of metastasis. Regular use of cyclooxygenase-2 (COX2) inhibitors, such as nonsteroidal anti-inflammatory drugs (NSAIDs), reduces the risk of developing CRC. Because COX2 overexpression reduces the growth suppressing effects of TGFB, we hypothesized that survival may depend on both SMAD7 genotype and prediagnostic NSAID use. Postmenopausal women, ages 50-74, diagnosed with incident invasive CRC from 1997 to 2002 were identified using t...

British Library Electronic Table of Contents (United Kingdom)

Histone deacetylase (HDAC) inhibitors have been actively exploited as potential anticancer agents. To identify gene targets of HDAC inhibitors, we found that HDAC inhibitors such as sodium butyrate, scriptaid, apicidin and oxamflatin induced the expression of 15-hydroxyprostaglandin dehydrogenase (15-PGDH), a potential cyclooxygenase-2 (COX-2) antagonist and tumor suppressor, in a time and concentration dependent manner in A549 and H1435 lung adenocarcinoma cells. Detailed analyses indicated that HDAC inhibitors activated the 15-PGDH promoter-luciferase reporter construct in transfected A549 cells. A representative HDAC inhibitor, scriptaid, and its negative structural analog control, nullscript, were further evaluated at the chromatin level. Scriptaid but not nullscript induced a signific...

Science.gov (United States)

The IRG protein Irgm3 preserves cell survival during coxsackievirus B3 (CVB3) infection. However, the molecular mechanisms are not clear. Here, we examined the effect of Irgm3 expression on ER stress triggered by pharmacological agents or CVB3 infection. In Tet-On/Irgm3 HeLa cells, Irgm3 expression suppressed either chemical- or CVB3-induced upregulation of glucose-regulated protein78. Further, Irgm3 strongly inhibited the activation of both the PERK and ATF6 pathways of ER stress responses, which further led to the diminished phosphorylation of eIF2?, reduced cleavage/activation of transcription factor SREBP1 and attenuated induction of proapoptotic genes CHOP and GADD34. These data were further supported by experiments using Irgm3 knockout mouse embryonic fibroblasts, in which the ER stress induced by CVB3 was not relieved due to the lack of Irgm3 expression. In addition, the tunicamycin-triggered ER stress promoted the subsequent CVB3 infection. The effect of ...

Science.gov (United States)

beta-Bungarotoxin (beta-Bgt), a presynaptic phospholipase A(2) (PLA(2)) neurotoxin isolated from the venom of Bungarus multicinctus, consists of A chain and B chain. The goal of the present study is to explore the functional contribution of the two subunits to the toxicity of beta-Bgt. beta-Bgt was found to induce apoptotic death of SK-N-SH cells via elevating intracellular Ca(2+) and intracellular ROS production. Moreover, an activation of p38 MAPK was associated with the cytotoxicity of beta-Bgt. SB202190 (p38 MAPK inhibitor), N-acetylcysteine (antioxidant reagent), 1,2-bis(2-aminophenoxy)ethane-N,N,N,N-tetraacetic acid (BAPTA) (Ca(2+) chelator) and the inhibitors of Ca(2+) release from intracellular depots (ruthenium red and 2-aminoethoxydiphenyl borate) effectively attenuated the cytotoxicity of beta-Bgt. In sharp contrast to the inability of A chain, B chain was able to induce cytotoxic effects on SK-N-SH cells as beta-Bgt did. Abolishment ...

UK PubMed Central (United Kingdom)

The canonical Wnt/β-catenin pathway plays a pivotal role in regulating embryogenesis and tumorigenesis by promoting cell proliferation. BAMBI (BMP and activin membrane-bound inhibitor) has...Full Text Available

UK PubMed Central (United Kingdom)

Since Src kinase inhibitors decrease brain injury produced by intracerebral hemorrhage (ICH) and thrombin is activated following ICH, this study determined whether Src kinase inhibitors decrease...Full Text Available

UK PubMed Central (United Kingdom)

Epidermal growth factor receptor (EGFR) related therapies – mainly tyrosine kinase inhibitors (TKIs) such as erlotinib and gefitinib, but also monoclonal antibodies targeting EGFR, for example,...Full Text Available

UK PubMed Central (United Kingdom)

Peptic ulcer bleeding is a common disease and recurrent bleeding is an independent risk factor of mortality. Infusion with proton pump inhibitors (PPIs) prevents recurrent bleeding after successful...Full Text Available

UK PubMed Central (United Kingdom)

4-methylumbelliferone (4-MU) is a hyaluronic acid (HA) synthesis inhibitor with anticancer properties; the mechanism of its anticancer effects is unknown. We evaluated the effects of 4-MU on...Full Text Available

Energy Technology Data Exchange (ETDEWEB)

The mechanisms involved in amino acid and sugar uptake by developing maize kernels were investigated. In the pedicel region of maize kernel, the site of nutrient unloading from phloem terminals, amino acids are accumulated in considerable amounts and undergo significant interconversion. A wide spectrum of enzymatic activities involved in the metabolism of amino acids is observed in these tissues. Subsequently, amino acids are taken up by the endosperm tissue in processes which require energy and the presence of carrier proteins. Conversely, no evidence was found that energy and carriers are involved in sugar uptake. This process of sugar uptake is not inhibited by metabolic inhibitors and shows nonsaturable kinetics, but the uptake is pH-dependent. L-glucose is taken up at a significantly reduced rate in comparison to D-glucose uptake. Based on analysis of radioactivity distribution among sugar fractions after incubations of kernels with ...

International Nuclear Information System (INIS)

Praseodymium-doped Bi_4Ti_3O_1_2 (BIT) with various compositions of dopant, Pr (x = 0.5, 0.6, 0.7, 0.8) in Bi_4_-_xPr_xTi_3O_1_2 (BPT) were synthesized using a low temperature wet chemical technique. Powders calcined at 800 deg. C exhibit a single phase polycrystalline perovskite bismuth-layered structure. Randomly oriented plate-like structures were observed under Scanning Electron Microscope (SEM). A small amount of Pr doping (x = 0.5) resulted in dramatically reduced of grain size from 2 #mu#m to less than 50 nm in which Pr plays the role as a grain growth inhibitor. However, by increasing the composition of Pr, bigger grain size of up to 1 #mu#m was observed for x = 0.8 that was caused by diffusion of Pr in the perovskite structure. Dielectric properties showed that dielectric permittivity decreased with the addition of x = 0.50, and increasing with further addition of Pr. Dissipation factor (tan #delta#) followed the same trend as ...

Energy Technology Data Exchange (ETDEWEB)

The subfornical organ is a major receptor area for one of the principal stimuli of thirst, the octapeptide, angiotensin II. In conscious water-sated rats, the authors examined the effects of intravenous infusion of angiotensin II on the rate of glucose utilization in the subfornical organ and in structures anatomically and functionally connected with it. Angiotensin II produced pressor and drinking responses and increased glucose utilization selectively in the subfornical organ and pituitary neural lobe and in no other brain structure. Treatment with the angiotensin II antagonist, sar1-leu8-angiotensin II, before intravenous administration of angiotensin II prevented metabolic stimulation of the subfornical organ and neural lobe. Captopril, an inhibitor of angiotensin-converting enzyme, reduced subfornical organ glucose metabolism to a level similar to that found in control animals. These results demonstrate that peripheral angiotensin II ...

Energy Technology Data Exchange (ETDEWEB)

SRS high-level radioactive waste tanks will not experience erosion corrosion to any significant degree during slurry pump operations. Erosion corrosion in carbon steel structures at reported pump discharge velocities is dominated by electrochemical (corrosion) processes. Interruption of those processes, as by the addition of corrosion inhibitors, sharply reduces the rate of metal loss from erosion corrosion. The well-inhibited SRS waste tanks have a near-zero general corrosion rate, and therefore will be essentially immune to erosion corrosion. The experimental data on carbon steel erosion corrosion most relevant to SRS operations was obtained at the Hanford Site on simulated Purex waste. A metal loss rate of 2.4 mils per year was measured at a temperature of 102 C and a slurry velocity comparable to calculated SRS slurry velocities on ground specimens of the same carbon steel used in SRS waste tanks. Based on these data and the much lower ...

International Nuclear Information System (INIS)

The microstructural development and grain-coarsening behavior of WC-Co alloys, with and without a VC additive, were investigated. The primary goal was to determine the mechanism through which VC acts as a grain-growth inhibitor. The study involved long-time sintering experiments (1 to 100 hours) on fully dense material, nascent stage sintering (90 to 1,320 seconds) starting with the green compact, and surrogate liquid phase experiments to characterize the WC powder prior to sintering. Quantitative microstructural analysis using intercept length distributions was performed for the long-term sintering. The nascent stage experiments involved the measurement of the specific surface area (S_v) of each type of interface separately allowing the determination of the contribution of each developing entity to the overall microstructural evolution. The VC addition has been found to enhance the breakup of multigrained particles in the earliest stages of sintering, producing a ...

Energy Technology Data Exchange (ETDEWEB)

Characteristics of sugar uptake by immature maize embryos were determined in vitro utilizing a /sup 14/C-sugar solution incubation method. Hexose uptake rates were greater than those for sucrose, however, all showed biphasic kinetics. Glucose and fructose saturable components were evidence at <50 mM and sucrose at <5 mM. Chemical inhibitors (CCCP, DNP, NaCN, and PCMBS) and low temperature reduced sugar uptake. Sucrose influx was pH dependent while glucose was not. Embryos maintained a high sucrose to hexose ratio throughout development. At 25 days after pollination sucrose levels exceeded 200 mM while hexose levels remained below 5 mM. Glucose was rapidly converted to sucrose upon transport into the embryo. These circumstantial data indicate that sugar uptake by immature maize embryos is metabolically dependent and carrier mediated. Furthermore, sucrose transport appears to occur against its concentration gradient involving a H+/sucrose ...

British Library Electronic Table of Contents (United Kingdom)

Aim/hypothesis We examined whether the renin inhibitor, aliskiren, provides similar or greater protection than ACE inhibition from non-proliferative diabetic retinopathy and from the proliferative neoangiogenesis of oxygen-induced retinopathy. Methods Transgenic (mRen-2)27 rats, which overexpress mouse renin and angiotensin in extra-renal tissues, were studied. For diabetic studies, non-diabetic, diabetic (streptozotocin, 55?mg/kg), diabetic + aliskiren (10?mg?kg?1?day?1, pump), or diabetic + lisinopril (10?mg?kg?1?day?1, drinking water) rats were evaluated over 16?weeks. For oxygen-induced retinopathy studies, rats were exposed to 80% oxygen (22?h/day) from postnatal days?0 to 11, and then room air from postnatal days?12 to 18. Aliskiren (10 or 30?mg?kg?1?day?1, pump) or lisinopril (10?mg...

KoreaScience (Korea)

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Energy Technology Data Exchange (ETDEWEB)

Qualifying corrosion inhibitors for use in high velocity multiphase flowlines in arctic or subsea environments is discussed. The tests include high velocity flow loop corrosion tests, pumpability through 0.125 (0.318 cm) inch capillary at low temperatures, compatibility with Nylon 11, emulsion tendency testing, and partitioning characteristics. Laboratory and field data show the importance for using the above criteria for inhibitor selection.

Energy Technology Data Exchange (ETDEWEB)

The acid corrosion inhibition process of mild steel in 1 M HCl by 1-butyl-3-methylimidazolium chlorides (BMIC) and 1-butyl-3-methylimidazolium hydrogen sulfate ([BMIM]HSO{sub 4}) has been investigated using electrochemical impedance, potentiodynamic polarization and weight loss measurements. Potentiodynamic polarization studies indicate the studied inhibitors are mixed type inhibitors. For both inhibitors, the inhibition efficiency increased with increase in the concentration of the inhibitor and the effectiveness of the two inhibitors are in the order [BMIM]HSO{sub 4} > BMIC. The adsorption of the inhibitors on mild steel surface obeyed the Langmuir's adsorption isotherm. The effect of temperature on the corrosion behavior in the presence of 5 x 10{sup -3} M of inhibitors was studied in the temperature range of 303-333 K. ...

Energy Technology Data Exchange (ETDEWEB)

Monitoring brine chemistry to determine the extent of potential adverse reactions was simplified by the development of a field brine test kit and a series of nomographs. Results of the kit analyses serve as input to the nomographs, which provide a graphic means of determining the scaling tendency (Saturation Index value) of a brine. Brines that do not tend to form scale may be corrosive. Saturation Index values have been correlated with various processes using data from geopressured wells in the Gulf Coast area. Control of scale in surface equipment of geopressured wells by chemical inhibitors has been successful. Downhole treatment with inhibitors to prevent scale formation in the production tubing is being investigated. Laboratory simulations indicate that an inhibitor squeeze treatment may be successful at the Gladys McCall No. 1 well. Inhibitor mixtures exhibit additive behavior at minimum ...

Energy Technology Data Exchange (ETDEWEB)

Previous studies have documented dissimilatory growth of bacteria on solid Mn{sup 4+} oxide, but Mn{sup 3+} oxides have not been previously studied; here the authors have demonstrated for the first time the bacterial reduction of manganite. Strain MR-4 of Shewanella putrefaciens was able to grow on and rapidly reduce insoluble needle-shaped crystals of synthetic manganite (MnOOH), converting them to soluble Mn{sup 2+} in the process. The rate of Mn{sup 3+} reduction was optimal at pH of 7.0 and 26 C consistent with an enzymatic reaction. In addition the rates of reduction were in proportion to the amount of manganite added, but nearly independent of the cell concentration present (e.g., cell number had only a small effect on the rate of Mn{sup 3+} reduction at early stages of growth) suggesting that surface properties were dictating the rates of metal reduction. This thesis was supported by major differences in reduction rates when Mn oxides of different surface ...

Energy Technology Data Exchange (ETDEWEB)

The effect of sodium gluconate anion (SG) on the corrosion and scale inhibition of ordinary steel in simulated cooling water has been studied using weight loss, polarisation curves, electrochemical impedance spectroscopy (EIS) and scanning electron microscopy (SEM) techniques. SG was studied in concentration from 10{sup -4} M to 10{sup -1} M. Results obtained reveal that SG perform excellently as corrosion and scaling inhibitor for ordinary steel in simulated cooling water. An increase of SG concentration leads to the increase of the corrosion potential towards the positive direction. The inhibition efficiency was a low temperature dependence. The inhibitor mechanism was treated as an adsorption process according to Langmuir adsorption isotherm. The SEM/EDAX data show that was a corrosion and scale inhibitor.

Science.gov (United States)

(NaMBT) inhibitor in ethylene glycol-water solutions. The improved method must be faster and more accur- ate than wet chemical techniques. ...

DEFF Research Database (Denmark)

Raltegravir is the first integrase inhibitor approved for treatment of HIV-infected patients harboring multiresistant viruses.

UK PubMed Central (United Kingdom)

Multiple myeloma is a highly radiosensitive skeletal malignancy, but bone-seeking radionuclides have not yet found their place in disease management. We previously reported that the proteasome inhibitor...Full Text Available

Energy Technology Data Exchange (ETDEWEB)

Bridged monobactam {beta}-lactamase inhibitors were prepared and evaluated as potential partners for combination with imipenem to overcome class C {beta}-lactamase mediated resistance. The (S)-azepine analog 2 was found to be effective in both in vitro and in vivo assays and was selected for preclinical development.

British Library Electronic Table of Contents (United Kingdom)

With collaboration between chemistry, X-ray crystallography, and molecular modeling, we designed and synthesized a series of novel piperazine sulfonamide BACE1 inhibitors. Iterative exploration of the non-prime side and S2prime sub-pocket of the enzyme culminated in identification of an analog that potently lowers peripheral Ab40 in transgenic mice with a single subcutaneous dose.

UK PubMed Central (United Kingdom)

1. Ro 15-8081 (Hoffmann-La Roche, Basle, Switzerland) is a novel mixed 5-HT/noradrenaline uptake inhibitor producing potent antinociceptive effects in animal pain models. 2. In healthy man, two models...Full Text Available

UK PubMed Central (United Kingdom)

BackgroundUpon CD95/Fas ligation, the initiator caspase-8 is known to activate effector caspases leading to apoptosis. In the presence of zVAD-fmk, a broad-spectrum caspase inhibitor,...Full Text Available

Energy Technology Data Exchange (ETDEWEB)

These studies were undertaken to assess the effects of increased galactose (v increased glucose) metabolism via the polyol pathway on vascular filtration function in the kidneys, eyes, nerves, and aorta. Quantitative radiolabeled tracer techniques were used to assess glomerular filtration rate (GFR) and regional tissue vascular clearance of plasma 131I-bovine serum albumin (BSA) in five groups of male Sprague-Dawley rats: nondiabetic controls, streptozotocin-diabetic rats, nondiabetic rats fed a 50% galactose diet, diabetic rats treated with sorbinil (an aldose reductase inhibitor), and galactose-fed rats treated with sorbinil. Sorbinil was added to the diet to provide a daily dose of approximately .2 mmol/kg body weight. After 2 months of diabetes or galactose ingestion, albumin clearance was increased twofold to fourfold in the eye (anterior uvea, choroid, and retina), sciatic nerve, aorta, and kidney; GFR was increased approximately twofold and urinary excretion ...

Energy Technology Data Exchange (ETDEWEB)

In situ assembly states of rat adipocyte glucose transport protein in plasma membrane (PM) and in microsomal pool (MM) were assessed by measuring target size (TS) of D glucose-sensitive, cytochalasin B binding activity. High energy radiation inactivated the binding in both PM and MM by reducing the total capacity of the binding (B/sub T/) without affecting the dissociation constant (K/sub D/). The reduction in B/sub T/ as a function of radiation dose was analyzed based on classical target theory, from which TS was calculated. TS in the PM of insulin-treated adipocytes was 58 KDa. TS in the MM of noninsulin-treated and insulin-treated adipocytes were 112 and 109 KDa, respectively. With MM, however, inactivation data showed anomalously low radiation sensitivities at low radiation doses showing a shoulder in the semilog plots, which may be due to an interaction with a radiation sensitive inhibitor. With these results, they propose the following ...

International Nuclear Information System (INIS)

We have investigated the nanocrystalline microstructure and the hard magnetic properties of Sm(Co_0_._7_2_5Fe_0_._1Cu_0_._1_2Zr_0_._0_4B_0_._0_1_5)_7_._4 melt-spun ribbons. The coercivity (H_c) of the as-spun ribbons increased with the wheel surface speed from 2.8kOe for 10m/s to 14.5kOe for 40m/s. The post-annealing of the melt-spun ribbons from 700 to 900 deg. C for 10min did not lead to a substantial increase of H_c. However, after isothermal aging at 820 deg. C and subsequent slow cooling (0.5 deg. C/min) to 120 deg. C, H_c increased from 2.8 to 10.9kOe for 10m/s, while it decreased from 14.5 to 13.5kOe for 40m/s ribbons. The grain size of the melt-spun ribbon reduced with structural transformation from 2:17H (Th_2Ni_1_7-hexagonal type) to 1:7H (TbCu_7-hexagonal type) as the wheel surface speed was increased. Three-dimensional atom probe analysis showed a boron enriched precipitate at the grain boundaries in the as-spun ribbons, which acts as the grain growth ...

Science.gov (United States)

Influenza virus infection during pregnancy has been implicated as one of cause of premature delivery, abortion and stillbirth. We have reported that cultured human fetal membrane chorion cells undergoing apoptosis by influenza virus infection secrete unidentified heat-stable monocyte differentiation-inducing (MDI) factors. In this study, cellular, biological and immunochemical characteristics of MDI factors were investigated using human monocytic leukemia THP-1 cells by nitroblue tetrazolium reduction and cell adhesion assays. The treatment of THP-1 cells with culture supernatants from the influenza virus-infected chorion cells induced the nitroblue tetrazolium reduction ability, which was inhibited by the addition of superoxide dismutase and diphenyleneiodonium chloride, an inhibitor for reduced nicotinamide adenine dinucleotide phosphate oxidase. The phenomenon was also observed in human peripheral blood monocytes and histiocytic leukemia ...

Energy Technology Data Exchange (ETDEWEB)

Although the intracellular ultrastructural processing of epidermal growth factor (EGF) and its receptor have been described in cell culture systems, very few studies have examined this phenomenon in intact tissues. We have examined the ultrastructural and biochemical handling of (/sup 125/I)EGF in the epidermis and hair follicle bulb of intact, viable, 3- to 5-day-old rat skin the EGF receptor distribution of which has already been documented and in which EGF has been shown to be biologically active. After incubation of explants with 10 nM (/sup 125/I)EGF for 2.5 h at 25 degrees or 37 degrees C, radiolabel was detected over the basal cells of the epidermis and hair follicle outer root sheath, confirming previous light microscope observations. More specifically, silver grains were observed near coated and uncoated plasma membrane and coated membrane invaginations, Golgi apparatus, lysosomal structures, and nuclei. Sodium azide inhibited internalization of label, whereas a series of ...

Energy Technology Data Exchange (ETDEWEB)

The objective of this work is to improve the process for CO{sub 2} capture by alkanolamine absorption/stripping by developing an alternative solvent, aqueous K{sub 2}CO3 promoted by piperazine (PZ). Pilot plant testing was performed in a 16.8-inch ID absorber and stripper with recirculation of air and CO{sub 2}. Three solvents (7 m MEA, 5 m K{sup +}/2.5 m PZ, and 6.4 m K{sup +}/1.6 m PZ) were tested in four campaigns with three different absorber packings. Pilot plant testing established that 5 m K{sup +}/2.5 m PZ requires two times less packing than 7 m MEA and three times less packing than 6.4 m K{sup +}/1.6 m PZ. A rigorous model of the thermodynamics and mass transfer was developed in the RateSep{trademark} block of AspenPlus{reg_sign}. The double matrix stripper reduces energy consumption by 5 to 15%. The best K{sup +}/PZ solvent, 4 m K{sup +}/4 m PZ, and the best process configuration, double matrix stripper with a double intercooled absorber, requires ...

Energy Technology Data Exchange (ETDEWEB)

Field and laboratory work sponsored by the Gas Research Institute (GRI) and the Department of Energy (DOE) have shown that calcium-carbonate scale formation in waters produced with natural gas and oil can be prevented by injection of phosphonate inhibitor into the formation, even if the formation is sandstone without calcite binding material. Inhibitor squeeze jobs have been carried out on DOE's geopressured-geothermal Gladys MaCall brine-gas well and GRI's co-production wells in the Hitchcock field. Following the inhibitor squeeze on Gladys McCall, the well produced over five million barrels of water at a rate of approximately 30,000 BPD without calcium-carbonate scaling. Before the inhibitor squeeze, the well could not be produced above 15,000 BPD without significant scale formation. In the GRI brine-gas co-production field tests, inhibitor squeezes have been ...

British Library Electronic Table of Contents (United Kingdom)

The effect of sodium gluconate anion (SG) on the corrosion and scale inhibition of ordinary steel in simulated cooling water has been studied using weight loss, polarisation curves, electrochemical impedance spectroscopy (EIS) and scanning electron microscopy (SEM) techniques. SG was studied in concentration from 10-4M to 10-1M. Results obtained reveal that SG perform excellently as corrosion and scaling inhibitor for ordinary steel in simulated cooling water. An increase of SG concentration leads to the increase of the corrosion potential towards the positive direction. The inhibition efficiency was a low temperature dependence. The inhibitor mechanism was treated as an adsorption process according to Langmuir adsorption isotherm. The SEM/EDAX data show that was a corrosion and scale inhi...

British Library Electronic Table of Contents (United Kingdom)

Vanadium carbide is the most effective grain growth inhibitor for ultrafine WC-Co composites due to its high solubility and mobility in the cobalt phase at relatively low temperatures; however, there are still some debates over the best way to introduce it into the WC-Co formulation. In this paper, the differences between admixed and chemically doped grain growth inhibitors on the microstructural development and properties of an ultrafine WC-10Co composite are discussed. The densification rate of chemically doped samples is slower in the early stage of sintering and the WC grain sizes of the sintered alloys are finer than those of admixed samples, leading to the increase of hardness and transverse rupture strength of the sintered alloys. The effectiveness of the chemically doped inhibitor ...

British Library Electronic Table of Contents (United Kingdom)

A study of the ordinary mild steel/cooling water interface, with and without inhibitor, was carried out using electrochemical impedance spectroscopy (EIS). EIS spectra in uninhibited medium reveal that a layer of corrosion and scale products is formed naturally and evolves with the immersion time. Monosaccharides derivatives were used as corrosion inhibitors. Most of them exhibit good behaviour against corrosion of ordinary steel in simulated water systems. Their inhibiting efficiency increases with concentration rise and depends on molecular structure especially -OH groups' position on two adjacent carbons and their number. In addition, the effect of MoO4^2^- on the corrosion inhibition in the presence of the best inhibitor was also studied by EIS. The addition of MoO4^2^- enhanced the in...

UK PubMed Central (United Kingdom)

Transformed Drosophila Kc cell lines, resistant to methotrexate, an inhibitor of de novo purine and pyrimidine synthesis, have been obtained by calcium phosphate transfection of plasmids containing...Full Text Available

UK PubMed Central (United Kingdom)

Hypoxia inducible factor-1 (HIF-1) promotes tumor cell adaptation to microenvironmental stress. HIF-1 is up-regulated in irradiated tumors and serves as a promising target for radiosensitization....Full Text Available

UK PubMed Central (United Kingdom)

Dominant mutations in sarcomere protein genes cause hypertrophic cardiomyopathy, an inherited human disorder with increased ventricular wall thickness, myocyte hypertrophy, and disarray. To understand...Full Text Available

UK PubMed Central (United Kingdom)

The treatment for erectile dysfunction (ED) was revolutionized with the development of phosphodiesterase type 5 (PDE5) inhibitors. Tadalafil (Cialis^®; Eli Lilly and Company, Indianapolis,...Full Text Available

UK PubMed Central (United Kingdom)

BackgroundCelecoxib, a selective cyclo-oxygenase-2 inhibitor has been recommended orally for the treatment of arthritis and osteoarthritis. Long term oral administration of celecoxib...Full Text Available

UK PubMed Central (United Kingdom)

Human cytomegalovirus (HCMV) in clinical material cannot replicate efficiently in vitro until it has adapted by mutation. Consequently, wild-type HCMV differ fundamentally from the passaged strains...Full Text Available

UK PubMed Central (United Kingdom)

Secreted human bronchial mucins, directly collected from macroscopically healthy bronchial mucosa, were prepared in the presence of six proteinase inhibitors, and analysed by electron microscopy. These...Full Text Available

UK PubMed Central (United Kingdom)

BackgroundAurora kinases play an essential role in orchestrating chromosome alignment, segregation and cytokinesis during mitotic progression, with both aurora-A and B frequently...Full Text Available

Energy Technology Data Exchange (ETDEWEB)

S-Adenosylmethionine decarboxylase (AdoMetDC) is a critical enzyme in the polyamine biosynthetic pathway and depends on a pyruvoyl group for the decarboxylation process. The crystal structures of the enzyme with various inhibitors at the active site have shown that the adenine base of the ligands adopts an unusual syn conformation when bound to the enzyme. To determine whether compounds that favor the syn conformation in solution would be more potent AdoMetDC inhibitors, several series of AdoMet substrate analogues with a variety of substituents at the 8-position of adenine were synthesized and analyzed for their ability to inhibit hAdoMetDC. The biochemical analysis indicated that an 8-methyl substituent resulted in more potent inhibitors, yet most other 8-substitutions provided no benefit over the parent compound. To understand these results, we used computational modeling and X-ray crystallography to study C{sup ...

UK PubMed Central (United Kingdom)

Mycophenolate mofetil (MMF) is an immunosuppressive drug that acts as a selective inhibitor of inosine monophosphate dehydrogenase (IMPDH). MMF has recently been shown to inhibit the enzymatic activity...Full Text Available

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The present invention relates to a method of acidizing a subterranean formation or well bore employing an acidic solution containing a corrosion inhibitor composition comprising an inhibiting effective amount of an acetylenic alcohol, a quaternary ammonium compound, an aromatic hydrocarbon and an antimony compound.

UK PubMed Central (United Kingdom)

The phenomenon of antibiotic resistance has created a need for the development of novel antibiotic classes with non-classical cellular targets. Unfortunately, target-based drug discovery against...Full Text Available

UK PubMed Central (United Kingdom)

Methylation of the arginine residues of histones by methyltransferases has important consequences for chromatin structure and gene regulation; however, the molecular mechanism(s) of methyltransferase...Full Text Available

UK PubMed Central (United Kingdom)

Protection from extinction of conditioned fear has been demonstrated when a conditioned inhibitor of fear is presented during extinction treatment. The present study assessed if similar results...Full Text Available

UK PubMed Central (United Kingdom)

AbstractPurposeThe aim of this study was to elucidate the effects of the Rho-kinase inhibitor, H-1152, on cultured human trabecular meshwork (HTM) cells, TM morphology,...Full Text Available

UK PubMed Central (United Kingdom)

Finasteride, a specific and competitive inhibitor of 5α-reductase enzyme Type 2, inhibits the conversion of testosterone to dihydrotestosterone (DHT). In adults, DHT acts as primary androgen...Full Text Available

DEFF Research Database (Denmark)

The notes describe in detail primary and secondary galvanic cells, fuel cells, electrochemical synthesis and electroplating processes, corrosion: measurments, inhibitors, cathodic and anodic protection, details of metal dissolution reactions, Pourbaix diagrams and purification of waste water from galvanic industries.

UK PubMed Central (United Kingdom)

Restenosis remains the main complication of balloon angioplasty and/or stent implantation. Preclinical testing of new pharmacologic agents preventing restenosis largely rely on porcine models, where...Full Text Available

UK PubMed Central (United Kingdom)

The p21-activated kinases (PAKs), immediate downstream effectors of the small G-proteins of the Rac/cdc42 family, are critical mediators of signaling pathways regulating cellular behaviors and...Full Text Available

UK PubMed Central (United Kingdom)

Terfestatin A (TrfA), terphenyl-β-glucoside, was isolated from Streptomyces sp. F40 in a forward screen for compounds that inhibit the expression of auxin-inducible...Full Text Available

UK PubMed Central (United Kingdom)

Oligopeptidic drugs such as β-lactams and angiotensin-converting enzyme inhibitors share the same carriers in humans and animals, which results in possible pharmacokinetic interactions. To model...Full Text Available

UK PubMed Central (United Kingdom)

The cyclic AMP content of acini, freshly prepared from mammary tissue of lactating rats, was measured during incubation in vitro. Neither adrenergic agonists nor cyclic AMP phosphodiesterase inhibitors...Full Text Available

International Nuclear Information System (INIS)

The inducible transcription factor NF-#kappa#B regulates divergent signaling pathways including inflammatory response and cancer development. Selective inhibitors for NF-#kappa#B signaling are potentially useful for treatment of inflammation and cancer. NF-#kappa#B is canonically activated by preferential disposal of its inhibitory protein; I#kappa#B, which suppresses the nuclear translocation of NF-#kappa#B. I#kappa#B#alpha# (a major member of I#kappa#B family proteins) is phosphorylated with an I#kappa#B kinase (IKK) and subsequently polyubiquitylated by SCF"#beta#"T"r"C"P"1 ubiquitin-ligase in the presence of E1 and E2 prior to proteasomal degradation. Here, we describe a novel inhibitor termed GS143, which suppressed I#kappa#B#alpha# ubiquitylation, but not I#kappa#B#alpha# phosphorylation, MDM2-directed p53 ubiquitylation, and proteasome activity in vitro. GS143 markedly suppressed the destruction of I#kappa#B#alpha# stimulated by ...

UK PubMed Central (United Kingdom)

PurposeTaxanes have effects on angiogenesis causing difficulties in separating biologic effects of chemotherapy from those due to angiogenesis inhibitors. This randomized...Full Text Available

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Nitrite is to be used to inhibit pitting corrosion during Extended Sludge Processing (ESP) at the Savannah River Plant. The required nitrite concentrations are expressed as a function of the slurries' nitrate ion concentration and temperature. In the most dilute slurries, the nitrite inhibitor requirement is independent of the nitrate ion concentration and depends only on the temperature of the waste. The nitrate-independent concentration ensures that there is sufficient inhibitor, in sludge slurries whose nitrate has been depleted by radiolysis, to prevent pitting corrosion induced by other corrosive anions (e.g., sulfate and chloride). The threshold nitrate concentration at which the nitrite level is expressed as a function only of temperature is 0.02 M.

International Nuclear Information System (INIS)

The objectives of the project were to develop operational techniques for promoting contaminant hideout return from tube support crevices and to identify the effect of chemical inhibitor application on corrodent transport. The implementation of routine procedures for promoting the return of sequestered corrodents could retard the progression of denting or other corrosion processes and improve steam generator availability. Tests also quantified the effect of inhibitor application on crevice hideout and hideout return processes, with the intention of developing a better understanding of the inhibition mechanism. By carefully monitoring the hideout and hideout return inventories, the program also has provided the opportunity to study steam generator concentration processes in general.

International Nuclear Information System (INIS)

Neuron differentiation is a complex process involving various cell-cell interactions, and multiple signaling pathways. We showed previously that CD40 is expressed and functional on mouse and human neurons. In neurons, ligation of CD40 protects against serum withdrawal-induced injury and plays a role in survival and differentiation. CD40 deficient mice display neuron dysfunction, aberrant neuron morphologic changes, and associated gross brain abnormalities. Previous studies by Tone and colleagues suggested that five isoforms of CD40 exist with two predominant isoforms expressed in humans: signal-transducible CD40 type I and a C-terminal truncated, non-signal-transducible CD40 type II. We hypothesized that differential expression of CD40 isoform type I and type II in neurons may modulate neuron differentiation. Results show that adult wild-type, and CD40"-"/"- deficient mice predominantly express CD40 type I and II isoforms. Whereas adult wild-type mice express mostly CD40 type I in ...

Science.gov (United States)

BackgroundXMRV (xenotropic murine leukemia virus-related virus) is the first known example of an exogenous gammaretrovirus that can infect humans. A limited number of reports suggest that XMRV is intrinsically resistant to many of the antiretroviral drugs used to treat HIV-1 infection, but is sensitive to a small subset of these inhibitors. In the present study, we used a novel marker transfer assay to directly compare the antiviral drug sensitivities of XMRV and HIV-1 under identical conditions in the same host cell type.ResultsWe extend the findings of previous studies by showing that, in addition to AZT and tenofovir, XMRV and HIV-1 are equally sensitive to AZddA (3'-azido-2',3'-dideoxyadenosine), AZddG (3'-azido-2',3'-dideoxyguanosine) and adefovir. These results indicate that specific 3'-azido or acyclic nucleoside analog inhibitors of HIV-1 reverse transcriptase (RT) also block XMRV infection with comparable efficacy in vitro. Our data ...

DEFF Research Database (Denmark)

The syntheses of N-alkylated deoxynojirimycin and 1,5-dideoxy-1,5-iminoxylitol derivatives having either a D- or an L-erythritol-3-sulfate functionalized N-substituent are reported. The alkylating agent used was a cyclic sulfate derivative, whereby selective attack of the nitrogen atom at the least hindered primary center afforded the desired ammonium salt. In aqueous solution, these salts were configurationally labile at the ammonium center. Sulfonium and/or selenonium analogues of the ammonium salts were prepared by analogous reactions. The chalcogen salts were obtained as mixtures of diastereomers, separable in some cases, differing only in the stereochemistry at the configurationally stable sulfur or selenium atoms. Proof of configuration and conformation of each compound was obtained by detailed NMR experiments. The compounds are six-membered ring analogues of salacinol, a known sulfonium-salt glucosidase inhibitor. Evaluation of the target compounds for ...

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The objective of this work was to investigate the efficiency of imidazole derivatives for corrosion inhibition of copper in 0.5 M hydrochloric acid. Corrosion inhibition was studied using impedance spectroscopy. Imidazole and its derivatives 4-methylimida-zole, 4-methyl-5-hydroxymethylimidazole, 1-phenyl-4-methylimidazole, 1-(p-tolyl)-4-methylimidazole were investigated. These studies have shown that 1-(p-tolyl)-4-methylimidazole is the best inhibitor in this series and that it acts as mixed inhibitor. The nature of the chemical interaction between these molecules and the copper surface was investigated by Cu exposed to solutions having two very different pH values: 0.5 M HCl and unbuffered purified water. X-ray photoelectron spectroscopy and secondary ion mass spectrometry were used to explore the nature of the interaction. Possible mechanisms of corrosion inhibition for these molecules are discussed.

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The methodology of the drip procedure of the Standard Test Method for Evaluating the Influence of Thermal Insulation on External Stress Corrosion Cracking Tendency of Austenitic Stainless Steel (ASTM C 692-95a) was used to research the effect of halogens and inhibitors on the external stress corrosion cracking (ESCC) of Type 304 stainless steel as it applies to the insulation industry. Simulated insulation extraction solutions were made with pure chemical reagents for the halogens and inhibitors. The results indicated that sodium silicate compounds that were higher in sodium were more effective for preventing chloride-induced ESCC in Type 304 austenitic stainless steel. Potassium silicate was not as effective as sodium silicate. Fluoride, bromide, and iodide may cause ESCC but they were much less active than chloride and could be effectively inhibited by sodium silicate compound. The addition of fluoride ions to the chloride/sodium silicate ...

British Library Electronic Table of Contents (United Kingdom)

Pulses are rich in nutrients. The existence of anti-nutritional components and the length of time required for preparation have, however, limited their frequency of use compared to recommended intake levels. Anti-nutritional components in pulses can be largely removed by heat treatment. Additionally pre-treatment of pulses with heat and processing of seeds into flour could further enhance their use by decreasing processing and preparation times. In this study, trypsin inhibitor activity, functional properties, and microstructural characteristics of flours prepared from different varieties of lentil, chickpea, and pea as affected by roasting and boiling were evaluated. Both thermal treatments resulted in significant reduction (p<0.05) in trypsin inhibitor activity ranging from -95.6% to -37...

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Reactive blue 2 (RB-2) had been characterized as a relatively potent ectonucleoside triphosphate diphosphohydrolase (E-NTPDase) inhibitor with some selectivity for NTPDase3. In search for the pharmacophore and to analyze structure-activity relationships we synthesized a series of truncated derivatives and analogs of RB-2, including 1-amino-2-sulfo-4-ar(alk)ylaminoanthraquinones, 1-amino-2-methyl-4-arylaminoanthraquinones, 1-amino-4-bromoanthraquinone 2-sulfonic acid esters and sulfonamides, and bis-(1-amino-4-bromoanthraquinone) sulfonamides, and investigated them in preparations of rat NTPDase1, 2, and 3 using a capillary electrophoresis assay. Several 1-amino-2-sulfo-4-ar(alk)ylaminoanthraquinone derivatives inhibited E-NTPDases in a concentration-dependent manner. The 2-sulfonate group ...

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Eight selected sulfonamide drugs were investigated as inhibitors of heat shock protein 90 (Hsp90). The investigation included simulated docking experiments to fit the selected compounds within the binding pocket of Hsp90. The selected molecules were found to readily fit within the ATP-binding pocket of Hsp90 in low-energy poses. The sulfonamides torsemide, sulfathiazole, and sulfadiazine were found to inhibit the ATPase activity of Hsp90 with IC50 values of 1.0, 2.6, and 1.5 mM, respectively. Our results suggest that these well-established sulfonamides can be good leads for subsequent optimization into potent Hsp90 inhibitors.

British Library Electronic Table of Contents (United Kingdom)

The world of antibiotic drug discovery and development is driven by the necessity to overcome antibiotic resistance in common Gram-positive and Gram-negative pathogens. However, the lack of Gram-negative activity among both recently approved antibiotics and compounds in the developmental pipeline is a general trend despite the fact that the plethora of covered drug targets are well-conserved across the bacterial kingdom. Such intrinsic resistance in Gram-negative bacteria is largely attributed to the activity of multidrug resistance (MDR) efflux pumps. Moreover, these pumps also play a significant role in acquired clinical resistance. Together, these considerations make efflux pumps attractive targets for inhibition in that the resultant efflux pump inhibitor (EPI)/antibiotic combination d...

British Library Electronic Table of Contents (United Kingdom)

Many existing agents for diabetes therapy are unable to restore or maintain normal glucose homeostasis or prevent the eventual emergence of hyperglycemia-related complication. Therefore, agents based on novel mechanisms are sought to complement and extend the current therapeutic approaches. Based on the initial paper research, we focused on active STAT3 as an attractive pharmacological target for type 2 diabetes. The subsequent text mining with a unique query to identify suppressors but not activators of STAT3 revealed the ERK2/STAT3 pathway as a novel diabetes target. The description of ERK2 inhibitors as diabetes target had not been found in our text mining research at present. The mechanism-based peptide inhibitor for ERK2 was identified using the knowledge of the KIM sequence, which ha...

International Nuclear Information System (INIS)

Soybean is one of the most economical and nutritious food packed with basic nutrients that combat diseases stemming from mal- and under-nutrition. Despite its rich nutritional profile, use of soybean in food has been limited because soybean proteins are often associated with compounds, which could exert a negative impact on the nutritional quality of the protein. Trypsin inhibitor (TI) is one of the important anti-nutritional factors that exert negative effect by causing growth inhibition. Soybean cultivar VLS-2 was irradiated with 250 Gy gamma rays in a gamma cell (200) with 60Co source installed at BARC to induce mutations for low trypsin inhibitor content. Three mutants with lower levels of TI content were identified and can be utilized for developing elite varieties of soybean. (author)

British Library Electronic Table of Contents (United Kingdom)

Abstract Imatinib mesylate is the first of a novel group of drugs that specifically target protein tyrosine kinases, which are central to the pathogenesis of human cancer. It has been approved for the treatment of chronic myeloid leukemia and gastrointestinal stromal tumor and has been found efficacious in other neoplastic diseases. Nilotinib and dasatinib, a second-generation of tyrosine kinase inhibitors (TKIs), were developed in response to findings of emerging imatinib resistance or intolerance to the drug. Cutaneous reactions are the most common nonhematologic side effect of these drugs, and their management is challenging especially in the absence of alternative anticancer agents. The present review focuses on the clinical characteristics and the hypothesized molecular pathogenesis o...

Environmental Research Database

No further description is available

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No abstract prepared.

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A novel class of pyrrolidinyl-acetyleneic thieno[3,2-d]pyrimidines has been identified which potently inhibit the EGFR and ErbB-2 receptor tyrosine kinases. Synthetic modifications of the pyrrolidine carbamate moiety result in a range of effects on enzyme and cellular potency. In addition, the impact of the absolute stereochemical configuration on cellular potency and oral mouse pharmacokinetics is described.

Science.gov (United States)

In view of the findings that several Kunitz-type protein inhibitors suppress tumor invasion and metastasis, the aim of the present study is to explore whether Bungarus multicinctus protease inhibitor-like protein-2 (PILP-2) and PILP-3 exhibit anti-tumor activity. Although approximately 28% of amino acid substitutions occurred between PILP-2 and PILP-3, molecular modeling suggested that PILP-2 and PILP-3 shared similar folded structures. Unlike PILP-2, PILP-3 showed a notable activity in abolishing migration and invasion of human neuroblastoma SK-N-SH cells. The ability of PILP-3 to inhibit matrix metalloprotease-2 (MMP-2) activity was higher than that of PILP-2. Pull-down assay revealed protein-protein interaction between PILP-3 and MMP-2. In contrast to mutation on N-terminal region, replacement of amino acids at C-terminus attenuated notably the ability of PILP-3 to inhibit cell invasion, cell migration and MMP-2 activity as well as the ...

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Azobenzene dyes are effective inhibitors for austenitic 304 L and 316 L stainless steel corrosion in high acidic medium up to 7N. A good efficiency is obtained from weight loss and electrochemical Rsub(p) measurements in hydrochloric acid, while no inhibition is observed in sulfuric solutions. Transformation from the primarily azobenzene to other compounds give rise to enhanced protection of steel samples, and probable structures of the inhibiting species are proposed in view of our results.

UK PubMed Central (United Kingdom)

Hematopoietic stem cells are resistant to HIV-1 infection. Here, we report a novel mechanism by which the cyclin-dependent kinase inhibitor (CKI) p21^{Waf1/Cip1/Sdi1} (p21), a known regulator...Full Text Available

Science.gov (United States)

Soluble epoxide hydrolase (sEH) plays an important role in the metabolism of endogenous chemical mediators involved in the regulation of blood pressure and inflammation. 1,3-Disubstituted ureas with a polar group located on the fifth atom from the carbonyl group of urea function are active inhibitors of sEH both in vitro and in vivo. However, their limited solubility in water and relatively high melting point lead to difficulties in formulating the compounds and poor in vivo efficacy. To improve these physical properties, the effect of structural modification of the urea pharmacophore on the inhibition potencies, water solubilities, octanol/water partition coefficients (log P), and melting points of a series of compounds was evaluated. For murine sEH, no loss of inhibition potency was observed when the urea pharmacophore was modified to an amide function, while for human sEH 2.5-fold decreased inhibition was obtained in the amide compounds. In addition, a NH group ...

UK PubMed Central (United Kingdom)

We have demonstrated that the 80 kDa POP Tc80 (prolyl oligopeptidase of Trypanosoma cruzi) is involved in the process of cell invasion, since specific inhibitors block parasite...Full Text Available

UK PubMed Central (United Kingdom)

Although matrix metalloproteinase-9 (MMP-9) is involved in cardiomyocytes contractility dysfunction, tissue inhibitor of metalloproteinase-4 (TIMP-4) mitigates the effect of MMP-9, and proteinase-activated...Full Text Available

UK PubMed Central (United Kingdom)

AbstractThe gag p6 region of HIV-1 has various nonsubstitutionary mutations, including insertions, duplications, deletions, and premature stop codons. Studies have linked gag p6 mutations...Full Text Available

Energy Technology Data Exchange (ETDEWEB)

The effect of WC particle size with the addition of VC as a grain growth inhibitor was investigated during the liquid phase sintering of WC-Co system. With increasing WC particle size at the same VC content, the effect of grain growth inhibition was increased. Also, with increasing the VC content, the grain shape of WC was changed from the faceted shape to the distorted shape, and the step density of the WC grain was increased. (orig.)

UK PubMed Central (United Kingdom)

Antimicrobial susceptibilities of 233 Gram-positive and 180 Gram-negative strains to two novel bis-indoles were evaluated. Both compounds were potent inhibitors of Gram-positive bacteria, with MIC₉₀...Full Text Available

UK PubMed Central (United Kingdom)

This study focuses on the effects of long-term renin-angiotensin system suppression and/or incretin mimetic therapies on the regulation and binding affinity of GLP-1 to its receptor in the coronary...Full Text Available

UK PubMed Central (United Kingdom)

1-Naphthylphthalamic acid (NPA) is a specific inhibitor of polar auxin transport that blocks carrier-mediated auxin efflux from plant cells. To allow identification of the NPA receptor thought to be...Full Text Available

Science.gov (United States)

Plerocercoids of the tapeworm Spirometra mansonoides produce a substance that stimulates growth of experimental hosts. We report purification of plerocercoid growth factor (PGF) to homogeneity by a process involving isolation and solubilization of plerocercoid membranes, isoelectric point selection by chromatofocusing chromatography or preparative isoelectric focusing, and anion-exchange chromatography. A radioreceptor assay (RRA) for human growth hormone (hGH) was used to detect PGF and purity of the 27.5-kDa protein was judged by sodium dodecyl sulfate-polyacrylamide gel electrophoresis (SDS-PAGE). Proteolytic activity was detected in the 27.5-kDa protein by gelatin substrate PAGE. Characterization of PGF as a neutral cysteine proteinase was based on substrate and inhibitor specificities and dependence on pH and thiol-containing reagents. The association of hGH agonist and proteinase activities was shown by comparing RRA and hydrolytic activities in the presence ...

Science.gov (United States)

Erectile dysfunction following radical prostatectomy remains a frequent problem despite the development of nerve-sparing techniques. This erectile dysfunction is believed to be neurogenic, enhanced by hypoxia-induced structural changes which result in additional veno-occlusive dysfunction. Recently, daily use of intracavernous vasoactive substances and oral use of PDE5-inhibitors have been clinically studied for treatment of postprostatectomy erectile dysfunction. Since these studies showed benefits of "penile rehabilitation therapy," these effects have been studied in a preclinical setting. We reviewed experimental literature on erectile tissue preserving and neuroregenerative treatment strategies, and found that preservation of the erectile tissue by the use of intracavernous nitric oxide donors or vasoactive substances, oral PDE5-inhibitors, and hyperbaric oxygen therapy improved erectile function by antifibrotic effects and preservation of ...

Energy Technology Data Exchange (ETDEWEB)

Chloride-induced pitting corrosion of stainless steel (Materials No. 1.4301 and 1.4571) was investigated with the aid of chronopotentiostatic tests. Oxide films upon the surface (temper colours), addition of inhibitors (sulphate and nitrate) and temperature were the testing variables. Two different critical pitting potentials have been found, which give information on the potential ranges for stable passivity, latent and stable pitting corrosion. The results only indicate a small effect of Mo content of the material and test temperature. The inhibitors (sulphate and nitrate) have a marked effect. Specimens with a clean surface produced by pickling are markedly more resistant against pitting corrosion than specimens with a yellow temper colour, whereas the difference in corrosion resistance between yellow and blue films is relatively small. The width of the critical potential range for pitting corrosion generally increases with increasing oxide ...

British Library Electronic Table of Contents (United Kingdom)

The corrosion inhibition of C38 steel in molar HCl by N,N-bis[2-(3,5-dimethyl-1H-pyrazol-1-yl)ethyl]buthylamine (P1) and 5-{N,N-bis[2-(3,5-dimethyl-1H-pyrazol-1-yl)ethyl] amino} pentanol (P2) has been investigated at 308?K using electrochemical and weight loss measurements. Measurements show that these compounds act as good inhibitors without changing the mechanism of the corrosion process. Moreover, the inhibiting efficiency increases with the increase in concentration of the studied inhibitors. Compound P2 showed better protection properties even at relatively higher temperatures when compared to P1. The associated activation corrosion and free adsorption energies have been determined. P1 and P2 are adsorbed on the C38 steel surface according to a Langmuir isotherm adsorption model.

British Library Electronic Table of Contents (United Kingdom)

Abstract Purpose: To describe the pattern of expression of the cyclin-dependent kinase inhibitors (CDKIs) p16, p21 and p27, and the cell cycle in SRA 01/04 cells relative to contact inhibition. Methods: SRA 01/04 cells were grown to overconfluence under normal conditions. At various phases of the cell growth, cells were assayed by flow cytometry and Western blotting for the expression of CDKIs. Results: Expression of p16 was detected from early logarithmic growth to stationary phases, during which the number of cells in G0/G1 increased from 46 to 69%. Expression of p21 was detected only during the overgrowth phase, when 60% of the cells were in G0/G1. Expression of p27 was not observed in SRA 01/04 cells. Conclusions: p16 expression was likely mediated by G0/G1 arrest to induce contact inh...

Science.gov (United States)

The ability to feed on vertebrate blood has evolved many times in various arthropod clades. Each time this trait evolves, novel solutions to the problem posed by vertebrate hemostasis are generated. Consequently, saliva of blood-feeding arthropods has proven to be a rich source of antihemostatic molecules. Vasodilators include nitrophorins (nitric oxide storage and transport heme proteins), a variety of peptides that mimic endogenous vasodilatory neuropeptides, and proteins that catabolize or sequester endogenous vasoconstrictors. A variety of platelet aggregation inhibitors antagonize platelet responses to wound-generated signals, including ADP, thrombin, and collagen. Anticoagulants disrupt elements of both the intrinsic and extrinsic pathways. Molecular approaches (termed 'sialomics') to characterize the full inventory of mRNAs transcribed in salivary glands have revealed a surprising level of complexity within a single species. Multiple salivary proteins may be ...

UK PubMed Central (United Kingdom)

OBJECTIVES: Personal and equipment assistance are common strategies to reduce disability. This study sought to determine how often assistance reduces or even completely resolves health-related difficulties...Full Text Available

International Nuclear Information System (INIS)

The threshold stress intensities for stress corrosion crack propagation in beta titanium alloy 38-6-44, Ti3Al-8V-6Cr-4Mo-4Zr, has been determined in salt water and methanolic solutions. The alloy was immune to stress corrosion cracking (SCC) in aqueous sodium chloride solutions (marine atmosphere). However, in methanolic solutions, the alloy was very susceptible to SCC. This marked susceptibility in methanolic solutions can be mitigated by the addition of an inhibitor: sodium nitrate. Crack extension in the alloy was transgranular and failure occurred by brittle quasi-cleavage in methanolic solutions.

British Library Electronic Table of Contents (United Kingdom)

In this paper, an environmentally friendly metal corrosion inhibitor, phytic acid, was assembled into the walls of silica nanoparticles via layer-by-layer self-assembly technique (LbL) with poly(allylamine hydrochloride). Such functionalized nanoparticles were uniformly distributed into sol-gel films for metal anticorrosion. The films showed very pronounced and lasting protective efficiency in concentrated salt aqueous solutions as indicated by electrochemical impedance spectroscopy (EIS) measurement. These results may provide a new route for the preparation of environment-friendly anticorrosion coatings.

Energy Technology Data Exchange (ETDEWEB)

This paper reports the presence of face centered cubic cobalt precipitates inside tungsten carbide in nanocomposite of WC-Co synthesized by spray conversion processing. EDS was used to identify the presence and micro-diffraction was employed to determine the nature of the precipitates. There is entrapment of cobalt in tungsten carbide during the spray conversion process used to form WC/Co powder. During consolidation, at high temperatures, the cobalt attains enough mobility to precipitate inside WC. A vanadium containing compound was seen at the interfaces in samples which incorporated VC as a grain growth inhibitor. (orig.)

Energy Technology Data Exchange (ETDEWEB)

This paper describes an exact solution to the problem of absorbing nitrogen dioxide into aqueous solution, in which case the nitrogen dioxide concentration is allowed to vary over a wide range. The authors have worked on the rate of calcium sulfate dihydrate scale formation on the reverse osmosis membrane and find this phenomena can be treated by the crystallization theory. The authors performed long-term experiments using calcium sulfate dihydrate solution with addition of sodium hexametaphosphate (SHMP) and commercially available organophosphates and investigated the mechanism of the inhibitor's action quantitatively.

Energy Technology Data Exchange (ETDEWEB)

The Purex process and the fluorescence spectrometry are first recalled, then uranyl fluorescence is studied in a pure nitric medium without other elements to establish a theoretical model, allowing the description of uranium fluorescence signal with a general equation. The influence of different parameters (temperature, inhibitors, dynamic quenching of iron and cerium) is investigated to develop the model. A quantitative analysis method without addition of reagents is proposed to validate the model.

British Library Electronic Table of Contents (United Kingdom)

Purpose - The purpose of this paper is to evaluate the corrosion inhibition potential of mangrove (Rhizopora apiculata) tannin in hydrochloric acid medium on copper with the view of developing a natural corrosion inhibitor. Design/methodology/approach - The mangrove tannin was extracted from the mangrove bark and its anticorrosion potential was studied by weight loss, electrochemical and scanning electron microscopy (SEM) analysis. Findings - It has been found that the mangrove tannin effectively inhibits the corrosion on copper metal in hydrochloric acid solution. The results of the electrochemical and weight loss methods showed that the inhibition efficiency of mangrove tannin increases with increasing its concentration. Inhibition is achieved through the adsorption of tannin molecules o...

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Trihydroxynaphthalene reductase catalyzes two intermediate steps in the fungal melanin biosynthetic pathway. The enzyme, a typical short-chain dehydrogenase, is the biochemical target of three commercial fungicides. The fungicides bind preferentially to the NADPH form of the enzyme. Three X-ray structures of the Magnaporthe grisea enzyme complexed with NADPH and two commercial and one experimental fungicide were determined at 1.7 {angstrom} (pyroquilon), 2.0 {angstrom} (2,3-dihydro-4-nitro-1H-inden-1-one, 1), and 2.1 {angstrom} (phthalide) resolutions. The chemically distinct inhibitors occupy similar space within the enzyme's active site. The three inhibitors share hydrogen bonds with the side chain hydroxyls of Ser-164 and Tyr-178 via a carbonyl oxygen (pyroquilon and 1) or via a carbonyl oxygen and a ring oxygen (phthalide). Active site residues occupy similar positions among the three structures. A buried water molecule that is ...

International Nuclear Information System (INIS)

The present study was undertaken to determine the involvement of calcium-protein kinase C pathway in the mechanism of action of Escherichia coli heat stable enterotoxin (STa) apart from STa-induced activation of guanylate cyclase in human colonic carcinoma cell line COLO-205, which was used as a model cultured cell line to study the mechanism of action of E. coli STa. In response to E. coli STa, protein kinase C (PKC) activity was increased in a time-dependent manner with its physical translocation from cytosol to membrane. Inhibition of the PKC activity in membrane fraction and inhibition of its physical translocation in response to IP_3-mediated calcium release inhibitor dantrolene suggested the involvement of intracellular store depletion in the regulation of PKC activity. Among different PKC isoforms, predominant involvement of calcium-dependent protein kinase C (PKC#alpha#) was specified using isotype-specific pseudosubstrate, which showed pronounce enzyme ...

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Phlorizin is a competitive inhibitor of Na/sup +//glucose symport in animal cells and of H/sup +//3-O-methylglucose (3-O-MeG) symport in liverworts. The effects of this compound on the uptake of (U-/sup 14/C) sucrose and of (/sup 14/C) 3-O-MeG by broadbean (Vicia faba L.) leaf discs were studied. Leaf discs without lower epidermis were preincubated in the dark for 30 min (fresh discs) or for 12 h (aged discs) on a medium buffered at pH 5.0 containing mannitol as an osmoticum. They were then incubated for 30 min in the light on a similar solution added with 1 mM (/sup 14/C) sucrose or (/sup 14/C) 3-O-MeG and 5 mM phlorizin. Phlorizin inhibited uptake of 3-O-MeG by 37 and 50% respectively in fresh and aged discs. Sucrose uptake was more sensitive to the inhibitor than 3-O-MeG uptake and was also more inhibited in aged than in fresh discs (76% inhibition vs 54%). Kinetic studies showed that the inhibition exerted by phlorizin in fresh material is ...

Science.gov (United States)

... ULTRASONIC VIBRATION TO PORTLAND CEMENT-WATER PASTE REDUCES THE ULTIMATE COMPRESSIVE STRENGTH OF MORTARS ...

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Short communication

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PMID:18830084

Science.gov (United States)

... entitled: In-country Pilot Activities: Reducing Emissions from Deforestation and Degradation)...

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The variation of surface composition and sintering of the binary Pd{sub 7}Ag{sub 3} nanoparticles prepared by chemical reduction were studied. The composition of the as-prepared Pd{sub 7}Ag{sub 3} nanoparticles across the diameter is inhomogeneous due to different reduction potentials of Pd and Ag. Upon heating, Ag will migrate to the surface because of its lower surface energy. Surface modification results in variation of surface composition during the sintering process. Stearic acid acts as a grain growth inhibitor. The migration of Ag to the surface is suppressed and the sintering is retarded. Modification by polyethylene glycol leads to more migration of Ag atoms from the core to the surface. This makes the nanoparticles easier to sinter.

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This study compares the microstructure and mechanical properties of plain and 0.9 or 3.6 wt% VC- or Cr{sub 3}C{sub 2}-doped WC-12 wt% Co hardmetals with 40 wt% NbC, prepared by pulsed electric current sintering (PECS) in the solid state for 4 min at 1240 deg. C and conventional pressureless liquid phase sintering (CS) for 1 h at 1420 deg. C. The addition of VC or Cr{sub 3}C{sub 2} was found to inhibit grain growth of the residual WC grains, whereas the size of the solid solution (Nb,W,V/Cr)C grains was hardly influenced. The type of grain growth inhibitor and densification temperature however, strongly influenced the composition of the NbC solid solution formed, which was thermodynamically and experimentally assessed.

British Library Electronic Table of Contents (United Kingdom)

Corrosion inhibition of iron in H2SO4 by polyacrylic acid (PAA) was investigated using electrochemical techniques at 30degreeC. Results obtained indicate that PAA inhibited the corrosion of iron in the acid medium. Inhibition efficiency increases with increase in PAA concentration and synergistically enhanced on addition of iodide ions. Potentiodynamic polarization results suggest that PAA functions as a modest cathodic inhibitor. The adsorption of PAA onto the iron surface followed Temkin adsorption isotherm. FTIR analysis revealed that the synergistic effect due to co-adsorption of iodide ions and PAA is co-operative in nature.

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This research investigated the inhibiting effects that sodium salts of linear monocarboxylic acids displayed towards the corrosion process of AZ31 Mg alloy in ASTM D 1387 saline solution (a synthetic industrial cooling water). The length of the aliphatic chain of the acids ranged between 7 and 15 carbon atoms. The inhibiting action of these salts can be related to the precipitation of an insoluble magnesium salt, which mainly affected the anodic reaction. The aliphatic chain length controlled the anion solubility and the reaction rate of magnesium carboxylate formation. For all the salts, an optimum concentration was experienced: 10{sup -2} M for sodium decanoate (caprate), 10{sup -3} M for sodium dodecanoate (laurate), 10{sup -4} M for sodium tetradecanoate (myristate); when this concentration was exceeded, a diminution (even a disappearance) in the inhibiting action was found. (Abstract Copyright [2009], Wiley Periodicals, Inc.)

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Cyclooxygenase-2 (COX-2) content is increased in many types of tumor cells. We have investigated the mechanism by which resveratrol, a stilbene that is pro-apoptotic in many tumor cell lines, causes apoptosis in human head and neck squamous cell carcinoma UMSCC-22B cells by a mechanism involving cellular COX-2. UMSCC-22B cells treated with resveratrol for 24 h, with or without selected inhibitors, were examined: (1) for the presence of nuclear activated ERK1/2, p53 and COX-2, (2) for evidence of apoptosis, and (3) by chromatin immunoprecipitation to demonstrate p53 binding to the p21 promoter. Stilbene-induced apoptosis was concentration-dependent, and associated with ERK1/2 activation, serine-15 p53 phosphorylation and nuclear accumulation of these proteins. These effects were blocked by ...

British Library Electronic Table of Contents (United Kingdom)

Dopant-free Bi2Ti2O7 thin films with pyrochlore structure and La-doped bismuth titanate thin films have been fabricated by means of chemical solution decomposition, and characterized by X-ray diffraction, atomic force microscopy, scanning electron microscopy and UV?Vis spectrophotometry in this study. Their photocatalytic activities have been evaluated by photodegrading methyl orange solution, and the optimum processing parameters for the highest photocatalytic activity have been found. Moreover, the effects of La-doping on the phase transformation and the photocalalytic activity have been studied. It has been deduced from the experiment result that substituted La3+ ions can act as a stabilizer of Aurivillus phase BLT and a grain?growth inhibitor in BLT thin films.

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Purpose The primary objective of this sub-study, undertaken as an extension to the previously reported phase-I study, was to explore the feasibility, tolerability and pharmacokinetics (PK) of belinostat when administered by the oral route. Preliminary pharmacodynamic (PD) studies were also performed to enable comparison of the biological effects of the oral and intravenous formulations. Patients and methods Oral belinostat was administered in a range of doses and schedules (once, twice or thrice daily), on either day 1 or days 1?5, of the second or a subsequent treatment cycle in 15 patients who were included in the phase-I trial of intravenous belinostat. Serial blood samples were collected for PK and PD (histone acetylation) analyses, and the results compared with corresponding analyses ...

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The use of selective additives such as MgO as a sintering aid and a rare earth oxide as a grain growth inhibitor, has allowed the manufacture of beryllia ceramics having close to theoretical density. The grain size and grain size distribution can be controlled by an optimum firing schedule leaving a remnant porosity which is extremely fine (0.2 {mu}m). This structure is compared with conventional BeO ceramics, densified by liquid phase sintering, which develops a glassy grain boundary and retains large pores up to 3 {mu}m. The significantly improved strength properties, extremely fine pores,the 'pinning effect' of rare earth oxide, and the superior surface finish both in the as-fired and polished state are discussed in relation to the micro-structure. (orig.).

Science.gov (United States)

Green crab (Scylla serrata) alkaline phosphatase (EC 3.1.3.1) is a metalloenzyme, which catalyzes the nonspecific hydrolysis of phosphate monoesters. The kinetics of inhibition of the enzyme by sodium (2, 2'-bipyridine) oxodiperoxovanadate, pV(bipy), has been studied. The time course of the hydrolysis of p-nitrophenyl-phosphate catalyzed by the enzyme in the presence of different pV(bipy) concentrations showed that at each pV(bipy) concentration, the rate decreased with increasing time until a straight line was approached, the straight line slopes are the same for all concentrations. The results suggest that the inhibition of the enzyme by pV(bipy) is a slow, reversible reaction with fractional remaining activity. The microscopic rate constants are determined for the reaction of inhibitor with the enzyme. PMID:10691182

International Nuclear Information System (INIS)

Corrosion tests of titanium alloys VTI-0, OT4, VT5-1 and steel Kh18N1OT in 10% and 18% HCl with additions of carnallite at 40 deg C have been carried out. It has been established that titanium alloys in 10% and 18% HCl containing 5 and 10% carnallite are sufficiently corrosion resistant in the presence of 0.1-1% FeCl or HNO_3 and can be used for manufacturing the equipment of recirculation gas scrubbers. Steel Kh18N10T is unstable in all the media tested. It is subjected to intensive pitting. Specimens of steel Kh18N10T have also revealed edge cracking.

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Extraction of hemicellulose from hardwood chips prior to pulping is a possible method for producing ethanol and acetic acid in an integrated forest bio-refinery, adding value to wood components normally relegated to boiler fuel. Hemicellulose was extracted from hardwood chips using green liquor, a pulping liquor intermediate consisting of aqueous NaOH, Na2CO3, and Na2S, at 160degreeC, held for 110min in a 20L rocking digester. The extracted liquor contained 3.7% solids and had a pH of 5.6. The organic content of the extracts was mainly xylo-oligosaccharides and acetic acid. Because it was dilute, the hemicellulose extract was concentrated by evaporation in a thin film evaporator. Concentrates from the evaporator reached levels of up to 10% solids. Inhibitors such as acetic acid and sodium ...

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Two grades of WC-10wt.%Co cemented carbide with or without addition of Cr3C2/VC grain growth inhibitor during liquid phase sintering were produced with the goal to investigate their reciprocating sliding friction and wear behaviour against WC-6wt.%Co cemented carbide under unlubricated conditions. The tribological characteristics were obtained on a Plint TE77 tribometer using distinctive normal contact loads. The generated wear tracks were analyzed by scanning electron microscopy and quantified topographically using surface scanning equipment. The post-mortem obtained wear volumes were compared to the online assessed wear. Correlations between wear volume, wear rate and coefficient of friction on the one hand and sliding distance and microstructural properties on the other hand were determ...

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Astrocytes have important immune functions in CNS, and astrocytes stimulated by interferon-g were showed to have direct antimicrobial function. However whether astrocytes without the stimulation of cytokines have antibacterial function, and how this function is regulated are still largely unknown. In this study, we found that primary cultured astrocytes inhibited the growth of both gram-negative and gram-positive bacteria. Further more, we showed that interleukin-1b (IL-1b) enhanced the antibacterial effect in a dose-dependent manner, and the antibacterial effect of astrocytes from IL-1b receptor-deficient mice failed to be enhanced by IL-1b. IL-1b stimulated IkBa degradation, NF-kB nuclear translocation, and transactivation in astrocytes. NF-kB inhibitors blocked NF-kB activation and the ...

International Nuclear Information System (INIS)

By varying different variables (potential, chloride content, surface pretreatment etc.) it is possible to show the effect of increasingly harsher corrosion conditions on passive-layer stability. These changes will not be detected by conventional methods e.g. measurement of passive current density, until a very late stage. Electrochemical noise measurement will allow the action of inhibitors to be detected in a rapid and effective manner. High-alloy steels and titanium claddings subjected to pitting corrosion in chloride-containing media demonstrate how to use this method for problem solutions and to open up new practical applications. The effect of mechanical stresses (natural, tensile) on the corrosion system can be detected by electrochemical noise which opens up new methods for crack corrosion studying and monitoring. (orig./DG).

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This new book presents a practical how to approach to understanding and solving the problems of corrosion of structural materials. Although it is written mainly for those having a limited technical background in corrosion, it also provides more experienced engineers with a useful overview of the principles of corrosion and can be used as a general guide for developing a corrosion-control program. Contents include: the effects and economic impact of corrosion; basic concepts important to corrosion; principles of aqueous corrosion; forms of corrosion: recognition and prevention; types of corrosive environments; corrosion characteristics of structural materials; corrosion control by proper design; corrosion control by materials selection; corrosion control by protective coatings and inhibitors; corrosion control by cathodic and anodic protection; corrosion testing and monitoring; techniques for diagnosis of corrosion failures; and glossary of corrosion-related terms.

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How does one assure that both quality and creativity are obtained in basic research environments QA theoreticians have attempted to develop workable definitions of quality, but in more reflective moments, these definitions often fail to capture the deeper essence of the idea of quality.'' This paper asserts that creativity (as a product of the human mind) is a concrete interface between perfunctory definitions of quality (conformance to specifications) and more philosophical speculations about the nature of quality- related ultimates'' like elegance or beauty. In addition, we describe the distinction between creative ideas and creative acts and highlight one of the major inhibitors of creativity, fear. Finally we show that highly creative people often have an irreverent attitude toward boundaries and established authority, and discuss how one can allow for this when designing a QA program in a basic research environment.

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Banana (Musa acuminata Colla AAA) peel extracts obtained in this work had a high capacity to scavenge 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2prime-azino-bis(3-ethylbenzothiazoline)-6-sulfonic acid (ABTS+) free radicals, and they were also good lipid peroxidation inhibitors. Acetone:water extracts were considerably more effective (compared with methanol, ethanol, acetone, water, methanol:water or ethanol:water) at inhibiting the peroxidation of lipids in the b-carotene/linoleic acid system or scavenging free radicals. However, aqueous extracts had a high capacity to protect lipids from oxidation in the thiobarbituric acid reactive substances (TBARS) test, as well as in the b-carotene bleaching assay. In addition, acetone:water most efficiently extracted all extractable components (54+-...

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Synchronized cultures of the green alga Scenedesmus quadricauda were grown in the absence (untreated cultures) or in the presence (FdUrd-treated cultures) of 5-fluorodeoxyuridine, the specific inhibitor of nuclear DNA replication. The attainment of commitment points, at which the cells become committed to nuclear DNA replication, mitosis and cellular division, and the course of committed processes themselves were determined for cell cycle characterization. FdUrd-treated cultures showed nearly unaffected growth and attainment of the commitment points, while DNA replication(s), nuclear division(s) and protoplast fission(s) were blocked. Interestingly, the FdUrd-treated cells possessed a very high mitotic histone H1 kinase activity in the absence of any nuclear division(s). Compared with the ...

British Library Electronic Table of Contents (United Kingdom)

WC-Co hardmetals with gradient structure comprising neither -phase nor grain growth inhibitors were produced for the first time by regulating the WC re-crystallisation and carbon content in their near-surface layer and core. Hardmetals with low Co contents in the surface region were obtained by selective carburisation of the near-surface zone of green articles with the original low carbon content and their consequent liquid-phase sintering. The surface region of such gradient hardmetals has a hardness of up 150 Vickers units higher and fracture toughness significantly superior than those of the core. Gradient hardmetals with high Co contents in the surface region were obtained by selective decarburisation of the near-surface zone of green articles with the original high carbon content and ...

UK PubMed Central (United Kingdom)

Patients who fail to attend initial appointments reduce clinic efficiency. To maximize attendance by newly referred outpatients, we introduced a mandatory group orientation clinic for all new patients...Full Text Available

UK PubMed Central (United Kingdom)

The disulfide-reduced form of bovine ribonuclease A (RNAse A), with the Cys thiols irreversibly blocked, was characterized by small-angle x-ray scattering (SAXS). To help resolve the conflicting...Full Text Available

UK PubMed Central (United Kingdom)

Background Since 2007, sex has been the major mode of HIV transmission in China, accounting for 75% of new infections in 2009. Reducing sexual transmission is a major challenge for China...Full Text Available

UK PubMed Central (United Kingdom)

Latent inhibition (LI) manifests as poorer conditioning to a CS that has previously been presented without consequence. There is some evidence that LI can be potentiated by reduced mesoaccumbal dopamine...Full Text Available

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The obligations under international law to reduce transfrontier air pollution is discussed in five chapters from various aspects. Consequences for the European Communities are gone into in five further chapters. (orig./HP)

Science.gov (United States)

A device for reducing the muzzle blast and flash from large caliber guns is disclosed. A container having a plurality of internal chambers and baffle plates filled with an aqueous foam is mounted to the muzzle of the gun barrel. The foam and chambers co-o...

UK PubMed Central (United Kingdom)

Healthcare-associated infections (HAIs) take a major human toll on society and reduce public confidence in the healthcare system. The current convergence of scientific, public, and legislative...Full Text Available

UK PubMed Central (United Kingdom)

We introduce in this paper a new method for reducing neurodynamical data to an effective diffusion equation, either experimentally or using simulations of biophysically detailed models. The dimensionality...Full Text Available

UK PubMed Central (United Kingdom)

Many plants are known to reduce the toxic effects of high soil boron (B) by reducing uptake of B, but no mechanism for limiting uptake has previously been identified. The B-tolerant cultivar of barley...Full Text Available

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The article describes the Solair 1 solar cell-powered aircraft. Measures to reduce the weight of the craft are cited.

Science.gov (United States)

... from theory to practice will be significantly reduced while intrinsically revolutionizing the approach to engineering network security architectures. ...

KoreaScience (Korea)

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... two sectors. ' One company used as example of this process is the Lord Corporation, which produces products that reduce ...

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Past airfoil configurations have been used to improve aerodynamic performance and engine efficiencies. The present airfoil configuration further increases component life and reduces maintenance by reducing internal stress within the airfoil itself. The airfoil includes a chord and a span. Each of the chord and the span has a bow being summed to form a generally "C" configuration of the airfoil. The generally "C" configuration includes a compound bow in which internal stresses resulting from a thermal temperature gradient are reduced. The structural configuration reduces internal stresses resulting from thermal expansion.

Science.gov (United States)

The steroidogenic factor 1 (SF-1, also known as NR5A1) is a transcription factor belonging to the nuclear receptor superfamily. Whereas most of the members of this family have been extensively characterized, the therapeutic potential and pharmacology of SF-1 still remains elusive. Described here is the identification and characterization of selective inhibitory chemical probes of SF-1 by a rational ultra-high-throughput screening (uHTS) strategy. A set of 64,908 compounds from the National Institute of Health's Molecular Libraries Small Molecule Repository was screened in a transactivation cell-based assay employing a chimeric SF-1 construct. Two analogous isoquinolinones, ethyl 2-[2-[2-(2,3-dihydro-1,4-benzodioxin-7-ylamino)-2-oxoethyl]-1-oxoisoquinolin-5-yl]oxypropanoate (SID7969543) and ethyl 2-[2-[2-(1,3-benzodioxol-5-ylmethylamino)-2-oxoethyl]-1-oxoisoquinolin-5-yl]oxypropanoate and (SID7970631), were identified as potent submicromolar inhibitors, yielding ...

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A systematic comparison was undertaken to characterize neurotoxic esterase (NTE) from rat and chicken brain in terms of inhibitor sensitivities, pH optima, and molecular weights. Paraoxon titration of phenyl valerate (PV)-hydrolyzing carboxylesterases showed that rat esterases were more sensitive than chicken to paraoxon inhibition at concentrations less than or equal to microM and superimposable with chicken esterases at concentrations of 2.5-1000 microM. Mipafox titration of the paraoxon-resistant esterases at a fixed paraoxon concentration of 100 microM (mipafox concentration: 0-1000 microM) resulted in a mipafox I50 of 7.3 microM for chicken brain NTE and 11.6 microM for rat brain NTE. NTE (i.e., paraoxon-resistant, mipafox-sensitive esterase activity) comprised 80% of chicken and 60% of rat brain paraoxon-resistant activity with the specific activity of chicken brain NTE approximately twice that of rat brain NTE. The pH maxima for NTE from both species was ...

International Nuclear Information System (INIS)

This study was carried out to evaluate the effects of irradiation (gamma irradiation at dose levels of 0.0, 2.5, 5.0, 10.0 or 20.0 kGy, He-Ne and their combination) on nutritive characteristics of Vicia faba L. seeds (Giza 843). Analyses included levels of anti-nutrients (total phenolic compounds, tannins, phytic acid, trypsin inhibitor and vicine), chemical composition (sugars, crude proteins, fat, dry matter and ash) and fatty acids profile. All treatments caused significant (P<0.05) decreases in the antinutrational factors under investigation. The reduction in the content of tannins and phenolic compounds were more pronounced with He-Ne alone or He-Ne in combination with gamma irradiation. At dose levels 10.0 and 20.0 kGy without or with combination of He-Ne were more efficiency in the reduction of phytic acid content by 24.3, 32.8, 34.5 and 45.5 %, respectively. Also, for trypsin inhibitor activity, the maximum inhibition was observed ...

Science.gov (United States)

Vildagliptin is a potent and selective dipeptidyl peptidase IV inhibitor in development for the treatment of type 2 diabetes that improves glycemic control by enhancing alpha- and beta-cell responsiveness to glucose. Two open-label, single-dose, randomized, crossover studies in healthy subjects (ages 18-45 years) investigated the dose proportionality of vildagliptin pharmacokinetics (n = 20) and the effect of food (n = 24) on vildagliptin pharmacokinetics. There was a linear relationship (r(2) = 0.999) between vildagliptin doses of 25, 50, 100, and 200 mg and area under the plasma concentration-time curve from time zero to infinity (AUC(0-infinity)) and maximum plasma concentration (C(max)). Dose proportionality was assessed using a statistical power model [X = alpha x (dose)(beta)]. The 90% confidence intervals of the proportionality coefficient, beta, for AUC(0-infinity) (1.15-1.19) and C(max) (1.04-1.14) indicated that deviations from dose proportionality were ...

International Nuclear Information System (INIS)

Treatment chemicals are used in all facets of the natural gas industry (NGI) from well development through transmission and storage of natural gas. The multitude of chemicals used, combined with the dozens of chemical manufacturers and/or suppliers has lead to the availability of hundreds of possible chemical products. Because of the widespread use of chemical products and their numerous sources, the NGI needs access to consistent data regarding their effectiveness and potential environmental impacts. The objective of this work was to evaluate the effectiveness and potential environmental impacts of, chemical products used in the NGI. This assessment was initially focused on biocides and corrosion inhibitors and their use in the gas production, storage and transmission facilities, The overall approach was obtain the necessary data on chemical use and effectiveness directly from the oil and gas industry, supplemented with data/information obtained from the published ...

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This paper presents results of a laboratory and field study of naphthenic acid corrosion and the development of an effective chemical inhibitor for this type of corrosive attack. In the laboratory corrosion test, which involved 20 hour weight loss measurements in high flash solvent with a total acid number (TAN) of 16 mg KOH/gm at a temperature of 600 F (316 C), blank corrosion rates averaged 140 to 150 mpy (3.56 to 3.81 mm/y). Inhibited rates averaged about 10 to 12 mpy (0.254 to 0.305 mm/y). The field test was carried out on a heavy vacuum gas oil (HVGO) stream at 550 F (288 C) . Blanks varied from a high of 425 mpy (10.79 mm/y) for a 24 hour test to a low of about 100 mpy (2.54 mm/y) for a 150 hour test. Both electrical resistance (ER) probes and weight loss coupons showed corrosion rates below 5 mpy (0.127 mm/y) as long as they were adequately passivated. Passivation consisted of exposing the coupons to a high inhibitor dosage for a ...

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Pairing correlations in multi-quasiparticle states in deformed nuclei are expected to be reduced because of blocking. New intrinsic states and their associated rotational bands have been identified allowing comparisons to be made as a function of seniority and between nuclei. The possible effects of the reduced pairing on the collective rotation, and its manifestation in terms of alignment, are discussed. 13 refs., 2 figs.

British Library Electronic Table of Contents (United Kingdom)

The extracts from kinnow peel, kinnow seeds, litchi pericarp, litchi seeds, grape seeds, and banana peel were screened for total phenolic content (TPC), trolox equivalent antioxidant capacity (TEAC), 1,1 diphenyl-2-picryl hydrazyl (DPPH) radical scavenging activity, as well as reducing power. Kinnow peel extract exhibited the highest reducing power, TEAC, and DPPH free radical scavenging activity, whereas, the phenolic content of 37.4 mg GAE/g-dw was highest for grape seed extract. Banana peel extract with a low TPC showed the lowest reducing power, TEAC as well as DPPH free radical scavenging activity among the fruit residue extracts examined in the present study. Correlation analysis between the reducing power and DPPH radical scavenging ability; reducing power and ABTS radical scavengin...

International Nuclear Information System (INIS)

Red mud (RM) is the main by-product of the Bayer process for alumina extraction from bauxite, and grey slurries (GS) are generated during the granite rocks transformation processes. the huge volume of those wastes generated every year suppose a serious environmental problem. Recent works by our group demonstrate the efficiency of both types of muds as corrosion inhibitors for iron and steel in alkaline media containing chlorides. The elemental analysis of these slurried shows that Al"3+ is the main common element. Therefore, the aim of this paper is to study the effect of the soluble Al"3+ in the electrochemical behaviour of iron in alkaline media, in presence and absence of chlorides. The electrochemical study using Cyclic Voltammetry (CV) and Electrochemical Impedance Spectroscopy (EIS) together with surface analysis techniques allowed to conclude that Al"3+ blocks the surface of steel in alkaline media chloride increasing the steel resistance to chlorides ...

British Library Electronic Table of Contents (United Kingdom)

CD44, a transmembrane receptor for hyaluronic acid, is implicated in various adhesion-dependent cellular processes, including cell migration, tumor cell metastasis and invasion. Recent studies demonstrated that CD44 expressed in cancer cells can be proteolytically cleaved at the ectodomain by membrane type 1-matrix metalloproteinase (MT1-MMP) to form soluble CD44 and that CD44 cleavage plays a critical role in cancer cell migration. Here, we show that transforming growth factor-b (TGF-b), a multifunctional cytokine involved in cell proliferation, differentiation, migration and pathological processes, induces MT1-MMP expression in MDA-MB-435s cells. TGF-b-induced MT1-MMP expression was blocked by the specific extracellular regulated kinase-1/2 (ERK1/2) inhibitor PD98059 and the specific pho...

Science.gov (United States)

Escherichia coli spheroplast protein y (EcSpy) is a small periplasmic protein that is homologous with CpxP, an inhibitor of the extracytoplasmic stress response. Stress conditions such as spheroplast formation induce the expression of Spy via the Cpx or the Bae two-component systems in E. coli, though the function of Spy is unknown. Here, we report the crystal structure of EcSpy, which reveals a long kinked hairpin-like structure of four ?-helices that form an antiparallel dimer. The dimer contains a curved oval shape with a highly positively charged concave surface that may function as a ligand binding site. Sequence analysis reveals that Spy is highly conserved over the Enterobacteriaceae family. Notably, three conserved regions that contain identical residues and two LTxxQ motifs are placed at the horizontal end of the dimer structure, stabilizing the overall fold. CpxP also contains the conserved sequence motifs and has a predicted secondary structure similar ...

Energy Technology Data Exchange (ETDEWEB)

A series of Gd-substituted M-type barium hexaferrites has been prepared by the ceramic route, according to the formula (Ba{sub 1-x}Gd{sub x})O.5.25Fe{sub 2}O{sub 3} (x=0-0.30). XRD analysis revealed that all the samples present primarily an M-type structure. Samples x=0 and x=0.05 are single-phase. Hematite (Fe{sub 2}O{sub 3}) and GdFeO{sub 3} were detected in the remaining samples. Coercivity (H{sub c}) shows remarkably high values, {approx}293kA/m for x=0.20 and 0.30 with a maximum of 322kA/m for x=0.25. Specific saturation magnetization ({sigma}{sub sat}) of the samples presents a small increase up to x=0.10. The microstructure examination indicates that Gd may act as a grain growth inhibitor.

International Nuclear Information System (INIS)

Vertical U-tube steam generators in Pressurized Water Reactors (PWRs) operating an All Volatile Treatment (AVT) secondary chemistry have experienced corrosion problems, particularly denting and sludges. The studies reported evaluate the feasibility of using a low-concentration (0.5 wt%) chemical cleaning process to remove corrosion product deposits from steam generator surfaces and magnetite from tube-to-support plate crevices of PWR steam generators. The process potentially may be applied at schedule intervals, such as during normal refueling outages, to maintain a steam generator in clean operating condition. This report describes the results of testing to evaluate the effectiveness of several chelant acids for dissolving steam generator sludges and crevice magnetite. Corrosion of carbon steel by the chelant acids and the effects of various inhibitors are evaluated. The effectiveness of ion-exchange regeneration of several chelant-based solvents is also ...

British Library Electronic Table of Contents (United Kingdom)

TaC-4wt.% CNT composites were synthesized using spark plasma sintering. Two kinds of CNTs, having long (10-20mm) and short (1-3mm) length, were dispersed by wet chemistry and spray drying techniques respectively. Spark plasma sintering was carried out at 1850^oC at pressures of 100, 255 and 363MPa. Addition of CNTs leads to an increase in the density of 100MPa sample from 89% to 95%. Short CNTs are more effective in increasing the density of the composites whereas long CNTs are more effective grain growth inhibitors. The longer CNTs are more effective in increasing the fracture toughness and an increase up to 60% was observed for 363MPa sample. Hardness and elastic modulus are found to increase by 22% and 18% respectively for 100MPa samples by addition of long CNTs. Raman spectroscopy, SEM...

International Nuclear Information System (INIS)

Nanocrystalline cemented tungsten carbide has attracted considerable interests for use in cutting tool because of its superior mechanical properties. In this study, nano-sized powders of mixed WC and Co were prepared from attrition-milled oxides by a gas reduction-carburization process. The effects of compacting pressure, heating schedule, additional ball-milling, and the presence of a grain growth inhibitor on the sintering properties of the nano-sized WC-Co powders were examined. The grain size and phases in WC-Co alloy were clearly affected by compacting pressure. Because of the trapped gases and the lower melting point of the cobalt binder, when a compact of nano-sized WC-Co powder was sintered through a heating schedule with holding steps, the sintered alloy maintained the small size of WC grains without any #eta# phase. In addition, the additional ball-milling improved the microstructure and mechanical properties of the nano-sized WC-Co powder by producing a ...

Science.gov (United States)

It is now over 30 yr since the original discovery was made that acetylenic compounds are effective in inhibiting the corrosion of iron in acid media. Since then, the industrial practice of oil-well acidizing has become well-established, with key acetylenic compounds such as propargyl alcohol, hexynol, and ethyl octynol assuming increasingly important roles. New and more stable triple-bonded compounds properly formulated and synergized with nitrogen compounds are expected to be used more extensively as temperature, stability, and performance requirements increase. An evaluation is made of the structural features which enhance or limit the corrosion performance of a given acetylenic. New data involving mixtures of acetylenics, hydrogen-bonded complexes, and the use of new nitrogen synergists are covered also. Tabular data at 200/sup 0/F approximate the more strenuous conditions of an oil-well acidizing job using N-80 tubing. The performance of such inhibitors as ...

Energy Technology Data Exchange (ETDEWEB)

The two-compartment radioassay for microbial kinetics based on continuous measurement of the {sup 14}CO{sub 2} released by bacterial metabolism of 14C-labeled substrate offers a valuable approach to testing the potency of antimicrobial drugs. By using a previously validated radioassay with gram-positive and gram-negative bacteria, a group of protein synthesis inhibitors was evaluated for their effect on microbial growth kinetics. All tested drugs induced changes in both the slopes and intercepts of the growth curves. An exponential growth model was applied to quantify the drug effect on the processes of bacterial {sup 14}CO{sub 2} liberation and cell generation. The response was measured in terms of a generation rate constant. A linear dependence of the generation rate constant on the dose of spectinomycin was observed with Escherichia coli. Sigmoidal-shaped curves were found in the assays of chloramphenicol and tetracycline. The implications of dose-response ...

Energy Technology Data Exchange (ETDEWEB)

The present investigation deals with the fabrication of liquid petroleum gas (LPG) sensor based on semiconducting oxide SnO{sub 2}. The gas sensor elements have been prepared by conventional solid state route. Addition of noble metal sensitizer, palladium and grain growth inhibitor, aluminum silicate to the base material SnO{sub 2}, not only improved the sensitivity towards LPG but also the selectivity in the presence of CO and CH{sub 4} gases. Out of various sensor compositions, SnO{sub 2}:Al{sub 2}Si{sub 2}O{sub 7} (35 wt.%):Pd (1.5 wt.%) sintered at 800 C for 5 h has shown high sensitivity (0.97) towards LPG at an operating temperature of 350 C. Different characterization techniques have been employed, such as differential thermal analysis (DTA), surface area analyzer, X-ray diffraction (XRD), to study the formation of SnO{sub 2}, surface area and crystallite size, respectively. The results suggested the possibility of utilizing the sensor element for the ...

Energy Technology Data Exchange (ETDEWEB)

Dopant-free Bi{sub 2}Ti{sub 2}O{sub 7} thin films with pyrochlore structure and La-doped bismuth titanate thin films have been fabricated by means of chemical solution decomposition, and characterized by X-ray diffraction, atomic force microscopy, scanning electron microscopy and UV-Vis spectrophotometry in this study. Their photocatalytic activities have been evaluated by photodegrading methyl orange solution, and the optimum processing parameters for the highest photocatalytic activity have been found. Moreover, the effects of La-doping on the phase transformation and the photocalalytic activity have been studied. It has been deduced from the experiment result that substituted La{sup 3+} ions can act as a stabilizer of Aurivillus phase BLT and a grain-growth inhibitor in BLT thin films.

International Nuclear Information System (INIS)

The preparation of wood-plastic combinations (WPC) using combined methods for curing intermediate products and final products is described. In the first step, impregnated wood was irradiated using doses of 1 to 10 kGy in the presence of chemical initiators of polymerization. Thereafter, curing of this partly cured impregnating mixture was accomplished in the wood at elevated temperatures with the aid of chemical initiators of polymerization. Impregnation mixtures based on unsaturated polyester resins and methyl methacrylate, and the wood species European Beech (Fagus silvatica) and Black Alder (Alnus glutinosa) were used. The results indicate that this method of preparing WPC allows substantially lower radiation doses to be used, i.e., doses in the range of 1 to 2.5 kGy. These doses gelatinate the impregnation mixture in the wood so that the subsequent curing by chemical polymerization initiators proceeds without the impregnation mixture flowing out of the wood, and without forming ...

Energy Technology Data Exchange (ETDEWEB)

Cell extracts of the thermophile Clostridium thermohydrosulfuricum catalyzed the phosphorylation by (..gamma..-/sup 32/P)ATP of several endogenous proteins with M/sub r/s between 13,000 and 100,000. Serine and tyrosine were the main acceptors. Distinct substrate proteins were found in the soluble (e.g., proteins p66, p63, and p53 of M/sub r/s 66,000, 63,000, and 53,000, respectively) and particulate (p76 and p30) fractions, both of which contained protein kinase and phosphatase activity. The soluble fraction suppressed the phosphorylation of particulate proteins and contained a protein kinase inhibitor. Phosphorylation of p53 was promoted by 10..mu..M fructose 1,6-bisphosphate or glucose 1,6-bisphosphate and suppressed by hexose monophosphates, whereas p30 and p13 were suppressed by 5 ..mu..M brain (but not spinach) calmodulin. Polyamines, including the odd polyamines characteristic of thermophiles, modulated the labeling of most of the phosphoproteins. Apart from ...

Scientific Electronic Library Online (English)

Abstract in english We hypothesized that chronic oral administration of the phosphodiesterase-5 inhibitor sildenafil could improve the exercise capacity and pulmonary hemodynamics in patients with pulmonary arterial hypertension (PAH) on the basis of previous short-term studies. We tested this hypothesis in 14 subjects with PAH, including seven patients with the idiopathic form and seven patients with atrial septal defects, but no other congenital heart abnormalities. Patients were subjected (more) to a 6-min walk test and dyspnea was graded according to the Borg scale. Pulmonary flow and pressures were measured by Doppler echocardiography. Patients were given sildenafil, 75 mg orally three times a day, and followed up for 1 year. Sildenafil therapy resulted in the following changes: increase in the 6-min walk distance from a median value of 387 m (range 0 to 484 m) to 462 m (range 408 to 588 m; P

International Nuclear Information System (INIS)

Morusin is a pure compound isolated from root bark of Morusaustralis (Moraceae). In this study, we demonstrated that morusin significantly inhibited the growth and clonogenicity of human colorectal cancer HT-29 cells. Apoptosis induced by morusin was characterized by accumulation of cells at the sub-G_1 phase, fragmentation of DNA, and condensation of chromatin. Morusin also inhibited the phosphorylation of IKK-#alpha#, IKK-#beta# and I#kappa#B-#alpha#, increased expression of I#kappa#B-#alpha#, and suppressed nuclear translocation of NF-#kappa#B and its DNA binding activity. Dephosphorylation of NF-#kappa#B upstream regulators PI3K, Akt and PDK1 was also displayed. In addition, activation of caspase-8, change of mitochondrial membrane potential, release of cytochrome c and Smac/DIABLO, and activation of caspase-9 and -3 were observed at the early time point. Downregulation in the expression of Ku70 and XIAP was exhibited afterward. Caspase-8 or wide-ranging caspase ...

Science.gov (United States)

Penile rehabilitation has been an area of intense study and debate over the last decade. Interest in this topic was stimulated by the observation that erectile dysfunction remained a significant problem after radical prostatectomy despite meticulous nerve-sparing technique. Smooth muscle alterations and fibrotic changes in the penis were identified as the underlying causes of penile atrophy, veno-occlusive dysfunction, and Peyronie's-like changes that were observed after surgery. Initial observations that intracavernous injection therapies used on a regular basis postoperatively resulted in improvements in the return of spontaneous erectile function led to the development of penile rehabilitation protocols. Chronic dosing of oral type V phosphodiesterase inhibitors is now commonly used by urologists after radical prostatectomy despite a lack of convincing evidence from randomized, placebo-controlled clinical trials. Use of local therapies to heal the penis may have ...

Science.gov (United States)

Summary.? It is widely believed that hepatocellular cancer (HCC), especially HBV associated HCC, is highly resistant to chemotherapy. To investigate the molecular influence of HBx protein on multidrug resistance (MDR) in HCC and the potential role of the NF-?B pathway in this process. We established HBx-expressing cells by liposome-mediated transfection of the HBx into the HepG2 cell line. We found that HBx expression in HCC cells induces drug resistance against multiple drugs, a significantly lower apoptosis ratio in HepG2-HBx and HepG2.2.15 cells, compared with HepG2 and HepG2-3.1 cells (P?HCC cells were downregulated by IMD-0354 treatment, which is the NF-?B pathway inhibitor. Taken together, these results suggest that HBx protein might be one of the causes for the occurrence of MDR in HCC, and the NF-?B pathway might be involved in this change. PMID:21914061

Science.gov (United States)

In drug development, Caco-2 cells are often employed to study the influence of membrane transporters on drug permeability. The aim of the current study was to characterize permeability and kinetic parameters of selected organic anionic compounds in Caco-2 cells, and to investigate whether the Caco-2 cell line may be used as an overall model to predict interactions on multiple membrane transporters in the intestine. Taurocholic acid (TCA) and estrone-3-sulfate (E(1) S) were used as model substrates. Possible inhibitors studied were TCA, E(1) S, taurolithocholic acid, fluvastatin, and glipizide. The effects of these compounds on initial uptake, apparent permeability, and intracellular end-point accumulations of the probe substrates were studied. Both interactions on apical and basolateral influx transporters were observed. These interactions were proposed to be mediated mainly by the apical sodium-dependent bile acid transporter and the organic solute transporter ...

Science.gov (United States)

Both ammonium and nitrite act as substrates as well as potential inhibitors of anoxic ammonium-oxidizing (Anammox) bacteria. To satisfy demand of substrates for Anammox bacteria and to prevent substrate inhibition simultaneously; two strategies, namely high or low substrate concentration, were carefully compared in the operation of two Anammox upflow anaerobic sludge blanket (UASB) reactors fed with different substrate concentrations. The reactor working at relatively low influent substrate concentration (NO(2)(-)-N, 240 mg-NL(-1)) was shown to avoid the inhibition caused by nitrite and free ammonia. Using the strategy of low substrate concentration, a record super high volumetric nitrogen removal rate of 45.24 kg-Nm(-3) day(-1) was noted after the operation of 230 days. To our knowledge, such a high value has not been reported previously. The evidence from transmission electron microscopy (TEM) showed that the morphology and ultrastructure of the Anammox cells in ...

Energy Technology Data Exchange (ETDEWEB)

The sucrose derivative 6'-deoxy-6'-(2-hydroxy-4-azido)benzamidosucrose (6'-HABS) was prepared from sucrose (via 6'-deoxy-6'-aminosucrose) and 4-amino-salicylic acid. 6'-HABS is a competitive inhibitor of sucrose influx into protoplasts from developing soybean cotyledons and of sucrose binding to membranes from the bacteria P. saccharophila. The Ki for inhibition in the soybean protoplasts was 75..mu..M. 6'-Deoxy-6'-(2-hydroxy-3-/sup 125/Iodo-4-azido)benzamidosucrose was prepared by lactoperoxidase iodination of 6'-HABS. Upon photolysis in the presence of membranes from P saccharophila, label from the photoprobe is incorporated into a sucrose inducible polypeptide of mass 84 KD in SDS-PAGE. The polypeptide is protected from labeling by the inclusion of sucrose in the photolysis mixture. Photolysis conditions which lead to specific labeling of the sucrose protectable polypeptide in ...

Energy Technology Data Exchange (ETDEWEB)

The effects of the dopants, Mg{sup 2+}, Sr{sup 2+}, Sc{sup 3+}, Yb{sup 3+}, Gd{sup 3+}, La{sup 3+}, Ti{sup 4+}, Zr{sup 4+}, Ce{sup 4+}, and Nb{sup 5+}, on the grain boundary mobility of dense Y{sub 2}O{sub 3} have been investigated from 1,500 to 1,650 C. Parabolic grain growth has been observed in all cases over a grain size from 0.31 to 12.5 {micro}m. Together with atmospheric effects, the results suggest that interstitial transport is the rate-limiting step for diffusive processes in Y{sub 2}O{sub 3}, which is also the case in CeO{sub 2}. The effect of solute drag cannot be ascertained but the anomalous effect of undersized dopants (Ti and Nb) on diffusion enhancement, previously reported in CeO{sub 2}, is again confirmed. Indications of very large binding energies between aliovalent dopants and oxygen defects are also observed. Overall, the most effective grain growth inhibitor is Zr{sup 4+}, while the most potent grain growth promoter is Sr{sup 2+}, both at ...

CERN Document Server

A complete macromolecule modeling package must be able to solve the simplest structure prediction problems. Despite recent successes in high resolution structure modeling and design, the Rosetta software suite fares poorly on deceptively small protein and RNA puzzles, some as small as four residues. To illustrate these problems, this manuscript presents extensive Rosetta results for four well-defined test cases: the 20-residue mini-protein Trp cage, an even smaller disulfide-stabilized conotoxin, the reactive loop of a serine protease inhibitor, and a UUCG RNA tetraloop. In contrast to previous Rosetta studies, several lines of evidence indicate that conformational sampling is not the major bottleneck in modeling these small systems. Instead, approximations and omissions in the Rosetta all-atom energy function currently preclude discriminating experimentally observed conformations from de novo models at atomic resolution. These molecular "puzzles" should serve as ...

Energy Technology Data Exchange (ETDEWEB)

The effects of Fe and B{sub 4}C on the sintering behavior and mechanical properties of TiB{sub 2} ceramics have been studied. Sintering was performed in an Ar atmosphere at 2000{degrees}C using attrition-milled TiB{sub 2} powder. When a small amount of Fe (0.5 wt%) was added, abnormal grain growth occurred and the sintered density was low. In the case of B{sub 4}C added along with 0.5 wt% Fe, however, abnormal grain growth was remarkably suppressed, and the sintered density was increased up to 95% of theoretical. But with excess Fe addition (5 wt%), B{sub 4}C grains did not act as a grain growth inhibitor, and B{sub 4}C grains were frequently trapped in large TiB{sub 2} grains. The best mechanical properties were obtained for the TiB{sub 2}-10 wt% B{sub 4}C-0.5 wt% Fe ceramics, which exhibited a three-point bending strength of 400 MPa and a fracture toughness of 5.5 MPa {center dot} m{sup 1/2}.

Energy Technology Data Exchange (ETDEWEB)

The effect of the external pH on the intracellular pH in mung bean (Vigna mungo (L.) Hepper) root-tip cells was investigated with the T P nuclear magnetic resonance (NMR) method. The T P NMR spectra showed three peaks caused by cytoplasmic G-6-P, cytoplasmic Psub(i) and vacuolar Psub(i). The cytoplasmic and vacuolar pHs could be determined by comparing the Psub(i) chemical shifts with the titration curve. When the external pH was changed over a range from pH 3 to 10, the cytoplasmic pH showed smaller changes than the vacuolar pH, suggesting that the former is regulated more strictly than the latter. The H -ATPase inhibitor, DCCD, caused the breakdown of the mechanism that regulates the intracellular pH. H -ATPase appears to have an important part in the regulation of the intracellular pH.

British Library Electronic Table of Contents (United Kingdom)

The nanocomposite WC-Co powders were prepared through planetary ball milling method. Effects of grain growth inhibitor addition and the vacuum sintering parameters on the microstructure and properties of ultrafine WC-10Co cemented carbides were investigated using X-ray diffractometer, scanning electron microscope and mechanical property tester. The results show that VC and NbC additions can refine the WC grains, decrease the volume fraction of Co3W3C phase in ultrafine WC-10Co cemented carbides, and increase the hardness and fracture toughness of the base alloys. After sintering for 60 min at 1400 degreeC, the average grain size and hardness of ultrafine-grained WC-10Co-1VC cemented carbide are 470 nm and HRA 91.5, respectively. The fracture toughness of cemented carbide WC-10Co-1NbC alloy...