The effect of small dose of topiroxostat on serum uric acid in patients receiving hemodialysis

Introduction : Topiroxostat, a recently developed xanthine oxidase inhibitor, is expected to have fewer adverse effects than allopurinol because it has different mechanism of action from alloprinol. However, its dosage, usage and safety have not been established in patients with impaired renal function or those undergoing dialysis at the development since no studies was conducted in these patients. Methods : Cross over clinical trial using 3 months of allopurinol and topiroxostat on 27 maintain Japanese HD patients were carried out. The effects on oxidative stress status of both drugs were also evaluated by measuring oxidation reduction potential. Findings : Twenty‐five of twenty‐seven patients completed study. The mean serum uric acid levels in the topiroxostat‐treated arm was significantly lower than it in the allopurinol‐treated arm time‐dependently (P < 0.0001). Corrected oxidative stress ratio defined as biological antioxidant potential/diacron reactive oxygen metabolites was significantly increased in topiroxostat‐arm (*P = 0.0035), but not in allopurinol‐arm (P = 0.1429). No significant difference was seen in diacron reactive oxygen metabolites, biological antioxidant potential, static oxidation‐reduction potential, and capacity oxidation‐reduction potential between pre and post treatment of both drugs. Discussion : It is suggested that a low dose of topiroxostat decreased serum uric acid sufficiently to maintain it below 7.0 mg/dL in patients receiving hemodialysis.     

Thermal decomposition of cellulose/synthetic polymer blends containing grafted products. V. Cellulose/polystyrene blends

Homogeneous grafting of styrene onto cellulose was carried out in a dimethylacetamide/lithium chloride solvent system. The grafted products were added to cellulose/polystyrene (PS) blends as compatibilizers. The thermal decomposition behavior of the blends was investigated by thermogravimetry. The thermal stability of the blends decreased with an increase in grafted product content. The crystallinity of the blends decreased with grafted product content. The microphase‐separated structures of the blends became finer with grafted product content. The glass transition temperatures for cellulose and PS in the blends were lowered with grafted product content. Differences in thermal decomposition behavior of the blends were correlated with compatibility. Thermogravimetry was effective for compatibility estimation in cellulose/PS blends containing grafted products. © 2010 Wiley Periodicals, Inc. J Appl Polym Sci, 2010     

Mixed powder coating film using thermoplastic polyester and its alkaline resistance

To improve alkaline resistance, a newly mixed powder coating film using thermoplastic polyethylene terephthalate (PET) was investigated. Two kinds of polyvinyl butyral (PVB) and two kinds of polyamide (PA) were chosen as the secondary polymer. The melting temperatures (T _ms) of these materials were lower than that of primary PET polymer so the mixed powder coating was able to form a dual phase film through a fluidized bed coating process. Microscope and Fourier transform infrared spectroscopy (FTIR) observations revealed that the dual phase structure was indeed successfully formed and there was a secondary layer over the entire surface area of the film. This mixed powder coating film significantly enhanced the alkaline resistance to an environment filled with NaOH solution at 40°C in which a secondary material would be effective in protecting the film. With regard to both alkaline resistance and film formability, PET/PVB was superior to the PET/PA mixture.     

DIRECT NUMERICAL SIMULATION OF BLUFF BODY FLOWS USING NON-STAGGERED GRIDS

The present authors pointed out in the previous paper [1] that the implicit SMAC scheme is quite efficient and non-staggered grid arrangement can decrease the computational effort and save the storage memory which is very important to the direct numerical simulation (DNS) of complicated 3-D flow fields. But using non-staggered grid arrangement, the pressure field oscillation (PFO) ordinarily occurs and also, the pressure on the solid walls including sharp corners need to be prescribed directly as the pressure boundary conditions.

In this paper, a new interpolation method, which is a modification to Cheng and Armfield's interpolation formulation, is presented in order to completely prevent PFO from occurring, Moreover, a more accurate specification method of wall pressures and special treatment of pressures at sharp corners are proposed. To test the new methods proposed, the DNS of flow past a square cylinder and flows over backward-facing steps, which are typical of the flow fields with sharp corners, is made using the implicit SMAC scheme combined with these methods. The calculated results are compared with the previous experimental and numerical data and show good agreement with them.     

Acrolein formation in the oxidation of ethane over silica catalysts supporting iron and cesium

A significant yield of aldehydes was obtained by the partial oxidation of ethane over alkali‐modified Fe/SiO₂ catalysts at 475°C (<2% in the case of Cs–Fe/SiO₂). Not only acetaldehyde and formaldehyde but also acrolein were produced in the present system. There are no reports regarding the catalysts for the direct acrolein formation from partial oxidation of ethane. Such significant promoting effect of alkali‐modified Fe/SiO₂ catalysts in the partial oxidation of hydrocarbons has never been observed. Aldol‐type condensation for formation of acrolein could occur in the partial oxidation of ethane over alkali‐modified Fe/SiO₂ catalysts. This revised version was published online in July 2006 with corrections to the Cover Date.     

ELASTOPLASTIC ANALYSIS OF W-Cu FUNCTIONALLY GRADED MATERIALS SUBJECTED TO A THERMAL SHOCK BY MICROMECHANICAL MODEL

We consider the transient elastoplastic behavior of the functionally graded divertor plate due to a thermal shock with temperature-dependent properties. The development of a micromechanical model for functionally graded materials is presented, and its application to thermoelastoplastic analysis is discussed for the case of the W-Cu functionally graded material for the international thermonuclear experimental reactor divertor plate. The divertor plate consists of a graded layer bonded between a homogeneous substrate and a homogeneous coating, and it is subjected to a cycle of heating and cooling on the coating surface of the material. The material properties of the divertor plate are dependent on the temperature and the position. Numerical results presented include the transient elastoplastic stresses.     

TRANSIENT THERMAL SINGULAR STRESSES OF MULTIPLE CRACKING IN A W-Cu FUNCTIONALLY GRADED DIVERTOR PLATE

We consider the transient thermal singular stresses of multiple cracking in a functionally graded divertor plate due to a thermal shock. The plate is made of a graded layer bonded between a homogeneous substrate and a homogeneous coating, and it is subjected to a cycle of heating and cooling on the coating surface of the plate. The surface layer contains a parallel array of embedded or edge cracks perpendicular to the boundaries. The thermal and elastic properties of the material are dependent on the temperature and the position. Finite element calculations are carried out, and the transient thermal stress intensity factors are shown graphically.     

Rapid evaluation of oxidation catalysis by gas sensor system: total oxidation, oxidative dehydrogenation, and selective oxidation over metal oxide catalysts

The rapid evaluation of catalysis is an indispensable technology for the success of combinatorial chemistry. A small-sized, less expensive, easily operating screening is desirable for parallel settings which dramatically shortens the evaluation time. Recent advances in gas sensors have enabled us to use them for the rapid evaluation of oxidation catalysis. Three typical catalytic oxidations over metal oxide catalysts were evaluated by gas sensor systems optimized for each catalytic system. The first one is the total oxidation of carbon monoxide in air. Five catalytic combustion-type gas sensors were used in a parallel reactor system to shorten the evaluation time. The second one is the oxidative dehydrogenation (ODH) of ethane over the mixed oxide of nickel and iron. The evaluation of the ODH catalysis was performed by a selective olefin sensor which determines the concentration of C₂H₄ in C₂H₆. The third one is the selective oxidation catalysis of propane over alkali modified Fe/SiO₂. The effluents including CO, CO₂, aldehydes and ketones in propane were analyzed by the CO, CO₂ and semiconductor-type gas sensors selective toward aldehydes and ketones. These evaluation results indicated that gas sensors have a good potential for the rapid evaluation of oxidation catalysts.     

Chemical Modification of Phage-Displayed Helix-Loop-Helix Peptides to Construct Kinase-Focused Libraries

Conformationally constrained peptides hold promise as molecular tools in chemical biology and as a new modality in drug discovery. The construction and screening of a target-focused library could be a promising approach for the generation of de novo ligands or inhibitors against target proteins. Here, we have prepared a protein kinase-focused library by chemically modifying helix-loop-helix (HLH) peptides displayed on phage and subsequently tethered to adenosine. The library was screened against aurora kinase A (AurA). The selected HLH peptide Bip - 3 retained the α-helical structure and bound to AurA with a K_D value of 13.7 μM. Bip - 3 and the adenosine-tethered peptide Bip - 3 - Adc provided IC₅₀ values of 103 μM and 7.7 μM, respectively, suggesting that Bip - 3 - Adc bivalently inhibited AurA. In addition, the selectivity of Bip - 3 - Adc to several protein kinases was tested, and was highest against AurA. These results demonstrate that chemical modification can enable the construction of a kinase-focused library of phage-displayed HLH peptides.