Screening of Inhibitors Targeting Heat Shock Protein 47 Involved in the Development of Idiopathic Pulmonary Fibrosis

Heat shock protein 47 (HSP47), a collagen-specific molecular chaperone, is causally related to fibrotic diseases, including idiopathic pulmonary fibrosis. The identification of Compounds that interfere with the HSP47-collagen interaction is essential for the development of relevant therapeutics. Herein, we prepared human HSP47 as a soluble fusion protein expressed in E. coli and established an assay system for HSP47 inhibitor screening. We screened a natural and synthetic Compound library established at Nagasaki University. Among 1023 Compounds, 13 exhibited inhibitory activity against human HSP47, of which three inhibited its function in a dose-dependent manner. Epigallocatechin-3-O-gallate, one of these three Compounds, is a typical polyphenol Compound derived from tea leaves. Structurally related Compounds were synthesized and examined for their activity, revealing a hydroxyl group at A-ring position 5 as important for its activity. The present findings provide valuable insight for the development of natural product-derived therapeutics for fibrotic diseases, including idiopathic pulmonary fibrosis.     

Characterization of blasted austenitic stainless steel and its corrosion resistance

It is known that the corrosion resistance of stainless steel is deteriorated by blasting, but the reason for this deterioration is not clear. A blasted austenitic stainless steel plate (JIS-SUS304) has been characterized with comparison to the scraped and non-blasted specimens. The surface roughness of the blasted specimen is larger than that of materials finished with #180 paper. A martensite phase is formed in the surface layer of both blasted and scraped specimens. Compressive residual stress is generated in the blasted specimen and the maximum residual stress is formed at 50–100 μm from the surface. The corrosion potentials of the blasted specimen and subsequently solution treated specimen are lower than that of the non-blasted specimen. The passivation current densities of the blasted specimens are higher those of the non-blasted specimen. The blasted specimen and the subsequently solution treated specimen exhibit rust in 5% sodium chloride (NaCl) solution, while the non-blasted specimen and ground specimen do not rust in the solution. It is concluded that the deterioration of corrosion resistance of austenitic stainless steel through blasting is caused by the roughed morphology of the surface.     

Kinetics of hydrogen absorption and desorption of magnesium nickel alloy

Reaction rates in the Mg₂Ni---H₂ system are still unclear, although they are needed for the process/optimization of hydrogen storage reactors. In this article, the rates of hydrogen absorption and desorption of the magnesium nickel alloy were investigated at different pressures up to 2.0 MPa using a constant-temperature thermogravimetric method. The powder of the alloy was microencapsulated with copper to improve the alloy properties (such as cycling strength) as a pretreatment. In the experiments, weight changes of the smallest amount possible of samples were monitored with the help of an ultra-accurate thermobalance, in order to avoid changes of the sample temperature due to the heat of the reaction. The reaction curves obtained revealed unique dependence of temperature and pressure and influence of thermal hysterisis. It is also possible that hydrogen-absorption and-desorption rates of this hydrogen storage alloy are expressed by the rate equation of first-order reversible reaction.     

Synthesis and properties of bismaleimide resins containing ether bonds

New bismaleimides containing ether bonds were prepared. The thermal properties of the bismaleimides were investigated by differential scanning calorimetry (DSC). The effects of structure of the bismaleimides and curing conditions on the thermal and mechanical properties of the cured resins such as initial decomposition temperature (T_d), glass transition temperature (T_g), and flexural strength were studied. The introduction of ether bonds to bismaleimide resins decreased the brittleness of the resins without reductions in their heat-resistant properties.     

Materials for global carbon dioxide recycling

CO₂ emissions, which induce global warming, increase with the development of economic activity. It is impossible to decrease the CO₂ emissions by suppression of the economic activity. Global CO₂ recycling can solve this problem. The global CO₂ recycling consists of three district: The electricity is generated by solar cells on deserts. At desert coasts, the electricity is used for H₂ production by seawater electrolysis and H₂ is used for CH₄ production by the reaction with CO₂. CH₄ which is the main component of liquefied natural gas is liquefied and transported to energy consuming districts where CO₂ is recovered, liquefied and transported to the desert coasts. A CO₂ recycling plant for substantiation of our idea has been built on the roof of the Institute for Materials Research in 1996. Key materials necessary for the global CO₂ recycling are the anode and cathode for seawater electrolysis and the catalyst for CO₂ conversion. All of them have been tailored by us. They have very high activity and selectivity for necessary reactions in addition to excellent durability. A pilot plant consisting of minimum units in an industrial scale is going to be built in three years.     

High‐pixel‐rate grating‐light‐valve laser projector

Abstract— A high‐pixel‐rate, high‐contrast (30,000:1) wide‐color‐gamut grating‐light‐valve laser projector is reported. A new optical engine enabling high‐frame‐rate (240 Hz) scan projection is employed. Panoramic wide‐angle‐scan projection with a 64:9 aspect ratio was also developed. Speckle noise is eliminated using a simple but highly efficient technique. The optical throughput efficiency of the grating‐light‐valve laser projector is reviewed.     

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.     

Shrinkable Nanotubes for Duplex Formation of Short Nucleotides

Molecular monolayer nanotubes produced by self‐assembly of an amphiphile modified with a 2‐nitrobenzyl group as a photoresponsive unit are able to encapsulate dinucleotides via electrostatic attraction. Upon photoirradiation, the 18 nm inner diameter of the nanotubes shrinks to less than 2 nm as a result of photochemical cleavage of the 2‐nitrobenzyl group in the amphiphile. This shrinking of the nanotube channels leads to a propulsive release of the dinucleotides into the bulk solution and simultaneously accelerates formation of the dinucleotide duplexes. The larger nanotube channels without photoirradiation merely release each dinucleotide into the bulk solution, indicating that the squeezing via transportation in the narrow nanotube channels is necessary for duplex formation. In addition to the size effect, water with a lower polarity confined within the narrow nanotube channels helps to stabilize the energetically unfavorable hydrogen‐bonded base pair between the dinucleotides. This system should enable researchers to perform biological reactions that occur only in specific environments and conditions in living organisms.     

A reduction method of dynamic false contour utilizing the frame‐rate‐control method with suppression of the side effect on PDPs

Abstract— The plasma‐display panel (PDP) is a type of flat‐panel display that can display a high‐quality image. However, when moving images are displayed, annoying disturbances such as false contour noise occurs. This noise is called dynamic false contour (DFC). To achieve a higher‐quality image, DFC has to be reduced. Therefore, a new method to reduce DFC is proposed. To find a way to reduce DFC, a new evaluation value for it has been defined: the evaluation value of dynamic false contour (EVDFC). This value is defined on the basis of a person's subjective evaluation. By applying this value, the cause that generates DFC can be identified. On the basis of these studies, a new method for reducing DFC by applying frame‐rate control (FRC) with suppression of the side effect is proposed. This improved method can be used to provide high‐quality images.     

A variational approach to multi-phase motion of gas, liquid and solid based on the level set method

We propose a simple and robust numerical algorithm to deal with multi-phase motion of gas, liquid and solid based on the level set method [S. Osher, J.A. Sethian, Front propagating with curvature-dependent speed: Algorithms based on Hamilton-Jacobi formulation, J. Comput. Phys. 79 (1988) 12; M. Sussman, P. Smereka, S. Osher, A level set approach for capturing solution to incompressible two-phase flow, J. Comput. Phys. 114 (1994) 146; J.A. Sethian, Level Set Methods and Fast Marching Methods, Cambridge University Press, 1999; S. Osher, R. Fedkiw, Level Set Methods and Dynamics Implicit Surface, Applied Mathematical Sciences, vol. 153, Springer, 2003]. In Eulerian framework, to simulate interaction between a moving solid object and an interfacial flow, we need to define at least two functions (level set functions) to distinguish three materials. In such simulations, in general two functions overlap and/or disagree due to numerical errors such as numerical diffusion. In this paper, we resolved the problem using the idea of the active contour model [M. Kass, A. Witkin, D. Terzopoulos, Snakes: active contour models, International Journal of Computer Vision 1 (1988) 321; V. Caselles, R. Kimmel, G. Sapiro, Geodesic active contours, International Journal of Computer Vision 22 (1997) 61; G. Sapiro, Geometric Partial Differential Equations and Image Analysis, Cambridge University Press, 2001; R. Kimmel, Numerical Geometry of Images: Theory, Algorithms, and Applications, Springer-Verlag, 2003] introduced in the field of image processing.