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.     

Carbonization of coals to produce anisotropic cokes. 1. Modifying activities of some additives in the co-carbonization of low-rank coals

Using low-rank coals, the modifying activities of some petroleum, coal tar and aromatic hydrocarbon additives have been examined to find procedures for their utilization in the preparation of blast furnace coke. Petroleum pitch, especially after hydrogenation, exhibited excellent modifying activity even with non-fusible coals. In contrast, the activity of coal tar was very limited with such coals. The napththenic component, revealed by n.m.r. of the additives, appears to be important in the co-carbonization by inducing fusibility and anisotropic development in such coals. Co-carbonization to recover the dehydrogenated additives was attempted. However, there was no development of the anisotropy in the resultant coke by dissolution of the coal particles although the coal particles were firmly fixed in the matrix. Acid-refluxing treatment of non-fusible coals was found to enhance their modification susceptibility, indicating that some of the acid-soluble mineral matter is important in the thermal depolymerization or fusion process of the coal.     

Multi-dimensional transient mathematical simulator of blast furnace process based on multi-fluid and kinetic theories

The ironmaking blast furnace is regarded as one of the biggest and most complex industrial reactors, because it includes various materials like gas, lump granular materials, liquids and powders and more than 30 major reactions and phase changes in a single reaction vessel. The mathematical simulator of this process developed in this study used the multi-fluid treatment as its framework, since the motions of these materials were governed by different flow mechanisms. The rates of the interactions among the phases and the chemical reactions were evaluated based on kinetic theories. The model successfully reproduced the fields of velocity, temperature and reaction in the furnace and its validity was confirmed. The simulator was also applied to a novel operation, namely the top gas recycling combined with the carbon-composite iron-ore charging and the waste plastics injection, and the advantages in furnace efficiency and environmental load were quantitatively indicated.     

Synthesis of Thermally Stable χ-Alumina by Thermal Decomposition of Aluminum Isopropoxide in Toluene

Thermal decomposition of aluminum isopropoxide in toluene at 315°C resulted in χ-alumina that had high thermal stability, whereas the reaction at lower temperatures resulted in formation of an amorphous product. The χ-alumina thus obtained directly transformed to α-alumina at ∼1150°C, bypassing the other transition alumina phases, whereas the amorphous product transformed to γ-alumina and then to θ-alumina before final transformation to α-alumina. When the χ-alumina, solvothermally synthesized at 315°C, was recovered by the removal of the solvent at the reaction temperature, thermal stability of the product was improved further. This procedure is convenient because it avoids bothersome work-up processes that yield large-surface-area and large-pore-volume alumina.     

Studies on biaxial stretching of polypropylene film. IX. Melting behavior of biaxially stretched film in one step

Melting temperature of a film biaxially stretched in one step in air at 152 or 140°C increases with increase of vA, whereas heat of fusion and density decrease with increase of vA, where vA is the degree of stretching in area. The rapid decrease in density occurs for vA > 10. Extrapolation of the plot of the density versus vA^?1/2 gives a value of 0.870 g/cm³ at infinite vA, which has been reported as the amorphous density of isotactic polypropylene by Farrow. This is so because the fine structure of the film becomes more and more amorphous with further stretching and reaches completely amorphous state at infinite vA. The temperature of stretching has a strong effect on the thermal behavior of a film; a low stretching temperature (140°C) brings about lower melting temperature, heat of fusion, and density. Crystallinity after melt press has not so large an effect on the melting behavior as the stretching temperature. Melting temperature and the shape of the thermogram also depend on the heating rate. There is an appropriate heating rate depending on vA which gives the minimum melting temperature. With stretched samples, a small side peak or a shoulder appears at a relatively low temperature in the thermogram when a high heating rate is used.     

Miscibility and Probe Tack of Acrylic Pressure Sensitive Adhesives—Acrylic Copolymer/Tackifier Resin Systems

Miscibility between acrylic copolymers and tackifier resins are investigated in terms of phase diagrams, and the probe tack of the blends are measured as a function of both temperature and rate of separation in order to obtain the master curves. It is found that the probe tack of the pressure sensitive adhesives are closely related to the miscibility between the components. The master curves of the miscible blends shift along the X(rate)-axis according to the change of T_g of the bulk materials with a gradual variation of the peak heights. However, those of the immiscible blends will not shift along the X(rate)-axis, but the magnitude will decrease with increase of a dispersed phase.     

Isotactic polypropylene hollow microfibers prepared by CO2 laser‐thinning

An isotactic polypropylene hollow microfiber was continuously produced by using a carbon dioxide (CO₂) laser‐thinning method. To prepare the hollow microfiber continuously, the apparatus used for the thinning of the solid fiber was improved so that the laser can circularly irradiate to the hollow fiber. Original hollow fiber with an outside diameter (OD) of 450 μm and an internal diameter (ID) of 250 μm was spun by using a melt spinning machine with a specially designed spinneret to produce the hollow fiber. An as‐spun hollow fiber was laser‐heated under various conditions, and the OD and the ID decreased with increasing the winding speed. For example, when the hollow microfiber obtained by irradiating the CO₂ laser to the original hollow fiber supplied at 0.30 m min^?1 was wound up at 800 m min^?1, the obtained hollow microfiber had an OD of 6.3 μm and an ID of 2.2 μm. The draw ratio calculated from the supplying and the winding speeds was 2667‐fold. The hollow microfibers obtained under various conditions had the hollowness in the range of 20–30%. The wide‐angle X‐ray diffraction patterns of the hollow microfibers showed the existence of the highly oriented crystallites. Further, the OD and ID decreased, and the hollowness increased by drawing hollow microfiber obtained with the laser‐thinning. © 2006 Wiley Periodicals, Inc. J Appl Polym Sci 102: 2600–2607, 2006     

Influence of Metal Ions on the Order-Disorder Transition Temperature of the Ba-M-O (M: La, Y, In, or Ga) System

Preparation of BaLa₂O₄, B_a3,Y₄O₉, B_a,In₂O₅, and Ba₃Ga₂O₆ powders and their sintering were investigated in Ar or air. These sintered bodies with perovskite-related structure were synthesized by reaction sintering, using mixed powders in the atomic ratios of Ba/La = 1, Ba/Y = 0.75, Ba/In = 1, and Ba/Ga = 1.5. The order-disorder transition temperatures of the BaLa₂O₄, Ba₃Y₄O₉, Ba₂In₂O₅, and Ba₃Ga₂O₆ sintered bodies were 270°, 350°, 880°, and 123O^oC, respectively. It was found that the temperatures were influenced by the ionic radius of cations in B sites, and the transition temperatures decreased with increasing ionic radius.     

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.     

Production of antimicrobially active silk proteins by use of metal‐containing dyestuffs

The work presented here discusses a new technique for preparing silk fibers and films with persistent antimicrobial activity through use of metallic dyestuffs during the fiber dyeing process. The length of the silk fibers investigated contracted when the fibers were immersed in concentrated neutral salt solutions, such as calcium or potassium nitrate, at elevated temperature levels. The birefringence and molecular orientation of the silk fibroin molecules became less ordered by the action of the neutral salt solutions, resulting in increased dyestuff absorption. Subsequently, contracted silk fibers were dyed with metallic dyestuffs containing Cr or Cu for the purpose of obtaining silk fibers with antimicrobial activity. Silk fibers dyed with metallic dyestuffs showed significant antimicrobial activity against the plant pathogen Cornebacterium and the human pathogen Coli bacillus. Tensile strength of the silk fibers after the salt shrinking and dyeing processes did not show a significant change, whereas the elongation at break was increased slightly. The techniques described here for preparing significantly active antimicrobial silk fibers are effective and economic ways of providing new materials for industrial and biomedical applications. © 2002 Wiley Periodicals, Inc. J Appl Polym Sci 86: 1181–1188, 2002