Design and Synthesis of A‐Ring Simplified Pyripyropene A Analogues as Potent and Selective Synthetic SOAT2 Inhibitors

Currently, pyripyropene A, which is isolated from the culture broth of Aspergillus fumigatus FO‐1289, is the only compound known to strongly and selectively inhibit the isozyme sterol O‐acyltransferase 2 (SOAT2). To aid in the development of new cholesterol‐lowering or anti‐atherosclerotic agents, new A‐ring simplified pyripyropene A analogues have been designed and synthesized based on total synthesis, and the results of structure–activity relationship studies of pyripyropene A. Among the analogues, two A‐ring simplified pyripyropene A analogues exhibited equally efficient SOAT2 inhibitory activity to that of natural pyripyropene A. These new analogues are the most potent and selective SOAT2 inhibitors to be used as synthetic compounds and attractive seed compounds for the development of drug for dyslipidemia, including atherosclerotic disease and steatosis.     

Ultra‐high‐resolution 1058‐ppi OLED displays with 2.78‐in size using CAAC‐IGZO FETs with tandem OLED device and single OLED device

We fabricated new 2.78‐in 1058‐ppi organic light‐emitting diode (OLED) displays. The displays used OLED devices with a tandem structure and a single structure and a field effect transistor (FET) using c‐axis aligned crystalline In–Ga–Zn–O (CAAC‐IGZO) for an active layer and employing the 1.5‐µm rule over a glass substrate. Even in the displays with such high resolution exceeding 1000 ppi, crosstalk that was observed in the lower luminance region was suppressed. The displays achieved high color reproducibility and reduced viewing angle dependence.     

Phase separation of polymerized lipids in hybrid liposomes

Summary Hybrid liposomes were prepared from the mixture of dipalmitoyl phosphatidylcholine (DPPC) and di-2,4-octadecadiene phosphatidylcholine (DODPC), and their phase separation behaviours was analyzed. In hybrid liposome systems, two transition temperatures (18 and 41°C for DODPC and DPPC, respectively) were clearly observed by means of DSC and fluorescence techniques. These two transition temperatures were also found after polymerization of DODPC molecules in hybrid liposomes by the UV irradiation. These strongly suggest that DPPC and DODPC molecules do not dissolve well but form clusters in the membrane. This phase separation was directly confirmed by freeze-fracture TEM technique.     

Cost Trends in Long Term Care in Japan and Sweden over the Period 2000 to 2010

Japan and Sweden have similar ambitions and both similarities and differences when it comes to provide long term care (LTC) for their old age citizens. The study compares cost increase for LTC in Japan and Sweden in the time period 2000–2010 by decomposing the changes in costs into changes in the size of the old age population (65 years and above) , the distribution on level of dependency /disability by age-group and gender, the volume of provided LTC services in relation to level of dependency/disability and the unit costs for provided services. The analysis of needs of LTC services is based upon nationally representative sample surveys population studies completed in each country: Nihon University Japanese Longitudial Study of Aging and the Swedish Survey of Living Conditions with 19. 602 and 9.433 observations respectively. Data on LTC services provision by level of dependency/ disability is taken from nine Japanese municipalities collected by assessments in the LTCI-system and from surveys in eight Swedish municipalities. It is shown by the analysis that the rapid cost increase in Japan in the period 2000–2010, 108 %, has mainly been driven by the increase in the old age population. However, another important factor in the period 2000–2005 has been increased provision of LTC services given level of dependency. In Sweden the cost increase depending on population increase has been countered by decreasing levels of disability by age-groupand gender. Services provision given needs of LTC has not increased very much. As a result the cost increase in the time period 2000–2010 has been much lower, +6 %.     

Note on the g-fold Joint Weight Enumerators of Self-Dual Codes over ℤ k

Recently there has been interest in self-dual codes over finite rings. In this note, g-fold joint weight enumerators of codes over the ring ℤ _k of integers modulo k are introduced as a generalization of the biweight enumerators. We establish the MacWilliams relations for these weight enumerators and investigate the biweight enumerators of self-dual codes over ℤ _k . We derive Gleason-type theorems for the corresponding biweight enumerators with the help of invariant theory. Received: March 13, 2000; revised version: December 11, 2000     

Release Property of Progesterone from a Mixed-Base Suppository Consisting of Witepsol® W35 and Witepsol® E85

The mechanism of drug release from progesterone suppositories that consist of two types of hard fat (Witepsol® W35 and Witepsol® E85) was investigated. The strength, the thermodynamic characteristics, the surface structures, the drug release property, methylene blue penetration into suppositories, and change of surface structure after the dissolution test were employed for detecting characteristics of progesterone suppositories. The formulation with a mixing ratio of Witepsol W35 and Witepsol E85 at a 1:1 ratio showed the maximum strength value. The peak temperature of the suppositories showed a tendency to increase with increases in the ratio of Witepsol E85. The maximum height of the profiles measured with laser microscopy, from 20.8 μm to 29.2 μm, reached a maximum after 3 h of the dissolution test. When the suppositories were immersed in pH 7.4 phosphate buffer containing 0.5% methylene blue at 37°C, the penetrating area increased with time. The weight of the suppositories also increased with time. According to these findings, it was suggested that the release of drug from a mixed type of suppository containing progesterone was via the matrix and pores.     

Effect of reaction temperature on Fe–Al analcime formation

The effects of reaction period, temperature, and iron species on the zeolite framework type were studied in this work. Gismondine (GIS) is usually synthesized by hydrothermal method at 80°C from sodium metasilicate and aluminum nitrate as starting materials preferentially independent of the presence/absence of iron source. However, the present work revealed that pure analcime (ANA) could be formed at temperatures more than 120°C. A large polyhedral ANA crystal with a diameter of 180 μm was obtained even at a comparatively low temperature such as 150°C at a short reaction period of 1 week. The presence of iron source promoted the formation of pure ANA. Infrared spectroscopy, X-ray diffraction, and ICP-OES analysis suggested that the iron component added as a reactant was incorporated into the ANA framework through the isomorphous substitution for Al.