Library

Notes: Abstract SCH 29851 [8-chloro[6,11-dihydro-11-(1-carboethoxy-4-piperidylidene)-5-H-benzo[5,6]cyclohepta[1,2-b]-pyridine] was discovered as part of a search for a new antihistamine without effects on the central nervous system (CHS). Antihistaminc potency and duration of action of SCH 29851 and other antihistamines were assessed by inhibition of histamine-induced lethality in guinea pigs and histamine-induced paw edema in mice. Evaluation of possible CNS effects included gross observation of mice, rats, dogs and monkeys, prevention of electroshock-induced convulsions, acetic acid-induced writhing and physostigmine-induced lethality in mice and biochemical measures related to sedative liability such as displacement ofin vivo 3H-mepyramine binding in mouse brain andin vitro 3H-WB 4101 binding in guinea pig cortex. Comparisons were made to several antihistamines considered to be sedative to varying degrees, including diphenhydramine, promethazine, chlorpheniramine and azatadine and to the newer antihistamines terfenadine and astemizole which are reported to be non-sedating in man at doses that antagonize the effects of histamine peripherally. SCH 29851 had antihistamine activity in the tests used with a potency at least comparable to most standards and was devoid of activity in all the functional and biochemical models used as indices of CNS activity. It is expected that SCH 29851 should be an effective, long acting, antihistamine in man without sedative effects at therapeutic doses.

Notes: Abstracts Aims/hypothesis. Infiltration of mononuclear cells and glomerular enlargement accompanied by glomerular cell proliferation are very early characteristics of the pathophysiology of diabetes. To clarify the mechanism of early diabetic nephropathy, we measured [3H]-thymidine incorporation and cell numbers to show the influence of a high ambient glucose concentration and the osmotic effect on rat mesangial cell proliferation. We also measured the effect of high glucose on the expression of intercellular adhesion molecule-1 and vascular adhesion molecule-1 by flow cytometry and semiquantitative RT-PCR in mesangial cells and the adhesion of leukocytes to mesangial cells. Methods/results. Cells exposed to high d-glucose (30 mmol/l) caused an increase in [3H]-thymidine incorporation and cell numbers at 24 and 48 h and normalized at 72 h (p 〈 0.05), whereas these changes were not found in high mannitol (30 mmol/l), IL-1β, or TNFα-stimulated mesangial cells. Cells exposed to high-glucose (15, 30, or 60 mmol/l) or osmotic agents (l-glucose, raffinose and mannitol) showed that intercellular adhesion molecule-1 expression began to increase after 24 h, reached its maximum at 24 and 48 h and gradually decreased afterwards. The stimulatory effects of high glucose and high mannitol on mRNA expression were observed as early as 6 h and reached its maximum at 12 h. Up-regulation of ICAM-1 protein and mRNA was also found in IL-1-β and TNF-α-stimulated mesangial cells. Neither vascular adhesion molecule-1 protein nor mRNA expression was, however, affected by high glucose and high mannitol. Notably, the protein kinase C inhibitors calphostin C and staurosporine reduced high glucose- or high mannitol-induced intercellular adhesion molecule-1 mRNA expression and high glucose-induced proliferation. Furthermore, the NF-ϰB inhibitor N-tosyl-l-phenylalanine chloromethyl ketone reduced high glucose- or high mannitol-induced intercellular adhesion molecule-1 mRNA expression and high glucose-induced proliferation. Results showed that high glucose (15, 30 mmol/l) or high concentrations of osmotic agents remarkably increased the number of adherent leukocytes to mesangial cells (p 〈 0.01) compared with control cells (5 mmol/l d-glucose). Functional blocking of intercellular adhesion molecule-1 on mesangial cells with rat intercellular adhesion molecule-1 monoclonal antibody, calphostin C, staurosporine, or N-tosyl-l-phenylalanine chloromethyl ketone significantly inhibited high glucose- or high mannitol-induced increase in leukocyte adhesion (p 〈 〈 0.05). Conclusion/interpretation. These results suggest that high glucose can upregulate intercellular adhesion molecule-1 protein and mRNA expression but not vascular adhesion molecule-1 expression in mesangial cells and promote leukocyte adhesion through up-regulation of intercellular adhesion molecule-1 through osmotic effect, possibly depending on the protein kinase C nuclear factor-kappa B (PKC-NF-ϰB) pathway. High glucose itself can also promote mesangial cell proliferation through the PKC-NF-ϰB pathways. We conclude that hyperglycaemia in itself seems to be an important factor in the development of early diabetic nephropathy. [Diabetologia (2000) 43: 1544–1553]

Notes: The relationship between the wax matrix in lipstick and sweating has been investigated by observing the change of size and shape of the wax matrix due to sweating by Scanning Electron Microscopy (SEM). For observation by SEM, a lipstick sample was frozen in liquid nitrogen. The oil in the lipstick was then extracted in cold isopropanol (−70 °C) for 1–3 days. After the isopropanol was evaporated, the sample was sputtered with gold and examined by SEM. The change of wax matrix underneath the surface from fine, uniform structure to coarse, nonuniform structure resulted from the caking of surrounding wax matrix. The oil underneath the surface migrated to the surface of lipstick with sweating; consequently the wax matrix in that region was rearranged into the coarse matrix. In case of flamed lipstick, sweating was delayed and the wax matrix was much coarser than that of the unflamed one. The larger wax matrix at the surface region was good for including oil. The effect of molding temperature on sweating was also studied. As the molding temperature rose, sweating was greatly reduced and the size of the wax matrix increased. It was found that sweating was influenced by the compatibility of wax and oil. A formula consisting of wax and oil that have good compatibility has a tendency to reduce sweating and increase the size of the wax matrix. When pigments were added to wax and oil, the size of the wax matrix was changed, but in all cases sweating was increased due to the weakening of the binding force between wax and oil. On observing the thick membrane of wax at the surface of lipstick a month after molding it was also found that sweating was influenced by ageing. In conclusion, the structure of the wax matrix at the surface region of lipstick was changed with the process of flaming, molding temperature, compatibility of wax and oil, addition of pigment, and ageing. In most cases, as the size of the wax matrix was increased, sweating was reduced and delayed.

Notes: Gamma irradiation was used to reduce the N-nitrosamines and residual nitrite in model system sausage during storage. Aerobic or vacuum packaged sausage was irradiated at 0, 5,10, 20, and 30 kGy. The residual nitrite levels were significantly reduced by gamma irradiation, and, in vacuum packaging, the reduction was dose dependent. The N-nitrosodimethylamine of the sausage irradiated at 10 kGy or above reduced in aerobic packaging, while a dose of 20 kGy was needed in vacuum packaging. The N-nitrosopyrrolidine reduction was found at 20 and 30 kGy-irradiation. Results indicated that high dose irradiation (〉 10 kGy) was needed to reduce the carcinogenic N-nitrosamine and nitrite levels in pork sausage during storage.

Notes: Low-fat pork was produced at extrusion temperatures (ET) of 25, 32.2,43.3,54.4, or 65.6°C with addition of soy protein isolate (SPI) at 0,1.5, or 3% and evaluated by measuring chemical and physical properties of low-fat pork sausage links. ET and SPI addition influenced moisture retention and fat reduction. The highest ET(65.5°C) gave the highest fat reduction in extrudates. TBARS decreased as ET and SPI increased. Extrudates at higher ET made darker and redder sausages. The hardness value of the control was not different from that of sausages from 65.6°C ET extrudates. The fat-reduced sausages were more springy and cohesive than the control. Depending on fat reduction, twin-screw extrusion influenced sausage color, texture, and lipid oxidation. The sausage links from 65.6°C ET extrudates with 1.5% SPI had the lowest fat, lowest TBARS, least cooking loss and were not different in hardness from control high-fat sausages.

Notes: The aim of this study was to compare the surface discoloration of polished and celluloid strip-finished composite surfaces in microhybrid type composites and to determine whether or not the discoloration of a celluloid strip-finished composite surface is reduced if oxygen inhibition on the surface can be prevented. The composite surfaces were celluloid-strip finished (group 1), polished (group 2), or celluloid-strip finished under nitrogen gas purging (group 3). Z100, Spectrum, and Aelitefil were used as the test materials. After each surface treatment, the samples were stored in 37 °C distilled water for 24 h and placed in a disclosing solution (0·2% Erythrosin, pH 7·0) for 7 days in the dark. A computer controlled spectrophotometer was used to determine the CIELAB co-ordinates (L*, a*, b*). For each composite, the degree of discoloration among the groups was compared with a one-way anova test. A Dunnett's t-test was then performed to compare the colour change in group 1 with that of group 2 or group 3. In all materials, there were no statistical differences in the surface discoloration between group 1 and group 2. In the Aelitefil and Spectrum test materials, the samples in group 3 showed a lower level of discoloration than the those in group 1. In Z100, there was no statistical difference. In microhybrid composites, there was no difference in surface discoloration between celluloid strip-finished and the polished surface. Nitrogen gas purging during the polymerization process on the celluloid strip-finished composite surface might be useful for reducing the discoloration celluloid strip-finished surface in microhybrid composites.

Notes: The microstructure of the NiFe/Co(CoFe)/Al(Ta)-oxide/Co(CoFe) ferromagnetic tunnel junction was investigated using cross-sectional transmission electron microscopy (TEM). The effect of the insulating layer on the magnetoresistive (MR) properties of the junction was studied. The multilayer junction was formed using magnetron sputtering and the insulating layer was created by plasma oxidation of the deposited metal film. TEM analysis showed that the MR ratio was highly dependent on the insulating layer. For the NiFe/Co/Al-oxide/Co junction, when the Al2O3 layer was 13 Å, the oxide layer was flat and the highest MR ratio of 15% was attained. As the Al2O3 thickness increased, the interface roughness rapidly increased, and the MR ratio also markedly dropped. In contrast, NiFe/CoFe/Al-oxide/CoFe junction showed a comparatively flatter interface and recorded a higher MR ratio. The Ta-oxide insulating layer remained flat regardless of the thickness; however, the largest MR ratio of only 9% was obtained within a narrow thickness range. We have demonstrated that there exists a direct correlation between the microstructure of the oxide layer and the MR ratio of the junction, which could be utilized to optimize the electrical properties of the ferromagnetic tunneling junction. © 2001 American Institute of Physics.