Staurosporine and its derivatives enhance f-Met-Leu-Phe-induced superoxide production via phospholipase D activation in human polymorphonuclear leukocytes

Staurosporine (STAR) is one of the most potent inhibitors of protein kinase C (PKC). It is known that in human polymorphonuclear leukocytes (PMNs), the phorbol ester-induced generation of superoxide anion (respiratory burst) is effectively inhibited by STAR in a dose-dependent manner, whereas superoxide generation induced by chemoattractants, e.g. n-formyl-methionyl-leucyl-phenylalanine (FMLP) or PAF, is regulated biphasically by STAR. We compared the effects of STAR and K252a on FMLP-induced superoxide production from PMNs and examined the effects of propranolol, a inhibitor of phosphatidic acid (PA) phosphohydrolase, on the potentiation of the production by STAR. We also examined the effects of some derivatives of STAR and K252a on the production and the alteration of the effects induced by propranolol pretreatment. When PMNs were stimulated with FMLP, STAR potentiated superoxide production by 240.5 +/- 30.9% at a low concentration (100 nmol/l). Propranolol pretreatment specifically inhibited the potentiation. When phorbol-12-myristate-13-acetate (PMA) was used as a stimulant, STAR inhibited superoxide production dose-dependently and did not enhance the production. K252a inhibited PMA or FMLP-induced superoxide production dose-dependently and did not enhance FMLP-induced superoxide production. STAR derivatives showed potentiation of FMLP-induced superoxide production similar to that of STAR at concentrations ranging from 10-100 nmol/l, and propranolol (200 mumol/l) effectively inhibited it. K252a derivative NA332 did not show any potentiative effect on the production. PMA-induced superoxide production was inhibited by all compounds dose-dependently.(ABSTRACT TRUNCATED AT 250 WORDS)     

Structure-activity relationships of alkylxanthines: alkyl chain elongation at the N1- or N7-position decreases cardiotonic activity in the isolated guinea pig heart

Relationships between the alkyl substitutions (C1-C6) and cardiac inotropic activities of xanthine derivatives were studied in isolated guinea pig heart muscles. Most of the alkylxanthines exhibited positive inotropic activity on the left atrium, which was increased with an elongation of alkyl chain at the N3-position but decreased by substitution of a long alkyl group at the N1- or N7-position of the xanthine skeleton. Although positive inotropic activity in the right ventricular papillary muscle was also increased by longer alkyl groups at the N3-position, the inotropic activity became negative with an increment in alkyl chain length at the N1- or N7-position. The positive inotropic activity of alkylxanthines was correlated with their inhibitory activity on the phosphodiesterase (PDE) III isoenzyme. Adenosine A1 antagonism and PDE IV inhibitory activity were also partly associated with the inotropic activity because H-89, an inhibitor of cyclic AMP-dependent protein kinase, diminished the positive inotropic action and potentiated the negative inotropic action. These results indicate that the positive inotropic activity of alkylxanthines becomes weak with elongation of alkyl chains at the N1- and N7-positions; In particular, xanthines having two long alkyl chains show a negative inotropic activity on the right ventricular papillary muscle, an effect that could not be elucidated from their cyclic AMP-dependent action.     

Prediction of spectral reflectance factor distribution of automotive paint finishes

It is necessary to determine the accurate reflectance of painted surfaces for the review of paint finishes by computer graphics (CG) before actual painting of the exterior color of automobiles, and for quality control during production and inspection processes. We have optimized a method for measuring reflectance by using a statistical technique. We have found that the reflectance of a painted surface is best measured at an incident angle of 60° and at five aspecular angles of 10°, 18°, 28°, 40°, and 90°. Our method makes it possible to accurately reproduce reflection characteristics of paint finishes containing special flake pigments, such as pearl mica. Also it was proved that our method can apply not only to solid and metallic coatings but to all painted surfaces. © 2005 Wiley Periodicals, Inc. Col Res Appl, 30, 275–282, 2005; Published online in Wiley InterScience (www.interscience.wiley.com). DOI 10.1002/col.20125     

The effects of R-75,317 on antiglomerular basement membrane glomerulonephritis in rats

Platelet-activating factor (PAF) is a potent inflammatory mediator which is released by various inflammatory cells and produced by certain tissues, including the kidney. PAF has been shown to increase glomerular permeability to protein and to decrease glomerular filtration rate (GFR) by contracting mesangium. On the basis of these observations, it has been suspected that PAF may play a role as mediator of glomerular damage in glomerular nephritis. To examine this possibility, we studied the effects of a specific PAF antagonist, R-75,317, on the development of an experimental model of anti-glomerular basement membrane (anti-GBM) glomerulonephritis. Glomerulonephritis was initiated by injecting rabbit anti-rat GBM serum into rats. Proteinuria gradually developed after serum injection, plateaued at week 2, and remained at the high level of week 2 throughout the experimental period (6 wk). Chronic treatment with R-75,317 (10 mg/kg/day i.p.) tended to delay the onset of proteinuria and significantly accelerated the recovery phase. Creatinine clearance (Ccr) fell to 40% at week 3. R-75,317 treatment completely prevented this decline of Ccr. Histological changes in this model (glomerular hypertrophy, proliferation of mesangial matrix and interstitial fibrosis) were also ameliorated by the R-75,317 treatment. The results suggest that PAF may play a role in the development of glomerulonephritis and that PAF antagonists could be used in the treatment of human renal disease. Based on a paper presented at the Third International Conference on Platelet-Activating Factor and Structurally Related Alkyl Ether Lipids, May 1989.     

Efficacy of morantel tartrate in a sustained release bolus on the control of subclinical gastrointestinal parasitism in first-year grazing dairy replacements

Thirty-four heifers (24 Holstein, 8 Ayrshire, 2 Jersey) and 12 Holstein steer calves were grouped into 23 blocks of 2 animals each according to breed, sex, and body weight. Animals in each block were randomly assigned to control or treated groups. The treated group received an anthelmintic bolus containing morantel tartrate before they were permitted access to pasture. A 2.6 ha pasture was divided in half with a double fence; the resulting two pastures had separate feed and water troughs. Steer calves were slaughtered upon termination of the trial to ascertain gastrointestinal parasite burdens. Two worm-free tracer calves were placed on each pasture every 2 mo and slaughtered after 4 wk of grazing to determine parasite infectivity of pastures. Herbage samples were obtained monthly and analyzed for infective larvae. The trial was conducted for 141 d during the grazing season. Treatment resulted in 90% reduction in infective larvae on pasture, 74% reduction in fecal worm-eggs, 91% reduction in adult worm burdens, and a trend toward reduced worm burdens in tracer calves by 52%. An overall average daily gain of .68 and .88 kg was obtained for control and treated animals. Reproductive data for the heifers remaining in the herd from the trial showed that treatment resulted in 44 less days to first breeding.     

Application of SiC-Si functionally gradient material to thermoelectric energy conversion device

Because of its high–temperature chemical stability, SiC ceramic is a promising material for high-temperature device applications such as thermoelectric energy converters. However, the electrical conductivity of SiC ceramic is too low for it to be used as a thermoelectric energy converter at the cold junction. Therefore, we propose a SiC-Si functionally gradient material (FGM) in order to improve the electrical conductivity of the SiC ceramic at the cold junction. An SiC rod was fired in a temperature gradient furnace. One end of the SiC rod was maintained at 2473 K and the other end was maintained at 1973 K for 30 min. After firing, the porous SiC edge fired at 1973 K was dipped into molten Si in order to infiltrate molten Si into the porous SiC. The microstructure of the FGM is classified into three regions: the SiC-Si composite material; the porous SiC ceramic; and the densified SiC ceramic. The electrical conductivity, the Seebeck coefficient and the thermal conductivity for each region of SiC-Si FGM was measured at 300 K; a figure of merit was calculated. The figure of merit of the SiC-Si FGM at the cold junction, at room temperature, was 10⁸ times higher than that of a nongradient SiC ceramic.     

Gas chromatographic separation of wax esters based on the degree of unsaturation

The wax esters of sperm whale head oil have been characterized by gas-liquid chromatography on an APOLAR 10C column according to their carbon number and number of double bonds. The novel technique permits the direct quantitative analysis of saturated and unsaturated wax esters.     

Antioxidant for fats and oils from canary seed: Sterol and triterpene alcohol esters of caffeic acid

Several kinds of seeds used as bird feed were extracted successively with hexane, ether and methanol. In the antioxidant test with extracts, the ether extract from canary seeds showed the highest activity. The antioxidant fraction separated from it by thin layer chromatography showed excellent activity for lard and sardine oil. The effective components were identified by gas chromatography and gas chromatography-mass spectrometry of the hydrolyzed products as the esters of caffeic acid with cycloartenol, gramisterol, sitosterol and campesterol with the minor amounts of 24-methylenecycloartanol, obtusifoliol, brassicasterol and Δ7-stigmastenol.     

Ring-opening polymerization of 2-oxazolines initiated by chloromethyl groups introduced onto carbon black surface

Summary The ring-opening polymerization of 2-oxazolines (OXZs) was found to be initiated by chloromethyl groups introduced onto carbon black surface. The introduction of chloromethyl groups onto the surface was achieved by the reaction of carbon black with 3,3-bischloromethylbenzoyl peroxide in carbon tetrachloride. During the polymerization, poly-OXZs were grafted from carbon black based on the propagation of the polymers from the surface: percentage of grafting increased with an increase of conversion and reached 40–60%. The polymerization was accelerated by the addition of potassium iodide. Poly-OXZ-grafted carbon black produced stable colloidal dispersions in both hydrophobic and hydrophilic solvents.