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.     

Humidity Sensor Characteristics of Woodceramics

The humidity sensor characteristics of Woodceramics were investigated. The Woodceramics used in this experiment were prepared at 650–900°C. The size of specimens selected was 1 × 1 × 10 mm . One was used as-cut and the other was polished. Above 700°C, the resistance of the specimen was below 50 and the decrease of resistance with increasing relative humidity was small. The specimen prepared at 650°C had a resistance of about 1 k. The resistance of as-cut specimens decreased with increase in relative humidity, but that of the polished specimen did not change significantly. The difference between as-cut and polished samples was explained by the differences in surface micro-structure.     

High oleic acid oil suppresses lung tumorigenesis in mice through the modulation of extracellular signal-regulated kinase cascade

This study was undertaken to estimate the effect of dietary high oleic acid oil (OA) on 4-(methylnitrosamino)-1-(3-pyridyl)-1-butanone (NNK)-induced lung tumorigenesis in mice. Diet containing 10% oil was fed to mice through experimental periods. On day 30 after NNK injection (100 mg/kg body weight, i.p.), the treatment increased the level of prostaglandin E₂ (PGE₂) as well as proliferating cell nuclear antigen, a marker of cell proliferation in a high linoleic acid oil (LA)-fed group but not in an OA-fed group. The NNK treatment also induced the activation of an extracellular signal-regulated kinase (Erk) cascade (Erk, Mek and Raf-1) in an LA-fed group. On the other hand, OA feeding abolished the NNK-induced activation of the Erk cascade. In conjugation with these events, OA feeding reduced lung tumor incidence and tumor multiplicity (percentage of mice with tumors) in mice compared with LA feeding at the 20th experimental week. These results suggest that OA suppresses lung tumorigenesis and that this suppression is correlated with the inhibition of PGE₂ production and inactivation of the Erk cascade.     

Combustion Characteristics of High Burn Rate Azide Polymer Propellant

The combustion characteristics of high burn rate azide polymer composite propellant were examined by using a chimney type strand burner, a Ø 80 mm × 140 mm small rocket motor and a L/D = 16 of Ø 70 mm heavy-wall rocket motor. The propellant, BAMO/NMMO copolymer was used as a fuel binder and AP as an oxidizer, burned approximately 29 mm/s at a pressure range of 7 MPa to 20 MPa with a plateau-mesa burning behavior. However, the pressure exponent rapidly increased at above the pressure of 20 MPa and was 0.52 between 20 MPa and 25 MPa. The low pressure exponent and high burn rate of the azide polymer propellant are suitable to the short burn time at the maximum expected operating pressure range of 15 MPa to 20 MPa. The high L/D heavywall rocket motor with volumeric mass fraction of 83% showed stable combustion without any pressure oscillation and severe erosive burning. The average burn rate in the high L/D motor was 10% larger than that estimated from the strand data. The theoretically calculated pressure-vs-time and thrust-vs-time curves were well consistent with the measured data. α = 20 and β = 180 for the Lenoir-Robillard equation were used to estimate the burn rate.     

Detection of aluminium by energy dispersive X-ray microanalysis at high accelerating voltages with semi-thin sections of biological sample

Aluminium (Al) was detected in semi-thin sections of three organs, the duodenum, liver and kidney, of ddY strain mouse by energy dispersive X-ray microanalysis at high accelerating voltages around 300 kV. Firstly, to determine the conditions best for detecting Al, several adult ddY mice were injected intraperitoneally with aluminium chloride (AlCl3) and the duodenums were fixed, embedded and sectioned at various thicknesses and subjected to energy dispersive X-ray microanalysis at various accelerating voltages from 100 to 400 kV. From the results obtained, 1.0 microm-thick sections observed at 300 kV resulted in the highest peak-counts/background ratios and were shown to be the most suitable for X-ray microanalysis. Secondly, ddY mice aged four weeks were administered orally with 2% AlCl3 at pH 2.5 for two weeks and the three organs (duodenum, liver and kidney) were subjected to X-ray microanalysis under the same condition found above. The results were compared with light microscopic Al staining of the same tissues. Aluminium was detected in lysosomes of the three kinds of tissues with higher sensitivity by energy dispersive X-ray microanalysis by light microscopic observation. From the results, it was suggested that Al dissolved in acidic water was absorbed in the duodenum and accumulated in the liver and kidney.     

Superhydrophobic/superhydrophilic micropatterning on a carbon nanotube film using a laser plasma-type hyperthermal atom beam facility

Superhydrophobic/superhydrophilic micropatterning on a carbon nanotube (CNT) film has been achieved using a laser plasma-type hyperthermal atom beam facility, which produces a small amount of damage and generates a highly anisotropic beam. Fluorination and oxidation on CNT films by exposure to fluorine-atom and oxygen-atom beams caused superhydrophobic and superhydrophilic surfaces, respectively, while maintaining the as-grown fibrous forms of the CNT films. Micropatterned oxidation on CNT films without using photoresists created superhydrophilic microdots and microchannels.     

Friction Properties of Carbon Nano-Onions from Experiment and Computer Simulations

The carbon nano-onion can be considered as a new kind of interesting lubricating nanoparticle. Used as lubricant additives, carbon nano-onions lead to a strong reduction of both friction and wear, even at low temperature. To better elucidate the mechanisms by which these processes occur, coupled experimental and computational investigations are carried out. In addition, it is found that lubricious iron oxide nanoparticles are generated in the core of the steel contact through mechanisms that are not yet known. The molecular dynamics simulations of carbon onions placed between sliding diamond-like carbon surfaces at high contact pressure indicate that the lubrication mechanism of the onions is based on a coupled process of rolling and sliding inside the contact area. We conclude that most of carbon onions seem to remain intact under friction processes and do not generate graphitic planes, which is in contrast to the previously determined behavior of MoS₂ fullerenes that are mainly exfoliated inside the contact area and liberate lubricating lamellar sheets of h-MoS₂.     

Effect of Oxygen Adsorption on Adhesion of W to Au Studied by Field Ion Microscopy

A field ion microscope has been used to investigate the influence of oxygen adsorption on adhesion of W to Au. An adhesion contact in ultrahigh vacuum of the field ion microscope was carried out using a W tip either with or without oxygen adsorption. It was found that adhesion force decreased with increasing oxygen exposures up to 60 Langmuirs (L). With an oxygen exposure of 16 L, an intermediate adhesion resulted. Adhesion is thus dependent upon the coverage of oxygen. The depth of adhesion-induced lattice defects was studied using the field evaporation technique. Over 200 L, adhesion force was not detectable, nor was distortion of W atoms.     

Evaluation of amorphous ursodeoxycholic acid by thermal methods

PURPOSE: The purpose of this study was to characterize the amorphous state of ursodeoxycholic acid (UDCA) samples by using isothermal microcalorimetry, X-ray diffraction, infrared (IR) spectroscopy and solid state carbon 13 nuclear magnetic resonance (13C-NMR) spectroscopy, and to demonstrate the application of the thermal methods (microcalorimetry and differential scanning calorimetry (DSC) for studying the amorphous state and clarifying the dissolution mechanism of UDCA. METHODS: Amorphous UDCA was prepared by grinding and rapid cooling of the melts. The heat of solution of UDCA was measured by an isothermal heat-conduction twin microcalorimeter at 25.0 degrees C. Some physicochemical properties of amorphous UDCA were also studied. RESULTS: The intensities of X-ray diffraction peaks of crystalline UDCA decreased with an increase in grinding time. The heat levels of solution of crystalline UDCA and UDCA ground for 1 min were endothermic, and became exothermic with an increase in grinding time. A good correlation was obtained between the heat of solution and the heat of crystallization determined from the peak area in DSC. Although no significant difference was observed in X-ray diffraction patterns of amorphous UDCA prepared by the two methods, significant differences were recognized in DSC, IR and 13C-NMR, and the heat of solution indicated different values among the two samples. The stability of amorphous UDCA samples stored under 74.5% relative humidity at 40 degrees C was found to depend upon the preparation methods. CONCLUSIONS: Different states of amorphous UDCA were obtained depending on the preparation method. The application of thermal methods to evaluate the amorphous state was demonstrated. The mechanism of dissolution of UDCA was discussed from the results of the heat of solution examination.