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.     

Oxidation of synthetic triacylglycerols containing eicosapentaenoic and docosahexaenoic acids: Effect of oxidation system and triacylglycerol structure

Thirteen synthetic triacylglycerols (TAG) containing eicosapentaenoic acid (EPA) or docosahexaenoic acid (DHA) were oxidized in the presence of 2,2′-azobis(2,4-dimethyl-valeronitrile) (AMVN) and 2,2′-azobis(2-amidinopropane)dihydrochloride (AAPH) as aqueous and nonaqueous radical initiators to investigate the influence of TAG structure and oxidation system on the oxidative stability of TAG that contain highly unsaturated fatty acids (HUFA). A 2:1 (mol/mol) mixture of trieicosapentaenoylglycerol and tripalmitoylglycerol was most susceptible to the AMVN-initiated oxidation among three types of TAG that contained EPA and palmitic acid (2:1, mol/mol). Compared with 1,2 (or 2,3)-dieicosapentaenoyl-3(or 1)-palmitoylglycerol (EEP) and 1,3-dieicosapentaenoyl-2-palmitoylglycerol (EPE), the oxidative rate of EEP was somewhat higher. A similar result was obtained for DHA-containing TAG. The oxidative rate of TAG that contained EPA and palmitic acid (1:2, mol/mol) showed a positive correlation with the amount of EPA in a single TAG molecule. Moreover, in the nonaqueous system, the oxidative rate of EPA-containing TAG was affected by unsaturation and carbon chainlength of constituent fatty acids. In the AAPH-initiated oxidation in the aqueous system, the oxidative rate of TAG with EPA and palmitic acid was higher with the increased quantity of EPA in a single TAG molecule. Also, constituent fatty acids modified the oxidative rate of EPA-containing TAG in an aqueous system. The glycerol position of EPA and DHA also affected the oxidative rate of the TAG. EPA and DHA located at the 1,2 (or 2,3)-position of glycerol were more oxidizable than those at the 1,3-position during AAPH-initiated oxidation. Thus, 1,2(or2,3)-dipalmitoyl-3(or 1)-eicosapentaenoylglycerol was oxidized faster than 1,3-dipalmitoyl-2-eicosapentaenoylglycerol. These observations suggest that the oxidative stability of TAG that contain HUFA could be modulated by the oxidation system and TAG structure.     

Application of full-factorial design for optimization of the moisture determination in wheat flour using infrared scales

We studied the parameters that may affect the analysis of the moisture content in wheat flour using infrared scales. The parameters were studied by one-factor at a time methodology and then, by full-factorial design (2³). The best condition using infrared scales occurred at 120 °C, with a sample weight of 1.5 g and an exposure time to infrared radiation of 6 min. We observed the interaction effect between the three factors studied. The analysis time was 60 times lower than classical method. The optimized method for determination of the moisture content in wheat flour using infrared scales was validated to range between 9 and 17 %.     

Determination of captafol,cyhexatin, 1-naphthylacetic acid and quintozene in apple,Japanese pear and melon by simultaneous extraction

A simple and rapid method is described for the determination of the non-registered pesticides, captafol, quintozene (PCNB), cyhexatin and 1-naphthylacetic acid (NAA), in fruits. These pesticides were extracted with acidified acetone, then captafol and PCNB were purified with a Florisil mini column and analyzed by GC-ECD. Cyhexatin was ethylated with ethylmagnesium bromide, and the ethyl derivative was analyzed by GC-FPD (Sn filter). NAA was purified with liquid-liquid extraction and determined by HPLC equipped with a fluorescence detector. These analytes were identified with GC/MS or LC/MS. The minimum identified concentration of the pesticides was below 0.2 ng per injection, which corresponds to a detection limit of below 0.02 microgram/g in the original samples. Recoveries of the pesticides spiked at 0.1 microgram/g into apple, Japanese pear and melon were greater than 61%.     

A method of creating new valency entries

Information on subcategorization and selectional restrictions in a valency dictionary is important for natural language processing tasks such as monolingual parsing, accurate rule-based machine translation and automatic summarization. In this paper we present an efficient method of assigning valency information and selectional restrictions to entries in a bilingual dictionary, based on information in an existing valency dictionary. The method is based on two assumptions: words with similar meaning have similar subcategorization frames and selectional restrictions; and words with the same translations have similar meanings. Based on these assumptions, new valency entries are constructed for words in a plain bilingual dictionary, using entries with similar source-language meaning and the same target-language translations. We evaluate the effects of various measures of semantic similarity.     

Study on sustainable redevelopment of a densely built-up area in Tokyo by introducing a distributed local energy supply system

“Distributed local energy systems” had been expected to rationalize the supply of energy to built-up areas, but until now very little research has been performed to estimate the effect of their application to actual cities. In this research, therefore, a future vision for the year 2030 in the Sancha Area (SANCHA VISION 2030), a typical densely built-up area in Tokyo, has been elaborated including a simulation to estimate benefits from the application of distributed energy systems in terms of reduced energy consumption and CO₂ emissions as well as mitigation of the heat-island phenomenon. As a result, it was demonstrated that a “distributed local energy system”, which provides a district with both electrical power and heat through an integrated distribution system, may contribute to a considerable improvement in energy efficiency for those areas. In addition, it may also provide other benefits, including enhancement of living amenity and urban security in times of emergency.     

Detection of moving object by mobile stereo omnidirectional system (SOS)

Moving object detection with a mobile image sensor is an important task in robotics and computer vision, when considering the practical use of robotics in human environments. In this paper, we propose a robust method that detects moving objects in the environment using the omnidirectional depth information obtained by a mobile Stereo Omnidirectional System (SOS). In order to detect only the moving objects within the depth image that are obtained by a sensor in motion, we first estimate the ego‐motion of the sensor, and generate a predicted depth image for the current time from the depth obtained at the previous time by only considering the ego‐motion of the sensor. Then the predicted depth image is compared with the actual one obtained at the current time, and the inconsistent regions are detected as moving objects. When the sensor moves, occlusions will occur in the scene and they will cause false detections. However, these false detections can be suppressed by estimating the occlusion regions using the ego‐motion parameters of the sensor and the jump edges in the depth image. The effectiveness of the method is shown with experimental results for a real environment. © 2005 Wiley Periodicals, Inc. Electr Eng Jpn, 152(3): 29–38, 2005; Published online in Wiley InterScience ( www.interscience. wiley.com ). DOI 10.1002/eej.20155     

Cloning and characterization of a 4-nitrophenol hydroxylase gene cluster from Rhodococcus sp. PN1

A 4-nitrophenol (4-NP)-degrading bacterium was isolated from activated sludge and identified as a Rhodococcus sp. This bacterium, designated as strain PN1, could utilize 4-NP as a sole carbon, nitrogen and energy source. Degradation tests of 4-NP using cell suspensions of strain PN1 revealed that the degradation was induced by 4-NP and that 4-nitrocatechol (4-NC) was one of the metabolites. A gene library was constructed from the total DNA of strain PN1 and introduced into Rhodococcus rhodochrous ATCC 12674. Two recombinant strains showed 4-NP hydroxylase activity, and a 9.1-kb DNA fragment encoding the activity was isolated from one of the strains. In addition, a 2.4-kb smaller fragment expressing the activity was subcloned from the 9.1-kb fragment and sequenced. The sequence analysis showed that the fragment encodes a two-component 4-NP hydroxylase, the predicted amino acid sequence of which exhibits significant similarity to those of phenol hydroxylases and 4-hydroxyphenylacetate 3-hydroxylases belonging to the two-component flavin diffusible monooxygenase (TC-FDM) family proposed by Galán et al. (J. Bacteriol., 182, 627-636, 2000).