A new metabolite of caffeine in the urine of the horse, rabbit, rat, and mouse was isolated and identified as α-[7-(1, 3-dimethylxanthinyl)] methyl methyl sulfoxide (II). Other two new metabolites were isolated from the urine of the mouse administered caffeine andidentified as α-[7-(1, 3-dimethylxanthinyl)] methyl methyl sulfide (I) and α-[7-(1, 3-dimethylxanthinyl)] methyl methyl sulfone (III), respectively. The structural elucidation of these metabolites is described.

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Propagation of waves in a medium homogeneous in space but with time-varying properties is considered. It is shown that this can result in compression of a signal and a gain in power. The signal becomes also frequency modulated. For nondispersive waves, such as acoustic waves, there is an increase in frequency, whereas for transverse electromagnetic waves the frequency is lowered for the particular scheme of propagation considered.

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Circadian variations in catecholamines (CA) in the Thoroughbred horse were investigated by determining plasma adrenaline (Ad) and noradrenaline (NA) concentrations every 2 hr by high-performance liquid chromatography with an electrochemical detector (HPLC-ED). The HPLC-ED method in the present study was sufficient for determining plasma CA concentrations. The elution of CA from alumina with a mixture of acetic acid and methanol (1:50, v/v) gave a good recovery. The detection limit for both Ad and NA was 10 pg/ml. A significant variation during the 24 hr was observed for plasma NA concentrations (P<0.01), but not for plasma Ad concentrations. From 14:00 hr to 18:00 hr, plasma NA concentrations were significantly higher than those observed from 02:00 hr to 04:00 hr (P<0.01). As a result of the cosinor analysis for individuals, a circadian rhythm of plasma concentrations of Ad and NA was demonstrated (mean ± SE, 26.3 ± . pg/ml and 66.3 ± 3.8 pg/ml; rhythm amplitude, 9.4 ± 1.4 pg/ml and 12.7 ± 1.2 pg/ml; time of trough, 02:34 hr: min ± 9.7 min and 02:54 hr: min ± 33 min for Ad and NA, respectively). The 6 hr continuous tie-stall-type restraint decreased plasma concentrations of Ad and NA and delayed their peaks by 4 hr and 2 hr, respectively. There was a significant correlation (n=48, r=0.562, P<0.001) between the circadian variations in plasma Ad and NA. In conclusion, it was found that circadian variations in plasma CA in the Thoroughbred horse were similar to those in humans. In addition, the present study suggests that the sustained stress may influence circadian variations in plasma CA.

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メチルキシレノールブルー(MXB)はアルミニウムまたはベリリウムと反応して,赤紫色または赤色の水溶栓錯体を生成する。各呈色溶液はそれぞれ,pH 2 2～2 5,波長578～583 nmおよびpH 5 9～6．5,波長513～517nmにおいて一定最大の吸光度を示す。検量線はアルミニウム濃度8～35μ9／25mlの範囲で,またベリリウムの場合は10μ9！25 mlまで直線性を示し,吸光度0．001に対する感度はアルミニウム濃度20μ9／25mzにおいて。 oo16μ9／cm2であり ベリリウムの場合は,ooo8 lzglcmsである。また,アルミニウム錯体およびベリリウム錯体の組成比をそれぞれpH 2．4およびpH 6．0で検討した結果,いずれめ場合も1：1と推定された。共存イオンについては,アルミニウムの定量に対し,ガリウム塾インジウム,ビスス(III),スカンジウム,トリウム,フヅ化物イオン,シュウ酸イオンが妨害し,ベリリウムの定量に対し,アルミニウム,トリウム,クロム(III),フッ化物イオンが妨害する。なお,アルミニウムとベリリウムを同時に含む溶液について,おのおのを逐次定量する方法を検討した。

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The 4′-O-glucosides of 2′,,′,′-tetrahydroxychalcone (THC) and 2′,3,,′,′-pentahydroxychalcone (PHC) are present in the yellow snapdragon (Antirrhinum majus) flowers and serve as direct precursors for the synthesis of aurones, the yellow pigments of the flowers. Despite the metabolic significance of these chalcones in aurone biosynthesis, the biochemical properties of chalcone synthase (CHS), the enzyme responsible for their synthesis, remains to be clarified. In this study, one known CHS cDNA (niv, also termed AmCHS1) and one CHS-related cDNA, AmCHS2, were isolated from yellow snapdragon buds. AmCHS1 mRNA specifically accumulated in the petals in a coloration-dependent manner, whereas AmCHS2 mRNA accumulated only negligibly in petals and other organs, corroborating the importance of AmCHS1 in chalcone synthesis in the yellow flower. Recombinant AmCHS1 that was heterologously expressed in Escherichia coli cells efficiently utilized both p-coumaroyl-CoA and caffeoyl-CoA (relative activity, 50% of the activity for p-coumaroyl-CoA) as a starting ester to produce THC and PHC, respectively. Previous studies predicted that a single Thr197Ala or the double Val196Met/Thr197Ala substitution in AmCHS1 may provide a wider space for hydroxycinnamoyl-group binding and might enhance the ability of this enzyme to produce PHC [Austin MB, Noel JP (2003) Nat Prod Rep 20: 79–110]. However, these substitutions led to a decreased PHC-producing activity, implying that other factors may also be important for the efficient utilization of caffeoyl-CoA.

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The easy and quick determination method of aldehydes as hazardous air pollutants in indoor air by use of a passive tube packed with silica gel coated with O-(2, 3, , 5, -pentafluorobenzyl) hydroxylamine (PFBOA) was investigated. The analytical procedure consists of the following 3 steps : concentration and derivatization of aldehydes in sample air by the passive tube, desorption of PFBOA-derivatives of aldehydes from an adsorbent with cyclohexane and determination of PFBOA-derivatives of aldehydes by GC-MS analysis. The diffusive uptake rates of aldehydes were calculated using the obtained data from both active and passive tube methods applied to some newly-built ferroconcrete uninhabited houses and single family houses. The rates of formaldehyde and acetaldehyde were 1.983±0.254ml/min (n=25, R.S.D. 12.8%) and 1.690±0.373ml/min (n=24, R.S.D. 22.0%), respectively. The detection limit of formaldehyde in indoor air by the passive tube method was 0.0156mg/m³ for 24h air sampling, and that of acetaldehyde was 0.0382mg/m³. The PFBOA passive tube method was applied to the determination of aldehydes in newly-built ferroconcrete uninhabited houses, and sufficient results were obtained.

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Cyclic adenosine monophosphate (cAMP) phosphodiesterase inhibitors present in Picrasma quassioides BENN. were identified as 1-methoxycarbonyl-β-carboline, 4, 5-dimethoxycanthin-6-one and 5-hydroxy--methoxycanthin--one. The structure-inhibitory activity relationships were studied in 31 derivatives of β-carboline, 2 dimeric derivatives of β-carboline and 12 derivatives of canthin-6-one. β-Carboline derivatives with a methoxycarbonyl group and canthin-6-one derivatives with a methoxyl group generally had a strong inhibitory effect on cAMP phosphodiesterase.

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In the presence of a nickel phosphine complex, the coupling reaction of Grignard reagents with chloropyrimidines such as 2-chloro-, -dimethyl-(III), 4-chloro-2, 6-dimethyl-(V), , -dichloro-2-methyl-(VIII), 2, -dichloro--methyl-(X), and 2, , -trichloro-pyrimidine (XIII) was studied to give the corresponding alkyl (or arkyl) substituted pyrimidines in yields ranging from 40 to 88%. Although in the cases of VIII, X, and XIII, the selectivity on the reaction due to the position of the chloride atom was not observed, this coupling was concluded to remove the defects of the Pinner reaction for the synthesis of polyalkyl (or polyaryl) pyrimidines.

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KL-6とSP-Dは共に，間質性肺炎に対する鋭敏な血清マーカーとして，診断や病勢把握，さらには予後予測因子として実地臨床にて頻用されている．一方，膠原病には高頻度に間質性肺炎が合併し，その臨床経過や予後を左右する重要な病態であると理解されている．血清KL-6やSP-Dを測定することにより，膠原病患者における間質性肺炎の合併をいち早く検出できる可能性があり，また，膠原病関連間質性肺炎と診断された場合には，これらのマーカーはその病勢を見る指標としても使用しうるものと期待される．ただし，測定値を解釈する際には，KL-6，SP-Dの生物学的特性と，その測定値が保持する有用性と問題点をしっかり把握しておく必要がある．

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は斜方晶系に属し，層状構造をもつ。は光触媒特性をもつ物質として知られている。これまでに，固相反応法，チョクラルスキー法，水熱合成法あるいはK₂CO₃フラックス法により，結晶は育成されている。環境調和を目指し，本研究では天然に豊富に存在する塩化物(KClなど)をフラックスとして用いた蒸発法や徐冷法にて，結晶を育成した。生成した結晶は無色透明の薄板状であった。生成する結晶相は，溶質濃度に依存することがわかった。

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From the fronds of Macrothelypteris torresiana CHING var. calvata HOLTT. (=M. oligophlebia CHING), two new coumarins were isolated together with maltol, maltol 3-O-β-D-glucoside, kaempferol, rutin and kaempferol 3-O-β-rutinoside. The structures of the new compounds were established as 7-hydroxy--isopropyl--methylcoumarin (I) and 7-hydroxy-4-isopropyl-3-methoxy-6-methylcoumarin (II) by the chemical and spectroscopic methods.

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Dephosphorylation of dihydroneopterin triphosphate (I) formed from GTP by GTP cyclohydrolase has remained as an unknown step in dihydrofolate (II) biosynthesis. The present author and Brown have found in Escherichia coli at least two hydrolytic enzymes : one, named as dihydroneopterin triphosphate pyrophosphohydrolase, catalyzes the removal of PPi specifically from (I) to give dihydroneopterin monophosphate (III) as the product, and the other catalyzes the hydrolysis of (III) to dihydroneopterin (IV). 2-Amino--hydroxy--carboxydihydropteridine (V), but not 2-amino--hydroxy--carboxypteridine (VI), inhibits enzymatic synthesis of (II) from GMP by specific attacking an enzyme reaction catalyzed by 2-amino--hydroxy--hydroxymethyldihydropteridine (VII) pyrophosphokinase. Also, (V) inhibits growth of E. coli, while (VI) does not affect the growth, demonstrating that (V) blocks the growth by antagonizing utilization of (VII) for (II) synthesis. The growth inhibition is reversed by 2-amino--hydroxy--formyldihydropteridine (VIII). But, when (V) is absent, (VIII) blocks the growth with an inhibitory power about equal to (V). The mechanism whereby this contradictory effect of (VIII) on the growth happens, and the biological significance of this phenomenon has been explored by following metabolism of (VIII) and 2-amino--hydroxy--formylpteridine (IX). Three possible directions of (IX) metabolism in vivo are estimated by testing the inhibitory powers on xanthine oxidase of various pteridines related to (IX) in their structures : the 1st conversion is to (VI), the 2nd to 2-amino--hydroxy--hydroxymethylpteridine (X), and the 3rd to (VIII). The most potent inhibitory action of (IX) is extremely reduced by these conversion, which are found in E. coli. Dihydropteroate (XI), a precursor of (II), is enzymatically formed from (VIII) and (IX) via (VII), since these transformations are inhibited strongly by (V). The enzymatic conversion of (VIII) to (VII) is catalyzed by a specific reductase dependent on NADPH, and the conversion of (IX) to (VIII) requires FAD and NADH as the cofactors. The transformation of (IX) to (VII) via (X) is not plausible, since the enzyme system is not found to reduce the pyrazine ring of (X). (VI) is produced from (IX) by a NAD^+-specific aldhyde dehydrogenase, but not by xanthine oxidase. The synthetic pathway of (II) from (IX) via (VIII) is characterized as a "salvage route" for formation of (II), which could function dominantly under reduction of folate coenzymes levels by blockage of the main biosynthetic pathway from GTP, resulting in reversal by (VIII) of E. coli growth inhibition produced by (V). Mathis and Brown (1970) have found the strong inhibition by (VIII) of dihydroneopterin aldolase in the biosynthetic pathway of (II). If (VIII) is produced as the catabolic product from the folate coenzymes, this inhibition may have a nature of "feed-back inhibition", whereby the physiological levels of folate coenzymes could be maintained in the cells, and excess addition of (VIII) results in inhibition of E. coli growth.

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This study was performed to clarify which factors affected damage to tame-ike (small embankment dams for irrigation) in Hokudan Town as a result of the January 17, 1995 Hyogoken-Nambu earthquake. Factors were assumed to be : Location (e.g., Distance to Epicenter, etc.), Structure (e.g., Angle to Nearest Fault, Embankment Volume, etc.), Soil Properties of Embankment, Geology of Dam Site and History (Era of Construction, Repaired, etc.). Multivariate statistical analyses were performed for documentary data (damaged : 181, undamaged : 328). Ordinary statistical analyses were conducted for the data investigated in situ for soil properties of the embankment. The results show that the factors causing damage to dam are : (1) Nearest Fault (Nojima, Mizukoshi and D2), (2) Distance to Nearest Fault (less than 500 m), (3) Distance to Epicenter (approximately 8 to 14 km, which almost agrees with the location of seismic intensity 7 JMA), (4) Elevation of Dam Site (higher than 100 m), (5) Embankment Volume (the greater the volume the more damage was caused), (6) Direction of Dam Axis (normal or diagonal to the epicenter or to nearest the fault), (7) Plan View of Dam Axis (3 or 4 axes), (8) Surface Geology of Dam Site (non-cohesive soil type ground), (9) Era of Construction (prior to 1891) and (10) Soil Properties of Embankment (sand, not silty sand or gravel, penetration resistance that is 10% smaller than the undamaged dams).

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This paper describes the results of two instrumented axial loading tests on large scale model stone columns, constructed similarly to the prototypes with a technique which employs ordinary pile driving equipment. Kaolin was used to simulate natural soil conditions. Pressure cells and electric piezometers were used to monitor lateral stresses and pore pressures respectively, during loading. A factual report of the data and a direct evaluation with respect to the load-deformation response and the mode of failure of the stone columns is provided. Two deformation models are examined : a triaxial specimen expanding laterally under compression and a skin friction pile. Furthermore, a trilinear load-settlement relation is proposed for design purposes, based directly upon the results of the model tests.

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The Prins reaction of alloocimene with formaldehyde proceeded smoothly in dichloromethane under reflux in the presence of acetic acid. The reaction products were mainly 2- (2- methy1-1-propeny1)-4, 5-dimethyl-5, 6-dihydro-2 H-pyran [2] and trans- or cis-4, 5-dimethy1-5- (4-methyl-1, 3-pentadienyl)-1, 3-dioxan, [3] or [4]. The stereochemistry of the dioxans, [3] and [4], was also discussed on the basis of the NMR spectra. The compositions of the products were dependent on the isomer ratio of alloocimene used.

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For the construction of new combinatorial libraries, a lead compound was created by replacing the core structure of a hit compound discovered by screening for cytotoxic agents against a tumorigenic cell line. The newly designed compound maintained biological activity and allowed alternative library construction for antitumor drugs.

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Two unusual flavones, 5, 5'-dihydroxy-2', 3', 6', 7-tetramethoxyflavone (1) from Gardenia cramerii and 4', 5-dihydroxy-3', 5', 6, 7-tetramethoxyflavone (6) from Artemisia mesatlantia, and their position isomers were synthesized to investigate the structural correlation in terms of spectral data. The structure of the flavone from G. cramerii is discussed.

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2,4-ジアミノ-6-ビニル-s-トリアジン (VT) とイソシアヌール酸の分子間化合物を合成し, エポキシドとの反応性についてIRスペクトルを用いて研究した. 分子間化合物とビスフェノールAのジグリシジルエーテル (DGEBA) を150℃に加熱すると, エポキシドはVTのアミノ基及びイソシアヌール酸と反応した. エポキシドに基づく吸収の消失はVTとDGEBAの場合より速く, イミダゾール化合物を加えると一層速くなる. 硬化物中ではイソシアヌール酸はエポキシドと反応してイソシアヌラート及びオキサゾリドン化合物の形で存在することがIRスペクトルから推定された. 2,4-ジアミノ-6-エチル-s-トリアジンとイソシアヌール酸の分子間化合物はVTの分子間化合物と同様にエポキシドと反応するが, メラミンの分子間化合物ではエポキシドとイソシアヌール酸の反応はほとんど見られなかった.

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