巻号一覧
26 巻, 11 号
選択された号の論文の55件中1～50を表示しています
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亀山 勉, 鵜飼 良, 鍋島 俊隆1978 年 26 巻 11 号 p. 3265-3270
発行日: 1978/11/25
公開日: 2008/03/31
ジャーナル フリーIn order to elucidate the mechanism of difenamizole (DFZ)-induced inhibition of Straub tail reaction (STR), the relationship between biogenic amines and DFZ-induced inhibition of STR (DIS) was particularly investigated in this experiment. 10 mg/kg of apomorphine and 2 mg/kg of methamphetamine decreased the DIS (intraperitoneal and intracerebral injection of DFZ) significantly without producing marked STR. Intracerebral injection of 50 μg/mouse of 5-hydroxytryptamine increased the DIS without affecting STR. On the other hand, the DIS was developed markedly, whether or not mice were pretreated with L-dopa, propranolol, disulfiram, L-5-HTP, tetrabenazine, nialamide, isocarboxazid and tranylcypromine. These results suggest that the DIS might at least be modulated by the variation in the activity of either catecholamine or tryptamine in the central nervous system of mice. In addition, the action mechanism of DFZ on STR was different from that on nociceptive reaction reported previously.抄録全体を表示PDF形式でダウンロード (659K) -
塚谷 博昭, 山田 貞二, 藤井 正信, 淡路 敏和, 岡本 正則, 伊丹 孝文1978 年 26 巻 11 号 p. 3271-3280
発行日: 1978/11/25
公開日: 2008/03/31
ジャーナル フリーA modified procedure for preparation of D-I was offered, and became possible preparation of highly purified material showing a single spot on thin-layer chromatography in a more effective manner. Further examinations on chemical characteristics of D-I involving assessments of functional groups by chemical inactivations treating with various agents were carried out. In Girard's separation, about 30% of depressor-activity was recovered in nonketonic fraction. By treatment with sodium borohydride, the hypotensive activity disappeared completely. It was abolished completely with treatment by hydrogen peroxide (0.1%) or permanganate, while the activity was recovered almost completely by treatment with ferric chloride. It was also damaged with bromine. D-I became substantially less active by treatment with succinic anhydride, and inactive by phenylisocyanate. By treatment with triphenylphosphine or diazomethane at cold D-I was unaffected. The attitudes of D-I against several spray reagents on TLC were further examined, and it was found that 2, 4-dinitrophenylhydrazine-ferricyanide, 2', 7'-dichlorofluorescein and others were useful for detection of D-I. Generally, absorptional pattern of D-I in infrared spectrum resembled that of lysophosphatidyl choline. D-I might be a choline-containing phospholipid having double bond, free hydroxyl, ester, whereas it has no free amino, free carboxyl, amide, peroxide nor vicinal hydroxyl group, and it might have no carbonyl group other than ester. However, it might be convertible readily to a ketonic compound by some causes.抄録全体を表示PDF形式でダウンロード (1018K) -
塚谷 博昭, 山田 貞二, 高内 健吉, 徳村 彰, 立道 広康, 久米川 清子1978 年 26 巻 11 号 p. 3281-3288
発行日: 1978/11/25
公開日: 2008/03/31
ジャーナル フリーStability of D-I preparation on standing at low temperature was examined. Standing in saline solution at 4°, the hypotensive activity was stable for the first 45 days, and lost completely within a following week. Standing as CHCl3-MeOH (2 : 1, v/v) solution at 4°, the decomposition began at 75 days later, and it reached a plateau maintaining about 20% of the initial activity. At-20°as a syrup form, the activity could be stored unaltered for 120 days. In the partition experiments, n-hexane and ethylether could extract little active component at all pH values tested (pH 4, 7 and 10). While n-butanol or Folch's solvent could extract unilaterally without any pH effects. The nuclear magnetic resonance spectrum of D-I strongly resembles that of lysophosphatidyl choline (LPCh). Specific optical rotation was also similar to that of LPCh. In the assessment of molecular weight on Sephadex LH-20 column eluting with 80% EtOH, the active substance was eluted in the neighbourhood of L-dipalmitoylphosphatidyl choline or L-1-palmitoyl-LPCh and its molecular weight was estimated to be about 500 to 800. In the analysis, the ratio of phosphorus, glycerol, choline and fatty acid was approximately 1 : 1 : 1 : 1, and oleic acid shared about half of the fatty acid composition. D-I might be a LPCh or closely related compound to it.抄録全体を表示PDF形式でダウンロード (784K) -
石光 進, 藤本 貞毅, 小原 晃1978 年 26 巻 11 号 p. 3289-3295
発行日: 1978/11/25
公開日: 2008/03/31
ジャーナル フリーThe mechanism of inactivation of papain by ascorbic acid in the presence of cupric ions was investigated. Dehydroascorbic acid and hydrogen peroxide which were oxidative product of ascorbic acid, were much less effective. In addition, bubbling nitrogen gas and radical scavengers prevented the inactivation by ascorbic acid and cupric ions. The results indicated that the inactivating effect of ascorbic acid was oxygen dependent and caused by free radicals formed during the autoxidation of ascorbic acid. The N-terminal amino acid and polyacrylamide disc gel electrophoretical patterns of the inactivated papain did not so differ from those of the native papain. On the other hand, the amino acids composition and fluorescence spectrum were changed in the inactivated papain as compared with the intact papain. These facts suggest that the cleavage of the S-S bond of papain molecule produced by the treatment with ascorbic acid and cupric ions resulted in inactivation.抄録全体を表示PDF形式でダウンロード (1078K) -
佐藤 誠, 田川 博昭, 小笹山 瑛, 内丸 文彦, 小島 浩, 山崎 輝清, 桜井 武男1978 年 26 巻 11 号 p. 3296-3305
発行日: 1978/11/25
公開日: 2008/03/31
ジャーナル フリーIn order to search for new psychotropic agents, several 1-butanone derivatives (VIII) substituted by pyridine, indole or quinoline were synthesized. And the carbonyl group of VIII was modified to methylene (XII), secondary alcohol (XIII) and vinyl (XIV). The effects of the compounds on spontaneous motor activity and rotarod test in mice were determined. The structure-activity relationships of these derivatives are discussed.抄録全体を表示PDF形式でダウンロード (1034K) -
矢沢 幸平, 今井 一洋, 田村 善蔵1978 年 26 巻 11 号 p. 3306-3311
発行日: 1978/11/25
公開日: 2008/03/31
ジャーナル フリーOligo-and poly-saccharides which are utilizcd only by B. infantis and B. breve and not by other intestinal bacteria such as E. coli, L. acidophilus, and S. faecalis were investigated in vitro for the purpose of producing bifidus-flora in human intestines. Raffinose, stachyose, and inulin were found to be specifically utilized by B. infantis and doubling time of the cells with them as energy source was as short as with glucose and lactose. Inulin of molecular weight higher than ca. 4500 was not utilized by B. infantis. Oligosaccharides more than trisaccharide from inulin and tri-to penta-saccharides from dextran obtained by acid hydrolysis followed by Sephadex gel chromatographic separation were utilized specifically by B. infantis, but oligosaccharides from amylose and cellulose were found nonspecific for B. infantis and B. breve. Suitability of sugars for producing bifidusflora in vivo is discussed.抄録全体を表示PDF形式でダウンロード (685K) -
菅原 洋一, 藤原 充雄, 三浦 勇二, 林田 幸吉, 高橋 忠男1978 年 26 巻 11 号 p. 3312-3321
発行日: 1978/11/25
公開日: 2008/03/31
ジャーナル フリーThe species differences in the metabolism of naproxen [(+)-6-methoxy-α-methyl-2-naphthaleneacetic acid] were investigated in 6 species of animals and man. 3H-naproxen was orally administered to mice, rats, rabbits, guinea pigs, dogs and miniature pigs (OHMINI-875) and cold naproxen to human subjects, and their urinary and biliary (rats only) metabolites were separated and characterized by thin-layer chromatography, gas chromatography, high-performance liquid chromatography and gas chromatographymass spectrometry. The excretion rates as % of dose of naproxen and its metabolites in the 24 hr urine were, in a decreasing order, miniature pig 82.5, mouse 80.4, rat 74.7, rabbit 70.3, guinea pig 48.5 and dog 23.0%. Naproxen and its metabolites, i.e., 6-hydroxy-α-methyl-2-naphthaleneacetic acid (6-DMN), naproxen glucuronide, 6-DMN glucuronide and 6-DMN sulfate, were found in the urines of all species. Urinary naproxen in the rat was only 0.2% and those in the other species of animals were 4.8-13.7% of the urinary radioactivity, while in man it was 1.3% of dose. The main urinary metabolite in rat, guinea pig, dog, mouse and rabbit was 6-DMN sulfate (87.3, 46.7, 42.9, 39.9 and 36.2% of the urinary radioactivity, respectively), while those in man and miniature pig were naproxen glucuronide (25.3% of dose) and 6-DMN (78.6% of the urinary radioactivity), respectively. The animals whose urinary metabolic profiles were the nearest to that of man were the guinea pig and mouse, while the animals that differed most from man in this regard were the rat and miniature pig.抄録全体を表示PDF形式でダウンロード (1159K) -
田中 博道, 高橋 隆子, 富樫 浩之, 上田 亨1978 年 26 巻 11 号 p. 3322-3329
発行日: 1978/11/25
公開日: 2008/03/31
ジャーナル フリーStarting from 1-β-D-ribofuranosyl-2-oxo-4-imidazoline-4-carboxylic acid (1), obtained from uridine, various 2, 5'-O-cycloimidazole nucleosides have been prepared. The 2-oxo function of 1 was also converted to the 2-chloro and 2-thione functions. Whereas the circular dichroism (CD) spectra of 1 and related 2-oxo derivatives exhibited negative bands, their 5-bromo derivatives showed positive bands. All 2, 5'-O-cycloimidazole nucleosides showed strong negative CD bands which were in contrast to the results in the 8, 5'-O-cyclopurine nucleosides. The relationship between the sign of the CD bands and the orientation of the base moieties in imidazole nucleosides was discussed.抄録全体を表示PDF形式でダウンロード (1002K) -
恩田 政行, 針谷 義弘, 堀江 鈍也1978 年 26 巻 11 号 p. 3330-3337
発行日: 1978/11/25
公開日: 2008/03/31
ジャーナル フリーThe 2-methyl ketone (2a, b), which are derived from the ketones (1a, b), afford the cis-imines (7a, b) and trans-imines (8a, b) by the Leuckart and Bischler-Napieralski reactions. Their methiodies (9a, b and 10b) are converted into the cis-lactams (15a, b) and trans-lactam (17b) via oxidation of the pseudo cyanides (14a, b and 16b). Bromination and successive dehydrobromination of 2a give the enone (20) which affords the cis-imine (23) and trans-imine (24) by the same procedure as above. The cis-methiodide (25) of 23 is reduced to give the cis-amine (26). The cis-lactams (15a, b) and cis-amine (26) can be connected with the synthetic methods of corynoline analogues, which were already known.抄録全体を表示PDF形式でダウンロード (1025K) -
崔 南虎, 坂元 晃史, 東 悳彦1978 年 26 巻 11 号 p. 3338-3346
発行日: 1978/11/25
公開日: 2008/03/31
ジャーナル フリーMessenger ribonucleic acid (mRNA) directing the biosynthesis of catalase [EC 1.11.1.6] was purified from bovine liver. The procedure consists of : (1) isolation of catalase-synthesizing polysomes by immunoprecipitation, (2) extraction of RNA from the polysomes with phenol, and (3) isolation of catalase mRNA by oligo (dT)-cellulose chromatography. Purified catalase mRNA has a molecular weight of 4-5×105 determined by electrophoresis on polyacrylamide-agarose gel. The mRNA stimulated catalase synthesis in a cell-free system derived from wheat germ ; i.e., the incorporation of 14C-amino acids into catalase increased proportionally to the amount of mRNA added in the cell-free system and with incubation time. On SDS-polyacrylamide gel the radioactivity peak of the cell-free products precipitated by anti-catalase antibody coincided with the migration of carrier catalase. In translating system the mRNA preparation directed the incorporation of 14C-amino acids into catalase at least 79% as efficiently as into total proteins.抄録全体を表示PDF形式でダウンロード (1063K) -
三輪 昭, 吉岡 正則, 田村 善蔵1978 年 26 巻 11 号 p. 3347-3352
発行日: 1978/11/25
公開日: 2008/03/31
ジャーナル フリーPreparation of the antibody for radioimmunoassay of epinephrine was examined and an antibody with proper titre was obtained. A procedure for radioimmunoassay of epinephrine was developed by use of a membrane filter to separate bound and free hapten. The dose-response curves of analogs of epinephrine obtained by this method showed that the specificity of the antibody to epinephrine was sufficiently high : The 50% inhibition value of epinephrine was 1 pmol, those of metanephrine and synephrine were 80 pmol and those of norepinephrine and dopamine were 6×102 pmol. The result indicates that the antibody recognizes not only the side chain but also the catechol moiety of the hapten. The sensitivity of this radioimmunoassay was high enough to determine 0.1 pmol of epinephrine.抄録全体を表示PDF形式でダウンロード (625K) -
西畑 利明, 矢田 登, 鎌田 皎1978 年 26 巻 11 号 p. 3353-3363
発行日: 1978/11/25
公開日: 2008/03/31
ジャーナル フリーPharmacokinetic behavior of chlorpropamide (CPA) and sulfadimethoxine (SDM) following intravenous administration were studied in rabbits under normal and alloxan diabetic condition. Plasma concentration of both drugs in the β phase in diabetic rabbits sustained a higher level than those under normal condition. The abnormal pattern of the concentration-time curve of SDM recovered to the normal pattern by the 5-day insulin treatment, but CPA was not the case. Renal clearances of CPA, SDM and N4-acetylsulfadimethoxine (N4-AcSDM) were found to be decreased under diabetic condition. The decreased renal clearances of CPA and N4-AcSDM were subjected to the blockade of proximal tubular secretion of both drugs and to the increased renal tubular reabsorption due to urinary acidification under diabetic condition. The decreased renal clearance of SDM was subjected to the increased renal tubular reabsorption alone. Plasma protein binding and distribution into red blood cells of the drugs were also studied under normal and diabetic conditions.抄録全体を表示PDF形式でダウンロード (1133K) -
夏目 充隆, 和田 盛隆, 小川 正志1978 年 26 巻 11 号 p. 3364-3372
発行日: 1978/11/25
公開日: 2008/03/31
ジャーナル フリーSensitized photooxidation of 5-cyano-1, 2-dihydropyridine derivative (3) afforded a crystalline and reactive endo-peroxide (4), and sulfur derivatives (5 and 6) as well as oxygen derivatives (9 and 10) were produced in good yield from this singlet oxygen adduct (4). 2-Methoxy derivative (9b) was found to be a good intermediate for production of 4-substituted compounds such as 5, 6, 7, 8, and 10, and 1-O-methyl-5-benzamido-5-deoxy-allopiperidinose (15a) and 1-O-methyl-5-benzamido-5-deoxyaltropiperidinose (17a) were synthesized from 13, which was obtained by the cis-dihydroxylation reaction of 9b. Formation of 9 from 4 was proved to be a multi-step reaction through 23 and 26.抄録全体を表示PDF形式でダウンロード (1132K) -
友田 正司, 小高 千英子1978 年 26 巻 11 号 p. 3373-3377
発行日: 1978/11/25
公開日: 2008/03/31
ジャーナル フリーA mucous polysaccharide, named Lilium-Ma-glucomannan, has been isolated from the bulbs of Lilium maculatum THUNB. It was homogeneous on glass-fiber paper electrophoresis and by ultracentrifugal analysis. The component sugars of the glucomannan were D-mannose and D-glucose in the molar ratio of 7 : 4, and its molecular weight was measured at 184000. Methylation, periodate oxidation, and partial acetolysis studies suggested that the polysaccharide is mainly composed of β-1→4 linked aldohexopyranose residues and it contains about seven aldohexose units per one end group on the average. D-Mannose units occupy non-reducing terminal positions and branching points linked through positions 2 or 3. The O-acetyl groups in the glucomannan were identified and determined as the content of 4.7%. They were located in positions 2, 3, 6, 3, 6, and 2, 3, 6 of a part of D-mannose units, and 6 and 2, 3, 6 of a part of D-glucose units.抄録全体を表示PDF形式でダウンロード (747K) -
西畑 利明, 矢田 登, 鎌田 皎1978 年 26 巻 11 号 p. 3378-3383
発行日: 1978/11/25
公開日: 2008/03/31
ジャーナル フリーA study was made on the mechanisms of increased renal tubular reabsorption of chlorpropamide, sulfadimethoxine and N4-acethylsulfadimethoxine in diabetic rabbits. Urinary acidification with NH4Cl increased the renal tubular reabsorption of the drugs. Reabsorption coefficients of undissociated and dissociated molecules of the drugs were calculated using data of renal clearance of the drugs in alloxan diabetic rabbits and in NH4Cl-treated rabbits. Excellent accordance of the reabsorption coefficients as well as apparent reabsorption ratios in diabetic rabbits with those in NH4Cl-treated rabbits was observed. It was concluded that renal tubular reabsorption of drugs depended exclusively on the urinary pH in the renal tubules. Parameters of renal tubular reabsorption in vivo could be well expressed by the parameters of distribution between CHCl3-CCl4 (1 : 1 by volume) containing soy bean lecithin and buffer solution.抄録全体を表示PDF形式でダウンロード (671K) -
井上 博之, 上田 伸一, 上里 新一, 小林 孝次1978 年 26 巻 11 号 p. 3384-3394
発行日: 1978/11/25
公開日: 2008/03/31
ジャーナル フリーAdministration of labeled compounds such as [10-3H]-10-hydroxygeraniol (8), [10-3H]-and [11-3H2]-iridodial (7), [10-3H]-and [11-3H2]-iridodial glucoside (9) to Lamium amplexicaule, Deutzia crenata and Galium spurium var. echinospermon established that lamioside (1), deutzioside (2), scabroside (3), ipolamiide (4), lamiide (5) and asperuloside (6) are biosynthesized in these plants via 10-hydroxygeraniol (8) and iridodial (7).抄録全体を表示PDF形式でダウンロード (1356K) -
亀井 鑠, 竹内 典子, 明石 修三, 利部 光四郎1978 年 26 巻 11 号 p. 3395-3403
発行日: 1978/11/25
公開日: 2008/03/31
ジャーナル フリーAn extracellular polysaccharide (referred to as Ps-III), which showed a positive immune activity to anti-Ps-III-sera obtained from a rabbit immunized with Escherichia coli 29M organisms, was isolated from the culture broth of E. coli 29M. By methylation, Smith degradation, partial acid hydrolysis and methanolysis of Ps-III, its repeating structure was postulated as given below : [numerical formula]抄録全体を表示PDF形式でダウンロード (887K) -
山中 宏, 坂本 尚夫, 坂内 由美, 小川 茂1978 年 26 巻 11 号 p. 3404-3409
発行日: 1978/11/25
公開日: 2008/03/31
ジャーナル フリーUnlike quinoline and isoquinoline N-oxides, 4, 6-dimethylpyrimidine 1-oxide reacted with active methylene compounds such as malononitrile, ethyl cyanoacetate, and ethyl ethoxycarbonylacetimidate to give ring-opened products. In these cases, none of pyrimidine derivatives with a substituent at the 2-position were isolated. On the other hand, the pyrimidine 1-oxide was condensed with 5-amino-3-methyl-isoxazole to give 2-(5-amino-3-methyl-4-isoxazolyl)-4, 6-dimethylpyrimidine. Comparing these two reactions, the driving force of the ring-fission of the reaction intermediates was discussed.抄録全体を表示PDF形式でダウンロード (657K) -
浄住 護雄, 児島 昭次1978 年 26 巻 11 号 p. 3410-3415
発行日: 1978/11/25
公開日: 2008/03/31
ジャーナル フリーThe excretion of cadmium through the bile and gastrointestinal mucosa after the intraperitoneal administration of cadmium chloride and the effect of the chelating agents such as citric acid, D-cysteine, and DL-penicillamine on its excretion were studied in rats pretreated with cadmium. Cadmium pretreatment caused an appreciable decrease in the biliary excretion of subsequently administered cadmium and had no effect on the excretion of the metal through the gastrointestinal mucosa. The chelating agents used had no stimulatory effect on the biliary excretion of cadmium and scarcely affected the excretion of the metal through the gastrointestinal mucosa in the pretreated rats. Moreover, a mechanism of the effect of cadmium pretreatment on the excretion of cadmium through the bile in rats was investigated. From findings relating to the contents of cadmium and zinc in the liver and kidney, the biliary and urinary excretion of both metals, and the binding characteristics of both metals to different proteins in the supernatant of liver, it was suggested that a part of subsequently administered cadmium replaced the zinc bound to metallothionein synthesized in the liver by the pretreatment, resulting in a decrease in the biliary excretion of cadmium and no stimulatory effect of the chelating agents on its excretion.抄録全体を表示PDF形式でダウンロード (701K) -
高橋 秀次, 北沢 栄一, 小木曽 彰1978 年 26 巻 11 号 p. 3416-3418
発行日: 1978/11/25
公開日: 2008/03/31
ジャーナル フリー(±)-Ligantrol (10), isolated from Liatris elegans, was synthesized from the hypothetical precursor, 18-hydroxygeranylnerol (2) which was a isomer of 18-hydroxygeranylgeraniol (1) isolated from Croton sublyratus as an antigastric ulcer principle.抄録全体を表示PDF形式でダウンロード (472K) -
仲井 由宣, 中島 新一郎, 山本 恵司, 寺田 勝英, 今野 勉1978 年 26 巻 11 号 p. 3419-3425
発行日: 1978/11/25
公開日: 2008/03/31
ジャーナル フリーSeveral drugs, such as benzoic acid, aspirin, salicylic acid, and methyl p-hydroxy benzoate, all of which had intermolecular hydrogen bondings, were ground with microcrystalline cellulose respectively. Each drug was ground with β-cyclodextrin too. The inclusion compounds of each drug with β-cyclodextrin were prepared from aqueous solution. When the drugs were ground with β-cyclodextrin, rapid disappearance of X-ray diffraction peaks and that of heat of fusion of drugs, compared with microcrystalline cellulose, were observed. About the inclusion compounds, it was concluded from X-ray diffraction, thermal analysis, and ultraviolet measurements that β-cyclodextrin formed 1 : 1 adduct with each drug and the drug molecules were preffered oriented. The conditions of the drug molecules in the ground mixtures and in the inclusion compounds were investigated using infrared spectroscopy, especially by monitoring the carbonyl stretching bands near 1700 cm-1. When the dispersion of drugs into matrices were completed, the distinct frequency shift of the carbonyl stretching bands was observed in the infrared spectra of these sample. From these results, it would be reasonable to consider that in the ground mixture of microcrystalline cellulose, the drug molecules were present monomolecularly, presumably interacting with cellulose molecules by hydrogen bondings.抄録全体を表示PDF形式でダウンロード (772K) -
千葉 拓, 手島 節三1978 年 26 巻 11 号 p. 3426-3432
発行日: 1978/11/25
公開日: 2008/03/31
ジャーナル フリーThe titled new reducing disaccharides were synthesized from a derivative of lactose. When 1, 6-anhydro-4-O-(2, 3-anhydro-4, 6-O-benzylidene-β-D-glucopyranose (2) was treated with boiling methanolic sodium methoxide, or LiAlH4 in boiling tetrahydrofuran, the trans-diaxial cleavage of the epoxide ring proceeded predominantly according to the Furst-Plattner rule. This agreed with the result obtained by treatment of 2 with KOH, reported previously [T. Chiba and S. Tejima, Chem. Pharm. Bull. (Tokyo), 25, 1049 (1977)]. After acetylation, the major and minor cleavage products of epoxide were isolated by column chromatography on silica gel. The structural assignments of individual products were described. The titled disaccharides were respectively prepared from the individual major product via a series of the following reactions : debenzylidenation, acetylation, opening of the 1, 6-anhydro ring, and removal of the acetyl groups.抄録全体を表示PDF形式でダウンロード (955K) -
松本 仁, 大倉 良昭1978 年 26 巻 11 号 p. 3433-3439
発行日: 1978/11/25
公開日: 2008/03/31
ジャーナル フリーThe π-π* absorption spectra of some psoralens with skin photosensitizing action were measured in various solvents, up to vacuum ultraviolet region. We found that these compounds exhibit six π-π* bands within 180-400 nm region and the longest wavelength absorption band of psoralen shows a blue shift with increasing polarity of the solvents. Furthermore, the molecular orbital calculation of the π-electronic systems of psoralens were carried out by means of the Pariser-Parr-Pople method. The obtained absorption π-π* bands were assigned on the basis of the calculated results.抄録全体を表示PDF形式でダウンロード (730K) -
梅山 秀明, 武田 収功, 小倉 治夫, 森口 郁生, 今村 詮1978 年 26 巻 11 号 p. 3440-3443
発行日: 1978/11/25
公開日: 2008/03/31
ジャーナル フリーIn order to elucidate origin of the Cotton effect of ε-caprolactam, the molecular orbital studies were performed by using the MO's obtained from the CNDO/2 method. It was shown that the sign of the n-π carbonyl Cotton effect for ε-caprolactam is due to the electronic structure of the neighboring carbon of the carbonyl group and the delocalization energy between-CONH-group and the two methylene groups of C (3) H2 and C (5) H2.抄録全体を表示PDF形式でダウンロード (458K) -
相見 則郎, 山口 啓一, 坂井 進一郎, 萩庭 丈寿, 久保 陽徳1978 年 26 巻 11 号 p. 3444-3449
発行日: 1978/11/25
公開日: 2008/03/31
ジャーナル フリー^<13>C-NMR spectra of several Gardneria alkaloids and their derivatives were studied. The chemical shifts of C(15) and C(21) were found to be diagnostic for the configuration of the side chain double bonds between C(19) and C(20). As a result of the present study the E configuration of the ethylidene side chain of chitosenine (V) was confirmed.抄録全体を表示PDF形式でダウンロード (679K) -
池川 繁男, 小畠 範子, 細田 宏, 南原 利夫1978 年 26 巻 11 号 p. 3450-3456
発行日: 1978/11/25
公開日: 2008/03/31
ジャーナル フリーIn order to clarify the metabolic fate of hydrogen at C-2 during microbial transformation of dehydroepiandrosterone into 1α-hydroxy-4-androstene-3, 17-dione, the stereospecific synthesis of epimeric 2-d1-dehydroepiandrosterones have been undertaken. A key intermediate leading to the required substrates, 5α-androst-2-ene-6β, 17β-diol 17-tert-butyl-dimethylsilyl ether, was prepared from dehydroepiandrosterone in several steps. Deuterioboration of the Δ2-olefin and subsequent oxidation of the organoborane afforded the 2α-deuterio-3α-ol. The trans-diaxial opening of the 2α, 3α-epoxide with lithium aluminum deuteride provided the 2β-deuterio-3α-ol. Being submitted to dehydration with phosphorus oxychloride in pyridine followed by usual elaborations, the C-2 deuterated 6β-hydroxysteroids were converted to the desired 2-d1-dehydroepiandrosterones.抄録全体を表示PDF形式でダウンロード (1017K) -
仲町 秀雄, 青木 勇, 朝川 博之1978 年 26 巻 11 号 p. 3457-3462
発行日: 1978/11/25
公開日: 2008/03/31
ジャーナル フリー3-(4-Carbamoyl-1-pyridiniomethyl)-7β-(D-α-sulfophenylacetamido)-ceph-3-em-4-carboxylate monosodium (cefsulodin sodium) was found to exist in crystals in three states of hydration. The hexahydrate was obtained by crystallization from aqueous ethanol and was dehydrated to the dihydrate and anhydrate. The properties of the crystal water in cefsulodin sodium were investigated.抄録全体を表示PDF形式でダウンロード (622K) -
Relationship between Partition Coefficients and Apparent Volumes of Distribution for Basic Drugs. II渡辺 淳, 小崎 章夫1978 年 26 巻 11 号 p. 3463-3470
発行日: 1978/11/25
公開日: 2008/03/31
ジャーナル フリーAccording to the previously proposed model for drug distribution in the body, the apparent volumes of distribution (Vd') of basic drugs with high apparent partition coefficients (P') were related to the blood plasma volume, the other non-lipid space, and the lipid space. The logarithm of Vd' values for basic drugs with P' of 3.2×100-6.7×102 had good correlation (r=0.937) with the logarithm of P'values. The relationship between Vd' and P' was estimated in the region of both low and high P'. The comparison of the result with the observed values indicated that the proposed model was considerably satisfactory, but that there were some other factors which fluctuated the values of Vd'.抄録全体を表示PDF形式でダウンロード (818K) -
財津 潔, 永井 秀明, 大坪 健司, 江藤 精二, 小橋 一彌, 大倉 洋甫1978 年 26 巻 11 号 p. 3471-3476
発行日: 1978/11/25
公開日: 2008/03/31
ジャーナル フリーAn assay method of human platelet monoamine oxidase is presented based on the fluorometric determination of benzaldehyde formed from the substrate benzylamine under the optimal enzyme reaction conditions by the 1, 2-diaminonaphthalene method. This method is very sensitive and permits the assay even with 50 μg of platelet protein. The method was successfully applied to the assessment of inhibitory effect of monoamine oxidase inhibitors (tranylcypromine, pargyline, iproniazid, nialamide, isoniazid and cuprizone).抄録全体を表示PDF形式でダウンロード (693K) -
上釜 兼人, 平山 文俊, 那須 正三, 松尾 直樹, 入江 徹美1978 年 26 巻 11 号 p. 3477-3484
発行日: 1978/11/25
公開日: 2008/03/31
ジャーナル フリーStability constant (Ke) for 1 : 1 inclusion complexes of α-and β-cyclodextrins with barbiturates, phenothiazines, sulfonylamides, and sulfonylureas were determined by high performance liquid chromatography (HPLC). The retention times of the drugs following the binding to cyclodextrins in aqueous mobile phase on ion exchange support were quantitatively treated to obtain the Ke values. The Ke values obtained by HPLC method were in fair agreement with those obtained by other methods such as solubility and spectroscopic methods. The advantages of HPLC method developed here were that Ke values could be rapidly obtained by simple procedure with minimum quantity of the drugs and reproducibility and accuracy were not less than other methods. Furthermore, this method was proved to be particularly suitable for chemically unstable compounds such as phenothiazines.抄録全体を表示PDF形式でダウンロード (768K) -
東野 武郎, 鈴木 清, 林 英作1978 年 26 巻 11 号 p. 3485-3491
発行日: 1978/11/25
公開日: 2008/03/31
ジャーナル フリーBoth the reactions of 3, 4-dihydro-4-quinazolinylmethyl alkyl ketones (4) with active methylene compounds or ketones (NuH) without a catalyst and in the presence of alumina as a catalyst were carried out, and resulted in the transformation of 4 into quinolines (3). Thus 2-(3, 4-dihydro-4-quinazolinyl) acetophenone (4a), 2-(3, 4-dihydro-4-quinazolinyl)-cyclohexanone (4b), and 1-(3, 4-dihydro-4-quinazolinyl)-2-propanone (4c) reacted with diethyl malonate (NuH-2), phenylacetonitrile (NuH-3), acetophenone (NuH-4), cyclopentanone (NuH-5), and cyclohexanone (NuH-6) without catalyst to give 2-phenylquinoline (3b), 1, 2, 3, 4-tetrahydroacridine (3c), and 2-methylquinoline (3d), respectively, together with the dissociation product, quinazoline (1a), although the yield of 3 was very poor. Alumina as a catalyst accelerated these reactions to give 3 in moderate yield. Even the reaction with chloroform (NuH-7) and ethyl orthoformate (NuH-8) gave 3 in good yield. The phenyl and methyl groups substituted at the 2-position prevented 4 from transforming into 3 in both the reactions without a catalyst and in the presence of alumina. A similar transformation was also found between 4, 5-dihydro-5-hydroxy-1-methyl-1H-pyrazolo [3, 4-d] pyrimidine-4-malononitrile (5) and NuH in the presence of alumina, and resulted in the formation of 6-amino-1-methyl-1H-pyrazolo [3, 4-b] pyridine-5-carbonitrile (8). The possible mechanism of the reaction was discussed.抄録全体を表示PDF形式でダウンロード (825K) -
土居 卓治, 中島 常隆, 西田 正行, 須山 忠和1978 年 26 巻 11 号 p. 3492-3497
発行日: 1978/11/25
公開日: 2008/03/31
ジャーナル フリーThree gamma-globulin (IgG) preparations were prepared by enzymatic digestion with plasmin [IgG (plasmin)] or pepsin [IgG (pepsin)] and by polyethylene glycol (PEG) fractionation [IgG (PEG)] and their efficacy was compared in terms of the ability to promote phagocytosis in vitro of three strains of pyogenic bacteria, Pseudomonas aeruginosa, Staphylococcus aureus and Streptococcus pneumoniae, by human polymorphonuclear leukocytes. IgG (plasmin) had the composition of IgG : Fab : Fc=60 : 26 : 14 ; IgG (pepsin), IgG : F (ab')2 : Fc=8 : 77 : 15 and IgG (PEG), 90% or more IgG. In the phagocytosis test, IgG (PEG) was the most efficient and IgG (plasmin) more than IgG (pepsin) though agglutinin titers of these were much the same. The F (ab')2 fragments were almost inefficient in spite of their agglutinin titer similar to those of the IgG preparations. The Fab and Fc fragments showed neither agglutinin titer nor the ability to promote phagocytosis. Since it has been confirmed by a previous study (ref. 16) on the phagocytosis mechanism that these differences in phagocytic effects result from a phagocytotic mechanism in which antigen bound to antibody at its Fab portion is phagocytized through receptors for Fc and complement present on the polymorphonuclear leukocyte surface, it may be concluded that an IgG preparation desirable for clinical use is that which contains intact IgG molecules as much as possible.抄録全体を表示PDF形式でダウンロード (872K) -
宇野 準, 黒川 美貴雄1978 年 26 巻 11 号 p. 3498-3503
発行日: 1978/11/25
公開日: 2008/03/31
ジャーナル フリーThe site of the electrophilic substitution of 1, 2-benzisoxazole-3-acetic acid (1) altered depending on species of electrophiles and reaction conditions. In halogenation, only the α-methylene group of 1 was substituted. In the chlorosulfonation, the α-methylene group was substituted at first and then the 5-position of the nucleus was substituted. On the other hand, in the nitration, the 5-position was substituted at first and the α-methylene group was substituted secondly.抄録全体を表示PDF形式でダウンロード (737K) -
舟越 和久, 園田 裕常, 園田 よし子, 浜名 政和1978 年 26 巻 11 号 p. 3504-3514
発行日: 1978/11/25
公開日: 2008/03/31
ジャーナル フリーThe reaction of quinoline 1-oxide with ethyl cyanoacetate and acetic anhydride in dimethylformamide (DMF) or dimethylsulfoxide (DMSO) at low temperatures was found to give quinolinium-ethoxycarbonylcyanomethylide as the main product besides the normal 2-substituted and 4-substituted products. This novel formation of N-ylide was examined under various conditions, and the following features were revealed. Acetic anhydride was most effective as acylating agent, and DMF and DMSO seemed most suitable media for the N-ylide formation. In addition to ethyl cyanoacetate, malonodinitrile, methyl cyanoacetate and benzoylacetonitrile also produced the corresponding N-ylides, but other active methylene compounds such as malonates, ethyl acetoacetate and cyanoacetamide gave no ylide, only 2-substituted or/and 4-substituted products being formed. As for aromatic N-oxide, pyridine and isoquinoline N-oxides were inert to the N-ylide formation. On the other hand, quinoline 1-oxides bearing an electrondonating group at the 4-position, i.e., lepidine, 4-methoxy-and 4-amino-quinoline 1-oxides, were highly reactive toward this type of N-ylide formation. A likely reaction mechanism was proposed.抄録全体を表示PDF形式でダウンロード (1000K) -
田村 恭光, 千 文宇, 権 順度, サイド モハメド, 岡田 智子, 池田 正澄1978 年 26 巻 11 号 p. 3515-3520
発行日: 1978/11/25
公開日: 2008/03/31
ジャーナル フリーReaction of benzo [b] furan with iodine azide gives in high yield a mixture of cis-and trans-2, 3-diazido-2, 3-dihydrobenzo [b] furans, both of which, upon treatment with alkali, are converted to 3-azidobenzo [b] furan. Similar reaction of 1-benzoyl-and 1-tosyl-indoles with iodine azide affords high yields of cis-and trans-1-benzoyl-and 1-tosyl-2, 3-diazidoindolines. Stereochemical assignment of the adducts is made on the basis of nuclear magnetic resonance spectroscopy.抄録全体を表示PDF形式でダウンロード (674K) -
百瀬 雄章, 田中 徹明, 横田 卓士, 永本 典生, 山田 和代1978 年 26 巻 11 号 p. 3521-3529
発行日: 1978/11/25
公開日: 2008/03/31
ジャーナル フリーThe reaction of alkyl 3-hydroxypyrrole-2-carboxylates (1) with some electrophiles was investigated. The alkylation of 1c occurred at the O and C-2 position as in the case of usual β-keto esters. An N-substituted 3-hydroxypyrrole-2-carboxylate (1e) reacted at the 2-position upon the Michael reaction. In addition to the C-2 adduct (9), an unexpected 2, 2-bis-adduct (10) was concurrently obtained possibly via the ketonic cleavage of the mono-adduct (9) followed by the second addition of acrylate. The N-unsubstituted one (1b) gave a mono-adduct at C-2 (12) and a bis-adduct at C-2 and N (13). Upon bromination, 1c reacted at the 4-and 5-position, not at the 2-position ; namely 1c reacted with bromine as an enamine or a pyrrole, and not as a β-keto ester. The Mannich reaction occurred rapidly and selectively at the 4-position, and the 4-bromo derivative (15) reacted preferentially at the 5-position. In the cyanation of the quarternary salts of the Mannich bases, a dimer (23), a trimer (24) and a dicyano compound (26) were obtained in addition to the expected cyanides (22, 25).抄録全体を表示PDF形式でダウンロード (1095K) -
池谷 理, 津田 俊郎, 山野 喜昭, 山西 嘉晴, 山津 清実, 大前 雅彦, 河部 靖, 西野 博人, 倉橋 辰雄1978 年 26 巻 11 号 p. 3530-3539
発行日: 1978/11/25
公開日: 2008/03/31
ジャーナル フリーA flow cell electrochemical detector (ECD) using a glassy carbon electrode for high-performance liquid chromatography (HPLC) was designed and characterized. The ECD examined by us showed the same property as the tubular type electrode. The linear dynamic range of norepinephrine (NE), dopamine (DA) and serotonin (5HT) peak current were about 104 (50 pg-1 μg) and the minimum detectable quantities for NE and DA were 5 and 10 pg. High-performance reversed-phase chromatography in combination with ECD permitted the simultaneous determination of NE, DA and 5HT in a whole mouse brain and mouse cerebellum. Assay of NE, DA and 5HT gave the mean values of 430, 872 and 749 ng/g wet tissue for whole mouse brain, and 259, 16 and 240 ng/g wet tissue for mouse cerebellum.抄録全体を表示PDF形式でダウンロード (1020K) -
三浦 俊明, 小木曽 健人1978 年 26 巻 11 号 p. 3540-3545
発行日: 1978/11/25
公開日: 2008/03/31
ジャーナル フリーThe formation of methemoglobin (metHb) from oxyhemoglobin (oxyHb) in the erythrocyte by O2-was studied under the O2--generating system of photoactivated riboflavin with oxygen by using a catalase inhibitor, 3-amino-1, 2, 4-triazole (AT). In the AT-treated erythrocytes in vitro which have little catalase activity, the rate of metHb formation was increased remarkably compared with that of untreated normal erythrocyte. Furthermore, catalase added to 60 unit/ml to the suspending medium contained AT-treated erythrocytes caused a strong inhibition of formation of metHb, suggesting that H2O2 is generating in the external medium of erythrocytes by the reaction of photoactivated riboflavin or spontaneous dismutation of O2-. Addition of superoxide dismutase (5μg/ml) caused an acceleration but not inhibition of the metHb formation. Hemolysis was scarcely observed in the time course of this experiment. These results may be interpreted that H2O2 generated in the outside of cells moves across the membrane and results in oxidative attack to oxyHb in the erythrocyte without the hemolytic effect. Another possible participation of O2- may be suggested to exert its enhanced oxidation of oxyHb, namely that O2- generated in the outside of cells may pass through the membrane directly.抄録全体を表示PDF形式でダウンロード (817K) -
安孫 子敬, 汲川 美保子, 太宰 幸子, 宇野 千賀子, 石崎 充, 高橋 寿, 関野 宏1978 年 26 巻 11 号 p. 3546-3551
発行日: 1978/11/25
公開日: 2008/03/31
ジャーナル フリーThe tetradecapeptide corresponding to position 1 to 14 of glucagon was synthesized by a conventional method. Though the suppression test of this peptide was tested against PHA-induced lymphocyte transformation, any reproducible and significant results were not obtained. In this finding, the effect on immunodeficiency of chronic renal failure was not because of glucagon fragment (1-14).抄録全体を表示PDF形式でダウンロード (854K) -
久木野 和暁, 出口 隆志1978 年 26 巻 11 号 p. 3551-3555
発行日: 1978/11/25
公開日: 2008/03/31
ジャーナル フリーThe anticonvulsant activity of sodium dipropylacetate (DPA) and its effects on the cerebral 5-hydroxytryptamine (5HT) and γ-aminobutyric acid (GABA) metabolisms in the reserpinized mice have been studied to know the mechanism of action of DPA. The results are as follows ; 1. DPA elevated the turnover of the cerebral 5HT and the content of the cerebral 5-hydroxyindoleacetic acid. Phenobartital sodium (PB) showed no effects. 2. DPA elevated the cerebral GABA content in the reserpinized mice. 3. In maximal electroshock seizure, the seizure-protecting activities of DPA and PB were lower in the reserpinized mice than in the normal. 4. In pentylenetetrazole seizure, the seizure-protecting activity of DPA in the reserpinized mice was the same as in the normal. In combined administration, L-di-hydroxyphenylalanine decreased the activity of DPA in the reserpinized mice. The activity of PB decreased in the reserpinized mice. From these results, it was suggested that DPA showed the anticonvulsant activity partially through its effect on the cerebral metabolism of 5HT as well as GABA.抄録全体を表示PDF形式でダウンロード (618K) -
古川 潮, 大川 原正, 野口 芳秀1978 年 26 巻 11 号 p. 3556-3558
発行日: 1978/11/25
公開日: 2008/03/31
ジャーナル フリーThe reactions of 2, 3-epoxypropylaryl ether with ethyl-N-phenylformimidate (I) and with N, N'-diphenylformamidine (II) were examined. It was found that the reactions gave the same product, N-(2-hydroxy-3-aryloxypropyl)-N-phenylformamide (III).抄録全体を表示PDF形式でダウンロード (440K) -
川島 啓助, 伊藤 博, 千畑 一郎1978 年 26 巻 11 号 p. 3558-3562
発行日: 1978/11/25
公開日: 2008/03/31
ジャーナル フリーA rapid method for evaluating antioxidant activity was developed. By this method as many as twenty samples can be evaluated simultaneously. Moreover, the procedure is facile and gives quick result. The test system consisted of linoleate emulsion dispersed in phosphate buffer (pH 7.0) containing hemin. The rapid oxygen uptake due to hemin-catalyzed oxidation of linoleic acid was manometrically measured with a Gilson differential respirometer. The rate of decrease in the oxygen uptake was used for evaluating antioxidant activity of samples. The activity of browning products formed by the reaction between amino acid and sugar was determined by this method, and the results were compared with those obtained by the active oxygen method.抄録全体を表示PDF形式でダウンロード (634K) -
鄭 大基, 手島 節三1978 年 26 巻 11 号 p. 3562-3564
発行日: 1978/11/25
公開日: 2008/03/31
ジャーナル フリーThe title branched trisaccharides were synthesized from 1, 2, 2', 3, 3', 4', 6'-hepta-O-acetyl-β-maltose (1). A modified Koenigs-Knorr condensation of 1 with 2, 3, 4, 6-tetra-O-benzyl-α-D-galactopyranosyl chloride or 2, 3, 4, 6-tetra-O-acetyl-α-D-galactopyranosyl bromide afforded a protected trisaccharide having α-D-or β-D-galactosidic linkage at the C-6 hydroxyl group in maltose, respectively. The yield was 37 or 52% from 1. The configuration of new galactosidic linkages in the trisaccharides was confirmed by comparison of the molecular rotation of their corresponding undecaacetates with the value of calculation. Deacetylation of the undecaacetates afforded the title trisaccharides.抄録全体を表示PDF形式でダウンロード (518K) -
桜井 邦好, 青柳 栄, 豊福 初則, 大木 実, 吉沢 豊吉, 黒田 敏男1978 年 26 巻 11 号 p. 3565-3566
発行日: 1978/11/25
公開日: 2008/03/31
ジャーナル フリーSelective N1-tetrahydrofurylation of uracils has been performed in satisfactory yield by direct addition of uracils to 2, 3-dihydrofuran in the presence of PCl5 in hexamethyl-phosphoramide (HMPA).抄録全体を表示PDF形式でダウンロード (379K) -
中川 明子, 大内 涼子, 吉沢 逸雄1978 年 26 巻 11 号 p. 3567-3571
発行日: 1978/11/25
公開日: 2008/03/31
ジャーナル フリー2, 3, 17 β-Trihydroxyestra-1, 3, 5 (10)-trien-6-one (7) and its methylated derivatives (6, 12, and 16) have been prepared for the biological investigation. The preparation method and the results of the instrumental analyses including nuclear magnetic resonance and ultraviolet spectra of these materials are described.抄録全体を表示PDF形式でダウンロード (662K) -
東 豊, 西畑 利明, 久保 一義, 矢田 登, 鎌田 皎1978 年 26 巻 11 号 p. 3572-3576
発行日: 1978/11/25
公開日: 2008/03/31
ジャーナル フリーDisplacement of eight sulfonamides by sodium salicylate from the binding sites of bovine serum albumin (BSA) was studied by the equilibrium dialysis method at pH 7.4 and 37°. Amount of sulfonamides displaced by the addition of salicylate (1 or 3 mM) were linearly correlated with their amount bound to the binding sites of BSA in the absence of salicylate. Double-reciprocal plots of the binding of sulfamethoxazole to BSA with and without salicylate, following Langmuir's isotherms, resulted in linear curves with a common ordinate intercept. This result suggests that the inhibitory effects of salicylate on the binding of sulfamethoxazole to albumin were competitively performed at the same binding site on the protein.抄録全体を表示PDF形式でダウンロード (619K) -
田中 昭, 臼井 敏直1978 年 26 巻 11 号 p. 3576-3579
発行日: 1978/11/25
公開日: 2008/03/31
ジャーナル フリーSeven kinds of 4-substituted 5-(5-nitro-2-furyl) thiazol-2-ones were obtained by the reaction of α-substituted β-(5-nitro-2-furyl) vinylamines (Ia-g) with chlorocarbonylsulfenyl chloride. Reaction of Ia and c with trichloromethylsulfenyl chloride gave 3-sub-stituted 4-(5-nitro-2-furyl)-5-chloroisothiazoles.抄録全体を表示PDF形式でダウンロード (518K) -
田中 信寿, 村上 孝夫, 斎木 保久, 陳 秋明 /, LUIS D. GOMEZ1978 年 26 巻 11 号 p. 3580-3582
発行日: 1978/11/25
公開日: 2008/03/31
ジャーナル フリーAus den oberirdischen Teilen von Pteris grandifolia L. wurden neben Quercitrin (3, 5, 7, 3', 4'-Pentahydroxy-flavon-3-mono-α-L-rhamnopyranosid) zwei neue Flavonol-acetyl-glykoside, d.h., 3"-O-Acetyl-quercitrin und 4"-O-Acetyl-quercitrin isoliert und identifiziert.抄録全体を表示PDF形式でダウンロード (482K) -
金子 主税, 林 令子, 藤井 春恵, 山本 敦1978 年 26 巻 11 号 p. 3582-3584
発行日: 1978/11/25
公開日: 2008/03/31
ジャーナル フリーThe successful use of 3-sulfolene as an alternative reagent for sulfur dioxide was demonstrated for the first time by two types of the reactions : i) deoxygenation of aromatic amine N-oxides and ii) isomerization of ergosterol and its derivatives.抄録全体を表示PDF形式でダウンロード (497K) -
高橋 幸太郎, 高荷 昌子1978 年 26 巻 11 号 p. 3585-3587
発行日: 1978/11/25
公開日: 2008/03/31
ジャーナル フリーIrradiation of d-usnic acid at -20° under oxygen atmosphere afforded 2, 4-diacetyl-6-methyl-phloroglucinol (IV), together with racemic usnic acid, and decarbousnic acid afforded also the same compound under the same conditions. The mechanism of the photo-oxidation of usnic-and decarbousnic-acids was studied.抄録全体を表示PDF形式でダウンロード (487K)