巻号一覧
98 巻, 3 号
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伊藤 一男, 頼 貞秀1978 年 98 巻 3 号 p. 249-256
発行日: 1978/03/25
公開日: 2008/05/30
ジャーナル フリーTriterpenoid compounds from the petroleum ether extracts of Marsdenia formosana MASAMUNE (Asclepiadaceae) were examined. The known triterpenoids, α-amyrin (I), α-amyrin acetate (II), α-amyrenone (III), α-amyrin cinnamate (IV), neoilexonol acetate (VI), lupeol (VII), lupenyl acetate (VIII), and lupenone (IX) were isolated and characterized. In addition to these known compounds, three new triterpenoids, one of which was named marsformol (XII), were also isolated. Structures (V, X, and XII) of these new triterpenoids were assigned from chemical and spectral data.抄録全体を表示PDF形式でダウンロード (1001K) -
栗山 澄, 松沢 幹彦, 宇野 政栄, 大石 義孝, 池本 雅彦1978 年 98 巻 3 号 p. 257-263
発行日: 1978/03/25
公開日: 2008/05/30
ジャーナル フリーAntibacterial activities of 2-nitrobenzofuran derivatives (NBFD) against 8 strains of gram-possitive and -negative bacteria were comparable to nitrofurantoin, or somewhat more potent than that. Elongated cells were occasionally observed in the culture medium containing NBFD. When NBFD (12.5-100 mg/kg) was orally administered to rats, the metabolites excreated in urine also showed antibacterial activity. The antibacterial spectrum of the urinary metabolites, however, was different from that of the intact compound. The cytotoxicity of NBFD and nitrofurantoin was examined using cultured chick embryo fibroblasts. The inhibition of cell multiplication appeared in the concentration range of 0.39-25μg/ml. It was noted that in the case of 7-substituted NBFD the compound which possesed a high antibacterial activity indicated a low cytotoxicity. A reverse relationship between antibacterial activity and cytotoxicity seemed to depend on the size of a substituent in the 7-position of NBFD.抄録全体を表示PDF形式でダウンロード (1643K) -
吉名 重多賀, 郭 盛助1978 年 98 巻 3 号 p. 264-271
発行日: 1978/03/25
公開日: 2008/05/30
ジャーナル フリーIn order to examine the biological activity of furo [3, 2-c] pyrazole derivatives, synthesis of some such derivatives was carried out. Bromination of 5-methyl-1, 3-diphenylfuro-[3, 2-c] pyrazole gave the 5-bromomethyl compound (A) which was used as the starting material for the syntheses of 1, 3-diphenylfuro [3, 2-c] pyrazol-5-yl methyl ethers, 1, 3-diphenylfuro [3, 2-c] pyrazol-5-ylmethylamines, 1, 3-diphenylfuro [3, 2-c] pyrazole-5-acetic acid, and 1, 3-diphenylfuro [3, 2-c] pyrazol-5-ylvinylenes. Satisfactory antibacterial activity in vitro against Staphylococcus, Escherichia coli, Shigella flexneri, Mycobacterium tuberculosis, Candida albicans, and Trichophyton mentagrophytes was found in 5-methylaminomethyl-1, 3-diphenylfuro [3, 2-c] pyrazole, 5-(1-pyrrolidinylmethyl)-1, 3-diphenylfuro [3, 2-c] pyrazole, and 5-(4-methyl-1-piperazinylmethyl)-1, 3-diphenylfuro [3, 2-c] pyrazole.抄録全体を表示PDF形式でダウンロード (837K) -
吉名 重多賀, 田中 昭, 郭 盛助1978 年 98 巻 3 号 p. 272-279
発行日: 1978/03/25
公開日: 2008/05/30
ジャーナル フリーSynthesis of 1, 3-diphenylfuro [3, 2-c] pyrazole-5-carboxaldehyde (A) by various methods was examined, and Kronke's method and oxidation with tertiary aliphatic amine oxide were found to be the most appropriate methods. Reaction of the aldehyde group in A showed that the reactivity of A was similar to that of aromatic aldehydes in general, like benzaldehyde and 2-furaldehyde, except for benzoin condensation. For example, A afforded a carboxylic acid by oxidation with silver oxide, an alcohol by reduction with sodium borohydride, and a Schiff base with primary amines. The Cannizzaro reaction, Wittig reaction, and aldol condensation of A respectively gave the anticipated products. Antibacterial test in vitro of the synthesized furo [3, 2-c] pyrazole derivatives showed that the condensation product with aminoquanidine had a broad antibacterial spectrum.抄録全体を表示PDF形式でダウンロード (879K) -
吉名 重多賀, 郭 盛助1978 年 98 巻 3 号 p. 280-285
発行日: 1978/03/25
公開日: 2008/05/30
ジャーナル フリーExamination of methods for the synthesis of α-methyl-1-(p-substituted phenyl)-3-phenylfuro [3, 2-c] pyrazole-5-acetic acid showed that the following route was found to be the most appropriate. 5-Benzoyl-2-furyl-α-methylacetonitrile is derived to methyl 5-benzoyl-α-methyl-2-furylacetate, which is oxidized with lead tetraacetate and boron trifluoride etherate, without isolation of the intermediate, followed by cyclization to methyl α-methyl-1, 3-diphenylfuro [3, 2-c] pyrazole-5-acetate which is hydrolyzed to the objective acid.抄録全体を表示PDF形式でダウンロード (710K) -
吉名 重多賀, 田中 昭, 臼井 敏直1978 年 98 巻 3 号 p. 286-292
発行日: 1978/03/25
公開日: 2008/05/30
ジャーナル フリーHydrolysis of 2-[α-amino-β-(5-nitro-2-furyl)vinyl] furan (I) gave 2-furyl 5-nitro-2-furfuryl ketone (II), and acetylation of I gave two kinds of compounds, mono- and diacetylamine. Results of other chemical reactions related to the amino group of I indicated that alkylation by propyl iodide, condensation with furfural, and amino group exchange reaction by morpholine were unsuccessful. Nine kinds of β-2-furoyl-β-(5-nitro-2-furyl)-vinyl derivatives and four kinds of 2-(2-furyl)-3-(5-nitro-2-furyl)-4, 5-disubstituted pyrrole derivatives were synthesized from II.抄録全体を表示PDF形式でダウンロード (783K) -
金尾 清造, 永嶋 伸也1978 年 98 巻 3 号 p. 293-296
発行日: 1978/03/25
公開日: 2008/05/30
ジャーナル フリーStructure of the reaction product of DL-pyroglutamic acid (pyrrolidonecarboxylic acid) with formaldehyde was determined by the X-ray diffraction method. An attempt was first made to determine the structure by a direct method using the crystal of the free acid, but did not succeed. Finally the structure was solved by the heavy atom method using a crystal of barium salt, (C6H8NO4)2·Ba·H2O. The barium salt crystallized in the orthorhombic space group Pbcn with a=12.73, b=14.20, c=8.935 Å, Z=8. Three dimensional X-ray diffraction data were collected by an automatic diffractometer. The atomic parameters were refined by the block-diagonal least-squares method leading to a final R-value of 7% for 658 observed reflections. This reaction product was found to be N-hydroxymethylpyrrolidonecarboxylic acid. The pyrrolidone ring is almost planar, and carbon atom of the hydroxymethyl group and oxygen atom of the carbonyl group are also approximately in this plane. The hydroxyl group and the carboxyl group are stretched to the opposite side of the ring plane. There are 8 molecules in the unit cell, and the barium atom and the oxygen atom of the water of crystallization occupy special positions on the two-fold axis.抄録全体を表示PDF形式でダウンロード (491K) -
伊藤 清, 五十嵐 健, 池本 雅彦, 永原 美知子, 中西 輝雄1978 年 98 巻 3 号 p. 297-301
発行日: 1978/03/25
公開日: 2008/05/30
ジャーナル フリーOptical isomers of 2-acetyl-7-(2-hydroxy-3-isopropylaminopropoxy) benzolfuran hydrochloride (BFE-60) were resolved with O, O'-di (p-toluoyl) tartaric acid. Their absolute configuration was determined by the direct synthesis of (R) (+)-BFE-60 from 2-acetyl-7-hydroxybenzofuran and (R) (+)-1-chloro-3-isopropylamino-2-propanol. The absolute configuration was also related on the basis of the partial resolution by chiral BFE-60 (Horeau's method) and was further supported by the induced circular dichroism on the n-π* transition of ion pairs of 2-benzoylbenzoic acid-chiral BFE-60.抄録全体を表示PDF形式でダウンロード (611K) -
杉山 信, 立脇 信清, 杉本 剛敏, 奥山 義男, 中川 隆1978 年 98 巻 3 号 p. 302-311
発行日: 1978/03/25
公開日: 2008/05/30
ジャーナル フリーThe metabolic fate and species difference of 4'-chloro-5-methoxy-3-biphenylylacetic acid (DKA-9), a newly developed anti-inflammatory drug, were studied in human and various animal species (mouse, guinea pig, rabbit, beagle dog, rhesus monkey) by intravenous, intraperitoneal, or oral administration of DKA-9. It was found that men, mice, guinea pigs, and rabbits excreted DKA-9 and its metabolites mainly in urine and the dog mainly in feces (78.8, 75.3, 77.3, 88.7 and 79.1% of the dose, respectively) and there was prolongation of urinary excretion in guinea pigs and rabbits. The detection and fractionation of metabolites in urine and bile were performed by the combination of solvent extraction, enzymic and chemical hydrolysis, and thin-layer chromatography, and nine metabolites were detected. The structures of metabolites fractionated were investigated from spectral analysis data and identified to be 4'-chloro-5-hydroxy-3-biphenylylacetic acid, 5-carboxymethyl-4'-chloro-3-biphenylyl hydrogen sulfate (mainly in mice, guinea pigs, and monkeys), 2-(4'-chloro-5-methoxy-3-biphenylyl)-2-hydroxyacetic acid (mainly in dogs), 4'-chloro-5-methoxy-3-biphenylylacetyl β-D-glucopyranosiduronic acid (mainly in men), 5-carboxymethyl-4'-chloro-3-biphenylyl β-D-glucopyranosiduronic acid (mainly in rabbits), and 4'-chloro-5-hydroxy-3-biphenylylacetyl-β-D-glucopyranosiduronic acid. A metabolite which may be hydroxylated at the 4- or 6-position of DKA-9, its sulfate, and its glucuronide were also detected in mouse and dog urine but not identified yet. Though there are considerable species difference of the metabolic pattern in urine, the main metabolite in the bile was 4'-chloro-5-methoxy-3-biphenylylacetyl β-D-glucopyranosiduronic acid, common to all species.抄録全体を表示PDF形式でダウンロード (1034K) -
小澤 光, 池田 實, 板垣 末広, 豊口 義夫, 東海林 徹1978 年 98 巻 3 号 p. 312-319
発行日: 1978/03/25
公開日: 2008/05/30
ジャーナル フリーCombined effect of adenosine 2'-monophosphate (2'-AMP) and adenosine 3'-monophosphate (3'-AMP) with aminopyrine, Naproxen and morphine-HCl was investigated and results were as follows. 1) The hypothermic action of the combined use of aminopyrine with 2'-AMP and with 3'-AMP in mice was additive. 2) The antipyretic action of aminopyrine with 3'-AMP in adjuvant-induced fever rat was additive. 3) Effect of aminopyrine with 2'-AMP and 3'-AMP on writhing response induced by 0.6% acetic acid was additive, whereas naproxen with aminopyrine was slightly potentiated in mice. 4) 3'-AMP and 2'-AMP enhanced analgesic action of aminopyrine as tested by the hot plate method in mice. 5) 3'-AMP enhanced slightly analgesic action of morphine-HCl, as tested by the pressure method in mice, whereas 2'-AMP was ineffective. It is assumed that the combined effect of 2'-AMP or 3'-AMP with aminopyrine is additive, but that these drugs may not act in the same site of action.抄録全体を表示PDF形式でダウンロード (863K) -
尾関 昭二, 手嶋 喜久雄1978 年 98 巻 3 号 p. 320-326
発行日: 1978/03/25
公開日: 2008/05/30
ジャーナル フリーThe binding of salicylates and hydantoin derivatives to bovine serum albumin (BSA) was studied by the fluorescence method, using 1-anilinonaphthalene-8-sulfonate (ANS) as a probe. Enhancement of the fluorescence of the probe upon addition to BSA and the subsequent decrease of fluorescence in the presence of the binding competitors were used to calculate the binding constants of the probe and the competitors. This method is simple, sensitive, and rapid to determine the binding parameter and the nature of binding to the protein. In this study, the compounds used were salicylates such as salicylic acid, o-anisic acid, salicylamide, methyl salicylate, and aspirin, and hydantoin derivatives such as 5-butyl-1-phenylhydantoin, diphenylhydantoin, 1-phenyl-2-thiohydantoin, 1-phenylhydantoin, and 5-butyl-3-phenylhydantoin. The binding constants at 27°and pH 7.4 were, salicylic acid 5.14×104 M-1, o-anisic acid 1.54×104 M-1, salicylamide 1.01×104 M-1, aspirin 1.00×104 M-1, methyl salicylate 6.5×103 M-1, 5-butyl-1-phenylhydantoin 1.40×104 M-1, diphenylhydantoin 7.1×103 M-1, 1-phenyl-2-thiohydantoin 5.0×103 M-1, and 1-phenylhydantoin 4.8×103 M-1. These results indicated that the compounds used, except 5-butyl-3-phenylhydantoin, were bound at the same binding sites as ANS. It appears that the salicylates compete with hydrantoin derivatives for the tryptophan-containing binding site on BSA molecule, and most of the binding energy is contributed by the hydrophobic and electrostatic interactions.抄録全体を表示PDF形式でダウンロード (748K) -
小泉 京子, 宇多村 敏子1978 年 98 巻 3 号 p. 327-334
発行日: 1978/03/25
公開日: 2008/05/30
ジャーナル フリーTritylation of cellobiose with 3 equivalents of trityl chloride in pyridine at 100°and subsequent acetylation at room temperature afforded a mixture of tritylcellobiose peracetates which were detritylated with 80% acetic acid at 100°, retritylated with an equimolar ratio of the reagent at 50°, and acetylated. From the resulting products, 6, 6'-di-O-trityl-α-cellobiose hexaacetate (IIa-α), 6, 6'-di-O-trityl-β-cellobiose hexaacetate (IIa-β), and 6'-O-trityl-β-cellobiose heptaacetate (IIIa-β) were isolated by chromatography on silica gel. 6-O-Trityl-β-cellobiose heptaacetate (IVa-β) was synthesized from 1, 6-anhydrocellobiose (cellobiosan) hexaacetate by an unambiguous route. A mixture of 6- and 6'-mono-, and 6, 6'-di-O-trityl-cellobiose (IV, III, II) was obtained by direct tritylation of cellobiose with 2 equivalents of the reagent. All three products were isolated by chromatography and were acetylated separately. Each pair of anomers of 6- and 6'-O-tritylcellobiose heptaacetates was separated on a silica gel column, and purification of the fraction containing mainly α-anomer by high-performance liquid chromatography led to the isolation of 6'-O-trityl-α-cellobiose heptaacetate (IIIa-α) and 6-O-trityl-α-cellobiose heptaacetate (IVa-α). The isomers having the trityl group on the reducing residue were less dextrorotatory than those having the trityl group on the nonreducing residue. Studies by the molecular rotation suggested that changes in conformation around the glycosidic linkage may affect the magnitude of optical rotations of these compounds. The unique chemical shifts of acetyl methyl protons in the nuclear magnetic resonance spectra of the tritylcellobiose peracetates gave some information about stereostructure of these compounds in solution.抄録全体を表示PDF形式でダウンロード (997K) -
佐藤 裕信, 下地 康雄, 遠藤 和夫, 西野 弘四, 小池 博之, 熊倉 清次1978 年 98 巻 3 号 p. 335-348
発行日: 1978/03/25
公開日: 2008/05/30
ジャーナル フリーSynthetic studies on pyrano [2, 3-c] pyrazolones were planned to find new cardiovascular drugs. A mixture of α-acetyl-γ-butyrolactone (ABL) and 3-methyl-2-pyrazolin-5-one (I1) was heated to give α-[1-(3-methyl-5-oxo-2-pyrazolin-4-yl)ethylidene]-γ-butyrolactone (II1). However, the desired ring closure product, 5-(2-hydroxyethyl)-3, 4-dimethyl pyrano-[2, 3-c] pyrazol-6(1H)-one (III1) was easily obtained under reflux in dimethylformamide (DMF). 5-Aminoethyl derivatives (IV) were produced from III in the usual manner. It was found that substitution reactions of pyrano [2, 3-c] pyrazoles with alkyl halides usually took place at the position 2 in preference to position 1. A novel ring opening-reclosure occurred in the reaction of 3, 4-dimethyl-1-(2-tosyloxyethyl) pyrano [2, 3-c] pyrazol-6(1H)-one (XXIII) with the appropriate amine to afford new pyrazolo [3, 2-b] [1, 3] oxazole compounds. In these compounds, pyrano [2, 3-c] pyrazolones possessing N-substituted phenylpiperazine moiety showed coronary vasodilating and antihypertensive activities.抄録全体を表示PDF形式でダウンロード (1190K) -
館 安英, 釜野 徳明, 沢田 二郎, 田中 一郎, 糸川 秀治1978 年 98 巻 3 号 p. 349-353
発行日: 1978/03/25
公開日: 2008/05/30
ジャーナル フリーThe normal paraffins and triterpenes contained in the leaves of six kinds of Quercus spp. (Q. serrata THUNB., Q. aliena BLUME, Q. monglica FISCHER var. grosseserrata BLUME, Q. dentata THUNB., Q. acutissima CARRUTH, and Q. variabilis BLUME) and five kinds of related genera (Fagus crenata BLUME, F. japonica MAXIM, Castanea crenata Sieb. et ZUCC, Castanopsis cuspidata THUNB. var. sieboldii MAKINO, and Pasania edulis MAKINO) were examined systematically. Normal paraffins in these plants consisted of pentacosane (C25) to tritriacontane (C33). The ratio of normal paraffin components was similar in taxonomically closely related plants. From the triterpene fraction, five known triterpenes (friedelin, epi-friedelanol, friedelanol, lupeol, and glutinol) were isolated, besides β-sitosterol. In the case of triterpenes, components were also similar in taxonomically closely related plants. This tendency of normal paraffin and triterpene components was similar to that found in subgenus Cyclobalanopsis of Quercus spp. Lupeol and glutinol were present in all of subgenus Lepidobalanus of Quercus spp., friedelin in all of section Aegilops of Lepidobalanus, and a large amount of friedelin was found in Pasania edulis MAKINO.抄録全体を表示PDF形式でダウンロード (571K) -
榎本 三郎, 上山 勉, 井上 正美1978 年 98 巻 3 号 p. 354-357
発行日: 1978/03/25
公開日: 2008/05/30
ジャーナル フリーThe liquid phase ammonolysis of hydroxyphenyl compounds with aqueous ammonia was carried out in the presence of metal salts catalysts. As an effective homogeneous catalyst system, NH4Cl-CoCl2 was found for the temperature range of 230°to 330°and the reaction time of 3 to 5 hr. Under these conditions, aniline, toluidines, xylidines, aminophenols, phenylenediamines, and naphthylamines were obtained selectively with an excellent yield from phenol, cresols, xylenols, dihydroxybenzenes, and naphthols, respectively. In contrast with the vapor-phase ammonolysis already known, this newly proposed reaction system can suppress the isomerization and decomposition of cresols and xylenols. The synthetic route for aromatic amines, in which preliminary nitration is difficult, was reduced by using this catalytic system.抄録全体を表示PDF形式でダウンロード (443K) -
鷹觜 照男1978 年 98 巻 3 号 p. 358-365
発行日: 1978/03/25
公開日: 2008/05/30
ジャーナル フリーMercuration of naphthalic anhydride and its derivatives was examined. Mercury was introduced into 1-position of 2- and 4-nitro derivatives and into 8-position in 3-nitro derivative. Naphthoic anhydride-mercury (II) compounds (IV) reacted with various nucleophilic reagents and produced 1-naphthoic acid derivatives with a substituent in the peri position.抄録全体を表示PDF形式でダウンロード (875K) -
金尾 素健, 松田 弘明1978 年 98 巻 3 号 p. 366-368
発行日: 1978/03/25
公開日: 2008/05/30
ジャーナル フリーTwo glycosides were obtained from the leaves of Lespedeza thunbergii. One was rhoifolin (apigenin 7-neohesperidoside) and the other was a new substance named miyaginin (p-vinylphenol O-D-xylosyl (1→6)-D-glucoside). The structure of the aglycone of miyaginin was proved by spectral and chemical methods after reduction over palladium-carbon.抄録全体を表示PDF形式でダウンロード (516K) -
坪田 宣之, 小澤 光1978 年 98 巻 3 号 p. 369-375
発行日: 1978/03/25
公開日: 2008/05/30
ジャーナル フリーIn order to obtain a large amount of immunologically homogeneous human chorionic gonadotropin (HCG), a method for its purification was devised, HCG of 5550 IU/mg (immunological activity) was obtained in 29% yield from a commercial crude HCG (immunological activity ; 1550 IU/mg) by using column chromatography with DEAE-Sephadex A-25, Con. A-Sepharose, and Sephadex G-100. The purified HCG appeared to be homogeneous by the Ouchterlony immunodiffusion, immunoelectrophoresis, and ultracentrifugation. The S20, W value was found to be 3.07 S. The Stokes'radius of HCG was determined as 37Å by gel filtration on Sephadex G-150. The amino acid composition and the content of carbohydrate were approximately equal to the values of other purified samples, taking the biological activity as an index. However, when analysis by disc electrophoresis revealed two bands close to each other and, analysis by isoelectrofocusing showed peakes of high specific activity at pH 3.90 and 4.05.抄録全体を表示PDF形式でダウンロード (1509K) -
坪田 宣之, 布施 一彦, 阿部 昭三, 沢田 良信, 小澤 光1978 年 98 巻 3 号 p. 376-381
発行日: 1978/03/25
公開日: 2008/05/30
ジャーナル フリーFundamental examinations were made on preparative conditions for the anti-human chorionic gonadotropin (HCG)-antibody-coated latex slide test for the immunological assay of HCG by using the rabbit antibody to immunologically homogeneous HCG. The relation between the antibody titer for HCG in the hemagglutination reaction, and the sensitivity and prozone phenomenon in the latex slide test indicated that the sensitivity and prozone became better as the antibody titer became higher. The relation between the diameter of latex particles and the sensitivity and prozone phenomenon indicated that the sensitivity becomes higher as the latex particle diameter becomes larger and, inversely, the prozone became lower with lowering of the sensitized amount of optimum anti-HCG-immunoglobulin G (IgG). However, amount of sensitized IgG per unit area of latex particles that showed optimum sensitivity and prozone gave a constant value (214-223 ng/cm2) even though the particle diameter was different. In the agglutination reaction between HCG and human luteinizing hormone (HLH) and human thyroid-stimulating hormone (HTSH), a crossreaction was observed when the sensitivity of the latex slide test for HCG was 0.6-1.0 IU/ml, at 1.7-4.0 IU/ml in HLH, and at 10-19 mUSP units/ml in HTSH.抄録全体を表示PDF形式でダウンロード (996K) -
中村 優, 堀田 桂子, 冨野 和子, 原 周司1978 年 98 巻 3 号 p. 382-385
発行日: 1978/03/25
公開日: 2008/05/30
ジャーナル フリーIt was found that the total mercury content of human growing hair had a tendency to decrease with the lapse of time. Long hair samples obtained from 252 females and 64 males, which were cut off at their scalp ends, were cut into 5 cm segments. Each segment was washed, dried, weighed, and its total mercury content was measured with a Zeeman-effect mercury analyzer. Distributions of total mercury along length of hair showed various patterns but, generally, the mean values of mercury content of the corresponding segments decreased in the order of scalp ends to the tips of hairs, regardless of sex or age. In order to clarify whether mercury escaped from growing hair with the lapse of time or whether mercury contamination of human body was progressing, which resulted in the increase of mercury content in the hair, hair samples obtained from 4 fixed persons were treated as above and stored, and then new hair samples from the same persons were obtained after the hair grew 5 cm, and the mercury content of the stored and new hair samples was compared. Its results indicated that mercury escaped from the growing hair with the lapse of time. From these facts measurement of the total mercury content in human hair should be carried out with samples cut at the scalp end and of a definite length.抄録全体を表示PDF形式でダウンロード (507K) -
小澤 光, 小松 敬知, 佐藤 正1978 年 98 巻 3 号 p. 386-389
発行日: 1978/03/25
公開日: 2008/05/30
ジャーナル フリーSince phenytoin was reported to be effective in reversing membrane properties of skeletal muscle from steroid myopathy in mice, examination was made to see if phenytoin was also effective in reversing the resting membrane potentials of skeletal muscle from genetically dystrophic mice and of denervated skeletal muscle from normal mice. Experiment was made on isolated extensor digitorum longus muscle, and membrane potential was recorded with a glass electrode filled with 3 M KCl. After 25 mg/kg of phenytoin was administered i.p. for 9-11 days, the resting membrane potential of dystrophic muscle recovered to the normal level (from -67.7 to -73.2 mV), whereas those of normal (from -75.0 to -73.2 mV) and denervated muscle (from -64.0 to -62.0 mV) were not affected. These results suggested that, as regards the resting membrane potential, genetically dystrophic mouse muscle has some properties in common with steroid-induced myopathy mouse muscle rather than to surgically denervated muscle.抄録全体を表示PDF形式でダウンロード (735K) -
杉山 信1978 年 98 巻 3 号 p. 389-394
発行日: 1978/03/25
公開日: 2008/05/30
ジャーナル フリーProtein binding of 4'-chloro-5-methoxy-3-biphenylylacetic acid (DKA-9), a newly developed anti-inflammatory agent, and its metabolites was examined using the equilibrium dialysis method. It was found from Scatchard plot data that they were bound strongly to bovine serum albumin and had two or more binding sites on the albumin molecule. The binding parameters were as follows : K1=2×104 M-1, K2=8×102 M-1, n1=11.5, n2=27.1 and these values were comparable with K1 of salicylic acid and quinidine, and of K1×n1 of phenylbutazone. In order to obtain a clue to the understanding of the species differences in ADME studies, the binding behavior of DKA-9 to various animal plasma was also investigated. The binding parameters were obtained from the modified Scatchard plot analysis and it was found that there were considerable species differences. It was also suggested that there was a correlation between the species difference in protein binding and that in drug elimination rate.抄録全体を表示PDF形式でダウンロード (672K) -
赤田 良信, 河野 貞子, 棚瀬 弥一郎1978 年 98 巻 3 号 p. 395-397
発行日: 1978/03/25
公開日: 2008/05/30
ジャーナル フリーA rapid and sensitive method using high-speed liquid chromatography was devised for the determination of hippuric acid in human urine. Separation is achieved within 15 min on a Zipax SAX column (1 m) using 0.3 M KH2PO4 (pH 4.35) as an eluant. The limit of detection is about 10 ng of hippuric acid. Hippuric acid in human urine was determined by this method, and the peak was identified as hippuric acid from ultraviolet absorption spectra and by thin-layer chromatography.抄録全体を表示PDF形式でダウンロード (478K) -
篠田 雅人, 太田 節子, 早瀬 幸俊1978 年 98 巻 3 号 p. 397-400
発行日: 1978/03/25
公開日: 2008/05/30
ジャーナル フリーRadiation protective effect of S, 2-aminomethylisothiuronium bromide hydrobromide and 2-mercaptoethylamine hydrochloride was tested on mice irradiated with soft X-ray of 70 kVp, using life-prolongation effect as an index. These compounds showed a marked effect on mice irradiated with 11000-13000 R, using a 10 mm acrylate filter. This method seemed to be usable as a potency testing for chemical radioprotectors.抄録全体を表示PDF形式でダウンロード (524K) -
原 昭二, 平沢 麻美子, 糸川 秀治1978 年 98 巻 3 号 p. 401-404
発行日: 1978/03/25
公開日: 2008/05/30
ジャーナル フリーBased on the recent concept of the mechanism of adsorption chromatography, an optimization of solvent systems for given solute compounds was investigated. Retention behavior of monosubstituted cholestane and disubstituted androstane derivatives as a function of binary solvent compositions on silica gel column was quantitatively determined by high-performance liquid chromatography. The slope and axis intercept of the linear relationship between the logarithmic values of the capacity factors and the solvent concentrations were calculated. A simple procedure to provide optimum binary solvents for a given compound was demonstrated. A design of equieluotropic binary solvent systems was worked out according to the quantitative data of the retention-solvent ratio correlations.抄録全体を表示PDF形式でダウンロード (482K)
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