YAKUGAKU ZASSHI
Online ISSN : 1347-5231
Print ISSN : 0031-6903
ISSN-L : 0031-6903
Volume 91, Issue 5
Displaying 1-17 of 17 articles from this issue
  • YOSHIYUKI SEYAMA, Yo MORI, SHINKICHI NIINOBE
    1971 Volume 91 Issue 5 Pages 511-517
    Published: May 25, 1971
    Released on J-STAGE: May 30, 2008
    JOURNAL FREE ACCESS
    The changes in the bone metabolism by the administration of aminoacetonitrile to young rats were examined. Biochemical analyses of the bone of young rats fed with 0.1% dietary aminoacetonitrile for 3-9 days showed that an increase in the solubility of collagen constituted the initial alteration. Then serum calcium concentration and serum alkaline phosphatase activity were increased after 9 days of aminoacetonitrile treatment. At the same time, there was an increase in the release of total hydroxyproline from metaphyses in vitro. Increase of dietary aminoacetonitrile from 0.1% to 0.2% further increased the amount of soluble collagen. Serum alkaline phosphatase activity and the release of total hydroxyproline from metaphyses were also increased. On the contrary, serum calcium concentration decreased, while the formation of multiple exostoses was observed. After 9 days of 0.2% dietary aminoacetonitrile treatment there was a great increase in the urinary total hydroxyproline excretion, indicating an increased rate of collagen turnover. Administration of calcitonin to lathyritic rats showed a significant hypocalcemic effect and the effect of lowering serum alkaline phosphatase activity.
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  • TADAMICHI KUBO, SHUN'ICHI TSUKIYAMA, AKIRA TAKAMURA, IWAO TAKASHIMA
    1971 Volume 91 Issue 5 Pages 518-521
    Published: May 25, 1971
    Released on J-STAGE: May 30, 2008
    JOURNAL FREE ACCESS
    A direct microscopic photography is proposed forthe particle size determination of liquid-liquid dispersion. The apparatus consists of a cylindrical vessel (dT=150 mm) made of clear acrylate resin and a Rushton-type impeller (dI=49 mm). A microscopic camera was immersed directly into the agitated liquid. Water and a mixture of C7H16 and carbon tetrachloride (s.g.=1.000) were used as continuous phase, and dispersed one. The photographs of the droplets were concurrently taken by the direct and indirect methods. The following results were obtained : 1) It was possible to take photographs of the droplets by the direct method as clear as those taken by the indirect method. 2) In the case of non-coalescence of the droplets, the mean diameter and particle size distribution were the same by both methods. It is, therefore, concluded that the direct method is better than the indirect one for the observation of unstable dispersions.
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  • MUNEHISA ARISAWA, NOBUKO MINABE, REIKO SAEKI, TOKUTARO TAKAKUWA, TASHI ...
    1971 Volume 91 Issue 5 Pages 522-524
    Published: May 25, 1971
    Released on J-STAGE: May 30, 2008
    JOURNAL FREE ACCESS
    From the standpoint of chemotaxonomy, components of the flavonoids in the leaves of Chenopodium ambrosioides L. (Chenopodiaceae) were examined. Ethyl acetate extract of the fresh leaves afforded two kaempferol glycoside of mp 242-243° (A) and mp 218- 221°(B), both in 0.046% yield. (A) was identified as kaempfrol-7-rhamnoside by direct comparison with the authentic sample. (B) was found to be composed of kaempferol-7-rhamnoside with 1 mole each of glucose and rhamnose. Since (B) is a new glycoside, it was named ambroside.
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  • TSUTOMU NOJIRI, FUMIHIKO TANAKA
    1971 Volume 91 Issue 5 Pages 525-533
    Published: May 25, 1971
    Released on J-STAGE: May 30, 2008
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    Effect of some of medium constituents on the levels of phosphotransacetylase in the extract of Lactobacillus fermenti 36 IFO No. 3071 was examined, using modified MaciasR's basal medium widely used in the microbiological assay of thiamine. Experimental demonstrated that D-xylose had a significant stimulatory effect on growth, but also had a results significant repressive effect on the phosphotransacetylase level of L.fermenti. It was also found that D-glucose had an effect of inducing the formation of phosphotransacetylase, and that this effect was completely inhibited by chloramphenicol. Pantothenate in the medium had no effect of inducing the enzyme. Other vitamins such as thiamine, biotin, and nicotinic acid, had some effect on both the growth and the enzyme level when they were compared with each other at lower levels of vitamins, whereas, bu no effect at a higher level. It was suggested that phosphotransacetylase of L.fermenti might be induced by D-glucose to perform hetero-lactic acid fermentation (as shown in Chart 2).
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  • RYOICHI ONISHI, KUNIO KAWAMURA, KAORU YAMAMOTO
    1971 Volume 91 Issue 5 Pages 534-541
    Published: May 25, 1971
    Released on J-STAGE: May 30, 2008
    JOURNAL FREE ACCESS
    In Craig-type countercurrent distribution, total quantity or material (Z) can be estimated by the equation derived from binomial distribution : [numerical formula] where W1 W2 and W3 are the quantities of material in the peak tube and the one before and after the peak tube, respectively, K the partition coefficient, n the number of transfers, and γ the number of tubes. When binomial distribution can be approximated by normal distribution, Z can be estimated, independently of n, γ and K, by the following formula : [numerical formula] where Wmax is the quantity of material in the peak tube, Wa(1) and Wa(2) are the quantities of material in the tubes of a-th before and after the peak tube respectively. Partition coefficients of chlorpheniramine maleate, dihydrocodeine phosphate, dlmethylephedrine hydrochloride, caffeine and 2-hydroxypropyl-7-theophylline were investigated, examined in several solvent systems, and they were found to be quantitatively separated with 50 transfers. By means of countercurrent separation followed by calculation of the total quantities of ingredients with above-mentioned equations, satisfactory results were obtained in separatory determination of mixed anti-cold pharmaceutical preparations.
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  • AKITADA MATSUDA, SHIGEO BABA, YUZO NAGASE
    1971 Volume 91 Issue 5 Pages 542-545
    Published: May 25, 1971
    Released on J-STAGE: May 30, 2008
    JOURNAL FREE ACCESS
    Excretion rate of ephedrine and its metabolites was examined by the tracer technique after oral administration of l-ephedrine [α-14C] in a rabbit. The metabolites in a 24 hours urine were examined by paper chromatography, and by reverse dilution and derivative reverse dilution analyses. The metabolites thereby found were norephedrine (av. 1.3%), p-hydroxyephedrine (0.7%), 1-phenyl-1, 2-propanediol (5.7%) and its conjugate (23.4%), 1-hydroxy-1-phenyl-2-propanone (0.8%), benzoic acid (19.1%), p-hydroxybenzoic acid (1.3%), hippuric acid (24.0%) and its conjugate (8.9%), p-hydroxyhippuric acid (8.8%). With the unchanged ephedrine (0.7%), these metabolites explained 94.7% of the radioactivity administered. The present results revealed that the main metabolic route of ephedrine in a rabbit is oxidation of its side chain.
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  • HIROSHI IMAMURA, EIICHI MATSUI, YASUYUKI KATO, TETSUYA FURUTA
    1971 Volume 91 Issue 5 Pages 546-549
    Published: May 25, 1971
    Released on J-STAGE: May 30, 2008
    JOURNAL FREE ACCESS
    ^<35>S-3-Ethoxycarbonyl-35S-2-amino-3-ethxycarbonyl-6-benzyl-4, 5, 6, 7-tetrahydrothieno-[2, 3-c] pyridine (35S-Y-3642) was metabolized in vitro to 32S-2-amino-3-ethoxycarbonyl-4, 5, 6, 7-tetrahydrothieno[2, 3-c]-pyridine (35S-debenzyl-Y-3642) by the liver homogenate of mice and rats, but was not metabolized by the brain, heart, or renal homogenate.35S-Y-3642 was also slightly metabolized by the lung homogenate, while 35S-debenzyl-Y-8642 was not detected. From the experiments using the subcellular fractions of rat liver, N-debenzylation reaction of 35S-Y-3642 was demonstrated to occur in the microsomal fraction, and to require NADPH (NADH) and molecular oxygen.
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  • HIKARU OZAWA, SHUICHI SETO, SHIGEO MURAI, YASUSHI OHIZUMI
    1971 Volume 91 Issue 5 Pages 550-559
    Published: May 25, 1971
    Released on J-STAGE: May 30, 2008
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    Pharmacological properties of 30 troponoid compounds, that have a seven-membered ring, were examined mainly for analgesic, anti-inflammatory, and hypothermic activity and the results obtained are summarized briefly below. 1) Compounds I, II, III, VII, VIII, IX, and X showed analgesic activity in mice. 2) Analgesic activity of I and VII was found to be the same as that of aminopyrine. 3) Inhibition of the central nervous system by I was less than 1/100 of that of chlorpromazine. 4) I and VII very strongly inhibited the enhancement of the capillary permeability induced by acetic acid in mice. 5) X inhibited the development of ultraviolet erythema. 6) I, II, III, VII, IX, X, and XIV showed a marked hypothermic action, and I and VII showed a more potent hypothermic action than aminopyrine.
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  • HIDEAKI SHIRAI, YOSHIRO SATO, NAOKI NAITO
    1971 Volume 91 Issue 5 Pages 560-564
    Published: May 25, 1971
    Released on J-STAGE: May 30, 2008
    JOURNAL FREE ACCESS
    The dehalogenation reaction of phenacyl bromide (I) and its related compounds by means of hexaethylditin (II) was found to give the following products : diphenacyl (III) and acetophenone (IV) from I ; isodidesyl (VII), didesyl (VIII), and deoxybenzoin (IX) from desyl bromide (VI). Irradiation of ultraviolet ray at a low temperature in these reactions mainly gave the dimerization products (III, VII, VIII), and the thermal reaction predominantly gave the hydrogenated products (IV, IX). The expected dimerization product (XVI) was not isolated from the reaction of α-bromo-α, α-diphenylacetophenone (XIV) with II, but a new compound (XV) having no carbonylgroup was obtained.
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  • YOSHIKI HAMADA, HIDEKO MATSUOKA, HIROMI FUKATSU
    1971 Volume 91 Issue 5 Pages 565-570
    Published: May 25, 1971
    Released on J-STAGE: May 30, 2008
    JOURNAL FREE ACCESS
    1) Acetylation of the thiocyanate compounds (I and II) with acetic anhydride in pyridine afforded the monoacetyl (III) and diacetyl (IV) compounds. 2) Halogenated arylthiocyanate compounds (V to XXVIII) were prepared by dissolving 3-chloro-4-thiocyanatoaniline, 1-amino-4-thiocyanatonaphthalene, 8-amino-6-chloroquinoline, or 8-amino-6-chloro-5-thiocyanatoquinoline in xylene, added with haloacetyl chloride, and heated under reflux for 1 hour. 3) An acid amide compound (XXIX) was prepared by the application of hydrogen peroxide to 5-cyano-1, 6-naphthyridine in acetone. 4) The compounds so synthesized (III to XXIX) were tested for their antibacterial activity in vitvo.
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  • SHIN-ICHI FUJITA, YOSHIYUKI ENOMOTO, RIKISAKU SUEMITSU, YASUJI FUJITA
    1971 Volume 91 Issue 5 Pages 571-574
    Published: May 25, 1971
    Released on J-STAGE: May 30, 2008
    JOURNAL FREE ACCESS
    The essential oils of Acorus Calamus LINN. var. angustatus BESS., collected from several localities in Japan, were examined. The yields of the essential oil were 0.24-0.48% from the leaves and rhizomes, 0.10-0.31% from the leaves, and 1.18% from the rhizomes. The oils consisted chiefly of β-asarone(20.5-75.6%) and cis-methylisoeugenol (2.4-48.9%), with the following minor components : Methyleugenol, eugenol, trans-methyl-isoeugenol, elemicine, sekishone, cis- and trans-isoelemicine, and asarone as the phenol ethers ; α-pinene, camphene, β-pinene, limonene, 1, 8-cineole, p-cymene, linalool, terpinen4-ol, α-terpineol, α-ylangene, β-elemene, β-gurjunene, δ-cadinene, calamenene, calacolene, epishyobunone, isoshyobunone, and shyobunone as the terpenoids, and some other compounds.
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  • JOJU HAGINIWA, SHIN-ICHIRO SAKAI, KATUHIRO TAKAOSHI, MINORU TAGUCHI, S ...
    1971 Volume 91 Issue 5 Pages 575-578
    Published: May 25, 1971
    Released on J-STAGE: May 30, 2008
    JOURNAL FREE ACCESS
    Uncarine C (Fig.1) and its isomers D and E were isolated from Uncaria fiorida VIDAL (collected in Formosa, Japanese namd "Togesoheba"), Uncarine A and B (Fig.1) from U.Kawakamii HAYATA (collected in Formosa), and rhynchophylline and isorhynchophylline from U.rhynchophylla MIQ. (collected in Japan) were isolated. Isolations of these substances are interesting from chemotaxonomical view.
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  • KOZO MARUYAMA, KOJI KAWANABE, AIKO FUJIOKA, SHIGEKO IIJIMA
    1971 Volume 91 Issue 5 Pages 579-583
    Published: May 25, 1971
    Released on J-STAGE: May 30, 2008
    JOURNAL FREE ACCESS
    A fluorometric determination of cyclohexylamine by the use of 5-dimethylaminonaph thalene-1-sulfonyl chloride (DNS-Cl) was devised. The recommended analytical procedure is as follows : to 2 ml of a sample solution (0.087-17.4 mM), 1 ml of saturated sodium hydrogen carbonate solution, 4-5 ml of acetone, and 0.5-1.0 ml of 0.5% acetone solution of DNS-Cl are added successively. After standing for 7 hr at room temperature, the solution mixture is made to 10 ml with acetone. A definite volume (0.01-0.05 ml) of the reaction solution is spotted on a thin-layer chromatographic plate (Silica gel H : Avicel SF : soluble strarch=20 : 10 : 1) and developed with chloroform-pyridine mixture (20 : 1). A definite area of Rf 0.52 is scraped off and extracted with 10 ml of acetone. Fluorescence is measured at 497 mμ by the excitation light of 350 mμ. The reading of fluorescence intensity is referred to the 0.5 μg/ml solution of fluorescein sodium. Cyclohexylamine, the hydrolysis product of cyclamate under various conditions, was determined by this fluorometric method. Hydrolysis of two cyclamates in citric acid solution, citric acid and Sn2+ solution, acetic acid solution sodium nitrate solution, and sodium nitrate and sodium chloride solution is shown in Tables III and IV. Hydrolysis being very small under these conditions.
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  • SHIGEO BABA, AKITADA MATSUDA, YUZO NAGASE, KUNIO KAWAI
    1971 Volume 91 Issue 5 Pages 584-586
    Published: May 25, 1971
    Released on J-STAGE: May 30, 2008
    JOURNAL FREE ACCESS
    In order to examine the metabolism of d- and l-ephedrine, d- and l-ephedrine [α-14C] (0.455 μCi/mg) was incubated with rabbit liver slices in a Krebs-Ringer phosphate buffer (pH 7.4) at 37°for 5 hours. The metabolites were separated by paper and thin-layer chromatography, and identified by the reverse dilution method on metabolites and their derivatives. The metabolites detected were norephedrine (39.1% from the d compound and 42.7% from the l compound), hippuric acid (10.9% and 30.7%), 1-phenyl-1, 2-propanediol (1.0% and 5.4%), benzoic acid (1.4% and 4.1%), and 1-hydroxy-1-phenyl-2-propanone (3.6% and 6.9%), with recovery of unchanged ephedrine (42.6% and 8.0%). From the comparison of recovered substrate, it was found that the d compound is less liable to be metabolized than the l compound. Both d and l compounds give approximately the same amount of norephedrine, but the amount of the other metabolites is much greater in the l-isomer. It was thereby revealed that deamination reaction has greater stereospecifisity than demethylation reaction.
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  • MUNEHISA ARISAWA, TOKUTARO TAKAKUWA, KAZUYOSHI HANDA
    1971 Volume 91 Issue 5 Pages 587-589
    Published: May 25, 1971
    Released on J-STAGE: May 30, 2008
    JOURNAL FREE ACCESS
    From the standpoint of chemotaxonomical studies, components of flavonoids in the leaves of Vicia genus plants (Leguminosae) were examined. Ethyl acetate extract of the fresh leaves of Vicia Faba L. afforded kaempferol-3-glucoside-7-rhamnoside as pale yellow needles, mp 231-234°, that of Vicia unijuga AL. Br. afforded cosmosiin (apigenin-7-glucoside) as pale yellow needles, mp 226-228°, and luteolin-7-glucoside as pale yellow needles, mp 242-243°.
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  • MINORU SHINDO, SAKAE TAKAKU, KANJI MORO, KEIICHI TAKAMURA
    1971 Volume 91 Issue 5 Pages 590-593
    Published: May 25, 1971
    Released on J-STAGE: May 30, 2008
    JOURNAL FREE ACCESS
    Analgesic 5-aminomethylsalicylic acid (V) was obtained by amination (Delepine reaction) of methyl 5-chloromethylsalicylate, prepared by chloromethylation (Blanc-Quelet reaction) of methyl salicylate by treating with formaldehyde and hydrogen chloride in the presence of zinc chloride. Total yield of V was 45% based on methyl salicylate. Similarly, chloromethylation of salicylic acid followed by amination gave V in 40% yield.
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  • ISAO KITAGAWA, TADASHI NISHIMURA, AMIKO FURUBAYASHI, ITIRO YOSIOKA
    1971 Volume 91 Issue 5 Pages 593-596
    Published: May 25, 1971
    Released on J-STAGE: May 30, 2008
    JOURNAL FREE ACCESS
    From the methanolic extract of the rhizome of Rehmannia glutinosa LIBOSCH. forma hueichingensis HSIAO, sucrose and catalpol (I) (0.11% from the fresh rhizome) were isolated and identified, in addition to D-mannitol. A comment on the pharmacological significance of catalpol in relation to the medicinal purpose of the rhizome was made.
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