YAKUGAKU ZASSHI
Online ISSN : 1347-5231
Print ISSN : 0031-6903
ISSN-L : 0031-6903
Volume 90, Issue 3
Displaying 1-28 of 28 articles from this issue
  • TERUO KUTSUMA, KAZUE SATO, TETSUYA CHIDA, YOSHINORI TSUKUNO
    1970 Volume 90 Issue 3 Pages 251-256
    Published: March 25, 1970
    Released on J-STAGE: May 30, 2008
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    The reaction of pyridinium dicyanomethylide (Ia) with sodium methoxide in methanol yields 2-methoxy-3-imidazo [1, 2-α] pyridinecarbonitrile (IVa). Similar reaction of Ia with sodium ethoxide gives 2-ethoxy-3-imidazo [1, 2-α] pyridinecarbonitrile (IVb). Structure of IVa was confirmed from the fact that the hydrolyzed product (XI) of IVa was identical with 2-hydroxy-3-imidazo [1, 2-α] pyridinecarboxylic acid, the hydrolyzed product of the methyl (XIIIa) or ethyl esters (XIIIb) prepared from the reaction of 2-aminopyridine with methyl or ethyl bromomalonate.
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  • KAZUO KIGASAWA, HIROAKI SHIMIZU, TAKEHIKO IWATA, HISAYOSHI TANAKA, HID ...
    1970 Volume 90 Issue 3 Pages 257-261
    Published: March 25, 1970
    Released on J-STAGE: May 30, 2008
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    Colorimetric determination of barbituric acid derivatives is made by hydrolysis with sodium hydroxide to cleave the ring and coloration with a mixed solution of dimethylglyoxime and thiosemicarbazide in hydrochloric acidity. Barbituric acid derivatives like secobarbital having a methyl group in the α-position of the side chain are hardly hydrolyzed by this method and cannot be determined. Improvement of hydrolytic condition for secobarbital was examined and it was found that pretreatment with hydrochloric acid and hydrogen peroxide markedly accelerated hydrolysis rate with alkali. This method was used to examine the method of determination. Secobarbital was heated in hydrochloric acid-hydrogen peroxide mixture for 10 minutes in a boiling water bath, hydrolyzed with alkali for 10 minutes, and then colored with dimethylglyoxime-thiosemicarbazide mixture. Measurement of absorbance of this solution at 530mμ gave a straight line in the range of 50-250μg/ml of secobarbital. This method was applied to commercial tablets of secobarbital and a good result was obtained.
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  • TANEKAZU NADAI, KINUYO NISHII, AKIRA TATEMATSU
    1970 Volume 90 Issue 3 Pages 262-266
    Published: March 25, 1970
    Released on J-STAGE: May 30, 2008
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    Effect of tetracycline on the absorption of sulfanilic acid was examined in the rat. It was found that, in the presence of tetracycline, sulfanilic acid disappeared faster from the small intestinal recirculating solution at pH 8.0. At pH 6.0, however, this absorption enhancement effect of tetracycline was not observed. Blood level analyses of sulfanilic acid were carrid out in the rat using in situ single loop preparation. In the presence of tetracycline, blood level of sulfanilic acid increased at pH 8.0 but not at 6.0 and this result agreed with the one obtained from intestinal recirculation method. Partition ratio (organic solvents/water) and UV spectral data of sulfanilic acid showed the absence of interaction between sulfanilic acid and tetracycline in recirculating solution. Results from tetracycline pretreatment experiments showed that sulfanilic acid disappeared faster from recirculating solution even in the absence of tetracycline. These results suggested that the increased absorption of sulfanilic acid is not due to complex formation with tetracycline in the gut lumen but to the direct effect of tetracycline on the absorptive membrane.
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  • MICHIO NAKANISHI, HIROSHI IMAMURA, EIICHI MATSUI, YASUYUKI KATO
    1970 Volume 90 Issue 3 Pages 267-271
    Published: March 25, 1970
    Released on J-STAGE: May 30, 2008
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    Oral administration of 1, 3-propanediol bis (α-p-chlorophenoxyisobutyrate) (CLY-503) to rats in a dose of 100mg/kg/day for 7 or 12 days resulted in a decrease of serum cholesterol (25-38%) and a slight increase in liver weight, but did not influence the growth of rats. Liver cholesterol decreased 12% by the treatment for 7 days, but did not differ significantly by the treatment for 12 days (p>0.05). CLY-503 markedly inhibited incorporation of acetate-14C into liver cholesterol (59-74%), but had no significant effect on that of mevalonate-14C (p>0.05). No significant effect of CLY-503 was observed on the incorporation of both acetate-14C and mevalonate-14C into cholesterol in serum and intestinal tract wall.
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  • MICHIO NAKANISHI, HIROSHI IMAMURA, YUTAKA MARUYAMA, HIROSUKE HOSHINO
    1970 Volume 90 Issue 3 Pages 272-276
    Published: March 25, 1970
    Released on J-STAGE: May 30, 2008
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    6-Substituted-2-amino-3-ethoxycarbonyl-4, 5, 6, 7-tetrahydrothieno [2, 3-c] pyridines were examined for their anti-edematous and analgesic activity. Derivatives substituted in 6-position with methyl (II), n-butyl (III), n-octyl (IV), allyl (V), propargly (VI), benzyl (VIII), phenethyl (X), and acetyl (XI), as well as 6-unsubstituted compound (I), were more active against carrageenin-induced rat paw edema than acetylsalicylic acid or aminopyrine. By oral administration of 250mg/kg of I, II, V and VI some rats died from the toxicity. In Randall-Selitto test, VIII and XI showed most potent analgesic activity. 6-Cyclohexyl (VII), (III), and (X) were more active than aminopyrine, and IV and 6-p-chlorobenzyl (IX) than acetylsalicylic acid which has weaker analgesic activity than aminopyrine. VIII also revealed potent activity in benzoquinone-induced writhing test in mice. VIII may serve as analgesics and anti-inflammatory agents.
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  • MICHIO NAKANISHI, HIROSHI IMAMURA, YUTAKA MARUYAMA
    1970 Volume 90 Issue 3 Pages 277-283
    Published: March 25, 1970
    Released on J-STAGE: May 30, 2008
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    2-Amino-3-ethoxycarbonyl-6-benzyl-4, 5, 6, 7-tetrahydrothieno [2, 3-c] pyridine (Y-3642) and its hydrochloride (Y-3642 HCl) showed the same potent analgesic activity as aminopyrine in both benzoquinone writhing test in mice and tail pressure test in rats, but in electric stimulation test, activity of Y-3642 HCl was one-half of that of aminopyrine. The mode of action of Y-3642 and its hydrochloride seemed to be similar to that of aminopyrine. These compounds inhibited non-specifically several experimental edemas induced by dextran, formalin, serotonin, and bradykinin. The anti-edematous action of Y-3642 and its hydrochloride is similar to that of acetylsalicylic aicd, but more active.
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  • MICHIO NAKANISHI, HIROSHI IMAMURA, YUTAKA MARUYAMA
    1970 Volume 90 Issue 3 Pages 284-290
    Published: March 25, 1970
    Released on J-STAGE: May 30, 2008
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    2-Amino-3-ethoxycarbonyl-6-benzyl-4, 5, 6, 7-tetrahydrothieno [2, 3-c] pyridine hydrochloride (Y-3642 HCl) inhibited the exudate formation in formalin-induced peritonitis and granuloma pouch test in rats, and dye leakage into the peritoneal cavity in Whittle test in mice. Y-3642·HCl had no effect on normal rectal temperature of rabbits, but displayed higher antipyretic potency than aminopyrine. This compound had no inhibitory effect in granuloma formation and did not delay the process of wound healing in rats. There was no difference in anti-edematous activity of this compound between intact and adrenalectomized rats. From these results it was suggested that the anti-inflammatory activity of this compound was not mediated by the adrenocortical functions.
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  • MICHIO NAKANISHI, HIROSHI IMAMURA, YUTAKA MARUYAMA
    1970 Volume 90 Issue 3 Pages 291-295
    Published: March 25, 1970
    Released on J-STAGE: May 30, 2008
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    Appearance of physical dependence of 2-Amino-3-ethoxycarbonyl-6-benzyl-4, 5, 6, 7-tetrahydrothieno [2, 3-c] pyridine (Y-3642) was tested on rats, comparing with that of morphine as a control. Y-3642 was given orally and morphine was given subcutaneously to test animals. Decrease in body weight due to physical dependence was observed, if the administration was discontinued or otherwise when either levallorphan or Y-3642 was administered instead of morphine after a repeated administration of morphine (100mg/kg/day) to rats twice a day. No decrease in body weight was observed in rats treated previously with repeated administration of Y-3642 (100mg/kg/day, twice a day), when the administration was stopped or levallorphan was given instead of Y-3642. In the rat tail pressure method, the analgesic activity of Y-3642 was not changed during repeated administration of Y-3642 (50 or 100 mg/kg/day, i.p. once a day). But that fo morphine (2.5 or 10mg/kg/day, i.p. once a day) was markedly decreased. These results suggest that analgesic action of Y-3642 is similar to non-narcotic analgesic such as aminopyrine, and the compound is not a narcotic substance.
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  • HIROSHI IMAMURA, EIICHI MATSUI, YASUYUKI KATO
    1970 Volume 90 Issue 3 Pages 296-301
    Published: March 25, 1970
    Released on J-STAGE: May 30, 2008
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    Radioactive compound, 14C-Y-3642-(benzyl-α-14C), of 2-amino-3-ethoxycarbonyl-6-benzyl-4, 5, 6, 7-tetrahydrothieno [2, 3-c] pyridine (Y-3642) was synthesized, and the distribution of radioactivity in mouse tissues was investigated by whole body autoradio-graphy. This compound was rapidly absorbed from the site of administration, and the radioactivity was highly distributed in the liver, kidney, adrenals and brown fat after oral or intraperitoneal administrations at the dose of 100 mg/kg. But only a small amount of radioactivity was found in the blood and central nervous system. Three hours after administration of 14C-Y-3642 as it was rapidly excreted the compound was scarcely detected in tissues, a large amount of it exsited in bile, urine and the gastrointestinal tract. Furthermore a part of radioactivity excreted into the gastrointestinal tract was suggested to be reabsorbed from the intestine. According to the relationship between blackening of the organs on the autoradiogram and radioactivity levels in the organs measured by a liquid scintillation counter, both data showed a good correlation under the limited radioactivity concentration.
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  • HIROSHI IMAMURA, EIICHI MATSUI, YASUYUKI KATO
    1970 Volume 90 Issue 3 Pages 302-307
    Published: March 25, 1970
    Released on J-STAGE: May 30, 2008
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    Absorption, excretion and metabolism of 2-amino-3-ethoxycarbonyl-6-benzyl-4, 5, 6, 7-tetrahydrothieno [2, 3-c] pyridine (Y-3642) were investigated using the radioactive compound (14C-Y-3642) in mice. Excretion of radioactivity (14C) was about 48% in urine, 49% in feces, within 3 days after oral administration of 14C-Y-3642 at the dose of 100mg/kg. When this compound was administered intraperitoneally, the same amount of 14C were excreted in urine and feces. Urinary 14C was extracted with chloroform : 6-11% from alkaline urine (F-1) and 68-76% from acid urine (F-2). According to the analysis of thin-layer chromatography and inverse isotope dilution method, 17-29% of 14C in F-1 was 14C-Y-3642, 48-59% of 14C in F-2 was 14C-hippuric acid, 4-6% of it was 14C-benzoic acid and 1-2% of 14C in the aqueous residue was 14C-benzoyl glucuronide. Furthermore in the case of direct analysis of urinary 14C, 0.4-1% of 14C in urine was 14C-Y-3642 and 42-50% was 14C-hippuric acid. Unchanged 14C-Y-3642 was found in the brain, but 14C-benzoic acid and 14C-hippuric acid mainly existed in the liver and kidney after oral administration of 14C-Y-3642 in mice.
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  • KAZUO KIGASAWA, HIROAKI SHIMIZU, MITSUYO FUJINO
    1970 Volume 90 Issue 3 Pages 308-316
    Published: March 25, 1970
    Released on J-STAGE: May 30, 2008
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    Spectral changes due to the bonding of bromophenol blue (I) and tertiary amines in ethyl acetate were examined and a method was established for a concurrent calculation of the two molar extinction coefficients, ε1 and ε2. In this method, I is reacted with amines of various concentrations, absorbance of the 1 : 1 and 1 : 2 conjugates present is measured, and the values of ε1 and ε2 were obtained as 2.5-2.6×104 and 4-5×104 liter/mole (15-45°), respectively. From these values, equilibrium constant, K2, was calculated and, it was thereby found that this method offered a simple method for the determination of a minute amount of amines in ethyl acetate.
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  • HIROSHI IMAMURA, EIICHI MATSUI, YASUYUKI KATO
    1970 Volume 90 Issue 3 Pages 317-323
    Published: March 25, 1970
    Released on J-STAGE: May 30, 2008
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    Absorption, distribution, excretion and metabolism of 2-amino-3-ethoxycarbonyl-6-benzyl-4, 5, 6, 7-tetrahydrothieno [2, 3-c] pyridine (Y-3642) were investigated using its 14C-labeled compound (14C-Y-3642) in rats. When this compound was orally administered in a dose of 100mg/kg, radioactivity (14C) was highly distributed in the liver, kidney, adrenals and peripheral fat. About 50% or more of 14C in the peripheral fat was extracted with chloroform its alkaline homogenate. The thin-layer chromatographic results revealed that larger amount of unchanged 14C-Y-3642 was present in the peripheral fat, a small amount in the liver and brain, but not at all in the kidney. Approximately 48% of the dose was excreted in urine and 49% in feces within 3 days after oral administration of 14C-Y-3642 (100mg/kg). Increased administration dose delayed, excretion of 14C into urine and feces, and 25% of 14C given was also excreted into bile during 24 hours. Result of thin-layer chromatography and inverse isotope dilution method of the chloro form extract showed the presence of a small amount of unchanged 14C-Y-3642 and a large amount of 14C-hippuric acid in urine, As the administered dose was increased, amount of 14C-hippuric acid excreted in urine decreased. These results clarified that 14C-Y-3642 underwent markedyl N-debenzylation in rats in vivo.
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  • KAZUKO NORO, SEIGO FUKUSHIMA
    1970 Volume 90 Issue 3 Pages 324-328
    Published: March 25, 1970
    Released on J-STAGE: May 30, 2008
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    Condensation of 8-hydroxy-2 (1H)-quinolone (VII) and ethyl trans-3-chlorocrotonate results in cyclization of the 1-position of the quinoline ring with oxazole ring to form ethyl 2-(2-methyl-4-oxo-2-oxazolo [5, 4, 3-i, j] quinolyl) acetate (VIII) and not ethyl 3-(1, 2-dihydro-2-oxo-8-quinolyloxy) crotonate (IX). Heating of 2-(2-methyl-4-oxo-2-oxazolo [5, 4, 3-i, j] acetic acid (X), obtained by hydrolysis of VIII, in polyphospholic acid ester produced 2-methyl-9-ethoxy-4H-pyrano [3, 2-h] quinolin-4-one (XI). By a similar method, 3-methyl-9, 10-dihydro-1H-pyrano [2, 3-h] quinolin-1, 9-dione (XVII) was obtained from 7-hydroxy-2 (1H)-quinolone (XIV).
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  • MICHIO NAKANISHI, HIROSHI IMAMURA, YUTAKA MARUYAMA
    1970 Volume 90 Issue 3 Pages 329-334
    Published: March 25, 1970
    Released on J-STAGE: May 30, 2008
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    2-Amino-3-ethoxycarbonyl-6-benzyl-4, 5, 6, 7-tetrahydrothieno [2, 3-c] pyridine hydrochloride (Y-3642·HCl) showed a very slight inhibitory effect on mouse locomotor activity and electric shock seizure, and did not prolong the thiopental sleep in mice. In anesthetized dogs, intravenous injection of Y-3642·HCl at 10mg/kg dose induced a marked increase of pulse rate and a slight fall in blood pressure, but there was no remarkable change in their electrocardiogram. In the isolated ileum of guinea pigs, Y-3642·HCl had a musculotropic antispasmodic action like papaverine. In anesthetized rabbits, Y-3642·HCl has no α-adrenergic blocking action or ganglion blocking action in the doses up to 10 mg/kg i.v.
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  • TOYOZO UNO, HIDEKI OKUDA
    1970 Volume 90 Issue 3 Pages 335-340
    Published: March 25, 1970
    Released on J-STAGE: May 30, 2008
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    The retention indices of monosubstituted benzene derivatives and monosubstituted toluene derivatives were measured on Squalane, Apiezon-L, D.N.P. and Emulphor-O as a stationary phase and the relation between their molecular structure and retention index was examined. It was found that there was an additive effect in retention index relative to molecular structure of monosubstituted toluene derivatives and the equation [chemical formula] was obtained. The measured retention indices were compared with those calculated and a good agreement was found between them.
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  • MASAITI YASUE, YUHMEEI LIN, JINSAKU SAKAKIBARA
    1970 Volume 90 Issue 3 Pages 341-343
    Published: March 25, 1970
    Released on J-STAGE: May 30, 2008
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    A new compound (I), mp 184°, [α]23D+7.1°(c=1.0, CHCl3), was isolated from the terpenoid fraction of the benzene extract of the leaves of Acanthopanax sciadophylloides. I was hydrolyzed by alkali to yield taraxerol and a mixture of higher fatty acids. The acidic fraction was methylated without purification and examined by gas chromatography. The main components of the mixture were methyl stearate (15.6%), arachidate (38.2%), behenate (20.8%), and lignocerate (16.5%), accompanied by a small amount of methyl esters of higher normal saturated fatty acids of C21, C23, C25, C26, C28 and C30-. Taraxeryl stearate, arachidate, behenate, and lignocerate were synthesized from taraxerol and GLC- pure acids. IR spectra of the natural mixture and the synthesized pure compounds were almost identical but differed in the range of 1180-1350cm-1, as shown in Fig. 1 and 2.
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  • YASUHISA SAIKI, MASAKO OKAMOTO, AKIRA UENO, MITSUO UCHIDA, SEIGO FUKUS ...
    1970 Volume 90 Issue 3 Pages 344-351
    Published: March 25, 1970
    Released on J-STAGE: May 30, 2008
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    Gas chromatographic examinations were made on the essential oils of Chinese and Japanese Gaobens (Kohon) and related plants, namely, Nothosmyrnium japonicum and Osmorhiza aristata. The essential oil of Chinese Gaoben, whose original plant is Ligusticum sinense, contains mainly 3-butylphthalide, cnidilide, and an un-didentified compound X, and its chemical nature is similar to that of Japanese Chuanxiong (Senkyu, Cnidii Rhizoma). One of Japanese Gaobens now on the market consists mainly of osmorhizole (2, 4-dimethoxy-1-allylbenzene), isoosmorhizole (nothosmyrnole, 2, 4-dimethoxy-1-propenyl-benzene), and anethole, and the chemical constituents are the same as those of the oil of Osmorhiza aristate. The oil of Nothosmyrnium japonicum contains mainly dillapiole, nothoapiole, and an un-identified compound, and the structure of nothoapiole is assumed to be 2, 3, 6-trimethoxy-4, 5-methylendioxy-1-allylbenzene. During synthesis of osmorhizole (Chart 1), the Claisen rearrangement was found to occur at two ortho positions.
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  • HIDEAKI SHIRAI, TAKANORI HAYAZAKI
    1970 Volume 90 Issue 3 Pages 352-358
    Published: March 25, 1970
    Released on J-STAGE: May 30, 2008
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    Reduction of 3-hydroxyimino-1, 2-dihydro-3H-pyrido [3, 2, 1-kl] phenoxazine (VIII) with lithium aluminium hydride gave 1, 2, 3, 4-tetrahydro [1, 4] diazepino [3, 2, 1-kl] phenoxazine (IX) and 3-amino-1, 2-dihydro-3H-pyrido [3, 2, 1-kl] phenoxazine (X). The Schmidt reaction of 3-oxo-1, 2-dihydro-3H-pyrido [3, 2, 1-kl] phenoxazine (VII) or the Beckmann rearrangement of VIII with polyphosphoric acid afforded 4-oxo-1, 2, 3, 4-tetrahydro-[1, 4] diazepino [6, 5, 4-kl] phenoxazine (XIV), 3-imino-3H-pyrido [3, 2, 1-kl] phenoxazine (XV) and 3-oxo-3H-pyrido [3, 2, 1-kl] phenoxazine (XVI). The structure of these compounds was clarified.
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  • GOICHI HIRATA
    1970 Volume 90 Issue 3 Pages 359-363
    Published: March 25, 1970
    Released on J-STAGE: May 30, 2008
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    Swelling of crosslinked polyacrylic acid (neutralization degree 0.9, mean polymerization degree between two adjacent crosslinks 4850) by water vapor was examined from polymer solution theory and introduction of swelling isotherm equation was attempted. Examinations were made on the adsorption isotherm equation of Rowen-Simha and swelling theory of Flory, et al., and some difference was observed between experimental results and theoretical values in the range of high relative vapor pressure. The modified equation formula obtaimed by application of the electrostatic interaction between counterion and polymeric ion derived by Voorn-Overbeck to Flory's swelling theory was found to satisfy the experimental results over a whole range of relative vapor pressure. Various differential thermodynamic functions obtained from the adsorption isotherm showed that the standard differential enthalpy of adsorption and standard differentical adsorption entropy are approximately equal to those for the condensation of water vapor to liquid water and there was found no special interatcion between crosslinked polyacrylic acid and water molecule.
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  • HIDETOSHI YOSHIMURA, HIROSHI SHIRAKI, KAZUTA OGURI, HISAO TSUKAMOTO
    1970 Volume 90 Issue 3 Pages 364-369
    Published: March 25, 1970
    Released on J-STAGE: May 30, 2008
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    The metabolic fate of pantethine was studied with rabbits and rats using 14C-labeled compound. When it was injected subcutaneously to rabbits, the radioactivity was excreted into 24 hr urine in the amount varying from 40 to 90% of the dose administered, and almost nothing into feces. Rats also excreted most of the radioactivity rather quickly into urine. The radioactivity was distributed almost uniformly over all of the tissues of rats examined one hour after the drug administration. Two major radioactive metabolites were isolated from the urine of rabbits injected a large amount of 14C-pantethine (500mg/kg), and they were proved to be pantothenic acid and unchanged drug by comparison of their Rf values in thin-layer chromatogram and IR absorption spectra with those of the authentic samples. β-Alanine was also detected as a minor urinary metabolite by paper and thin-layer chromatographies. When injected 20mg/kg of 14C-pantethine, rabbits excreted unchanged pantethine, pantothenic acid, and β-alanine which accounted for about 15, 50, and 0.2% of the radioactivity in 24 hr urine.
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  • MASAO KONOSHIMA, MAMORU TABATA, HISAKO YAMAMOTO, NOBORU HIRAOKA
    1970 Volume 90 Issue 3 Pages 370-377
    Published: March 25, 1970
    Released on J-STAGE: May 30, 2008
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    1. Callus tissues were obtained from the stems and seeds of Datura stramonium L., D. stramonium var. tatula (L.) TORREY, D. stramonium L. var. godronii DANERT, and D. innoxia MILL. on the RM-1964 medium supplemented with 10-6M 2, 4-D and 0-2 ppm kinetin. Factors affecting the growth and alkaloid content of the callus were examined. 2. The growth of callus tissue was best when cultured with glucose or sucrose ; and mannose, maltose, and fructose were also utilized by the callus tissue. 3. Growth and alkaloid content of the callus decreased when cultured on a meduim supplemented with a single nitrogen source instead of a mixture of ammonium nitrate and potassium nitrate contained in the basal medium. 4. When callus tissues were cultured on media containing various concentrations of 2, 4-D and kinetin, the best growth was obtained at 10-5M 2, 4-D, although alkaloid content was the lowest in the same concentration of 2, 4-D. Higher concentrations of kinetin tended to decrease alkaloid content. 5. Free amino acids in callus tissue were analyzed by paper chromatography ; glutamine and asparagine were abundant, and aspartic acid, glutamic acid, alanine, and serine were also detected. 6. Addition of the precursors to the medium was not effective for alkaloid production excepting DL-tropic acid (500 μM) and tropine (250μM). Peptone and yeast extract increased alkaloid content to 0.034% and 0.038%, respectively. 7. Thin-layer chromatograms of alkaloids in callus tissues resembled one another regardless of the differences in species or substances added to the medium. Atropine, scopolamine, tropine, apoatropine, and five unidentified alkaloids were detected.
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  • HISASHI NOGAMI, MANABU HANANO, SHOJI AWAZU, KIKUKO IMAOKA
    1970 Volume 90 Issue 3 Pages 378-383
    Published: March 25, 1970
    Released on J-STAGE: May 30, 2008
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    When sulpyrins is administered to the rat, unchanged sulpyrin, and 4-monomethyl-aminoantipyrine (MAA), 4-aminoantipyrine (AA), and 4-acetylaminoantipyrine (AcAA), which are the metabolites, are detected in the urine. This study was undertaken to determine these excretions by colorimetric method, after being separated by paper chromatography. The determinations of sulpyrin, MAA, AA, and AcAA by colorimetric method are as follows. Sulpyrin and MAA are extracted from the paper with pH 5.9 buffer solution, colored by phosphomolybdic acid, and their absorbances are measured at 810mμ. AA and AcAA are extracted with 0.5N HCl, colored by α-naphthol, and their absorbances are measured at 490mμ. It was found that each of the substances in the standard mixed solution containg sulpyrin, MAA, AA, and AcAA (150μg/0.1ml each) showed a high recovery rate and reproducibility. Especially, the stability of sulpyrin increased markedly, and its value was indicated correctly. These excretions in the rat urine after administration of sulpyrin were separated clearly by the present method. Effective results were obtained even in a small amount of substances in the rat urine.
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  • MASAYUKI NAKAGAKI, TADAO FUJIE
    1970 Volume 90 Issue 3 Pages 384-389
    Published: March 25, 1970
    Released on J-STAGE: May 30, 2008
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    Changes in the nitrogen gas adsorption by synthetic sodium X-type zeolite by pretreatment conditions were examined, and the relationship between the rate of dehydration and amount of nitrogen gas adsorption was clarified. The sample dehydrated at 10-4 mmHg and below 50° dose not show adsorption of nitrogen gas into the zeolite lattice and adsorption occurs at above 70°, and at 10-1 mmHg, adsorption of nitrogen gas did not occur until above 100°. By the use of differential thermal balance at a reduced pressure, effective volume of water contained in 1g of dehydrated zeolite was calculated as 0.4ml and that of nitrogen as 0.3 ml. This difference was considered to be due to the presence of a lattice space in which water molecule can enter but not nitrogen molecule. The failure of nitrogen gas adsorption even after desorption of about 50% of water was assumed to be due to interference of ice remaining in the lattice space.
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  • TAICHI OHMOTO, TAMOTSU NIKAIDO, KAZUYO NAKADAI, EMI TOHYAMA
    1970 Volume 90 Issue 3 Pages 390-393
    Published: March 25, 1970
    Released on J-STAGE: May 30, 2008
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    Distribution of triterpenoids and related compounds was examined for six species of Gramineae plants with special reference to their chemotaxonomy view. The triterpenoids thereby identified are shown in Table I. Fern-9 (11)-en-3α-ol (IIb), a new triterpene alcohol isolated from the whole herb of Zoysia matrella MERR., was identified with the synthetic specimen. Seasonal variation in the content of arundoin (IIc), arundoin-12-one (IIe), and fernenone (IIf) in the whole herb of Zoysia matrella MERR. was also examined.
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  • KOITI KIMURA, HARUYA SHIMADA, SHINTARO NOMURA, YOICHI HISADA, TOSHIHIR ...
    1970 Volume 90 Issue 3 Pages 394-397
    Published: March 25, 1970
    Released on J-STAGE: May 30, 2008
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    Determination of arbutin in crude drugs is made by the use of thin-layer chromatography (TLC) and photometry. The aqueous solution of arbutin is colored by diazotised sulfanilic acid to orange yellow, whose absorption maximum is at 505mμ. In this condition there is a good corrleation between weight of arbutin and absorbance. The arbutin spot isolated by TLC from the extract of a crude drug is similarly colored, its absorbance is measured, and then the concentration of arbutin in the crude drug can be caliculated from the calibration curve.
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  • MADOKA SHIBATA
    1970 Volume 90 Issue 3 Pages 398-404
    Published: March 25, 1970
    Released on J-STAGE: May 30, 2008
    JOURNAL FREE ACCESS
    Symptoms such as fever, abdominal pain, and/or stiffness in abdominal region are characteristic indications of Chinese medicines containing Bupleurum. Furthermore, inflammatory or ulcerative diseases such as pneumonia, hepatitis, or peptic ulcer, and neurosis are main indications of these medicines. Crude Saikosides are a crude saponin fraction extracted from Bupleurum falcatum L. and a specific component of this oriental plant. Crude Saikosides showed potent sedative, analgesic, antipyretic, antitussive, and anti-inflammatory actions in mice, rats, and guinea pigs. Therefore, it may be cncluded that there is a close correlation between experimental pharmacological results and clinical applications of Bupleurum found in the literature on Chinese medicine.
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  • OSAMU TAMEMASA, TAKUJI FUJITA, TOSHIKO KIMURA
    1970 Volume 90 Issue 3 Pages 405-407
    Published: March 25, 1970
    Released on J-STAGE: May 30, 2008
    JOURNAL FREE ACCESS
    In an attempt to develop new pancreas-scanning agents, examination was made on the distribution of berberine hydrochloride in mouse pancreas in comparison with those in the liver and the spleen by measuring the radioactivity of its tritiated derivative. The result obtained did not show the distribution so sufficient that the compound might be used as a material for pancreas-scanning agents.
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  • CHIAKI TANI, ISAMU IMANISHI, JUZIRO NISHIJO
    1970 Volume 90 Issue 3 Pages 407-411
    Published: March 25, 1970
    Released on J-STAGE: May 30, 2008
    JOURNAL FREE ACCESS
    Since there has been no report on the quaternary bases of Corydalis platycarpa MAKINO, this quaternary base portion was reduced with sodium borohydride and dl-tetrahydrocorys-amine, and dl-tetrahydrojatrorrhizine were isolated and identified. dl-Corybulbine was also isolated and identified with the sample prepared from dl-tetrahydrojatrorrhizine. dl-Isocorybulbine was also synthesized. dl-Corybulbine obtained here is a reduced compound and should be present in the plat as the quaternary base dehydrocorybulbine. This is the first time that the base was obtained in this reduced form.
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