YAKUGAKU ZASSHI
Online ISSN : 1347-5231
Print ISSN : 0031-6903
ISSN-L : 0031-6903
92 巻 , 5 号
選択された号の論文の23件中1~23を表示しています
  • 田村 恭光, 南川 純一, 鈴木 護, 池田 正澄
    1972 年 92 巻 5 号 p. 521-524
    発行日: 1972/05/25
    公開日: 2008/05/30
    ジャーナル フリー
    The reaction of 2, 7-dioxo-1, 2, 3, 4, 4a, 5, 6, 7-octahydroquinoline (V) with N-bromosuccinimide (NBS) in chloroform containing a small amount of methanol has been found to afford five products, VI, VII, VIII, IX, and XI, depending on the amount of NBS used and the working-up conditions. It is suggested that the reaction proceeds by initial bromination at C-8 of V to give VI, followed by aromatization or further bromination of the latter.
  • 田中 康雄, 小谷 功
    1972 年 92 巻 5 号 p. 525-530
    発行日: 1972/05/25
    公開日: 2008/05/30
    ジャーナル フリー
    "Shiunko"is an old Japanese medicinal prescription and is an effective purple ointment from Lithospermi (or Macrotomiae) Radix, Angelicae Radix, Oleum Sesami, Cera Flava, and Adeps Suillus. This ointment have been used for suppurative skin diseases such as eczema, haemorrhoids, pimple, dermatophytosis, callus. Antibacterial substances in"Shiunko"were found to be coloring compounds contained in"Nanshikon" (a kind of Shikon). These compounds were extracted and isolated. Five naphthoquinone derivatives, β, β-dimethylacryl-shikonin (II), acetyl-shikonin (III), teracryl-shikonin (IV), shikonin (V), and β-hydroxyisovaleryl-shikonin (VI) were obtained and their antibacterial action tested. All the pigments inhibited the growth of Bacillus subtilis, Staphylococcus aureus, and Sarcina lutea, but not that of Escherichia coli.
  • 久保田 幸穂, 植木 寛, 市下 浩子, 庄司 省三
    1972 年 92 巻 5 号 p. 531-534
    発行日: 1972/05/25
    公開日: 2008/05/30
    ジャーナル フリー
    Biological activities of Saliva-parotin-A (SPA) were investigated by its intravenous injection into parotidectomized rabbits. No difference was found in the number of circulating leukocytes and the serum calcium and citrate levels between the operated and normal rabbits. The leukocytosis-promoting and hypocalcemic activities of SPA increased slightly in the operated group. After 24 hr of control feeding, the citrate level in the operated group was much higher than that in the normal group. The citrate-lowering activity of SPA was almost the same degree in both groups, but the deviation of the mean value of the citrate level in the operated group was larger than that in the normal group. The oxygen uptake of liver and kidneys in parotidectomized mouse was not affected by the injection of SPA. The possibility that one of the action mechanisms of SPA is the stimulation or inhibition of the citrate metabolism in kidney may thus be excluded.
  • 大和 正利, 橋垣 国子, 桑野 泰代, 小山 鷹二
    1972 年 92 巻 5 号 p. 535-538
    発行日: 1972/05/25
    公開日: 2008/05/30
    ジャーナル フリー
    On the basis of the previous findings, 3-(3-hydroxy-4-methoxyphenyl-3, 4-dihydroisocoumarin (VIII) and β-(3-hydroxy-4-methoxyphenyl) ethylbenzene (XV) were synthesized. Both VIII and XV had a sweet taste whereas VII, XIII, and XIV were all tasteless, suggesting the essential part (XV) of the molecule of sweet 3, 4-dihydroisocoumarins.
  • 青沼 繁, 三村 務, / 乾 容子, YOKO INUI
    1972 年 92 巻 5 号 p. 539-545
    発行日: 1972/05/25
    公開日: 2008/05/30
    ジャーナル フリー
    A serum calcium-decreasing principle was isolated in homogenous state from the culture filtrate of Bacillus subtilis K without damage of its biological activity, using acrylamide gel electrophoresis by means of electrofocusing on Carrier Ampholyte, and it was named α-factor. As a result of chemical analysis, the principle was considered to be a lipoprotein, and 17 kinds of amino acid were detected as the componental amino acids in protein moiety of α-factor. The N-terminal and C-terminal amino acids in α-factor were identified as leucine and serine, respectively. This substance not only lowered the serum calcium level but also increased markedly the inorganic phosphorus level in serum and the citric acid level in blood of a rabbit, and prevented the urinary excretion of calcium in a rabbit. Moreover, the calcium decreasing activity of the radioiodinated α-factor preparation was largely retained the characteristically a large amount of radioactivity was demonstrated in the thyroid, hypophysis, parotid, and submaxillary glands which are related to calcium metabolism in mammals, even at 3 hr after the administration of 131I-α-factor to a rabbit.
  • 田村 恭光, 辻本 信子, 平野 由美
    1972 年 92 巻 5 号 p. 546-550
    発行日: 1972/05/25
    公開日: 2008/05/30
    ジャーナル フリー
    Reaction of various nucleophiles with N-(3-oxo-1-cyclohexenyl) pyridinium chloride (1a), which was prepared from an equimolar mixture of pyridine and 3-chlorocyclohex-2-en-1-one, was examined. Nucleophiles such as sodium hydroxide, aniline, and active methylenes caused N-C bond cleavage of the pyridine ring of Ia, giving glutaconaldehyde derivatives (2, 4 and 6). On the other hand, carbonyl reagents such as semicarbazide, phenylhydrazine, and hydroxylamine attacked the carbonyl group of cyclohexene moiety in Ia, producing Schiff base-type compounds (7).
  • 吉川 正美, 佐藤 善重
    1972 年 92 巻 5 号 p. 551-564
    発行日: 1972/05/25
    公開日: 2008/05/30
    ジャーナル フリー
    Absorption, distribution and excretion of 14C-DL-and 14C-L-DOPA in mice were studied by whole-body autoradiography and liquid scintillation counting. The absorption of L-DOPA from the gastrointestinal tract was more rapid than that of DL-DOPA, the half-life being 14 min for the former and 11 min for the latter. The urinary and fecal excretion of the radioactivity was not significantly different between L-and DL-DOPA. Then amount of radioactivity taken up by mouse brain was slightly more for L-DOPA than that DL-DOPA. When the mouse was treated with α-methyldopa, the uptake of 14C-L-DOPA into the brain, especially into caudate nucleus, increased compared to that in untreated animal. The autoradiograms of cat brain 30 min after administration of 14C-L-DOPA showed that the concentration of radioactivity in caudate nucleus and putamen was especially high but that in white matter was low. The time-dependent autoradiograms of mouse that received 14C-L-DOPA indicated a longer lasting accumulation of radioactivity in adrenal medulla. However, when the mouse was kept in a cold bath, the radioactivity accumulated in adrenal medulla decreased markedly.
  • 上田 武雄, 高田 純, 小林 憲明
    1972 年 92 巻 5 号 p. 565-569
    発行日: 1972/05/25
    公開日: 2008/05/30
    ジャーナル フリー
    Alkaline conversion reaction of D-tartaric acid was investigated. D-Tartaric acid was heated at 130°in potassium hydroxide solution for 10 hr. The reaction mixture was acidified and DL-tartarate was precipitated as a monopotassium salt. To the mothor liquor was added calcium chloride solution and meso-isomer was obtained as a calcium salt. Conversion ratio of this reaction was determined by both gravimetriy and X-ray diffraction, and the reaction in 40% potassium hydroxide solution was optimal for the formation of meso-tartarate. No conversion occured in the reaction using 20% potassium hydroxide solution while oxalate was produced in the reaction using 50% or higher concentration of the reagent.
  • 小澤 光, 村井 繁夫
    1972 年 92 巻 5 号 p. 570-574
    発行日: 1972/05/25
    公開日: 2008/05/30
    ジャーナル フリー
    Pharmacological properties of 3-isopropyl-5, 7-dimorpholinomethyltropolone hydrochloride (IDMT) were examined and it was concluded that the mechanism of the depressor action of IDMT consists of the dilation of the peripheral vessels which is similar to that induced by papaverine, and inhibition of the activity of vasomotor center and negative inotropic action are also further associated with this mechanism. It was also concluded that inhibition to the intestinal smooth muscle by IDMT is weak compared to that of papaverine (about 1/5), but dilating action on smooth muscles of vessels including the coronary vessel is at least five to ten times stronger than the action of papaverine and sodium nitrite.
  • 嶋田 健次, 松本 潮, 長瀬 雄三
    1972 年 92 巻 5 号 p. 575-581
    発行日: 1972/05/25
    公開日: 2008/05/30
    ジャーナル フリー
    The isotope dilution method was established for the determination of d-dethiobiotin. This compound reacts with p-(dimethylamino) cinnamaldehyde (p-DACA) to develop an intense color having an absorption maximum at 533 mμ. By using the proposed isotope dilution analysis in conjunction with the absorbancy and radioactivity, the average recovery rate of d-dethiobiotin and d-biotin from synthetic mixed sample showed as 100.9% for d-dethiobiotin and 100.4% for d-biotin. By this method d-dethiobiotin and d-biotin were determined periodically up to 10 days in the culture filtrate of Aspergillus niger incubated in a medium containing d-dethiobiotin. As the cultivation proceeds, the amount of d-biotin produced increased gradually and reached approximately 14% of the d-dethiobiotin added, which decreased simultaneously. By means of the reverse isotope dilution method, the amount of 3H-d-biotin produced from 3H-d-dethiobiotin (4.67 μmole) was 1.48% for a 2-day incubation and 5.97% for 4 days, as a total yield in the cell and the culture filtrate.
  • 久野 拓造, 西 知行, 市川 正孝
    1972 年 92 巻 5 号 p. 582-587
    発行日: 1972/05/25
    公開日: 2008/05/30
    ジャーナル フリー
    Thiopilinanilides were found to react with anthranilic acid, in the presence of amines, and formed a 4 (3H)-quinazolinone ring in a good yield. In this case, there is a possibility that aromatic primary amines might react first with thiopicolinanilides to form amidines which might take part directly in cyclization to 4 (3H)-quinazolinone. Examinations were therefore made on the reaction of the corresponding N, N'-diphenylpicolylamidines and anthranilic acid, and it was thereby found that amidines show a similar reactivity as thiopicolinanilides and formed 4 (3H)-quinazolinones in almost the same yield. Therefore, thiopicolinanilide and aniline were reacted and formation of amidine during the reaction was examined, and the formation of amidine under the reaction conditions thought to be responsible for the above reaction was only about 11%. Consequently, it was assumed that amidine formation was not an important factor in the said reaction mechanism. Active methyl compounds, aromatic primary amines, and anthranilic acid were reacted in the presence of sulfur to examine direct cyclization to 4 (3H)-quinazolinone and the reaction was found to afford 2-pyridyl-3-phenyl-4 (3H)-quinazolinone derivatives quite easily.
  • 気賀沢 和雄, 五十里 紀子, 飯村 秀樹, 渡部 一夫
    1972 年 92 巻 5 号 p. 588-591
    発行日: 1972/05/25
    公開日: 2008/05/30
    ジャーナル フリー
    Flow property of fluids, including powder and liquid, was examined by using the variable rotating cylinder method. A large difference and similarlity were observed in the rotating speed of samples of powder and liquid in rotation adhering completely to the inner wall of the variable rotating cylinder. Correlation was found between the viscosity of liquid and the rotating speed in some liquids. On the other hand, rotating speed seemed to express a physical value related to the flow property considered to be the deformability against stress other than the viscosity.
  • 小野 泰道, 立脇 信清, 大北 敦彦, 桂 義和
    1972 年 92 巻 5 号 p. 592-598
    発行日: 1972/05/25
    公開日: 2008/05/30
    ジャーナル フリー
    Tissue distribution and gastro-intestinal absorption of tritiated 1-β-D-arabinofuranosylcytosine (AC) were investigated in rats and mice. The concentration of AC in various tissues except in brain decreased rapidly by a pseudo-first-order reaction and coincided with that in blood, while AC in the kidney was 2.5 times higher than in others. Its concentration in the brain was lower than those in other tissues and the concentration curve showed a characteristic pattern that had a peak at 2 hr after intravenous administration. Metabolites of AC were not found in the urine. The absorption of AC by its oral administration to rats was calculated from urinary excretion and was found to be approximately 6%. 1-β-D-Arabinofuranosyluracil (AU) was also present in the urine, although it was not produced in the rat tissues. It became apparent that the transformation of AC to AU occurred mainly by the intestinal microflora. In order to examine the effect of antibiotics on the absorption of AC, antibiotics were orally administered to rats and its absorption increased twice that of the control one.
  • 中垣 正幸, 中村 康彦
    1972 年 92 巻 5 号 p. 599-603
    発行日: 1972/05/25
    公開日: 2008/05/30
    ジャーナル フリー
    When Na2SiO3 and AlCl3 solutions were mixed, the pH of mixed solution at a constant ratio was different according to the order of mixing, but the composition and pH of suspension in water were not different. The composition of the products varied with the mixing ratio of Na2SiO3 to AlCl3. In the case of the mixing ratio below 1.7, aluminum hydrogen silicates were mainly obtained and the ratio of Si/Al in the products became the higher, the lower the mixing ratio was. When the mixing ratio increased from 1.7 to 2.0, aluminum began to be taken into silicate structure and sodium also began to be taken as counter ion of aluminosilicates, so that the products changed from aluminum hydrogen silicates to sodium aluminum aluminosilicates. Above 2.0 of the mixing ratio, all of aluminum was taken into the silicate structure and sodium was taken as the counter ion. As a result, sodium aluminosilicates, Na (AlSi2O6), were obtained. Then the pH of the solution in which Na2SiO3 and AlCl3 were mixed was kept constant by pH-Statt with HCl or NaOH solution. The composition of products synthesized in strong alkaline solution was sodium aluminosilicates, Na (AlSi2O6), which was not affected by the mixing ratio. The composition of the product obtained in weak alkaline solution, however, changed according to the ratio of mixing.
  • 青沼 繁, 三村 務, 久岡 正史, 大谷 正洋, 近藤 覚
    1972 年 92 巻 5 号 p. 604-610
    発行日: 1972/05/25
    公開日: 2008/05/30
    ジャーナル フリー
    A substance promoting the function of toad heart was obtained as an isoelectric precipitate by adjusting pH of the culture filtrate of Bacillus subtilis K to 3.0. The precipitate was purified by chromatography on DEAE-cellulose column and then gel chromatography on Sephadex G-75. The substance was finally isolated by column chromatography over acid alumina. It seemed to be homogeneous by electrophoresis on polyacrylamide gel disc. This substance was found to be a lipoprotein which was derived from the cytoplasmic membrane fraction of the vegetative cells according to immunological examination. This substance increased the 32P-uptake into chick myocardium 2 hr after intraperitoneal injection of 0.5 mg/chick.
  • 中垣 正幸, 半田 哲郎
    1972 年 92 巻 5 号 p. 611-615
    発行日: 1972/05/25
    公開日: 2008/05/30
    ジャーナル フリー
    Disodium lauryl phosphate was synthesized by pyrophosphoric acid method, and the degree of hydrolysis was measured at various initial concentrations, temperatures, and alkali concentrations. The hydrolyzed product, inorganic phosphate, was determined by colorimetry with ammonium molybdate at 660 mμ, but co-existent alkyl phosphate was observed to give a negative effect on the coloration. By applying a suitable correction, the degree of hydrolysis was obtained. It was found that this hydrolysis reaction was a 2nd order, reversible reaction, and the relation between the degree of hydrolysis (x) and reaction time (t) was represented by the following equation : [numerical formula] where k1 is the rate constant of hydrolysis reaction, x is the degree of hydrolysis at equilibrium, co is the initial concentration, and CNaOH is the alkali concentration. The activation energy obtained was 7.48 kcal/mole. It was also concluded that the degree of the hydrolysis would be very low at room temperature.
  • 塩田 順造, 上田 陽, 大倉 洋甫, 百瀬 勉
    1972 年 92 巻 5 号 p. 616-620
    発行日: 1972/05/25
    公開日: 2008/05/30
    ジャーナル フリー
    The reaction products (I, II, III and IV) were separated as their methyl ethers from the color reaction mixture of 2, 4-dinitrophenol with potassium cyanide in aqueous solution, and their chemical structures were elucidated mainly by their spectral properties. III and IV, nitro-substituted 2, 3-dihydro-3-oxo-1H-indazoles, were the main coloring matters in this reaction, and III was found to be formed through the intermediates, I and II (Chart 1). This fact confirmed the previously postulated mechanism of the color reaction between m-dinitrobenzene derivatives and alkali cyanide.
  • 井上 博之, 十倉 一也, 林 利光
    1972 年 92 巻 5 号 p. 621-630
    発行日: 1972/05/25
    公開日: 2008/05/30
    ジャーナル フリー
    A new glucoside, trametoside, was isolated from Trametes dickinsii BERK. (Polyporaceae), besides polyporenic acid C and allied substances, and it was found to be a glucoside mixture formed from tumulosic acid and dehydrotumulosic acid whose C-21 carboxyl group was linked with D-glucose. Almost all the compounds obtained here were a mixture of Δ8 and Δ7, 9 (11) compounds having a side-chain double bond, like trametoside. It was found that these mixtures can be converted to a single Δ7, 9 (11) compound by selective dehydrogenation.
  • 山根 靖弘, 大多和 昌克, 飯郷 正明
    1972 年 92 巻 5 号 p. 631-634
    発行日: 1972/05/25
    公開日: 2008/05/30
    ジャーナル フリー
    4-Nitroquinoline 1-oxide (4-NQO), which is a potent carcinogen, is metabolized to 4-hydroxyaminoquinoline 1-oxide (4-HAQO), 4-aminoquinoline 1-oxide (4-AQO), and 4-hydroxyquinoline 1-oxide (4-(OH) QO) by some microbes and mammalian tissues, but the separation and sensitivity in the determination of 4-NQO and its metabolites are not yet adequate. Therefore, an attempt was made to determine 4-NQO and its metabolites in biological materials more sensitively. 4-NQO was extracted from the homogenized tissue with benzene, and absorption of the extract was measured at 392 mμ by a spectrophotometer. After removal of 4-NQO by benzene, the aqueous layer was washed with chloroform. After addition of ascorbic acid and HCl-ethanol, the aqueous layer was evaporated to dryness under a reduced pressure at room temperature. The metabolites in the residue were extracted with warm ethanol-water (1 : 1) solution. An aliquot of the extract was spotted on a silica gel thin-layer plate, and metabolites were separated by using the upper layer of a mixture of sec-butanolethyl acetate-water (2 : 1 : 1) as the developing solvent. Two main bands having blue fluorescence were detected under UV light. One band having Rf 0.60 was identified as 4-HAQO, the other band of Rf 0.45 contained 4-AQO and 4-(OH) QO. The band corresponding to 4-HAQO was extracted with isobutanol-water, while from the other band 4-AQO and 4-(OH) QO were extracted with isoamyl alcohol and Na2CO3 solution, respectively. The fluorescence intensities of 4-HAQO in isobutanol, of 4-AQO in isoamyl alcohol, and of 4-(OH) QO in Na2CO3 solution were measured at 475 mμ, excited by 375 mμ, at 480 mμ excited by 370 mμ, and at 480 mμ excited by 360 mμ, respectively. Each range of determination for 4-NQO, 4-HAQO, 4-AQO, and 4-(OH) QO was 1-25, 0.05-0.2, 0.02-0.5, and 0.02-0.5μg/ml, respectively.
  • 栗原 藤三郎, 菊地 正雄
    1972 年 92 巻 5 号 p. 635-638
    発行日: 1972/05/25
    公開日: 2008/05/30
    ジャーナル フリー
    The neutral volatile oil of the flower stalk of Petasites japonicus was separated into 17 parts by gas chromatography and the substances corresponding to peaks 6, 8, 14, 3', and 17 were respectively proved to be 3-acetoxy-1-nonene, 1, 4, 7-tridecatrienene, β-bisabolene, p-cymene, and bakkenolide-A. As 3-acetoxy-1-nonene is thought to be the principle of the fragrance of the flower stalk of Petasites japonicus, several kinds of 3-acetoxy-1-alkene and 4-acetoxy-1-alkene were synthesized, comparing their fragrance with that of the neutral component.
  • 気賀沢 和雄, 斎藤 守弘, 飯村 秀樹, 渡部 一夫
    1972 年 92 巻 5 号 p. 639-643
    発行日: 1972/05/25
    公開日: 2008/05/30
    ジャーナル フリー
    A method for determination of the flow property of each powder was studied and a new method better reproducibility was established by evaluating the flow property with the speed of a rotating cylinder when a sample in the variable rotating cylinder (Fig. 1) is completely adhesive to the inner wall of the cylinder. Further, this method is can be used extensively for the determination of flow property of liquids like water, oils, and viscous liquids, and powder such as polysaccharides and inorganic salts. There was a correlation between the rotating speed of the cylinder and the angle of repose. Further, the effect of particle size and shape on the rotating speed of the cylinder was found.
  • 丹野 慶紀, 田上 恵美子, 二木 敬一郎, 佐々木 吉幸
    1972 年 92 巻 5 号 p. 644-648
    発行日: 1972/05/25
    公開日: 2008/05/30
    ジャーナル フリー
    Some experiments were carried out on the mixing properties of medicinal powders and lactose granules of various particle sizes, using radionuclide indium-113m which has a short half life. 113mIn was adsorbed by some medicinal powders such as lactose, crystalline lactose, Hustagin, Mino-Aleviatin, corn starch, and synthetic aluminum silicate. Lactose granules were prepared by the conventional method, using 10% starch paste as a binder, dried, and shifted into six particle sizes of 20-28, 28-35, 35-42, 42-65, 65-100, and 100-200 mesh. Mixing of medicinal powder and lactose was carried out with a YMQ-type dispensing mixer, three times for 5 seconds each. Mixing ratio was 1 : 2, 1 : 1, and 2 : 1 for medicinal powder to lactose granules. Experimental results indicated that the mixing properties were greatly affected by the physical properties of the medicinal powder, and this was especially marked in the case of Mino-Aleviatin and crystalline lactose, whose mixing became worse with increasing particle size of lactose granules. In a mixing ratio of 1 : 2, lactose, corn starch, and synthetic aluminum silicate showed good mixing with 100-200 and 28-35 mesh lactose granules. Mino-Aleviatin, Hustagin, and crystalline lactose showed poor mixing with lactose granules with particle size above 42-65 mesh. In 1 : 1 mixing ratio, lactose, Hustagin, corn starch, and synthetic aluminum silicate showed good mixing with lactose granules of all particle sizes. In 2 : 1 mixing ratio, synthetic aluminum silicate showed a poor mixing. It was concluded from these experiments that the fine granules used for dispensing should be of small particle size of less than 200μ (65 mesh).
  • 坂口 武一, 好光 幸子
    1972 年 92 巻 5 号 p. 649-651
    発行日: 1972/05/25
    公開日: 2008/05/30
    ジャーナル フリー
    Variation in the amount of ATP and GTP in the liver of a rat injected with tetracycline was examined. The amount of ATP was reduced for 3 hr after administration of tetracycline, which indicated the possibility that tetracycline inhibited the synthesis of ATP.
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