YAKUGAKU ZASSHI
Online ISSN : 1347-5231
Print ISSN : 0031-6903
ISSN-L : 0031-6903
99 巻, 6 号
選択された号の論文の23件中1~23を表示しています
  • 篠田 雅人, 太田 節子, 早瀬 幸俊
    1979 年 99 巻 6 号 p. 551-555
    発行日: 1979/06/25
    公開日: 2008/05/30
    ジャーナル フリー
    Protective effect of 2-mercaptoethylamine against skin injury in mice by whole-body irradiation of soft X-ray of 30 kVp was measured to examine conditions for potency test with protective effect as an index, and the following results were obtained. 1) Intraperitoneal administration of 2.0-0.25 mmol/kg of 2-mercaptoethylamine in mice showed a significant protective effect on the head and dorsum, at a dose of 1.0 mmol/kg. 2) The optimum period of the administration of 2-mercaptoethylamine was found to be 30-5 min before irradiation. 3) Potency test with skin injury as an index calls for the measurement of protective potency on skin injury from the score obtained by observations during 40 days after irradiation of 4000-7000 R of soft X-ray of 30 kVp, 10 mA.
  • 杉浦 道治, 濱田 喜樹
    1979 年 99 巻 6 号 p. 556-563
    発行日: 1979/06/25
    公開日: 2008/05/30
    ジャーナル フリー
    Reaction of 4-bromo-2-cyano-1, 3-dimethoxy-1, 2, 3, 4-tetrahydroisoquinoline with aniline (or diethylamine), in the presence of a phase-transition catalyst, results in fascile formation of 4-anilino (or diethylamino)-2-cyano-1, 3-dimethoxy-1, 2, 3, 4-tetrahydroisoquinoline. Application of sodium borohydride to this compound in ethanol afforded 4-anilino (or diethylamino)-2-methyl-1, 2, 3, 4-tetrahydroisoquinoline in a high yield. Use of methylmagnesium iodide in place of sodium borohydride produced 4-anilino-2-cyano-1-methyl-1, 2-dihydroisoquinoline and 4-anilino-1-methylisoquinoline. It was clarified from these products that the reduction of N-C≡N group passed through a diaminomethane derivative.
  • 中垣 正幸, 半田 哲郎, 大橋 佳代子
    1979 年 99 巻 6 号 p. 564-569
    発行日: 1979/06/25
    公開日: 2008/05/30
    ジャーナル フリー
    DSC curves of mixtures of synthetic L-dipalmitoyl phosphatidylethanolamine (DPPE) and water were measured for samples prepared in various conditions. The various kinds of phase transitions were detected and the values of transition temperature and transition enthalpy were obtained from the DSC curves. Between 30° and 145°, there are three lyotropic polymorphs, each with several thermotropic polymorphs. In the case of anhydrous DPPE, there is a quasi-stable noncrystalline solid phase which is easily annealed to a crystalline phase. In the case of mixtures, there are two hydrous forms of DPPE which have the hydration number of 1 and 8 respectively. On the basis of these results, the phase diagram of DPPE-water system was drawn.
  • 岡田 寿太郎, 福森 義信, 平井 淑子, 山根 洋子
    1979 年 99 巻 6 号 p. 570-575
    発行日: 1979/06/25
    公開日: 2008/05/30
    ジャーナル フリー
    During the compaction in a die with a single-punch, the particles of potassium chloride powders cause fracture and fragmentation, and these phenomena are recognised even by the naked eye. On the photomicrographs of the surfaces in contact with upper and lower punches, the particle contact-area was measured. A significant relationship (Eq. (5)) was obtained between punch pressure and the ratio of actual contact-area to total surface area. Using Eq. (5), the radial distribution of the vertical pressure on the two surfaces was determined. This contact-area method is suitable for pharmaceutical powder beds, which are soft and water-soluble. On the surfaces in contact with the upper punch, the pressure distribution curves had the maximum value at the periphery, and they crossed at the average punch pressure of 1000 [kg/cm2]. As the thickness of the tablets increased, the gradients of these curves were intensified. On the surfaces in contact with the lower punch, the curves had the maximum value at the center, and the shape of the curves did not change on increasing tablet thickness.
  • 相本 太刀夫, 増田 千春, 村田 敏郎
    1979 年 99 巻 6 号 p. 576-582
    発行日: 1979/06/25
    公開日: 2008/05/30
    ジャーナル フリー
    Disposition of 3H-labelled clofluperol (3H-CLO) following oral dosage was studied in Wistar male and female rats. Urinary and biliary excretion of 3H was greater in males than in females, while tissue radioactivity examined was, in general, somewhat higher in females than in males. Only a small amount of unchanged CLO was excreted in urine, bile and feces, and the major urinary metabolite of CLO was identified as p-fluorophenaceturic acid. Selective accumulation and prolonged retention of radioactivity were observed in the exocrine and endocrine glands such as salivary gland, pancreas, adrenal and ovary, and in the liver and kidney. Most tissue radioactivity in male rats tested was found in the unchanged CLO fraction. In regional distribution study of CLO in male rat brains, radioactivity was evenly distributed except for the pituitary in which comparatively high radioactivity was found during the initial 4 hr after administration.
  • 影井 健吾, 池田 信, 里 忠, 緒方 善武, 豊島 昭二, 松浦 信
    1979 年 99 巻 6 号 p. 583-587
    発行日: 1979/06/25
    公開日: 2008/05/30
    ジャーナル フリー
    Cullus tissues were induced from the shoot of Duboisia leichhardtii F. MUELL (Solanaceae) on R-2-V agar medium supplemented with casein (0.2%) and 6-benzyladenine (0.5 ppm). Cultured cells were obtained from R-2-V liquid medium without cytokinin. Terpenoids (ubiquinone and triterpenoids) in cultured cells and intact plant were examined and compared. Main ubiquinone in cultured cells and intact plant was identified as ubiquinone-10 by the high performance liquid chromatography method. Ubiquinone-10 content in cultured cells (50-80 μg/g dry wt.) was higher than in intact plant (12.6 μg/g dry wt.). Triterpenoids in cultured cells and medium were different from intact plant. Triterpenoids in cultured cells and medium were identified as lupeol and phytosterols, on the other hand, ursolic acid, oleanolic acid, 3-keto-oleanolic acid, acetylursolate, and phytosterols were obtained from intact plant.
  • 久保 一夫, 伊藤 徳樹, 磯村 八州男, 僧都 勲, 有馬 英樹, 本間 弘茂, 村上 増雄
    1979 年 99 巻 6 号 p. 588-597
    発行日: 1979/06/25
    公開日: 2008/05/30
    ジャーナル フリー
    3- or 4-Substituted N-alkyl-6-chloro-2 (1H)-pyridones (II) were prepared from the corresponding 6-chloro-2 (1H)-pyridones (I) by alkylation. 4-Substituted N-aryl-6-halo-2 (1H)-pyridones (XII) were prepared by the condensation of N-arylpropiolamide with diethyl malonate followed by the treatment with phosphorous oxychloride and hydrolysis. II and XII were converted to 2 (1H)-pyridone derivatives having amino (III, XVIII), alkoxy (IV, XIX) or alkylthio (V) group at 6-position. Their anti-inflammatory activity and analgesic activity were examined by the inhibition of carrageenin foot edema and acetic acid writhing. Some of them showed strong activities as anti-inflammatory and analgesic agents.
  • 浅川 直樹, 服部 禎一, 上山 政晤, 篠田 愛信, 三宅 康夫
    1979 年 99 巻 6 号 p. 598-601
    発行日: 1979/06/25
    公開日: 2008/05/30
    ジャーナル フリー
    A method was established for the quantitative determination of paeoniflorin in Paeony extract by high performance liquid chromatography. Paeoniflorin can be separated using a μ-Bondapak C18 column with a mobile phase (CH3CN : H2O : CH3COOH=15 : 85 : 1) at ambient. Paeony extract contains paeoniflorin as the main ingredient, and albiflorin, oxypaeoniflorin and benzoylpaeoniflorin. Paeoniflorin cannot be determined exactly by the gas liquid chromatography method by separating it from other sub-ingredients. While high performance liquid chromatography methods, such as the absolute and the gradient method, have been reported for the determination of paeoniflorin, comparison of our method with others revealed that the present method is superior due to simplicity, analytical time and accuracy.
  • 栗原 藤三郎, 菊地 正雄
    1979 年 99 巻 6 号 p. 602-606
    発行日: 1979/06/25
    公開日: 2008/05/30
    ジャーナル フリー
    The essential oils of the flowers and leaves of Anthriscus sylvestris HOFFM. were examined. Phenol, o-cresol, eugenol, β-myrcene, d-limonene, γ-terpinene, p-cymene, benzyl alcohol, phenethyl alcohol, l-linalool, β-farnesene and d-sabinyl acetate were identified from the flowers, and phenol, cresol (o-, m-, p-), guaiacol, eugenol, p-cymene, α-pinene, β-myrcene, d-limonene, γ-terpinene, terpinolene, β-farnesene, cis-3-hexen-1-ol, benzyl alcohol, phenethyl alcohol, d-sabinyl acetate, l-α-fenchyl acetate and chrysanthenyl acetate were identified from the leaves. It was found that d-sabinol was converted into p-cymene and β-thujone when preserved in CHCl3, CCl4 and others, and by treatment with methanolic potassium hydroxide chrysanthenyl acetate into 4, 6, 6-trimethyl-3-cyclohexenecarbaldehyde. Luteolin, apigenin and caffeic acid were isolated from the flowers, and desoxypodophyllotoxin, stigmasterol, β-sitosterol, n-paraffins, n-alcohols, fatty acids and esters were isolated from the flowers and leaves.
  • 池北 雅彦, 守屋 寛, 森脇 千秋, 瑠璃川 崇
    1979 年 99 巻 6 号 p. 607-611
    発行日: 1979/06/25
    公開日: 2008/05/30
    ジャーナル フリー
    A modified method to purify the anti-bradykinin substance from beet roots was established and its strong inhibitory effects on some biological activities of bradykinin both in vitro and in vivo experiments were examined. The final purest preparation gave a single spot on silica gel thin-layer chromatograms and inhibited bradykinin 70.8 μg per A280 by means of measuring contraction of the isolated guinea-pig ileum. It was concluded that this anti-bradykinin substance in beets must be norepinephrine or its related catecholamine, judging from the results obtained regarding its chemical and other properties.
  • 山原 條二, 壬生 寛之, 沢田 徳之助, 藤村 一, 白川 清治, 吉川 雅之, 北川 勲
    1979 年 99 巻 6 号 p. 612-617
    発行日: 1979/06/25
    公開日: 2008/05/30
    ジャーナル フリー
    The anti-inflammatory actions of Mi-saponin, which was isolated from the seeds of Madhuca longifolia L. and whose structures are closely related to those of the saponins of Senega and Polygala, were compared with those of two standard drugs, phenylbutazone and β-escin which is the saponin mixture present in the seeds of Aesculus hippocastanum L. (1) Mi-saponin was found to have anti-edematous action on carrageenin edema and inhibitory actions against increased vascular permeability, cotton pellet granulation and peritonitis-induced inflammatory exudate. (2) The anti-inflammatory actions of Mi-saponin were nearly equal to those of β-escin, whereas the actions of Mi-saponin were weaker than those of phenylbutazone in general. (3) In some cases the concurrent use of Mi-saponin with phenylbutazone exerted anti-granulation action stronger than that of the individual compounds.
  • 中垣 正幸, 嶋林 三郎, 早川 栄治, 小槻 節
    1979 年 99 巻 6 号 p. 618-627
    発行日: 1979/06/25
    公開日: 2008/05/30
    ジャーナル フリー
    The amounts of both Ca2+ and Na+, x and y, respectively, bound to C-type chondroitin sulfate (Chs) from an aqueous solution of CaCl2 mixed with NaCl were obtained by the membrane equilibrium method. To estimate x and y under the effect of the Donnan equilibrium, [Ca2+] and [Cl-] for both sides of the dialysing tube and [Chs] for the inner side were analysed. The binding isotherm for Ca2+ was of the Langmuir type, and both x and kCa2+, the binding constant for Ca2+, decreased with ionic strength, J. On the other hand, the binding isotherm for Na+ was not of the Langmuir type but its shape was explained as the competitive adsorption of the two components, Na+ and Ca2+, because Ca2+ binds more strongly to Chs than Na+ and, therefore, the effect of coexistence of Ca2+ with Na+ cannot be neglected when the Na+ binding is examined. It was also suggested that y and kNa+ decreases with J when the amount of the occupied site by the Ca2+ is kept constant at x. The degree of the ionization, z, of Chs was found to be 0.40-0.41 for Na2Chs and 0.20-0.21 for CaChs by this membrane equilibrium method assuming x+y+z=1. These values coincide with those obtained from the vapour pressure osmometry by the authors and with the literature values calculated with considering the Manning theory.
  • 宮本 茂敏, 重岡 叡, 黒野 昌庸
    1979 年 99 巻 6 号 p. 628-632
    発行日: 1979/06/25
    公開日: 2008/05/30
    ジャーナル フリー
    (3RS)-4-Amino-3-hydroxybutanamide (III) was prepared from epichlorohydrine in high yield. Resolution of racemic 4-amino-3-hydroxybutanamide (III) to optically active (3R)-4-amino-3-hydroxybutanamide (VII) and (3S)-4-amino-3-hydroxybutanamide (VIII) was performed by fractional crystallization of corresponding salts with (1R)-camphor-10-sulfonic acid and (1S)-camphor-10-sulfonic acid in 61.6% and 55.4% yield, respectively. To confirm the optical purity of these amides, (VII, VIII) were converted by hydrolysis on a resin into (3R)-4-amino-3-hydroxybutanoic acid (XI) and (3S)-4-amino-3-hydroxy-butanoic acid (XII).
  • 宮本 茂敏, 重岡 叡, 黒野 昌庸
    1979 年 99 巻 6 号 p. 633-641
    発行日: 1979/06/25
    公開日: 2008/05/30
    ジャーナル フリー
    (3RS)-4-Amino-3-hydroxybutananilide (XI) was synthesized from diketene in 71.8% yield. Resolution of the compound (XI) was carried out with (2R, 3R) (+)-tartaric acid or (2S, 3S) (-)-tartaric acid. Hydrolysis of optically active (3S)-4-amino-3-hydroxy-butananilide (XI3) and (3R)-4-amino-3-hydroxybutananilide (XIR) on the strongly acidic resin afforded the corresponding (3S)-4-amino-3-hydroxybutanoic acid (XS) and (3R)-4-amino-3-hydroxybutanoic acid (XR) in 95% yield.
  • 宮本 茂敏, 黒野 昌庸
    1979 年 99 巻 6 号 p. 642-646
    発行日: 1979/06/25
    公開日: 2008/05/30
    ジャーナル フリー
    (3RS)-4-Amino-3-hydroxybutanoic acid (II) is a racemic compound, and direct resolution of this compound (II) is impossible. Then (3RS)-4-amino-3-hydroxybutanoic acid was converted into a racemic mixture as the corresponding salt of m-xylenesulfonic acid. Resolution of (3RS)-4-ammonio-3-hydroxybutanoic acid m-xylenesulfonate could be accomplished by selective crystallization. Optically active (3R)-4-ammonio-3-hydroxybutanoic acid m-xylenesulfonate (IR) and (3S)-4-ammonio-3-hydroxybutanoic acid m-xylensulfonate (IS) were converted by treatment of resin into (3R)-4-amino-3-hydroxybutanoic acid (IIR) and (3S)-4-amin -3-hydroxybutanoic acid (IIS).
  • 坂井 進一郎, 高山 広光, 岡本 敏彦
    1979 年 99 巻 6 号 p. 647-656
    発行日: 1979/06/25
    公開日: 2008/05/30
    ジャーナル フリー
    Reinvestigation of the alkaloidal constituents of Aconitum japonicum THUNB. of Mt. Takao (Tokyo) was made. In addition to the reported constituents, i.e. isohypognavine, delcosine and dehydrodelcosine, two known compounds, isotalatizidine and condelphine, were isolated. Furthermore, five new bases, i.e. 11-acetylisohypognavine, diacetylisohypognavine, 14-acetyltalatizamine, takaosamine and takaonine, were isolated and their structures were elucidated. Takaosamine was proved to be 18-O-demethyldelcosine from the spectroscopic study on the parent material and the acetyl derivatives, and from the chemical correlation with known diterpene alkaloids, gigactonine and delsoline. The structure of takaonine was deduced to be 2, 3-dehydro-14-dehydrodelcosine on the basis of 13C-nuclear magnetic resonance spectral evidence and the derivation to the known diterpene alkaloid, delcosine, by catalytic hydrogenation.
  • 飯沼 宗和, 松浦 信
    1979 年 99 巻 6 号 p. 657-662
    発行日: 1979/06/25
    公開日: 2008/05/30
    ジャーナル フリー
    5, 2'-Dihydroxy-6, 8-dimethoxyflavone (I), 5, 2'-dihydroxy-7, 8-dimethoxyflavone (II), 5, 2'-dihydroxy-6, 7-dimethoxyflavone (III), and 5, 2'-dihydroxy-6, 7, 8, 6'-tetramethoxyflavone (IV) were prepared in order to confirm the proposed structures for skullcapflavone I and II isolated from the roots of Scutellaria baicalensis GEORGI. The structure of IV was identified with that of skullcapflavone II, but the spectral properties of skullcapflavone I were different from those of I or III, being coincident with those of II. Therefore the structure of skullcapflavone I should be corrected to II. The generalization of cyclization of 2'-benzyloxy-dibenzoylmethanes, which are the precursors of 2'-hydroxyflavones, in the presence of conc. H2SO4, was also considered.
  • 柴田 丸, 藤井 三映子, 山口 良二
    1979 年 99 巻 6 号 p. 663-668
    発行日: 1979/06/25
    公開日: 2008/05/30
    ジャーナル フリー
    F I (precipitate), F II (sugar fraction, mol. wt.>10000) and F III (sugar fraction, mol. wt. 5000-10000) were obtained by further purification of a water-soluble fraction (crude Folin) extracted from Sasa albomarginata MAKINO et SHIBATA (Bambusaceae). Acute toxicity and pharmacological effects were examined mainly with F III in small animals. F III showed no apparent toxic effect in mice. It effected a significant decrease of rat dextran edema by topical administration. However, oral administration effected a decrease in the early and an increase in the later stage of rat dextran edema. Antagonistic effect was also observed against contraction induced by serotonin and nicotine in the isolated guinea-pig ileum. The therapeutic effect on rat stress ulcer was in the potency order of F III>F II>F I. F II and F III had no antibacterial effect. No remarkable effects were observed in surface anesthesia of guinea-pig carrageenin edema and urinary excretion of rats treated with F III. Furthermore, F II showed a slight antitumor effect against S180A in mice.
  • 佐野 洋, 中垣 正幸
    1979 年 99 巻 6 号 p. 669-673
    発行日: 1979/06/25
    公開日: 2008/05/30
    ジャーナル フリー
    Sodium chondroitin sulfate, as a mucopolysaccharide, shows the effects of ionizable sulfate and carboxyl groups of the polyelectrolyte on selective counter ion binding. When the electrolytes were added to its aqueous solution, pH decreased due to counter ion binding to the chondroitin sulfate ion. The decrease of pH with the addition of the electrolyte was in the sequence of Li+<Na+<K+<NH4+ for 1 : 1 electrolytes and Sr2+<Co2+<Mg2+<Ni2+<Cd2+ for 2 : 1 electrolytes. When sodium chloride was added to the chondroitin sulfate of various degrees of neutralization, the values of the apparent dissociation constants for the carboxyl group of chondroitin sulfate increased with the increase of sodium chloride concentration. It is concluded that metal ion and hydrogen ion bound competitively to the carboxyl group of chondroitin sulfate ion, and that the difference in the decrease of pH, which depends on the kind of metal ion, is due to the difference in the binding affinity of the metal ions to the carboxyl group.
  • 山口 秀夫, 有本 正生, 山本 起巳子, 沼田 敦
    1979 年 99 巻 6 号 p. 674-677
    発行日: 1979/06/25
    公開日: 2008/05/30
    ジャーナル フリー
    Four kinds of lignans were isolated from the seeds of Hernandia ovigera L. collected in Okinawa besides the previously reported desoxypodophyllotoxin (I). Oily substance II, named bursehernin, C21H22O6, was confirmed to be lignan-2 isolated from Bursera schlechtendalii. III, mp 171-173°, and IV, mp 125-126°, were determined as desoxypicropodophyllin and podorhizol obtained from Podophyllum emodi WALL. respectively. V, mp 270-275°, could not be clarified due to its small amount.
  • 岡田 敏史, 中垣 正幸
    1979 年 99 巻 6 号 p. 677-682
    発行日: 1979/06/25
    公開日: 2008/05/30
    ジャーナル フリー
    Electric conductivity in aqueous solutions of two phenothiazine (PTZ) dihydrochlorides, which are fluphenazine (FPZ)·2HCl and perphenazine (PPZ)·2HCl, and of hydroxyzine (HXZ)·2HCl, which is not phenothiazine (Table IV), was measured at various temperatures in order to elucidate the aggregation of diprotonated phenothiazine (PTZH22+). The plots of Λ-(I)1/2 showed upper shifts from the estimated value. From the concentration dependence of pH for their salt (B·2HCl) solutions, it was observed that this upper shift was the result of acid dissociation of BH22+ ion. By the determination of the first acid dissociation constant (pKa), concentration of each ionic species at a salt concentration was calculated, and limiting equivalent conductivity, λ1°, of BH+ and BH22+ ion was estimated by Stokes'law. Total specific conductivity, k, of the solutions were estimated by Eq. (6), assuming that the present salt solutions were composed of 3 kinds of strong electrolytes, B·2HCl, B·HCl, and HCl. The concentration dependence of k for FPZ·2HCl solutions at various temperatures agreed well with the calculated ones, if λ°FPZH22+ were estimated to be 2 times of λ°FPZH+. On aqueous FPZ·2HCl and PPZ·2HCl solutions, apparent critical micelle concentration (cmc') was determined by a break point in the pH-concentration plots. Based on the assumption that each aggregate was composed of monoprotonated phenothiazine (PTZH+) alone, cmc of each PTZH+ was estimated. It was suggested that the estimated cmc was reasonable in comparison with that of chlorpromazine and triflupromazine.
  • 赤田 良信, 河野 貞子, 後藤 正子, 棚瀬 弥一郎
    1979 年 99 巻 6 号 p. 683-687
    発行日: 1979/06/25
    公開日: 2008/05/30
    ジャーナル フリー
    A rapid estimation of phyllodulcin (Phy.) and hydrangenol (Hyd.) in sweet hydrangea (Hydrangea serrata var. Thunbergii) by the use of high-speed liquid chromatography is described. Phy. and Hyd. are separated by the 25 cm column of Zorbax CN, using a Shimadzu-Du Pont LC-2 liquid chromatograph with water-tetrahydrofuran (60 : 40, v/v) as an eluent, and is completed within 15 min. Phy. and Hyd. in the crude drugs is extracted with methanol and the extract is injected into the column. Accuracy in this method was found to be less than ±2%.
  • 赤田 良信, 河野 貞子, 棚瀬 弥一郎
    1979 年 99 巻 6 号 p. 687-690
    発行日: 1979/06/25
    公開日: 2008/05/30
    ジャーナル フリー
    A rapid sensitive method using high-speed liquid chromatography was devised for the determination of ascorbic acid 2-sulfate (AsS) in human urine and rat plasma. Separation was achieved within 15 min on a Permaphase ODS column (50 cm), using gradient from 0.04 w/v% cetyltrimethylammonium bromide to CH3CN as an eluant with a Shimadzu Du Pont LC 2 liquid chromatograph. AsS in human urine and rat plasma was determined by this method, and the peak was identified as AsS from ultraviolet absorption spectra and thin-layer chromatography. The limit of detection was 1μg in 1 ml human urine or rat plasma. Accuracy in this method was about ±2%.
feedback
Top