YAKUGAKU ZASSHI
Online ISSN : 1347-5231
Print ISSN : 0031-6903
ISSN-L : 0031-6903
107 巻, 4 号
選択された号の論文の11件中1~11を表示しています
  • 有田 隆一, 宮崎 克巳
    1987 年 107 巻 4 号 p. 249-261
    発行日: 1987/04/25
    公開日: 2008/05/30
    ジャーナル フリー
    This paper reviews the researches on the intestinal absorption mechanisms of ionized drugs such as β-lactam antibiotics, quaternary ammonium compounds, and tertiary amines. Although these compounds revealed an ionized form in the gastrointestinal tract, absorption from the intestine was well or rapid, and it has been pointed out that a specialized transport system participated in these absorption processes. As a specialized intestinal absorption mechanism of zwitter ionic β-lactam antibiotics the carrier-mediated transport related to dipeptide absorption and the binding to the intestinal mucosa are discussed. In the case of quaternary ammonium compounds and tertiary amines various absorption systems including the binding to the gastric mucin, active secretion to the intestinal lumen, correlation with choline transport, binding to the brush border membrane, and participation of electrical potential difference across brush border membrane are reviewed.
  • 吉川 和子, 竹本 常松, 在原 重信
    1987 年 107 巻 4 号 p. 262-267
    発行日: 1987/04/25
    公開日: 2008/05/30
    ジャーナル フリー
    New saponins, named gypenosides LXVIII (1), LXIX (2), LXX (3) and LXXI (4) were isolated from the aerial parts of Gynostemma pentaphyllum MAKINO collected in Miyagi pref. On the basis of chemical and physicochemical evidence, they were characterized as follows : 1, 2α, 3β, 12β, 20 (S), 25-pentahydroxydammar-23-ene 3-O-β-sophoroside-20-O-β-primeveroside : 2, 3β, 12β, 20 (S), 25-tetrahydroxydammar-23-ene 3-O-β-sophoroside-20-O-β-primeveroside : 3, 3β, 12β, 20 (S), 26-tetrahydroxydammar-24-ene 3-O-β-sophoroside-20-O-β-primeveroside : 4, 3β, 12β, 20 (S), 24 (S)-tetrahydroxydammar-25-ene 3-O-β-sophoroside-20-O-β-primeveroside.
  • 小瀬木 幸司, 石塚 泰博, 澤田 全宏, 嶋村 浩, 市川 テル, 佐藤 誠, 柳沼 英哉
    1987 年 107 巻 4 号 p. 268-273
    発行日: 1987/04/25
    公開日: 2008/05/30
    ジャーナル フリー
    A series of 3-benzoylacrylic acids and the related propionic acids were prepared and evaluated for antiallergic activity in the rat passive cutaneous anaphylaxis (PCA) assay. Several analogues of the 3-(4-substituted benzoyl) acrylic acids exhibited significant activity by oral administration, while none of the corresponding propionic acids were active. Structure-activity relationships were discussed.
  • 北川 静香, 西部 三省, 馬場 久衛
    1987 年 107 巻 4 号 p. 274-278
    発行日: 1987/04/25
    公開日: 2008/05/30
    ジャーナル フリー
    It was revealed that the fruits of Forsythia koreana NAKAI (Oleaceae) contain four phenylpropanoid glycosides, suspensaside, β-hydroxyacteoside, forsythiaside and acteoside. Antibacterial activity of phenolic compounds isolated from Forsythia fruits and the aqueous extracts of the fruits were examined. Four phenylpropanoid glycosides and the aqueous extracts of the fruits of Forsythia suspensa showed high antibacterial activity against Staphylococcus aureus TERASHIMA.
  • 新井 賢, 藤本 憲二, 橋本 竹二郎, 滝島 常雄, 小屋 佐久次
    1987 年 107 巻 4 号 p. 279-286
    発行日: 1987/04/25
    公開日: 2008/05/30
    ジャーナル フリー
    In order to identify the constituents of ethanol-extractable amino acids from Pinus densiflora SIEB. et ZUCC. leaves, high performance liquid chromatography (JASCO TWINCLE amino acids analyzer system) was used. According to the results obtained, ethanol-extractable amino acids confirmed to be such 19 different kinds, as Asp, Thr, Ser, Asn, Glu, Gln, Pro, Gly, Ala, Val, Met, Ile, Leu, Tyr, Phe, Lys, His, Arg and γ-aminobutyric acid (GABA). There was a seasonal fluctuation in the amount of free amino acids constituent, and three different patterns of changing in the amount were noticed. The major constituents of free amino acids were found to be GABA and Ala. There were similarities in the patterns of free amino acids contents among new buds, one year leaves and two year leaves. However few amount of Met and His were detected from the stage of the new buds than any other. Basic amino acids were found more in the one year leaves and the two year leaves than in the new buds. The contents of Gln, Lys and Arg increased in the germination stage of the new buds, and the contents of GABA, Pro, Ala and Asn decreased in the growing stage of the new shoots. The above facts lead to the conjecture of that these free amino acids were involved deeply in the growth of Pinus densiflora SIEB. et ZUCC. leaves.
  • 湯田 康勝, 平野 文也, 田中 淳子
    1987 年 107 巻 4 号 p. 287-293
    発行日: 1987/04/25
    公開日: 2008/05/30
    ジャーナル フリー
    The peroxidation of lipids in rat liver and the activities of the related enzymes, such as superoxide dismutase (SOD), glutathione peroxidase (GSH-Px), were studied by means of adjuvant induced arthritis. The injection of adjuvant into rats was found to be associated with a transient increase of lipid peroxidation in the liver. However, the level of lipid peroxides rapidly diminished. This diminution of lipid peroxidation was shown to be neither related with the GSH-Px nor with the SOD activity. The level of lipid peroxides in the liver was found to be not correlated with that in the serum. The decrease of lipid peroxidation in the liver seemed to have some relations to the inflammatory process on adjuvant arthritis. Principal component analysis of these parameters was carried out. It was suggested that the inflammatory process of adjuvant arthritis can be divided into three stages. Namely, the first stage (day 4-14) which represents an acute phase ; the second stage (day 14-56) which represents a subacute phase, or so-called secondary lesions ; and the third stage (day 56-70) which represents the chronic, or stationary phase of the inflammatory process.
  • 仲井 由宣, 山本 恵司, 寺田 勝英, 小口 敏夫, 山本 勝
    1987 年 107 巻 4 号 p. 294-300
    発行日: 1987/04/25
    公開日: 2008/05/30
    ジャーナル フリー
    Benzoic acid and aspirin crystals were mixed with various kinds of light anhydrous silicic acid (LASA), having different surface areas, and the state of the medicinals in the mixtures was investigated by using differential scanning calorimetry, powder X-ray diffractometry and infrared spectroscopy. It was found that benzoic acid and aspirin became amorphous in the mixtures with LASA at a low concentration level of the medicinals, and that the larger the specific surface area, the higher the ratio of an amorphous state to a crystalline state. The adsorption of the medicinal molecules on the surface of LASA is considered to be a possible mechanism for this phenomena. Hydrogen bonding between medicinal molecules and Si-OH groups of LASA may play an important role on the adsorption. The stability of aspirin in the mixtures was also investigated at 0 and 79% relative humidity at 50°C. The decomposition of aspirin in the mixtures was faster than that of the aspirin crystal. Aspirin in the silica gel mixture had the fastest decomposition rate among the tested samples, due to the adsorption and condensation of aspirin molecules in capillaries of silica gel.
  • 芝本 伸二, 西村 民男
    1987 年 107 巻 4 号 p. 301-307
    発行日: 1987/04/25
    公開日: 2008/05/30
    ジャーナル フリー
    3-Alkylthio- and 3-hydrazino-1, 2, 4-triazines were synthesized and examined for their antiviral activities against influenza virus A2/Adachi strain in the chorio-allantoic membrane culture. 3-Alkylthio-1, 2, 4-triazines exhibited weak inhibitory and relatively strong virucidal activities. The most active 3-hexylthio- and 3-octylthio-6-methyl-5-phenyl-1, 2, 4-triazines showed the virucidal activity at a concentration of 0.32 μg/ml. Similarly to 3-alkylthio derivatives, 3-(substituted benzylidenehydrazino)-6-(4-chlorophenyl)-1, 2, 4-triazines exhibited weak inhibitory and relatively strong virucidal activities. The most active compounds were 3-(4-acetaminobenzylidenehydrazino)- and 3-(9-chloro-10-anthridenehydrazino)-6-(4-chlorophenyl)-1, 2, 4-triazines, and they showed a 50% virucidal concentration of 0.51 μg/ml. 3-Hydrazino-1, 2, 4-triazines exhibited weak inhibitory and virucidal activities. 3-Isopropylidenehydrazino-1, 2, 4-triazines exhibited relatively strong inhibitory and virucidal activities. 5-Methyl-6-phenyl derivative showed a 50% inhibitory concentration of 6.25 μg/ml and 6-methyl-5-phenyl derivative exhibited a 50% virucidal concentration of 0.1 μg/ml.
  • 金庭 延慶, 大塚 誠, 市川 順一, 林 哲男, 林 健児, 梅沢 修
    1987 年 107 巻 4 号 p. 308-314
    発行日: 1987/04/25
    公開日: 2008/05/30
    ジャーナル フリー
    The dissolution behaviour of indomethacin (IMC) polymorphs, pure α and γ forms prepared by the method described in our previous paper, was investigated in detail. The solubility of α form was larger than that of γ form, and the heats of solution of α and γ forms obtained by the relationship between the solubility and temperature were 8.91 and 9.50 kcal/mol, respectively. The dissolution rate was measured by two methods, stationary disk and rotating disk methods. The heat of dissolution obtained by measurement of the initial dissolution rate at various temperatures was almost the same as that obtained by the two dissolution methods. The apparent dissolution rate constant, Kapp, the rate constants of interfacial chemical reaction and of transport process, Kr and Kt, and the diffusion coefficient, D were determined, and the activation energies of the interfacial chemical reaction and of the transport process were calculated by analyzing the values of Kr and Kt, respectively. The activation energies of the transport process of α and γ forms were the same value, 2.0 kcal/mol, and the activation energy of the interfacial chemical reaction of α form was larger than that of γ form. These results suggested that the dissolution of IMC proceeds with two processes of reaction and diffusion. Further, the laminar and turbulent flow were discussed in comparison with the two dissolution methods.
  • 田中 稔幸, 梅村 和志, 飯沼 宗和, 水野 瑞夫
    1987 年 107 巻 4 号 p. 315-317
    発行日: 1987/04/25
    公開日: 2008/05/30
    ジャーナル フリー
    2', 5, 7-Trihydroxy-(1), 2', 3', 5', 7-tetrahydroxy-(2), 2', 5-dihydroxy-6, 7, 8-trimethoxy-(4), 2', 5, 5'-trihydroxy-6, 7, 8-trimethoxyflavone (5) and 2', 5, 6', 7-tetrahydroxyflavanone (3), isolated from Scutellaria baicalensis, were synthesized to confirm their proposed structures. The respective synthetic flavonoids were in good agreement with the corresponding natural flavonoids.
  • 桑山 知成, 加藤 節子, 八代 有
    1987 年 107 巻 4 号 p. 318-322
    発行日: 1987/04/25
    公開日: 2008/05/30
    ジャーナル フリー
    Chemical species of flurazepam in an acidic aqueous solution (0.5 N DCl) were studied by means of carbon-13 nuclear magnetic resonance (13C-NMR) spectroscopy. Flurazepam was present in the form of a protonated iminium structure immediately after preparation of the solution, and subsequently underwent hydrolysis of the iminium moiety to give a ring-opened benzophenone structure, which was in equilibrium with the ring-closed iminium structure. The proportion of the benzophenone structure in the equilibrium solution was greater than that of the iminium structure. The carbon-13 signals of these compounds and of the corresponding aminobenzophenone derivatives isolated under strongly acidic conditions were assigned.
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