YAKUGAKU ZASSHI
Online ISSN : 1347-5231
Print ISSN : 0031-6903
ISSN-L : 0031-6903
106 巻 , 12 号
選択された号の論文の12件中1~12を表示しています
  • 片山 誠二
    1986 年 106 巻 12 号 p. 1069-1083
    発行日: 1986/12/25
    公開日: 2008/05/30
    ジャーナル フリー
    Recent progress in the area of polymer gel is one of the great current research interests. Major and exciting advance can be found in both characterization of a water molecule confined in gel matrix and finding of novel critical phenomena of the ionic gel. In the present review, comprehensive characteristics of free water, bound water and unfrozen water in gel, freezing-thawing mechanism of gel, and effect of molecular void space of gel are referred in the first half, and the reversible, discontinuous volume phase transitions of the ionic gels are outlined in the latter half.
  • 谷口 克, 平林 義雄
    1986 年 106 巻 12 号 p. 1084-1091
    発行日: 1986/12/25
    公開日: 2008/05/30
    ジャーナル フリー
    The immunological and chemical properties of melanoma antigens have been analysed by using C57BL/6 derived B16 melanoma cells. Cytotoxic T lymphocytes or helper T cells involved in the positive immune responses were easily induced by the antigen on the cell surface, whereas soluble melanoma antigens secreted into the culture medium selectively stimulate and induce antigen-specific suppressor T cells. Furthermore, the soluble antigen works as an inhibitor for the blocking of the cytotoxic T cell activity. Therefore, the soluble melanoma antigen stimulates the negative immune response in order for tumor cells to escape from immune system. By using two syngeneic monoclonal antibodies against the soluble melanoma antigens (M2590 and M562), we found that the melanoma antigen was composed of GM3 (NeuAc) in association of proteins. M2590 recognized GM3 carbohydrate moiety with cross-species specificities, while M562 reacts with the protein with species specific melanoma antigenic determinant. M2590 can react with the extracted GM3 from normal cells, not with normal cells expressing GM3 on the cell surface. Thus, this suggests that the tertially structure of GM3 on melanoma cells is different from that of normal cells. Finally, we succeeded in cloning of the genomic deoxyribonucleic acid (DNA) which contains genes encoding melanoma antigen with species specific determinant (M562). The B16-melanoma DNA cosmid libraries were constructed with the shuttle vector pCV103. They were infected into ED8767 E. coli, and then transfected into the human melanoma cell line P-36 by protoplast fusion with polyethylene glycol. The transfectants were selected in the presence of mycophenolic acid, stained with FITC-labeled M562, and selected by FACS. Total DNA was isolated from the transfectants, and the B16 genomic DNA clones were rescued by the in vitro packaging with lysogenic bacterial extracts. pD2-7 (34.8kb) reproducibly expressed M562 determinants in the p-36 human melanoma cells.
  • 門田 重利, 島 岳彦, 菊池 徹
    1986 年 106 巻 12 号 p. 1092-1097
    発行日: 1986/12/25
    公開日: 2008/05/30
    ジャーナル フリー
    Separation of the steroidal components of I-tiam-hong (Nervilia purpurea SCHLECHTER and Nervilia aragona GAUD) and Cordyceps sinensis (BEAK.) SACC., was effectively achieved by reversed-phase high-performance liquid chromatography (HPLC). It was found that HPLC is of great value for the separation and identification of each sterol from complex mixtures.
  • 松田 芳郎, 富永 義則, 田島 泰司, 粟屋 博義, 倉田 啓二, 後藤 洋
    1986 年 106 巻 12 号 p. 1098-1107
    発行日: 1986/12/25
    公開日: 2008/05/30
    ジャーナル フリー
    By a reaction of inodolizine derivatives (9) with tetrachlorocyclopropene (TCCP) in the presence of KOH, 4, 5-bis(2-phenyl-3-indolizinyl)-3H-cycl[3.3.2]azin-3-ones (12) were obtained. 1, 3, 5, 5a-Tetrahydro-2, 3, 5-triphenyl-4H-cycl[3.3.2]azin-4-ones (14) and 2, 3, 5-triphenyl-4H-cycl[3.3.2]azin-4-ones (15) were prepared by a reaction of 9 and α, α'-dibromodibenzylketone (13) in the presence of Fe2(CO)9 or Cu-NaI. The 1H-nuclear magnetic resonance spectral data (CF3COOH) of 15a may be interpreted in terms of the aromatic charactor.
  • 奥田 拓男, 波多野 力, 縣 功, 西部 三省
    1986 年 106 巻 12 号 p. 1108-1111
    発行日: 1986/12/25
    公開日: 2008/05/30
    ジャーナル フリー
    The main polyphenolic compound in the leaves of Perilla frutescens var. crispa, which is responsible to the tannic activity of the leaf extract, was isolated and identified as rosmarinic acid. Contrary to the phenomena observed for geraniin in geranii herba, a decrease in rosmarinic acid by decomposition was not observed when decoction of perillae folium was continued for 70 min, while rosmarinic acid was decomposed to a large extent when collected leaves were dried at the temperature over 50°C. Rosmarinic acid has also been isolated from the spikes of Prunella vulgaris var. lilacina and from the leaves of Glechoma hederacea var. grandis. The high performance liquid chromatography analysis showed that Agastache rugosa, Isodon japonicus and several Mentha species contain fairly large amount of rosmarinic acid.
  • 稲垣 承二, 住田 克己, 吉田 滋, 廣瀬 信吾
    1986 年 106 巻 12 号 p. 1112-1117
    発行日: 1986/12/25
    公開日: 2008/05/30
    ジャーナル フリー
    Concentration of compound AB can be determined by acid base titration from Eq. 1. CAB=[CH-{(KaIND·((1-φ))/φ)+CIND·(1-φ)}]·(1+KaAB/KaIND·φ/((1-φ))) (1) CAB : molar concentration of AB, CIND : molar concentration of indicator, CH : hydrogen concentration of the solution, KaAB : acid dissociation constant of AB, KaIND : acid dissociation constant of indicator, φ : color transition ratio of indicator. In Eq. 1 value of φ can be measured by complementary tristimulus colorimetry (CTS method). Values of CH, CIND, KaAB and KaIND are determined by using an appropriate kind of method before the titration. AB can be determined by setting the values of parameter to the Eq. 1. By this principle aminopyrine (2.2-2.85g) could be determined by adding a prescribed amount of 0.5 N HCl standard solution in ±2% and by using bromphenol blue as a indicator.
  • 石橋 正兀, 渡辺 恵子, 宮崎 浩 /, STEFAN KROLIK
    1986 年 106 巻 12 号 p. 1118-1125
    発行日: 1986/12/25
    公開日: 2008/05/30
    ジャーナル フリー
    A diethylhydrogensilyl-cyclic diethylsilylene (DEHS-DES) derivative of thromboxane B2 (TXB2) methyl ester-methyloxime was prepared by treating with diazomethane, O-methylhydroxyamine and then with N, O-bis(diethylhydrogensilyl)trifluoroacetamide. The gas chromatogram of the reaction product showed a well-resolved doublet when analyzed using a 5% phenylmethylsilicon-cross linked fused silica capillary column, being considered to correspond to syn- and anti-isomers. These components gave the ion of m/z 269 as a base peak or prominent peak and many characteristic ions which reflected the TXB2 system with moderate intensity. The ion of m/z 269 consists of the fragment of DES ring moiety and the α-side-chain. The mass spectrum (MS) of the second eluting component was considerably more complex than that of the first one. Almost all of the fragment ions in the MS of the first eluting component were also observed as characteristics common to the second eluting component. This ion made it possible to utilize internal standards for gas chromatography-selected ion monitoring (GC/SIM), which have been synthesized with deuterium (atom) labels at α-side-chain. Cl(NH3)-MS of these components were much simpler than the corresponding electron impact-MS, and they gave the protonated molecular ion with low intensity and the characteristic fragment ion of [MH-DEHSOH]+ (m/z 480) as the base peak. The 6-keto-PGF methyl ester-methyloxime-DEHS-DES derivative has the same molecular weight as the corresponding derivative of TXB2, but its MS is considerably more simple and lacks an ion of m/z 269 which is typical of aldehydic unit of TXB2 system. This 6-keto-PGF derivative gave a base peak at m/z 157, which was formed by the cleavage of F-prostaglandin ring system with a migration of hydrogen atom at C-10 to C-12. When GC/HR-SIM was carried out at the resolution power of 8000 by monitoring the ion of m/z 269.1573 which was specific for GC/SIM as structural integrity of TXB2, the SIR of its 25 pg of present derivative showed a well-resolved doublet with S/N of more than 300. These facts strongly indicates that the present derivative may be useful for the microanalysis of TXB2 by GC/SIM in biological materials.
  • 上釜 兼人, 前田 照利, 有馬 英俊, 入江 徹美, 平山 文俊
    1986 年 106 巻 12 号 p. 1126-1130
    発行日: 1986/12/25
    公開日: 2008/05/30
    ジャーナル フリー
    Inclusion complex formation of anti-inflammatory drug biphenyl acetic acid (BA) with β-cyclodextrin (β-CyD) in water and in solid state was assessed by solubility method and powder X-ray diffractometry. The release of BA from suppository base in saline was significantly increased by the β-CyD complexation. The serum level of BA after the rectal administration in complex form to rats was higher than that of the drug alone. No appreciable change in irritation of the complex on rectal membrane in rats was obserbed in comparison with that of the drug alone in spite of the increase of bioavailability. The present data suggested that β-CyD seems to be useful for improving the pharmaceutical properties of BA in suppository formulation.
  • 大西 憲明, 横山 照由, 梅田 常雄, 清原 義史, 黒田 勤, 喜多 良昭, 黒田 耕司
    1986 年 106 巻 12 号 p. 1131-1136
    発行日: 1986/12/25
    公開日: 2008/05/30
    ジャーナル フリー
    In order to apply cellulose acetate phthalate (CAP)-polyethylene glycol 4000 (PEG) matrix to the oral sustained-release dosage form, CAP-PEG matrix granules including nifedipine (NF) were prepared by the fusion method. Oral administration of these matrix granules to rabbits resulted in sustained-release characteristics. From the results of the pharmacokinetic study, it was considered that the plasma concentration-time course of NF after oral administration of these matrix granules follows a one-compartment model with instantaneous release and two consecutive first-order input steps. It appeared that in CAP-PEG matrix granules, PEG partly acts as a fast-release compartment and enhances the bioavailability of NF, and CAP controls the release rate of the PEG-entrapped NF. The CAP-PEG matrix appeared to be a suitable carrier of the oral drug-delivery preparation offering sustained-release.
  • 渡辺 和夫, 柴田 昌裕, 矢野 真吾, 蔡 陽, 渋谷 博孝, 北川 勲
    1986 年 106 巻 12 号 p. 1137-1142
    発行日: 1986/12/25
    公開日: 2008/05/30
    ジャーナル フリー
    Effects of 8 extracts (YK-1 to YK-8) from Zedoary [Curcuma aeruginosa ROXB. (=C.zedoaria non ROSCOE)] (Gajutsu) cultivated in Yakushima (Japan) and 7 isolated compounds from the extracts on experimental gastric ulcerations were studied. Oral and subcutaneous administrations of the extracts significantly inhibited stress ulcer formation in restrained and water-immersed mice. A n-hexane soluble fraction (YK-3) was more effective than a methanol soluble fraction (YK-2) of the original methanol extract (YK-1). Among the isolated compounds from subfractions (YK-4, YK-5, YK-6) of YK-3, furanogermenone and (4S, 5S)-(+)-germacrone 4, 5-epoxide had a potent preventive effect against stress ulceration. Moreover, oral administration of YK-3, YK-4 and YK-8 significantly inhibited formation of both HCl-induced and indomethacin-induced gastric ulcers. In experiments on effect of YK-3 on gastric secretion and motility, neither of both functions was affected by antiulcer doses of YK-3. These data show that some of extracts and isolated compounds produce a potent inhibition of acute experimental gastric ulcers, partly through their cytoprotective action.
  • 藤巻 ゆう子, 津村 光義, 立沢 晴男
    1986 年 106 巻 12 号 p. 1143-1145
    発行日: 1986/12/25
    公開日: 2008/05/30
    ジャーナル フリー
    A rapid, simple and sensitive method for the quantitative determination of ticlopidine in the human serum has been developed. Ticlopidine and internal standard (5-(o-fluorobenzyl)-4, 5, 6, 7-tetrahydrothieno[3, 2-c]-pyridine maleate) were extracted from the alkalized serum. After purification on SEPPAK cartridge, the eluate of the cartridge was analyzed by high performance liquid chromatography by using Nucleosil 7C18 as a column packing and a mixture of 1/30 M phosphate buffer (pH 7.0) and acetonitrile (4 : 6) as a mobile phase. The recovery of added ticlopidine was more than 83% and the coefficient of correlation for the calibration curve in the concentration range of 0.06 to 3.53 μg/ml was 0.9998. Coefficients of variation in the same concentration range were 0.2-4.2%. The detection limit was 50 ng/ml in the human serum. It is conceivable that this method is accurate and useful for therapeutic drug monitoring.
  • 今村 順茂, 宮下 英一, 小田切 優樹
    1986 年 106 巻 12 号 p. 1146-1150
    発行日: 1986/12/25
    公開日: 2008/05/30
    ジャーナル フリー
    Salicylic acid markedly reduced the blood concentration of sulfisoxazole after oral administration. On the other hand, salicylamide markedly enhanced the blood concentration of sulfisoxazole after oral administration. In addition, the effects of salicylic acid and salicylamide on sulfisoxazole disposition were examined. The results indicated that salicylic acid affects the processes involved in the absorption and distribution of sulfisoxazole, while salicylamide affects the process involved in the elimination of sulfisoxazole.
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