YAKUGAKU ZASSHI
Online ISSN : 1347-5231
Print ISSN : 0031-6903
ISSN-L : 0031-6903
107 巻, 1 号
選択された号の論文の12件中1~12を表示しています
  • 立石 満, 富澤 宏樹, 深沢 英雄, 市原 成泰
    1987 年 107 巻 1 号 p. 1-16
    発行日: 1987/01/25
    公開日: 2008/05/30
    ジャーナル フリー
    Mercapturic acids (N-acetylcysteine conjugates) are converted to methylthio-containing metabolites by the action of several enzymes ; deacetylases for mercapturic acids, C-S lyases for cysteine conjugates, aminotransferase for cysteine conjugates, C-S lyase for thiopyruvic acid conjugates, and methyltransferases for thiols. Methylsulfides thus formed are subsequently oxidized to methylsulfoxides or methylsulfones prior to excretion. In some cases methylsulfoxides are susceptible to enzymatic reduction.
  • 藤田 勇三郎, 駒越 圭子, 佐々木 洋子, 上原 郁恵, 奥田 拓男, 吉田 隆志
    1987 年 107 巻 1 号 p. 17-22
    発行日: 1987/01/25
    公開日: 2008/05/30
    ジャーナル フリー
    Inhibitory effects of tannins and related compounds on Cu (II)-catalyzed autoxidation were studied by kinetic and ESR measurements. The order of inhibition was as follows : ellagic acid>quercetin>geraniin>tannic acid>gallic acid>(-)-epicatechin gallate>control=pyrogallol=(-)-epicatechin. Formation constant of Cu (II) complex with tannic acid JP was found to be larger than that with geraniin by the method of Scatchard plot. Therefore, the effectiveness of geraniin over tannic acid JP is attributable to the radical scavenging ability rather than the Cu (II)-blocking ability. Polyphenols of smaller molecules, such as gallic acid and pyrogallol, etc. showed a minor inhibitory effect. The radical scavenging mechanism was supported by the electron spin resonance (ESR) measurements of these inhibitor radicals. The inhibitor with a large inhibitory effect exhibited a stable ESR signal, while polyphenols of smaller molecules exhibited only unstable or no ESR signals. Quercetin, a flavonoid, also showed a stable ESR signal and had a large inhibitory effect. Ellagic acid, in spite of its smaller molecular weight, showed the strongest inhibitory effect and exhibited a large and stable ESR signal.
  • 菊地 正雄, 山内 洋子
    1987 年 107 巻 1 号 p. 23-27
    発行日: 1987/01/25
    公開日: 2008/05/30
    ジャーナル フリー
    Five new iridoids, named syringopicrogenin-A, -B, -C, syrigopicroside-B and -C, have been isolated together with syringopicroside from the leaves of Syringa reticulata (BLUME) HARA, and their structures have been elucidated on the basis of chemical and spectral evidence. Three secoiridoid glucosides have been also isolated from the same extract, and each of the compounds were identified by direct comparison with authentic samples.
  • 川久保 弘, 曾根 孝範, 脇川 耕一, 成田 勉
    1987 年 107 巻 1 号 p. 28-36
    発行日: 1987/01/25
    公開日: 2008/05/30
    ジャーナル フリー
    We reported an interesting anti-inflammatory effect of one of 3-aminoindazole derivatives in the proceeding paper. We wish to report the anti-inflammatory, analgesic and antipyretic effect of 3-aminoindazole derivatives. Several new derivatives of 3-aminoindazole were synthesized. They were examined for their anti-inflammatory effect by the method of anti-inflammatory assays by using carrageenin edema, dextran edema, serotonin edema, histamine edema and bradykinin edema. The analgesic effect in mice was examined by using the acetic acid writhing test and the antipyretic effect in rats was examined with yeast. 3-(3-Morpholinopropylamino) indazole which is a representative compound was found to possess three times more effective anti-inflammatory property with the carrageenin edema than the reference drug, tiaramide and the same analgesic property as tiaramide. 3-(3-Morpholinopropylamino) indazole is thought to possess different mechanism of acidic non-steroidal anti-inflammatory drugs such as indomethacin and mefenamic acid because this compound inhibited the hind paw edema induced with histamine, serotonin, bradykinin and dextran. It was found that this compound at 50mg/kg, p.o. was as effective in its antipyretic action as indomethacin at 10mg/kg, p.o. Among other 15 new derivatives, 3-[3-(2, 6-dimethylpiperidino) propylamino] indazole was also found to possess a similar degrees of anti-inflammatory, analgesic and antipyretic effect as 3-(3-morpholinopropylamino) indazole.
  • 澤井 弘行, 角 由貴江, 蔵野 聡子, 権平 栄, 加藤 敬香, 冨安 郁子, 今泉 貞雄, 金田 研司, 矢野 郁也
    1987 年 107 巻 1 号 p. 37-45
    発行日: 1987/01/25
    公開日: 2008/05/30
    ジャーナル フリー
  • 蔵野 聡子, 杉本 信子, 角 由貴江, 澤井 弘行, 加藤 敬香, 金田 研司, 矢野 郁也
    1987 年 107 巻 1 号 p. 46-52
    発行日: 1987/01/25
    公開日: 2008/05/30
    ジャーナル フリー
    Five glycolipids (GM-1, GM-2, GM-3, GM-4 and GM-5) were isolated from slightly acid-fast bacterium, Rhodococcus terrae. They were identified as trehalose dimycolate (GM-4), trehalose monomycolate (GM-5), glucose monomycolate (GM-3) and two newly isolated glycolipids (GM-1 and GM-2), respectively. Gaschromatography-mass spectrometry analysis revealed that the new glycolipids contained long-chain alcohols. Total carbon numbers of mycolic acid moieties of the glycolipids, similarly to other lipids, were ranging from C52 to C62 with three or four double bonds and C14 or C16 α-chain carbon numbers. After intravenous administration of the glycolipids to ICR mice in W/O/W emulsion, granulomatous changes were observed in the lungs and spleen, although they showed differences in potency depending on their sugar and acyl moieties. The toxicity of the glycolipids, indicated by the decline of body weights, were highly correlated to lung granuloma formation, but not to spleen granuloma formation.
  • 山田 千秋, 中桐 信夫, 醍醐 晧二
    1987 年 107 巻 1 号 p. 53-59
    発行日: 1987/01/25
    公開日: 2008/05/30
    ジャーナル フリー
    The fibrinolytic activity in the presence of sodium alginate was examined. The inhibitions of fibrin degradation by plasmin were observed by the fibrin agar plate method or the dissolution method of fibrin suspension. The same result was obtained by testing the fibrin agar plate made from the fibrinogen and thrombin or the solubility of the fibrin clot made from fibrinogen and thrombin in the presence of sodium alginate. The solubility of clot prepared from euglobulin in the rat plasma was prolonged. The effect of sodium alginate on fibrinolysis was very weak compared with that of tranexamic acid. The hydrolytic activities of plasmin against substrate S-2251 and TAME were not inhibited by sodium alginate. This result suggests that the antifibrinolytic effect of sodium alginate may be based on the interaction of fibrin or fibrinogen and sodium alginate.
  • 李 文昇
    1987 年 107 巻 1 号 p. 60-64
    発行日: 1987/01/25
    公開日: 2008/05/30
    ジャーナル フリー
    Core protein of molecular weight of 24 kilo dalton (p24) was prepared from detergent extracts of HTLV-1 by affinity chromatography with a monoclonal antibody, FR24. 1) FR24 antibody precipitated specifically core protein p24 from lysates of HTLV-I or TCL-Kan cells labeled with [35S] cysteine, and precipitated p36 and p53 from lysates of labeled TCL-Kan cells. 2) By FR24 antibody-affinity chromatography, p24 was from HTLV-I lysates in approximately 17% yields. 3) The purified material gave a single band on SDSPAGE and reacted specifically with ATLA-positive sera and FR24 antibody by western blotting analysis. 4) Standard curve for measurement of core protein p24 was obtained by sandwich ELISA using purified material, and the linear working range was from 0.1 to 10μg/ml. 5) MT-2 cell lysates contained core protein p24 higher than other HTLV-I producer cells, and the HTLV-I negative cell lines did not contain core protein p24.
  • 杉山 正, 安田 公夫, 今枝 憲重, 古沢 玉彦, 山添 喜久雄, 水上 勇三
    1987 年 107 巻 1 号 p. 65-69
    発行日: 1987/01/25
    公開日: 2008/05/30
    ジャーナル フリー
    In connection with our studies on the determination of isosorbide dinitrate (ISDN), a high sensitive determination of isosorbide 5-mononitrate (5-ISMN) in the human plasma was developed by using electron capture detector gas chromatography on a silicone OV-101 fused silica capillary column. 5-ISMN was extracted with ether from the plasma and reacted with acetyl chloride. This method provided linear calibration curve ranging 1 to 50ng/ml and the limit of detection was 1ng/ml in the human plasma. The measurement of plasma concentration of ISDN and 5-ISMN after a single oral administration of ISDN tablet and a single application of sustained-release ISDN tape by our method were satisfactory. Thus, this method was applicable to pharmacokinetic studies of ISDN preparations.
  • 太田 節子, 桜井 信子, 井上 隆夫, 篠田 雅人
    1987 年 107 巻 1 号 p. 70-75
    発行日: 1987/01/25
    公開日: 2008/05/30
    ジャーナル フリー
    The radiation protection against mice radiated with soft X-ray of lethal dose was studied by use of 58 kinds of crude drugs, 12 kinds of essential oil and 9 kinds of fatty oil. As a result of these study, survival effects to foeniculi Fructus, Corydalis Tuber, Astragali Radix, Coptidid Rhizoma, Grycyrrhizae Radix, Dioscoreae Rhizoma, Cnidii Rhizoma, Atractylodis Rhizoma, Polygoni avicularis Herba and Oleum Sesami were observed.
  • 藤吉 俊夫, 飯田 博之, 村上 元哉, 植松 利男
    1987 年 107 巻 1 号 p. 76-81
    発行日: 1987/01/25
    公開日: 2008/05/30
    ジャーナル フリー
    The inhibitory effects of EB-382, a non-steroidal antiinflammatory agent, on platelet aggregation and prostaglandin biosynthesis were studied. EB-382 exhibited a dose-dependent inhibitory effect on the collagen and arachidonic acid-induced rabbit platelet aggregation in vitro, and its IC50 values were 231.2 and 116.1μM, respectively. The efficacy of EB-382 was about twice less potent than that of ibuprofen. EB-382 exhibited a dose-dependent inhibitory effect on the collagen-induced rat platelet aggregation ex vivo, and its ED50 value was 62.5mg/kg, p.o. The efficacy of EB-382 was about twice less potent than that of ibuprofen. EB-382 did not affect the ADP-induced platelet aggregation both in rabbits in vitro and rats ex vivo. EB-382 inhibited dose-dependently the arachidonic acid-induced pulmonary thrombotic mortality in mice, and its ED50 value was 62.9mg/kg, p.o. The efficacy of EB-382 was about twice less potent than that of ibuprofen. EB-382 exhibited a dose-dependent inhibition of prostaglandin synthetase activity, and its IC50 value was 1.9×10-4M. The efficacy of EB-382 was about 10 times less potent than that of ibuprofen. These results indicate that EB-382 affect platelet aggregation through the inhibition of the prostaglandin biosynthesis, but its efficacy on the platelet aggregation is fairly less potent, comparing with its inflammatory, analgesic and antipyretic activities.
  • 高橋 雅行, 中陳 静男, 篠田 雅人
    1987 年 107 巻 1 号 p. 82-85
    発行日: 1987/01/25
    公開日: 2008/05/30
    ジャーナル フリー
    The inhibitory effects of ketoconazole and various steroids against Δ16-C19-steroid synthesizing activity and 17α-hydroxylase activity in testicular microsomes of neonatal pig were investigated. Against these two enzyme activities in microsomes ketoconazole showed a concentration-dependent inhivitory effect and 50% inhibition concentration against the above two enzyme activities was about 0.6μM. Moreover, various steroids had a similar inhibitory effect against both of these activities, and 20α-hydroxypregn-4-en-3-one and 20β-hydroxypregn-4-en-3-one showed strong inhibitory effects. In the reconstitutional system consisting cytochrome P-450 (17α-hydroxylase/lyase), P-450 reductase, cytochrome b5, ketoconazole or 17α-hydroxyprogesterone showed similar inhibitory effects against these two enzyme activities. The inhibition constants (Ki) of ketoconazole to Δ16-C19-steroid synthesizing activity and 17α-hydroxylase/lyase were 0.22μM and 0.11μM, respectively. On the other hand, the Ki values of 17α-hydroxyprogesterone against the both activities were 15.7μM and 11.6μM, respectively.
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