YAKUGAKU ZASSHI
Online ISSN : 1347-5231
Print ISSN : 0031-6903
ISSN-L : 0031-6903
96 巻, 9 号
選択された号の論文の17件中1~17を表示しています
  • 石塚 泰博, 有吉 敏彦
    1976 年 96 巻 9 号 p. 1049-1056
    発行日: 1976/09/25
    公開日: 2008/05/30
    ジャーナル フリー
    Blood concentration, tissue distribution, and excretion of drugs and drug-metabolizing enzyme activities were examined using 14C-labeled compounds; 5, 5-diphenylhydantoin (14C-DPH) and 2-guanidinomethyl-1-monoazacyclooctane sulfate (14C-EGYT-739) in male rats with a mercuric chloride-induced kidney injury. Carbon-14 radioactivity in blood of kidney-damaged rats was higher than that of the control, and the biological half-life of 14C-DPH in blood was prolonged by kidney injury. Considerably high level of radioactivity was found in the kidney 24 hr after dosing, and the prolongation of half-life was also observed in the damaged kidney of rats. Urinary and fecal excretion of 14C radioactivity were unchanged in kidney injury, whereas biliary excretion was significantly increased 6 to 24 hr after dosing of 14C-EGYT-739, and slightly increased after dosing of 14C-DPH. A single administration of mercuric chloride reduced aminopyrine demethylase and aniline hydroxylase activities in the liver, but did not change cytochrome P-450 and b5 content. However, addition of mercuric chloride at a final concentration of 9.97×10-5M to the microsomal suspension resulted in a partial conversion of cytochrome P-450 to cytochrome P-420.
  • 青沼 繁, 小浜 靖弘, 川野 博子, 和田 昌師, 大塚 悦子, 赤井 邦久
    1976 年 96 巻 9 号 p. 1057-1066
    発行日: 1976/09/25
    公開日: 2008/05/30
    ジャーナル フリー
    During studies on the humoral factor affecting heart function, three different lipoproteins promoting the function of a frog heart, Fr. I-A, Fr. I-B, and Fr. II, were obtained from the calf thymus by extraction with 2 N acetic acid, followed by column chromatography over Sephadex G-25, Sephadex G-50, CM-cellulose, and DEAE-cellulose. The N-terminal amino acids in them were lysine, lysine and glutamic acid, and their molecular weights were 17500, 17500, and 3000, respectively. These lipoproteins increased the 32P-uptake into chick myocardium 2 hr after intraperitoneal injection of 0.5 or 2.0 mg/chick, but did not show any effect on rabbit blood pressure and the kallikrein-like arginine esterase activity. Active principles in molecule of these lipoproteins seemed to be a protein, not lipid. The biological and physico-chemical differences between heart-promoting substances from calf thymus and from myocardium were discussed. Another lipoprotein, Fr. III, promoting an antibody production competence was isolated from the calf thymus. Fr. III increased a hemolytic titer, plaque-forming cells of the spleen, and respiration of spleen cells in neonatally thymectomized mice. The rabbit antiserum against extract from mouse thymus, which possessed the same activity as Fr. III, inhibited the antibody production competence of mouse in vivo.
  • 中垣 正幸, 二宮 宏
    1976 年 96 巻 9 号 p. 1067-1075
    発行日: 1976/09/25
    公開日: 2008/05/30
    ジャーナル フリー
    Effects of methylcellulose and sodium dodecyl sulfate (SDS) on the dispersion and sedimentation bed of Griseofulvin (GR) was examined by the measurement of apparent degree of aggegation (γmo), amount of adsorption (X), ζ-Potential, porosity (ε), and tortxosity (q) of the sedimentation bed. When methylcellulose was added to the suspension prepared in water or SDS solution, γmo and ε decreased and q increased with the increasing amount of methylcellulose added in the case of water and 0.8 mM SDS solution, while each of the above quantities remained constant in 8 mM SDS solution. The ζ-potential in 10 mM NaCl decreased with the increase of methylcellulose, but gave a constant value against methylcellulose in the presence of SDS. The amount of methylcellulose adsorbed decreased with the increase of SDS concentration, and adsorption was not observed in 8 mM SDS solution. When SDS was added to the suspension prepared in water or methylcellulose solution, γmo and ε decreased and q increased with the increasing amount of SDS added in the case of water, while these values showed a maximum value against the SDS concentration at about 2.5 mM in the case of a suspension prepared in methylcellulose solution. The ζ-potential increased with the increase of SDS concentration in water or methylcellulose solution. Amount of SDS adsorbed was almost equal in both water and methylcellulose solution. Vertical tortuosity, qv, showed a higher value than horizontal tortuosity, qM, in all cases, and they were almost equal in concentrated dispersant solxtion. All the data plotted to see the relation between q and ε fell on the same line, showing that q decreased with the increase of ε. qv/qM took the value near 1 and increased with the increase of ε.
  • 宮沢 三雄, 亀岡 弘
    1976 年 96 巻 9 号 p. 1076-1080
    発行日: 1976/09/25
    公開日: 2008/05/30
    ジャーナル フリー
    The steam volatile oil of Polygonum reynoutria MAKINO from Nara Prefecture was examined. The yield of leaf oil was about 0.004%, oil of stem was 0.003%, and that of root stock was 0.005%. The steam volatile oils were separated into individual components by the combination of chemical method and preparative gas chromatography or elution chromatography. Seventy-one compounds in the oil have been characterized.
  • 岡田 寿太郎, 中野 功一, 真崎 規夫, 飯塚 久雄, 寺田 幸正
    1976 年 96 巻 9 号 p. 1081-1084
    発行日: 1976/09/25
    公開日: 2008/05/30
    ジャーナル フリー
    Among the several photoreaction products of 1, 2-cyclohexanedione, the structure of the crystalline compound (IIa) with a molecular formula of C12H18O5 was established as perhydro-2, 3'; 2', 3-diepoxy-1, 1'-biphenyl-2, 3, 3'-triol by means of the X-ray crystallographic analysis. The formation process of this compound was also discussed.
  • 小澤 光, 三浦 力, 佐藤 正
    1976 年 96 巻 9 号 p. 1085-1088
    発行日: 1976/09/25
    公開日: 2008/05/30
    ジャーナル フリー
    In order to observe the membrane property in steroid myopathy, the ouabain-sensitive (Na++K+)-ATPase activities of skeletal muscle, kidney, and brain membrane fractions were studied with the mice administered dexamethasone intraperitoneally for 7.0 -8.5 weeks at a dosage of 5.5 mg/kg. The results obtained were as follows. 1) The body weight of mice treated with dexamethasome for 7.0-8.5 weeks decreased by approximately 5 g (ca. 20% of the control body wt.) against that of saline-treated mice. 2) The ouabain-sensitive (Na++K+)-ATPase activity of skeletal muscle sarcolemmal fraction from the steroid-treated mice was significantly higher than that from control by 30-50%. 3) With kidney and brain membrane fractions, no differences were observed between control and steroid-treated mice in the ouabain-sensitive (Na++K+)-ATPase activity. These results show that the membrane property of skeletal muscle is specifically influenced by the long-term administration of dexamethasone.
  • 西川 洋一, 渡辺 四男也, 瀬戸 隆子, 安田 一郎
    1976 年 96 巻 9 号 p. 1089-1093
    発行日: 1976/09/25
    公開日: 2008/05/30
    ジャーナル フリー
    Two new sesquiterpenoids were isolated from the hexane extract of the rhizome of Atractylodes lancea DE CANDOLLE (Compositae). Their structures were identified as 3β-acetoxyatractylon and 3β-hydroxyatractylon from chemical and spectral data.
  • 吉村 実, 畠田 孝幸, 出来 三男, 杉井 通泰
    1976 年 96 巻 9 号 p. 1094-1102
    発行日: 1976/09/25
    公開日: 2008/05/30
    ジャーナル フリー
    The systematic synthesis and thin-layer chromatography (TLC) of S-substituted thiouracil derivatives were carried out to examine the analytical properties of thiouracils. The Rf values on the TLC plate increased with increasing carbon number of alkyl group in S-substituted thiouracil derivatives, using a solyent system of acetone-benzene-MeOH-28%NH4OH (6 : 2 : 1 : 1). When the copper sulfate-pyridine mixture and of bromine were used as the coloring agent, the spots of purple color appeared very clearly. Subsequently, in order to clarify the relationship between thiouracils and bromine, the reaction chromatography with bromine was carried out. Methylthiouracils on the reaction chromatography plate was separated into some spots using a solvent system of CHCl3-MeOH-28% NH4OH (6 : 3 : 1). Among these spots, two spots were identified as 5-bromo-6-methyluracil (VIIIB) and 5, 5-dibromo-6-hydroxy-6-methylhydrouracil (IXB). 5, 5-Di-bromo-6-methoxy-6-methylhydrouracil (X) was formed by recrystallization of IXB from MeOH.
  • 山崎 和男, 玉木 太郎, 三川 潮, 柴田 承二
    1976 年 96 巻 9 号 p. 1103-1106
    発行日: 1976/09/25
    公開日: 2008/05/30
    ジャーナル フリー
    Paeonol (I) in Paeonia suffruticosa was proved to be the metabolite of shikimic acid via phenylalanine and cinnamic acid. Feeding of 14C-labeled phenylalanine and cinnamic acid to the plants resulted in efficient incorporation of 14C into the corresponding position of I. On the other hand, neither acetate nor malonate was incorporated significantly into I.
  • 中垣 正幸, 宮田 堅司
    1976 年 96 巻 9 号 p. 1107-1113
    発行日: 1976/09/25
    公開日: 2008/05/30
    ジャーナル フリー
    In order to investigate the mobilities of ions in capsule and cellulose membranes, bi-ionic potential was measured, the membrane potential in a system consisting of two electrolyte solutions being in contact across the membrane. The two solutions were the same in concentration but of different kinds and either their cation or anion was in common. The theoretical equations for bi-ionic potential was derived and by using the observed values of bi-ionic potential in a high concentration range, the ratios of ionic mobilities in the membrane were determined as a function of the membrane charge density. These values were different from the corresponding values in aqueous solution. They were also different from the corresponding values which were determined by membrane potential in a similar system that consisted of two same kinds of electrolyte solutions of different concentration. The theoretical values of bi-ionic potential calculated by applying these parameter values to the theoretical equations were in good agreement with the experimental values over all the concentration ranges studied.
  • 坂野 俊行, 天野 為之
    1976 年 96 巻 9 号 p. 1114-1121
    発行日: 1976/09/25
    公開日: 2008/05/30
    ジャーナル フリー
    Primary amines react with homophthalaldehyde in 100% or 50% acetic acid to yield 2-substituted isoquinolinium derivatives which are classified into three groups; group A (excitation (Ex.) at 340 nm, emission (Em.) at 380 nm), group B (Ex. 310 and 350 nm, Em. 400 nm), and group C (Ex. 350 nm, Em. 500nm). Best conditions for determinations of each group were examined, based on the difference in fluorescence characteristics of the reaction products and conditions. Selective and sensitive fluorometric method for determination of benzylamine, sulfanilamide, and p-anisidine with homophthalaldehyde was established. The procedure for this determination is as follows : i) To 2 ml of acetic acid solution of benzylamine, 2 ml of a 40 mg/100 ml reagent solution (homophthalaldehyde in acetic acid) is added, mixed well and heated for 40 min at 60°. The mixture is cooled and diluted to 10 ml with acetic acid, and fluorescence intensity is determined (at Ex. 343 nm, Em. 380 nm). ii) To 4 ml of 50% acetic acid solution of sulfanilamide, 4 ml of a 5 mg/100 ml reagent solution is added, mixed well, and left to stand for 30 min, fluorescence intensity of this solution is determined (at Ex. 304 nm, Em.404 nm). iii) To 4 ml of acetic acid solution of p-anisidine, 4 ml of a 15 mg/100 ml reagent solution is added, mixed well, the mixture is allowed to stand for 20 min, and its fluorescence intensity is measured (at Ex. 350 nm, Em. 478 nm).
  • 池上 清輝, 平野 茂, 今村 博
    1976 年 96 巻 9 号 p. 1122-1126
    発行日: 1976/09/25
    公開日: 2008/05/30
    ジャーナル フリー
    The effect of hexoprenaline (ST-1512), a selective β2-adrenergic stimulant, on the content of cyclicAMP in slices of the lung, liver, and heart of rats and on the activities of adenyl cyclase in them was examined. Maximum increase of cyclicAMP in slices caused by hexoprenaline was observed in order of the lung (300%), liver (230%), and heart (60%), while that with DL-isoproterenol was in the order of the lung (490%), heart (375%), and liver (270%). The concentration (PC50) of hexoprenaline which gives half maximal increase of cyclicAMP was approximately equal to that of isoproterenol in the lung and liver, but was larger than that in the heart. The increase of cyclicAMP content in the liver by hexoprenaline was inhibited by β-blockers such as bufetolol and practolol. Hexoprenaline stimulated adenyl cyclase of the tissues tested. The order of maximum increase in the liver and heart caused by hexoprenaline and isoproterenol was the same as that of the cyclicAMP content in slices, and PC50 of both compounds for the stimulation of adenyl cyclase was close to those of cyclicAMP content in the liver and heat. The stimulation of liver adenyl cyclase by hexoprenaline was blocked by bufetolol. These results suggest that the selective β2-adrenergic stimulating activity of hexoprenaline may be attributable to the increase in cyclicAMP content resulting from the selective stimulation of adenyl cyclase of the tissues which have β2-adrenergic receptors.
  • 中垣 正幸, 二宮 宏
    1976 年 96 巻 9 号 p. 1127-1136
    発行日: 1976/09/25
    公開日: 2008/05/30
    ジャーナル フリー
    The effect of sodium polyacrylate on the aggregation and sedimentation states of griseofulvine (primary particle size γo of 1.2μ) and calcium carbonate γo(of 1.8μ) were studied, in the presence of sodium dodecyl sulfate (SDS), methylcellulose, polyoxyethylenesorbitane oleate (POE-SO), sodium chloride, or polyvinylpyrrolidone (PVP), by measuring degree of apparent aggregation γmo, amount of adsorption (X), and ζ-potential in the suspensions, and by measuring porosity (ε) and tortuosity (q) of the sedimentation bed. Reduced viscosity (ηsp/C) of PANa increased in the presence of MC and decreased in the presence of other additives. Values of γmo and ε showed a maximum on their plots against the concentration of PANa, at 0.0075 g/100 ml for GR, and at 0.005 g/100 ml for CaCO3. This tendency was not affected by the coexisting materials. These values shifted to higher values by the addition of MC at 0.05 g/100 ml, and to lower values by the addition of other materials. Values of γmo.ε, and X decreased, and q and ζ-potential increased with the increase of pH. For both GR and CaCO3, these quantities gave different values when the order of addition of PANa and SDS to the CaCO3 suspension was changed. The adsorption isotherms of PANa on GR and CaCO3 at 25° were of Langmuir type. The ζ-potential was increased with the increase of PANa concentration. In the graph showing the relation between ε and q, all plots fell on the same line. The ratio, of qV/H. which indicates the anisotropy of sedimentation bed, increased with the increase of ε, where qH is the horizonta tortuosity and qv is the vertical tortuosity.
  • 坂口 武一, 藤田 忠男
    1976 年 96 巻 9 号 p. 1137-1142
    発行日: 1976/09/25
    公開日: 2008/05/30
    ジャーナル フリー
    The hindered intermolecular rotation of C-N bond was examined with metal complexes containing uracil. Parameters of rotation were calculated by using the Eyring and Arrhenius equation. From the total line shape analysis by nuclear magnetic resonance spectra, the electronic configuration of the metal complexes was studied. HgCl2-diuracil has two electronic configurations, and their rate constant, coalescence temperature, free enthalpy of activation, and entropy of activation were calculated. It was concluded that the mercury co-ordination hindered the C-N bond rotation. CdCl2-diuracil was isolated from water and it was postulated that the co-ordination atom was C(4)=O. In IR spectra only relatively minor changes occurred in the uracil modes upon binding to CdCl2 and it was cosidered that the frequency of stretching modes involving the C(4)=O increased in the double bond region because of the replacement of a hydrogen bond by a bond to cadmium constraining any motion of the oxygen atom.
  • 奥田 拓男, 毛利 和子, 林 範子
    1976 年 96 巻 9 号 p. 1143-1149
    発行日: 1976/09/25
    公開日: 2008/05/30
    ジャーナル フリー
    The factors which might cause errors upon the relative astringency (RA) determination with hemoglobin, and the ellagitannin determination (RE determination) by coloring with nitrous acid, were examined to establish facile determination methods for tannin. Comparison of the first method with the hide powder method was also carried out. The RA and RE determinations were then applied to the tannin of Geranium thunbergii, and of four other species of Geranium, and also to geraniin, the pure ellagitannin obtained from the formerly reported tannin 1, to give following results : The main constituents of the tannin in these plants are ellagitannins, and the ratios of ellagitannin to the whole tannin in these plants are generally analogous. G. thunbergii collected periodically exhibited the largest amount of tannin in summer, and almost the same ratio of ellagitannin to the whole tannin in this plant all the time. There was practically no difference of the results between this plant of white flower and that of red flower by the two methods. The RA and RE values decrease markedly when G. thunbergii was dried and stored. RA and RE values of geraniin, and of G. thunbergii extract, in boiling water vary only to a small extent within 2 hr.
  • 小澤 光, 弘中 豊
    1976 年 96 巻 9 号 p. 1150-1156
    発行日: 1976/09/25
    公開日: 2008/05/30
    ジャーナル フリー
    Hypotensive activities of dl-2-(3, 4-methylenedioxyphenyl)-2-hydroxyacetamidine hydrochloride (dl-mandelamidine) and its optical isomers were compared and the following results were obtained. (1) The depressor response in rats induced by isoproterenol was hardly affected by dl-, l-, and d-mandelamidine. (2) All of dl-, l-, and d-mandelamidine caused a transient vasodilation of the perfused leg artery of dogs. Vasodilation caused by d-mandelamidine was weaker than that by dl- and l-mandelamidine. l-Mandelamidine caused a transient vasodilation followed by a long-lasting one, while in the case of d-mandelamidine, a slight and transient vasodilation was followed by a slight but continuous vasoconstriction of the perfused leg artery in dogs. (3) In rats pretreated with nialamide (40 mg/kg, s.c.) for 2 days, d-mandelamidine but not dl- and l-mandelamidine caused a long-lasting hypertensive action. (4) In rats pretreated with reserpine (2 mg/kg, i.p.) for 2 days or pretreated with cocaine (5 mg/kg, i.v.), such a phenomenon as observed in (3) was not elicited by d-mandelamidine. (5) Both d- and dl-mandelamidine potentiated the pressor responses of rats and contractile responses of cat nictitating membrane to norepinephrine and epinephrine. In contrast, these responses by norepinephrine and epinephrine were inhibited by l-mandelamidine. The potentiating effect of dl-mandelamidine was weaker than that of d-mandelamidine. On the other hand, the action of tyramine on blood pressure and nictitating membrane was inhibited by these three compounds. (6) From these results it is suggested that a long-lasting hypotensive action of l-mandelamidine is mainly due to the direct dilating action on the peripheral vascular smooth muscle, and the action of d-mandelamidine may be mainly related to the inhibition of catecholamine release from the adrenergic nerve terminals.
  • 上田 陽, 小川 建志
    1976 年 96 巻 9 号 p. 1157-1160
    発行日: 1976/09/25
    公開日: 2008/05/30
    ジャーナル フリー
    Fluorescence and nuclear magnetic resonance spectra of 22 kinds of aromatic o-hydroxy-aldehyde para-substituted benzylidene-hydrazones (Ar(OH)-CH=N-N=CH-Ar'-R) were determined. Fluorescence spectra of these compounds were found to have char-acteristically large Stokes shifts. Both the exciting and emission maximum wavelengths were found to shift to a longer wavelength region as the electron-withdrawing nature of the substituent increases. The emission intensity was also found to depend on the electronic nature of the substituent. The results of the measurement of proton magnetic resonance spectra showed that the substituents exert their mesomeric effect on the whole molecule. Satisfactory linear correlations were obtained between chemical shifts of methine protons of-CH=N-N=CH-groups and the Taft's σR values.
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