YAKUGAKU ZASSHI
Online ISSN : 1347-5231
Print ISSN : 0031-6903
ISSN-L : 0031-6903
92 巻 , 8 号
選択された号の論文の22件中1~22を表示しています
  • 小早川 敬博
    1972 年 92 巻 8 号 p. 919-926
    発行日: 1972/08/25
    公開日: 2008/05/30
    ジャーナル フリー
    Biological activities were examined on sodium chondroitin polysulfate of low molecular weight, which was obtained from natural chondroitin sulfate-C. Some of them demon-strated lipemia-clearing and anticoagulative activities which were examined in hyperlipemic mice and intact rats, respectively. Sodium chondroitin polysulfate (molecular weight, 4000-6000 ; sulfur content, 13-16%) (CPS) has been selected as having the lowest molecular size with high biological activity. Following results were obtained from pharmacological examinations in view of the antiatherosclerotic activity. 1) Oral Treatment : Hypotriglyceridemia associated with activation of lipopretein lipase was observed acutely in intact and hyperlipemic rats. After a 6-month succesive administation, hypotriglyceridemia was recognized, while normal blood coagulation was observed in intact rats treated with CPS. 2) Intraperitoneal Treatment : Fibrinolytic activity, determined by the time of lysis of euglobulin, is elevated in rats treated with CPS. Further, lipotropic activity of CPS was observed from the experiments on CCl4-induced injury of rat liver. From these results, characteristic feature of CPS was also discussed with respect to the antiatherosclerotic properties.
  • 加納 三郎
    1972 年 92 巻 8 号 p. 927-934
    発行日: 1972/08/25
    公開日: 2008/05/30
    ジャーナル フリー
    2-Methylimidazo [2, 1-b] benzothiazole (III1) was prepared in a good yield by heating 2-imino-3-(2-propynyl)-2, 3-dihydrobenzothiazole hydrobromide (II) obtained from 2-aminobenzothiazole (I) and propargyl bromide with two equivalent amounts of sodium ethoxide in ethanol. Three kinds of 2-phenylimidazo [2, 1-b] benzothiazoles (III2-4) were obtained in a good yield by treatment of I with phenacyl bromide in butanol for 2 hr at 110-115°. Thiocyanation of III1-4 was carried out by the bromine method and the urea method, and the corresponding 3-thiocyanato derivatives (IV1-4) were obtained in a good yield. 3-Methylthiazolo [3, 2-a] benzimidazole (VIII) was prepared in a good yield from 2-(2- propynylthio) benzimidazole hydrobromide (VII·HBr) and two equivalents of sodium ethoxide. Thiocyanation of VIII and the corresponding 3-phenyl derivatives (X1-3) did not proceed, the starting materials being recovered, whereas 2-bromo derivatives (XI<1-4>) were obtained in a good yield by bromination of VIII and X1-3.
  • 加納 三郎
    1972 年 92 巻 8 号 p. 935-944
    発行日: 1972/08/25
    公開日: 2008/05/30
    ジャーナル フリー
    6-Methylimidazo [2, 1-b]-1, 3, 4-thiadiazoles (III1, 2) were prepared in a good yield by treatment of 2-amino-1, 3, 4-thiadiazoles (I1, 2) with bromoacetone in H2O for 1 hr at 95-100°. Six kinds of 6-phenylimidazo [2, 1-b]-1, 3, 4-thiadiazoles (VI1-6) were obtained in a good yield by treatment of 2-imino-3-phenacyl-△4-1, 3, 4-thiadiazoles (V1-6) with polyphosphoric acid (PPA) for 2 hr at 135-140°. Thiocyanation of III1, 2 and VI1-6 was carried out by the bromine method and the urea method, and the corresponding 5-thiocyanato derivatives (VII1-8) were obtained in a good yield. The preparation of 5-methylthiazolo [3, 2-b]-s-triazoles (XII1, 2) was effected in a good yield by treatment of 3-(2-propynylthio)-1, 2, 4-triazole hydrobromides (X1, 2) with two equivalents of sodium ethoxide in ethanol, and XII2 was also obtained by treatment of 3-acetonylthio-5-methyl-1, 2, 4-triazole (XII2') with PPA for 2 hr at 140-145°. Six kinds of 5-phenylthiazolo [3, 2-b]-s-triazoles (XIV1-6) were prepared in a good yield by treatment of 3-phenacylthio-1, 2, 4-triazoles (XIII1-6) with PPA for 2 hr at 150-160°. Thiocyanation of XII and XIV did not proceed, whereas the corresponding 6-bromo derivatives (XV1-8) were obtained in a good yield by bromination of XII1, 8 and XIV1-6.
  • ヒキノ ヒロシ, 大泉 康, 竹本 常松
    1972 年 92 巻 8 号 p. 945-950
    発行日: 1972/08/25
    公開日: 2008/05/30
    ジャーナル フリー
    Absorption, distribution, metabolism, and excretion of the insect metamorphosing hormone, ecdysterone, were investigated using its 3H-labeled derivative in mice. 1) When 3H-ecdysterone was administered intraperitoneally, radioactivity in all the organs examined reached the highest level 10 minutes after the administration, and decreased rapidly thereafter. After its oral administration, the initial increase and subsequent decrease of radioactivity in the organs were slow. Accumulation of radioactivity in the liver, blood, and kindeys is much greater after intraperitoneal administration than after oral administration. These findings demonstrate that its absorption from the peritoneum is easy while that from the gastrointestinal tract is poor. 2) 3H-Ecdysterone was selectively distributed in the liver in a high concentration by either route of administration, showing it to be especially concentrated, within the liver by an active transport mechanism. 3) Examination of the subcellular distribution of 3H-ecdysterone in the liver revealed that more than 80% of the radioactivity was present in the supernatant fraction and a small amount of radioactivity in other fractions. 4) In the case of intraperitoneal injection, excretion of tritium into feces and urine was fast, while tritium was excreted slowly when given orally. 5) By either route of administration, radioactivity was found much more in feces than in urine, indicating that 3H-ecdysterone absorbed is excreted mainly from the liver into the intestine via the bile. 6) Examination of radioactive substances present in the liver by means of silica gel thinlayer chromatography revealed that ecdysterone was metabolized fairly rapidly.
  • 高木 敬次郎, 李 殷芳
    1972 年 92 巻 8 号 p. 951-960
    発行日: 1972/08/25
    公開日: 2008/05/30
    ジャーナル フリー
    Pharmacological studies were made on crude platycodin, a saponin fraction extracted from the roots of Platycodon grandiflorum A. DC. The present study is concerned with its acute toxicity and its depressant effect on the central nervous system. From the LD50 values determined, crude platytodin showed much weaker toxicity in oral administration than in intraperitoneal. Local irritation and hemolytic activity were observed. The central depressant effect of crude platycodin was preliminarily shown in behavioral observations of mice. From further investigations, its pharmacological activities in mice were as follows. Its activity on spontaneous movements was significantly depressed in both the climbing test and the hole cross method. Hexobarbital sodium-induced sleeping time was prolonged following its administration, but this result was devoid of statistical significance. Ataxia was very weak in both the rotarod and the inclined plane methods. Marked hypothermic and antipyretic effects were shwon, and analgesic effect on the acetic acid-induced writhing response and on the tail pressure pain was found to be positive, but convulsions induced by electroshock and by pentetrazole were not inhibited by its administration. These findings may be summarized to indicate that crude platycodin has a central depressant effect, showing mainly sedative and analgesic-antipyretic. In addition, the possibility of the existence of anti-inflammatory effect was suggested.
  • 高木 敬次郎, 李 殷芳
    1972 年 92 巻 8 号 p. 961-968
    発行日: 1972/08/25
    公開日: 2008/05/30
    ジャーナル フリー
    Pharmacological studies were made on crude platycodin, a saponin fraction extracted from the roots of Platycodon grandiflorum A. DC., in addition to previous studies which revealed its central depressant effect, mainly sedative and analgesic-antipyretic. Results obtained by the present study were as follows : Crude platycodin significantly inhibited the rat paw edema induced by carrageenin and by acetic acid, and also inhibited significantly the formation of granulation tissue and the arthritis induced by Freund's complete adjuvant in rats. Antianaphylactic effect in mice, as measured by the rectal temperature, was shown following its prolonged administration after the sensitization, whereas the effect was not observed by its single pretreatment just before the challenge. It also decreased significantly the vascular permeability of Pontamine Sky Blue into the mouse peritoneal cavity in anaphylaxis. Its antagonistic effect against contraction induced by histamine and by acetylcholine was identified in the guinea-pig ileum preparation, but no antagonistic effect was observed against serotonin and bradykinin in the rat stomach fundus and uterus, respectively. The time to death in histamine shock of guinea pigs was prolonged by the administration of crude platycodin. It is, therefore, concluded that crude platycodin shows antihistaminic and anticholinergic effects, but not antiserotonin or antibradykinin effect, and has a potent anti-inflammatory effect. A discussion on the possible mechanism of its anti-edematous effect was added.
  • 高木 敬次郎, 李 殷芳
    1972 年 92 巻 8 号 p. 969-973
    発行日: 1972/08/25
    公開日: 2008/05/30
    ジャーナル フリー
    Pharmacological studies on crude platycodin, a saponin fraction extracted from the roots of Platycodon grandifiorum A. DC., were carried out in addition to previous studies which revealed antihistaminic, anticholinergic, and potent anti-inflammatory effect. Results obtained from the present study were as follows : In guinea-pigs, a median antitussive dose (AtD50) of crude platycodin is 6.4 mg/kg, i.p., and the permeability of Evans Blue into the respiratory tract fluid was increased significantly by its divided oral administrations. A transient hypotension, a decrease in heart rate, and depression of respiration were observed by its intravenous administration in anesthetized rats. The femoral and coronary blood flows in anesthetized dogs were considerably increased by its close arterial injections and these effects were found to be more potent than those of papaverine hydrochloride. In the isolated atrium of guinea-pigs, a negative inotropic effect was exhibited only in the high concentrations of crude platycodin, and its antagonism against acetyl-choline was observed. A mydriatic effect, inhibition of intestinal propulsion, and lack of local anesthetic effect were also found. It is, therefore, concluded that crude platycodin has antitussive, expectorant, hypotensive, and vasodilative effects, and the anticholinergic effect was reconfirmed.
  • 庄司 省三, 久保田 幸穂
    1972 年 92 巻 8 号 p. 974-979
    発行日: 1972/08/25
    公開日: 2008/05/30
    ジャーナル フリー
    A parotin-like substance, fraction E-I, was separated in a highly purified form from the bovine parotid gland by mild procedures which comprised isoelectric fractionation, chromatography on CM-and ECTEOLA-cellulose. This substance produced hypocalcemia and leukocytosis preceded by transient leukopenia in rabbits by a single intravenous injection of 0.1 mg/kg. It also elicited depression of the serum acid phosphatase activity at a dose of 0.1 mg/kg. It has a molecular weight of 20000 and contains 33.00% hexose (galactose, glucose) and 18.89% glucosamine. The relation of this substance to other parotin-like substances from bovine parotid gland and human saliva is discussed.
  • 西海枝 東雄, 高井 啓二
    1972 年 92 巻 8 号 p. 980-985
    発行日: 1972/08/25
    公開日: 2008/05/30
    ジャーナル フリー
    5-Nitro-2-furylcarbamoyl derivatives were found to form a colored complex by the action of a strong base. It was assumed from the ultraviolet, infrared, and nuclear magnetic resonance spectra of these colored complexes that the N-proton of the corresponding carbamoyl group is extracted by the action of a strong base and the molecule as a whole becomes an anion to form the complex.
  • 大塚 峯三, 仲村 進, 佐藤 善重
    1972 年 92 巻 8 号 p. 986-996
    発行日: 1972/08/25
    公開日: 2008/05/30
    ジャーナル フリー
    Absorption, distribution, and excretion of 14C-labelled 6, 6, 9-trimethyl-9-azabicyclo-[3, 3, 1] non-3β-yl α, α-di (2-thienyl) glycolate hydrochloride monohydrate (PG-501), which has a potent anti-parkinsonian action, were studied in the rats and mice by means of whole-body autoradiographic procedure and the tracer technique. The orally administered drug reached a maximum plasma level at 30 min in the rat. The time course of absorption showed two phases, a rapid phase with a half-life of about 5.8 min and a slow phase with that of 138 min. The distribution of N-14CH3-PG-501 in the mouse after oral administration showed that the radioactivity was concentrated in tissues of the brain, liver, intestine, lung, Harder's gland, salivary gland, and kidneys. When the drug was administered intravenously to the mouse, high radioactivity was found in the brown fat, salivary gland, Harder's gland, and adrenal cortex. This drug was rapidly taken up in the brain and passed through the placental barrier. Excretion of radioactivity was about 25% in urine, 8% in feces, and 37% in the expired air within 24 hr and about 23% in bile within 6 hr after oral administration of N-14CH3- PG-501 at the dose of 12.5 mg/kg. After intravenous administration of the drug to the rat, the excretion rate was 41% in urine, 8% in feces, and 30% in the expired air during 24 hr, and 26% in bile within 6 hr.
  • 荒田 義雄, 越中 栄一, 川畑 光政, 加藤 日出男
    1972 年 92 巻 8 号 p. 997-999
    発行日: 1972/08/25
    公開日: 2008/05/30
    ジャーナル フリー
    Phenylhydrazone and para-substituted phenylhydrazones of 5-nitrofurfural were subjected to coupling reaction with diazonium salts and the resulting formazan derivatives (II) were treated with sulfuric acid to give some benzotriazine compounds (III). Of these compounds tested, the benzotriazine derivatives, IIIa, IIIb, and IIId, showed relatively intense antibacterial activities.
  • 中垣 正幸, 中村 康彦
    1972 年 92 巻 8 号 p. 1000-1008
    発行日: 1972/08/25
    公開日: 2008/05/30
    ジャーナル フリー
    ξ-Potential of spherical glass particles measured by streaming potential method showed a negative value, and had minimum in 1 mM NaCl concentration. In higher concentration, ξ-value decreased gradually because of the effect of ionic strength. ξ-Potential of glass particles in NaCl solution showed a higher value when the solution contained dodecyl-amine than in its absence, but the value was negative even in saturated solution of dodecylamine. It was confirmed microscopically that the glass particles were smoothly coated with dodecylamine by fusion-dispersion-cooling method and that these were stable in NaCl solution for several hours. As the amount of dodecylamine coating on glass particles increased, ξ-potential increased and reached zero with the thickness of the amine layer of 100-150 Å, and had a maximum point at 400 -500 Å thickness and showed a constant value was found, after gradual decrease with the increasing thickness of the dodecylamine layer. Almost the same value as the maximum value was obtained by electrophoresis method, and, therefore, these particles were regarded to be very densely covered with dodecylamine. The charge density of the surface, σ, and the amount of excessive adsorption of ions to bare glass surface, (△σ/F), were calculated from the Gouy-Chapman equation. With the increasing amount of the coated dodecylamine, σ of coated particles increased to possitive values, in NaCl solution of constant concentration. When the amount of dodecylamine coated on the glass was more than 7 mg/g, σ showed a constant value because only the dodecylamine near the surface of the coated particles was capable of dissociating electrically.
  • 気賀沢 和雄, 清水 弘明, 伊吹 美登里
    1972 年 92 巻 8 号 p. 1009-1016
    発行日: 1972/08/25
    公開日: 2008/05/30
    ジャーナル フリー
    Photometric titration of tertiary amines was examined with Bromophenol Blue (I) as a titrant in benzene. This method depends on the fact that an increase in absorbance at 410 mμ is proportional to the concentration of amines according to equation (1) if I is present in greater concentration than the amine. H2A+B&rlarr;BH+·HA- [BH+·HA-]/[H2A][B]=K1 (1) BH+HA-+B&rlarr;BH+(BH+·A2-) [BH+(BH+·A2-)]/[BH+·HA-][B]=K2 (2) where H2A is I, B is amine, BH+HA- and BH-(BH+·A2-) are (1 : 1) and (1 : 2) compounds, respectively. The effect of (1 : 2) compound on the titration curve was discussed, and the limit of equilibrium constant K1 and the concentration of amine determined. Next, this method was applied to the determination of drugs (amine type) such as chloropromazine hydrochloride, diphenhydramine hydrochloride, etc. These studies led to the conclusion that a minute quantity of amines in benzene (2×10-6M solution) can be easily and accurately determined with 0.0002M of I as a titrant by means of photometric titration if K1 between I and amines is greater than 107 (pK2=8).
  • 成戸 俊介, 金子 秀彦
    1972 年 92 巻 8 号 p. 1017-1023
    発行日: 1972/08/25
    公開日: 2008/05/30
    ジャーナル フリー
    In order to examine the anti-gastric ulcer activity of dehydrocorydaline derivatives, 13-substituted berberine (4a-g) and the partial O-demethylated derivatives of dehydrocorydaline were synthesized. Demethylation of dehydrocorydaline by refluxing with concentrated hydrochloric acid gave a mixture of 2-monophenol (7a), 9-monophenol (7b), and 2, 9-diphenol (7c). The structures of these phenols were deduced from the nuclear magnetic resonance and mass spectra of their tetrahydroderivatives (8a-c). It was found that the chemical shifts of aromatic protons were informative for assinging the position of the phenolic group in 2, 3, 9, 10-substituted tetrahydroprotoberberine alkaloids.
  • 加藤 鉄三, 新妻 卓逸
    1972 年 92 巻 8 号 p. 1024-1029
    発行日: 1972/08/25
    公開日: 2008/05/30
    ジャーナル フリー
    Reaction of 3-acylamido-4-chloro-2, 6-lutidine (Ia-d) with KNH2 in liq. NH3 was carried out and 3-acetamido-(Ia) and 3-benzamido-4-chloro-2, 6-lutidine (Ib) were converted into the oxazolopyridine derivatives (II and V) and 3-acylamido-4-amino-2, 6-lutidine (III and VI), respectively. Similar reaction of 3-phenylacetamido-(Ic) and 3-acetoacetamido-4-chloro-2, 6-lutidine (Id) gave the oxazolopyridine derivatives (VII and XIV) and the pyrrolinopyridine derivatives (VIII and XV), respectively. Acylation of VIII afforded 6-acetyl derivatives (X), and methylation of VIII with methyl iodide gave 1, 3, 5, 7-tetramethyl derivatives (IX). Catalytic reduction of XV with platinum afforded 3-ethyl-3-hydroxy derivatives (XVIII).
  • 許 弘卿, 菊地 豊彦, 青柳 栄, 飯田 英夫
    1972 年 92 巻 8 号 p. 1030-1033
    発行日: 1972/08/25
    公開日: 2008/05/30
    ジャーナル フリー
    Bischler-Napieralski reaction of phenolic amide (V), which was obtained by condensation of 3-benzyloxy-4-methoxyphenethylamine and methyl 2-bromo-4, 5-dimethoxyphenyl-acetate followed by bromination, afforded the isoquinoline derivative (VI), which was further reduced with sodium borohydride to the 1, 2, 3, 4-tetrahydroisoquinoline compound (III). Intramolecular Ullmann reaction of III in the presence of potassium carbonate and cupric oxide in pyridine gave the expected compound (VII) which, on debromination with lithium aluminum hydride, gave dl-cularimine. Similarly, dl-cularine was synthesized from III by subsequent N-methylation, Ullmann reaction, and debromination.
  • 砂田 久一, 中垣 正幸
    1972 年 92 巻 8 号 p. 1034-1038
    発行日: 1972/08/25
    公開日: 2008/05/30
    ジャーナル フリー
    By the use of a spherical model granules having variously sized intergranular interactions, sedimentation layers were formed with spherical and nonspherical granules with different porosity, ε, and the rate for vertical and horizontal directions of this sedimentation layer, qz and qxy, were theoretically calculated. It was thereby found that the rate changed with porosity and that the sedimentation layer was anisotropic in vertical and horizontal directions, even if the granules were spherical. In nonspherical granules, the rate was apparently different from that of spherical granules and the rate changed according to porosity and the ratio of radius (γa) in the direction of rotary ellipsoid to that (γb) in vertical direction to γa, i.e., γba, and the sedimentation layer was also found to have anisotropy in vertical and horizontal directions. When solvation layer is taken into consideration, the effect of solvation layer on rate was found to be greater, the lager the axial ratio.
  • 今村 博, 中村 忠男, 乾 淳, 安田 寛, 大菅 邦男, 竹内 正紀
    1972 年 92 巻 8 号 p. 1039-1051
    発行日: 1972/08/25
    公開日: 2008/05/30
    ジャーナル フリー
    Y-6124, a new adrenergic β-receptor blocking agent, antagonized lipolysis in the isolated fat cells of rats, increase of free fatty acid in rat plasma, and hyperglycemia in mice and rats induced by epinephrine. The compound also possessed an antagonistic activity against response induced by isoproterenol in the duodenum of rats. Y-6124 had a local anesthetic activity, i.e., activities of infiltration, surface and conduction anesthesia. Local anesthetic activity of this compound may contribute to its antiarrhythmic activity. This compound showed a slight diuretic activity, but had no analgenic, anti-inflammatory, or sensitisation activities. Y-6124 did not show any influence on the central and autonomic nervous systems, coagulation and fibrinolysis of the blood, antibody formation, nor estrus cycle in rats, in a dose to expect β-blocking activity of the compound. These results may suggest the possibility of a clinical application of Y-6124 as an adrenergic β-receptor blocking agent.
  • 森田 直賢, 下郡山 正已, 清水 苓夫, 有沢 宗久
    1972 年 92 巻 8 号 p. 1052-1054
    発行日: 1972/08/25
    公開日: 2008/05/30
    ジャーナル フリー
    The presence of two unknown compounds, now named iristectorin B (IIB) and tectoruside (IV), in the rhizome of Iris tectorum Maximowicz (Iridaceae) was reported in a previous paper1) and their nature was examined in the present series of work. The aglycone of iristectorin B (named iristectorigenin B), C17H14O7, mp 153-155°, colorless microneedles, was assumed to be 5, 7, 4'-trihydroxy-6, 3'-dimethoxyisoflavone, and tectoruside, C21H30O13H2O, mp 207-209°, colorless microneedles, was assumed to be acetovanillone-β-D-diglucoside.
  • 出口 正一, 国重 忠男, 屋敷 幹雄
    1972 年 92 巻 8 号 p. 1055-1058
    発行日: 1972/08/25
    公開日: 2008/05/30
    ジャーナル フリー
    Zirconium formed a blue-green complex with Methylxylenol Blue (MXB) in the presence of zephiramine in weakly hydrochloric acid solution, which had an absorption maximum at 627 mμ. Maximum color development of the complex was obtained in the pH range of 1.15-1.35. The calibration curve was linear for 3 -40 μg of zirconium in 25 ml of solution. The molar absorptivity was about 43000 at 627 mμ. The analytical procedure for zirconium was as follows : A sample solution containing 3-40 μg zirconium was taken into 25 ml measuring flask. Suitable amounts of 1N hydrochloric acid, 0.5 ml of 10-2M zephiramine solution, 2.0 ml of 2% acacia gum solution, and 2.5 ml of 0.1% MXB solution were added to it, and the mixed solution was made up to 25 ml with water (final pH 1.15-1.35). The solution was heated in a water bath of 90±2° for 3 min. After cooling for 7 min, the absorbance of the colored solution was measured at 627 mμ against the reagent blank. Many ions did not interfere with the experiment, but bismuth, thorium, hafnium, and iron (III) interfered even when their amount was the same as that of zirconium. The permissible amount of iron(III) was increased by addition of L-ascorbic acid. The sensitivity of the proposed method is better than that of the previous method.2)
  • 1972 年 92 巻 8 号 p. 1058-1060
    発行日: 1972/08/25
    公開日: 2008/05/30
    ジャーナル フリー
  • 藤本 琢憲, 津田 喜典
    1972 年 92 巻 8 号 p. 1060-1061
    発行日: 1972/08/25
    公開日: 2008/05/30
    ジャーナル フリー
    A substance, designated as an active diuretic principle by Kurzen, was isolated from the aqueous extract of Kumis Kutjing and it was proved to be identical with myo-inositiol.
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