巻号一覧
109 巻, 9 号
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瀬崎 仁1989 年 109 巻 9 号 p. 611-621
発行日: 1989/09/25
公開日: 2008/05/30
ジャーナル フリーSome recent advances pertaining to the biopharmaceutical aspects of drug delivery are briefly given, followed by a review of the current status of the application of soluble macromolecular carriers for drug delivery. The dextran conjugates were selected as model compounds to demonstrate the implications of the biopharmaceutical approach in the design, evaluation, and delivery of macromolecular conjugates.抄録全体を表示PDF形式でダウンロード (1163K) -
野本 明男1989 年 109 巻 9 号 p. 622-635
発行日: 1989/09/25
公開日: 2008/05/30
ジャーナル フリーMolecular genetic studies of the antigenicity and the attenuation phenotype of type 1 poliovirus were described. Antigenic sites were identified on the genome of type 1 poliovirus by the determination of nucleotide sequence of the genome of variants that were not neutralized by the neutralizing monoclonal antibodies. The solution of the crystal structure of poliovirus revealed that all mutations found as above are located at the surface of the virion and cluster into three distinct sites. These regions probably represent distinct antibody binding sites. To study expression of the attenuation phenotype of type 1 poliovirus, a number of recombinant polioviruses were constructed in vitro by using infectious complementary deoxyribonucleic acid clones of the virulent Mahoney and attenuated Sabin 1 strains of type 1 poliovirus. Biological tests including a monkey neurovirulence test were performed on the recombinants. The results indicated that the 5'noncoding region harbors a relatively strong determinant influencing the attenuation. Further studies revealed that an adenine residue (Mahoney type) at nucleotide position 480 importantly contribute to the expression of the neurovirulence phenotype. However, a guanine residue (Sabin 1 type) at position 480 was not sufficient for full expression of the attenuation phenotype encoded by this genome region. These results suggested that the expression of the attenuation phenotype depends on the highly ordered structure formed in the 5'noncoding sequence and that the formation of such a structure is possibly influenced by the nucleotide position 480. To investigate the structure and function of the 5' noncoding region, many insertion and deletion sequences were introduced into the genome region. Replication processes of the mutants were analysed and second-site mutations in the genome of the variants that partially restored the phenotypes of the parental viruses were identified. The results indicated that interactions between different loci, for example at around positions 200 and 500, are important for maintaining the viral replication efficiency.抄録全体を表示PDF形式でダウンロード (1730K) -
岩田 稔夫, 鶴田 峯生, 出水 賢一, 磯部 正雄, 高松 陸男, 横部 哲朗1989 年 109 巻 9 号 p. 636-641
発行日: 1989/09/25
公開日: 2008/05/30
ジャーナル フリーThe urinary metabolites of sodium 4-[α-hydroxy-5-(1-imidazolyl)-2-methylbenzyl]-3, 5-dimethylbenzoate (Y-20811) in dog were investigated. The main metabolite was isolated by high performance liquid chromatography and subsequent preparative thin layer chromatography. The structure of this metabolite was established as 4-[α-hydroxy-2-hydroxymethyl-5-(1-imidazolyl) benzyl]-3, 5-dimethylbenzoic acid on the basis of spectral analyses and confirmed by its total synthesis.抄録全体を表示PDF形式でダウンロード (642K) -
今野 昌悦, 渡辺 亮, 山中 宏1989 年 109 巻 9 号 p. 642-649
発行日: 1989/09/25
公開日: 2008/05/30
ジャーナル フリーThe reaction of 2, 4-dimethylthieno [2, 3-d] pyrimidine (1) with benzaldehyde in acetic anhydride resulted in exclusive formation of the 4-styryl compound. Similar site-selectivity of the two methyl groups was observed on the nitrosation of 1 with propyl nitrite in acidic conditions, on the oxidation of 1 with selenium dioxide, and on the bromination of 1 with bromine in chloroform. In the respective reactions, the 4-functionalized products were obtained selectively in reasonable yields. In order to confirm the structures of the products obtained by the above reactions, alternative syntheses were additionally investigated.抄録全体を表示PDF形式でダウンロード (821K) -
原 昭二, 安藤 達彦, 中山 義之1989 年 109 巻 9 号 p. 650-655
発行日: 1989/09/25
公開日: 2008/05/30
ジャーナル フリーA high performance liquid-liquid partition chromatographic system involving two immiscible liquid phases, water and a binary organic solvent, was made from a slurry packed silica gel column, operated by a droplet current to pump the organic solvent equilibrated at the same time as the water and a ultraviolet detector provided with a flow-type cell. The binary organic solvent, water saturated and containing diethyl ether or ethanol in n-hexane as a phase system was used for the measurement of the retention indices of lipophilic components in biological substances such as cholesterol esters, lipophilic vitamins and steroid hormones. The molecular structure of each solute was found to be correlated to its respective retention index by a linear relation between the logarithm of the capacity ratio and that of solvent composition in the mobile phase solvent. The retention data thus obtained were directly related to the liquid-liquid distribution coefficient and thus applicable to making the better selection of an appropriate optimum phase system for use in solvent extraction processes.抄録全体を表示PDF形式でダウンロード (598K) -
渡辺 善照, 本郷 秀二, 松本 光雄1989 年 109 巻 9 号 p. 656-661
発行日: 1989/09/25
公開日: 2008/05/30
ジャーナル フリーTransdermal permeation of drug across the excised skin of Asian pond loach (Misgurnus anguillicaudatus CANTOR) was studied in vitro. Ten kinds of drugs, D-glucose, L-glucose, sucrose, salicylic acid, cefazolin, urea, antipyrine, naphazoline, propranolol and enviomycin were permeated through the excised loach skin, whereas dextran, a polysaccharide, could not be permeated through the skin. The observed transdermal flux (J), the slope of the line obtained from plots of the cumulative amount of drug permeated vs. time, increased as the drug concentration in the donor compartment solution (50→300mM), as the temperature of the skin (test solution) increased (4→37°C), or as the molecular weight of compound decreased. These results suggested that the transport of drug across the loach skin was due to the passive diffusion mechanism. The effect of pH on the permeation of drug could not be elucidated since the loach skin was drastically impaired below pH 5.0. The J values of antipyrine and naphazoline varied in proportion to the drug concentration in the donor compartment solution at time zero (C0). The permeability constants (Kp, cm·H-1) of antipyrine and naphazoline were 12.9×10-2 and 9.2×10-2, respectively. However, the J values of salicylic acid and urea were not proportional to C0 in high concentration (300 mM). Probably, these results were related to the irritative effect of salicylic acid or urea on the skin.抄録全体を表示PDF形式でダウンロード (690K) -
中沢 憲一, 藤森 観之助, 井上 和秀, 関田 節子, 高仲 正1989 年 109 巻 9 号 p. 662-671
発行日: 1989/09/25
公開日: 2008/05/30
ジャーナル フリーEffects of extract from a herb, Cnidium rhizome (Senkyu), on isolated guinea pig atria were investigated pharmacologically and electrophysiologically. The methanol extract from Cnidium rhizome decreased the contraction and slightly increased the heart rates of the isolated atria. Extracts from five other herbs, such as Japanese anglica root (Toki), Peony root (Shakuyaku), Moutan bark (Botanpi), Glycyrrhiza (Kanzo), Bupleurum (Saiko), affected neither the contraction nor the heart rates. The methanol extract from Cnidium rhizome was fractionated with chloroform and water fractions. The chloroform fraction exerted potent negative inotropic and chronotropic effects in isolated atria. The contraction was attenuated by two major components in the chloroform fraction, ligustilide and senkyunolide, but the heart rates were scarecely affected by these components. The chloroform fraction induced changes in resting potentials and configurations of normal action potentials recorded in the isolated left atria : the resting potentials were depolarized, and the upstroke velocity of the action potentials decreased. Neither ligustilide nor senkyunolide exerted such effects. The upstroke velocity of action potentials recorded in partially depolarized atria was reduced by the chloroform fraction as well as ligustilide and senkyunolide. The mechanisms underlying the effects of the extract from Cnidium rhizome were discussed.抄録全体を表示PDF形式でダウンロード (947K) -
内山 務, 上川 浩, 荻田 善一1989 年 109 巻 9 号 p. 672-676
発行日: 1989/09/25
公開日: 2008/05/30
ジャーナル フリーIn chinese medicine, Phellodendri Cortex (Phellodendron amurense RUPRECHT) has been used to treat the patient who suffers from gastroenteritis, abdominal pain or diarrhea. Berberine has been identified as a major component in this plant, and it has biological activities, such as bactericidal activity, anti-cholera toxin effect, anti-inflammatory effect, stimulative effect of bile secretion or bilirubin discharge. In the previous study, we have shown the presence of anti-inflammatory activity in the berberine-free fraction of the extract from this plant. In the present study, we also found anti-ulcer activity in the fraction. The fraction significantly inhibited the formation of ethanol-induced ulcer, aspirin-induced ulcer (s.c., p.o.), pylorus-ligated ulcer (p.o., i.d.) in rats, as well as that of stress ulcer in restrained and water-immersed mice (p.o.). In addition, gastric acid secretion was significantly reduced in pyrolus-ligated rats by subcutaneous or intraduodenal administration of the fraction, but not by oral administration. These findings suggest that the supression of ulcer formation may be due to the additive effect of the cytoprotection effect and the reduction of gastric acid secretion by administration of the berberine-free fraction.抄録全体を表示PDF形式でダウンロード (597K) -
北島 潤一, 田中 靖子1989 年 109 巻 9 号 p. 677-679
発行日: 1989/09/25
公開日: 2008/05/30
ジャーナル フリーA mixture of α-spinasterol, stigmast-7-en-3β-ol (1) and its 3-O-β-D-glucopyranoside (2), bryonolic acid (3), 23, 24-dihydrocucurbitacin B (4), cucurbitacin B (5), cucurbitacin D (6) were obtained from the fresh roots of Trichosanthes multiloba MIQ. (Cucurbitaceae). 1, 2, 4, 5 and 6 were also obtained from the fresh roots of Trichosanthes miyagii HAY. From the chinese crude drug "Karo-Kon", which was considered to be prepared from the roots of Trichosanthes kirilowii MAXIM., 1, 2 and 3 were provided.抄録全体を表示PDF形式でダウンロード (438K) -
飯塚 幸澄, 櫻井 栄一, 引地 登, 丹羽 弘司1989 年 109 巻 9 号 p. 680-684
発行日: 1989/09/25
公開日: 2008/05/30
ジャーナル フリーThe activities of lysosomal maltase in the serum, bile and liver were determined in intrahepatic cholestasis rats induced by α-naphtylisothiocyanate (ANIT, 200 mg/kg, i.p.), and compared with changes in alkaline phosphatase (ALP) activity. Moreover, the influences of endogenous bile acids on the release of maltase activity from the liver in intrahepatic cholestasis rats were studied. The maltase activities in the serum and bile significantly increased from 4 and 8 h after the intraperitoneal administration of ANIT, respectively. Conversely, a significant decrease in liver maltase activity was observed from 4 h after the injection of ANIT. On the other hand, total bile acid concentrations in the serum and bile significantly increased immediately after the treatment of ANIT, when biliary bile acid, exogenous bile acid or Triton X-100 was added to lysosomal fraction in the liver, the maltase activity in the supernate after the reaction significantly increased in proportion to the concentration of each substance added to the liver lysosome. These results suggested that maltase might be released from liver lysosomal membrane by surface active-action of bile acid accumulated in the liver after the administration of ANIT. Moreover, the changes in ALP activities in the serum, bile and liver after the administration of ANIT were almost similar to those in maltase activity.抄録全体を表示PDF形式でダウンロード (562K)
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