YAKUGAKU ZASSHI
Online ISSN : 1347-5231
Print ISSN : 0031-6903
ISSN-L : 0031-6903
107 巻, 6 号
選択された号の論文の8件中1~8を表示しています
  • 瀬川 富朗
    1987 年 107 巻 6 号 p. 385-400
    発行日: 1987/06/25
    公開日: 2008/05/30
    ジャーナル フリー
    One of the most important function for the cells is to receive the signal from other cells, to recognize it by receptive substances and to transmit it to another cells. These signalling process in synapse is mediated through chemical substances, neurotransmitters. In order to identity 5-hydroxytryptamine (5-HT, serotonin) and substance P (SP) as a neutrotransmitter in central nervous system (CNS), uptake, storage and release mechanism, characterization of receptor and processing from precursor proteins were investigated and as a results, we obtained several kinds of evidence suggesting that both 5-HT and SP are neurotransmitters in CNS.
  • 藤田 佳平衛
    1987 年 107 巻 6 号 p. 401-415
    発行日: 1987/06/25
    公開日: 2008/05/30
    ジャーナル フリー
    Chemical construction of enzyme-like function by use of cyclodextrins and modified cyclodextrins is reviewed. Activation (sulfonylation) methods of C2-OH, C3-OH, and C6-OH of cyclodextrins and transformation of the activated cyclodextrins to artificial enzymes are summarized.
  • 村上 孝夫, 木戸 庸裕, 堀 一之, 佐武 紀子, 斎木 保久, 陳 秋明
    1987 年 107 巻 6 号 p. 416-419
    発行日: 1987/06/25
    公開日: 2008/05/30
    ジャーナル フリー
    A flavanone with a modified B-ring, 'protofarrerol (I)', which is biogenetically unusual and has never been found in any other ferns than Leptorumohra miqueliana H.ITO (Aspidiaceae), was found together with violantin (VI) in the fronds of Monachosorum henryi CHRIST (Pteridaceae). This finding, plus certain morphological features, suggests an alliance of M. henryi to L. miqueliana, and provides a phytochemical support for Christensen's (1938) and Mickel's ideas (1973), that Monachosorum is better placed with the aspidioid ferns on the basis of the morphological resemblance. From the fronds of L. miqueliana two new glycosides (IV and V) were further isolated and identified as 7-O-β-D-glucopyranoside of protofarrerol (I) and leptorumol (II) respectively.
  • 富永 道明, 小川 英則, 楊 永雄, 山下 修司, 薮内 洋一, 中川 量之
    1987 年 107 巻 6 号 p. 420-428
    発行日: 1987/06/25
    公開日: 2008/05/30
    ジャーナル フリー
    Many 3, 4-dihydro-6-(substituted 1-oxoalkyl)-2 (1H)-quinolinone derivatives were synthesized and examined for positive inotropic activity on the canine heart. Among them, 3, 4-dihydro-6-[2-(N-methyl-4-methoxybenzylamino) acetyl]-2 (1H)-quinilinone (Va-2), 3, 4-dihydro-6-[2-(N-methyl-4-cyanobenzylamino) acetyl]-2 (1H)-quinolinone (Va-3) and 6-[2-(N-methyl-4-methoxybenzylamino) acetyl]-2 (1H)-quinolinone (XI) were found to have potent positive inotropic activity with little chronotropic effect.
  • 松田 秀秋, 土肥 玉枝, 西口 進, 岩村 淳一, 久保 道徳
    1987 年 107 巻 6 号 p. 429-434
    発行日: 1987/06/25
    公開日: 2008/05/30
    ジャーナル フリー
    Physical characters of six inulins isolated from Costi Radix, Taraxaci Radix cum Herba, Atractylodis ovatae Rhizoma, Atractylodis lanceae Rhizoma, Asteris Radix and Dipsaci Radix, and the effects of their inulins on phagocytosis in mouse reticuloendotherial system were investigated. The structures of the inulins from crude drugs were identified only by comparing its spectral evidence with that of authentic samples. Molecular weight, solubility (H2O, 30°C for 6 h) and specific rotation ([α]28D in 1% NaOH aq.) of these inulins were 3500-4000, 0.85-1.14 and -20--35, respectively. Among these inulins, three inulins from Taraxaci Radix cum Herba, Atractylodis ovatae Rhizoma and Atractylodis lanceae Rhizoma promoted phagocytosis in mouse reticuloendotherial system in vivo. The correlation between physical characters and the phagocytosis stimulating activity of six inulins was not observed.
  • 宮地 洋, 真鍋 明義, 徳森 恒雄, 隅田 葉子, 吉田 隆志, 西部 三省, 縣 功, 野村 太郎, 奥田 拓男
    1987 年 107 巻 6 号 p. 435-439
    発行日: 1987/06/25
    公開日: 2008/05/30
    ジャーナル フリー
    The supercritical fluid extraction was applied to coumarins, lignans and prenylflavonoids of crude drugs. Scoparone (1) and capillarisin (2), main components of Artemisia capillaris, were easily extracted with supercritical carbon dioxide. Scopoletin (3), fraxidin (6), isofraxidin (7) and fraxinol (8), which have a hydroxyl group on the coumarin skeleton, were also extracted from Fraxinus japonica and F. mandshurica var. japonica, and when ethanol was used as an entrainer, the amounts of these coumarins were comparable to those obtained with boiling methanol. However, esculetin (4) and fraxetin (5) possessing two hydroxyl groups on the coumarin ring, were not extracted even in the presence of ethanol or water as an entrainer. Between two lignans, (+)-fraxiresinol (9) and (+)-1-hydroxypinoresinol (10), only the latter was extracted from F. japonica and F. mandshurica var. japonica, with supercritical carbon dioxide by using water or ethanol as an entrainer. Water was more efficient than ethanol as an entrainer for the supercritical extraction of 10, although ethanol was better than water for the extraction of the other compounds in this paper. Extractabilities of the lignans of Forsythia suspensa and F. viridissima, by the supercritical carbon dioxide were similar to those by boiling n-hexane, and similar to those by boiling methanol in the presence of the entrainers. Among the prenylflavonoids in the barks of Morus species, morusin (15) and sanggenon A (19) having less than three hydroxyl groups were extracted without using the entrainers, while those having more than four hydroxyl groups were not extracted even in the presence of entrainers.
  • 諏訪 俊男, 浦野 英俊, 辻 彰
    1987 年 107 巻 6 号 p. 440-448
    発行日: 1987/06/25
    公開日: 2008/05/30
    ジャーナル フリー
    The pharmacokinetics of oxaprozin, an anti-inflammatory agent, were studied in healthy volunteers and dogs. After oral administration of oxaprozin (400 mg) to the volunteers, the maximum serum concentration of 57.0 μg/ml was attained at 5 h and then decreased with a mean half-life of 50.2 h. In the multiple dosing with 400 mg of the drug once a day for 10 d, the serum concentrations reached a plateau within 6 d and the levels were about 80% of those estimated from the single dosing experiments. Total serum clearance (Cltot/F) where F is the fraction absorbed at steady state was 161 ml/h, which was significantly higher than that (113 ml/h) with the single dosing. Similar tendencies were observed in dogs after the intravenous administrations of oxaprozin (10 mg/kg). On the other hand, the fraction of unbound drug to serum protein was found to be nonlinear to the total drug in clinically relevant concentrations. No significant difference of pharmacokinetic parameters such as area under the concentration versus time curve (AUCt) or Cltot/F of unbound drug was observed between single and multiple-doses experiment both in human and dogs. Thus, the clearance of oxaprozin was closely related to the fraction of unbound drug. These results indicate that multiple-doses of oxaprozin resulted in a plateau effect, which was due to the accelerated Cltot in steady state conditions caused by an increase in the fraction of unbound drug in the serum.
  • 上釜 兼人, 正木 勝広, 有森 和彦, 入江 徹美, 平山 文俊
    1987 年 107 巻 6 号 p. 449-456
    発行日: 1987/06/25
    公開日: 2008/05/30
    ジャーナル フリー
    The fast dissolving form of the inclusion complexes of prednisolone (PD) with β-cyclodextrin (β-CyD) and dimethyl β-cyclodextrin (DM-β-CyD) in a molar ratio of 1 : 2 was prepared to examine the in vitro/in vivo relation of percutaneous drug absorption from various ointments containing β-CyDs complexes. The release rate of PD from the ointments containing water (hydrophilic ointment, absorptive ointment and aqueous polyacrylic acid gel) and white petrolatum was significantly increased by both β-CyDs, while retarded in the cases of FAPG and macrogol ointments. The enhanced release of PD seemed to be due to the increase in apparent solubility and/or diffusibility of the drug in the ointment bases by means of water soluble inclusion complex formation. The percutaneous absorption experiments in vivo revealed that the disappearance of PD from the hydrophilic ointment and the appearance of PD in the skin after application to dorsal skin of rabbits were signiflcantly enhanced by both β-CyDs. The in vitro and in vivo data suggested that DM-β-CyD may be particularly useful to improve the topical bioavailability of PD, when an ointment base containing water was used.
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