YAKUGAKU ZASSHI
Online ISSN : 1347-5231
Print ISSN : 0031-6903
ISSN-L : 0031-6903
96 巻 , 12 号
選択された号の論文の20件中1~20を表示しています
  • 小延 鑑一, 高雄 弘, 黒田 真里子
    1976 年 96 巻 12 号 p. 1379-1384
    発行日: 1976/12/25
    公開日: 2008/05/30
    ジャーナル フリー
    血清脂質は遊離型およびエステル型のコレステロール(ChおよびCh-E), トリグリセライド(TG)にジーおよびモノグリセライド(DGおよびMG)を含む中性脂肪(NF), 遊離脂肪酸(FA), リン脂質(PL)に加えて少量の脂溶性物質からなる複雑多種類の混合物であるため, これらの成分を分離するために各種の溶体クロマトグラフィーガ工夫されている.そのなかで固定相に固形担体を使用しない向流分配法Countercurrent Distribution(C.C.D.)による脂質の分離は装置の複雑さ, 振とう静置の後2層に分離するためエマルジョンができやすいこと, 加えて分配回数は100回以上を必要とするために所要時間や溶媒の使用量, さらには操作の面倒さなどの点でその利用は極めて少ない.著者らは谷村らにより開発された向流クロマトグラフィーの一種である液滴法Droplet Countercurrent Chromatography(D.C.C.)は従来のC.C.D.の使いにくい面が改良され, 更にC.C.D.では得られなかった連続的分配が容易に行なえる点で脂質の分離に適したものと考え, 内径2.4mm, 長さ1200mmのガラス管をカラムにしたD.C.C.装置を自製して血清脂質の分画を試みた.溶媒は2層に分離しやすさを考えてheptane : butanol : 60% acetic acidを一応基準に選び, これにchloroform(CHCl3), methanol(MeOH)あるいはbenzene(PhH), ethanol(EtOH)を種々の比率にて組み合せた4-5成分の混合溶媒系について, 各上層液upper phase(U-P)と下層液lower phase(L-P)との比重差, 脂質の分配係数, カラム内での液滴の形成およびTLCを用いて脂質の分離などを調べて使用溶媒系を選定した.その結果heptane : butanol : chloroform : methanol : 60% acetic acid(3 : 2 : 2 : 3 : 5,v/v)およびheptane : benzene : chloroform : ethanol : 60% acetic acid(2 : 3 : 1 : 4 : 3,v/v)の2種が著者らのカラムサイズでのD.C.C.に適していることを認め, この溶媒系を用いて血清脂質を一応NF, FAおよびPLの3つに分画できた.
  • 吉田 集而, 新田 あや
    1976 年 96 巻 12 号 p. 1385-1392
    発行日: 1976/12/25
    公開日: 2008/05/30
    ジャーナル フリー
    The inner structure of the bark of Cinnamomum burmanni BL. has been investigated. Some variation was observed in the structure and the bark was divided into three types ; Sinoa type, Padang type, and Tjibodas type. Sinoa type is characterized by the presence of small stone cell groups in the secondary cortex, many thick-walled and lignified parenchyma cells, and very few fibers. Padang type has an interrupted stone cell ring, a large amount of big stone cell groups rarely has thick-walled and lignified parenchyma cells, and not many fibers. Tjibodas type has a continuous stone cell ring, few small stone cell groups near the ring, many fibers in the secondary cortex, and many thick-walled and lignified parenchyma cells form a mechanical tissue.
  • 吉田 集而, 新田 あや
    1976 年 96 巻 12 号 p. 1393-1400
    発行日: 1976/12/25
    公開日: 2008/05/30
    ジャーナル フリー
    Histological examinations were made on cinnamon and allied barks in the market of Jawa, Indonesia. Barks marketed as"kayu manis"and"manis jangan"have a sweet taste and smell of cinnamaldehyde. Barks commercially designated as"sintok"or"kayu sintok"are pungent and/or astringent. Fourteen samples of such a bark were examined and classified into six types, with one of them further divided into two subtypes. Types A-α and A-β were identified respectively as the Tjibodas type and Padang type of Cinnamomum burmanni BL., and types B and C were identified as the bark of C. cassia PRESL. and C. sintoc BL., respectively. The remaining three types, D, E, and F were not identified.
  • 野瀬 敦子, 工藤 忠宏
    1976 年 96 巻 12 号 p. 1401-1406
    発行日: 1976/12/25
    公開日: 2008/05/30
    ジャーナル フリー
    Reactions of carboxylic acids and esters with sodium borohydride were examined. With an equivalent mol of sodium borohydride, caproic acid (I) was reduced to 1-hexanol (II) in the absence of a solvent at 300°(bath temperature), and hexyl caproate (III) was obtained with 1/4 equivalent mol of sodium borohydride. Similarly, aliphatic and aromatic carboxylic acids were reduced to the corresponding alcohols with an equivalent mol of sodium borohydride. Reaction of esters with sodium borohydride gave the corresponding alcohols.
  • 栗原 藤三郎, 菊地 正雄, 鈴木 稠徳, 豊田 栄子
    1976 年 96 巻 12 号 p. 1407-1411
    発行日: 1976/12/25
    公開日: 2008/05/30
    ジャーナル フリー
    Dendropanoxide, α-amyrin, β-amyrin, α-acetylamyrin, β-acetylamyrin, friedelin, epifriedelinol, uvaol, ursolic acid, and 18 kinds of paraffin were isolated from etherial extract of the leaves of Rhododendron degronianum CARR. by silica gel column chromatography. From the methanolic extract of the leaves, grayanotoxin I, rhododendrin, quercetin, and isoquercitrin were isolated, and from the aqueous extract of the leaves. 11 kinds of amino acid were identified. Ten kinds of inorganic cation were detected from the ashed leaves.
  • 金尾 義治, 甲斐 明美, 吉柳 節夫, 井口 定男
    1976 年 96 巻 12 号 p. 1412-1416
    発行日: 1976/12/25
    公開日: 2008/05/30
    ジャーナル フリー
    現在, 種々の非ステロイド性抗炎症剤が開発され, 既に臨床的に用いられているものもかなりの数に上っている.これら非ステロイド性抗炎症剤を大別すると, カルボン酸系(酸性)と異項環塩基系(塩基性)に分類しうるが, 特に前者に属するものが多い.ところで非ステロイド性抗炎症剤は一般に水に難溶性で, 蛋白結合性が極めて高いのが特徴である故, これら薬物の生体内移行における蛋白結合の役割を検討することは, 非ステロイド性抗炎症剤の研究においては特に重要な意義をもつものと思われる.薬物の蛋白結合性を比較する場合には, KlotzあるいはScatchardらの方法に従って最大結合部位数n, 結合定数Kの物理化学的パラメータの算出を行なうのが, まず一般的な常套手段とされてきたが, さらに詳細な検討の結果, 多くの薬物は蛋白上の2種以上の結合部位と相互作用を及ぼしあっていると推定される様になり, 最近では結合部位を2種と仮定して解析を行なった報告も数多くみられる.そこで今回著者らは, まず代表的な非ステロイド性抗炎症剤をとりあげ, これら薬物の蛋白結合性を結合部位が2種存在するものと仮定して解析を行なうと共に, 油水分配率を測定して, 結合性との関連性の検討などを試みた.
  • 野田 浩司, 成松 一久, 浜名 政和
    1976 年 96 巻 12 号 p. 1417-1420
    発行日: 1976/12/25
    公開日: 2008/05/30
    ジャーナル フリー
    In order to explore the anticipated nitrone-like property of the N-oxide group of 3, 2'-diquinolyl 1-oxide (2), some usual nucleophilic reactions of 2 were examined and it was found that all attempted reactions proceeded normally. Thus, treatment with sulfuryl chloride, benzoyl chloride-potassium hydroxide solution, and benzoyl chloride-potassium cyanide gave 2- and 4-chloro (3 and 4), 2-hydroxy (6), and 2-cyano (7) derivatives, respectively. Reactions in the presence of acylating agents with ethanol-triethylamine, ethyl cyanoacetate, and 1-morpholinocyclohexene also afforded the respective 2-substituted products (10, 12, and 13) in the usual way.
  • 久保田 幸穂, 庄司 省三, 山中 照明, 大和 正明
    1976 年 96 巻 12 号 p. 1421-1425
    発行日: 1976/12/25
    公開日: 2008/05/30
    ジャーナル フリー
    Carboxypeptidase Sa was composed of 716 amino acid residues, 90 hexose residues (as galactose), and 31 hexosamine residues (as glucosamine) ; these were Trp14, Lys42, His15, Arg21, Asp77, Thr42, Ser60, Glu50, Pro34, Gly48, Ala57, Val50, Met6, Ile56, Leu93, Tyr22, and Phe34. Carboxypeptidase Sb was composed of 969 amino acid residues but was free from hexose and hexosamines ; these were Trp21, Lys62, His19, Arg35, Asp109, Thr49, Ser73, Glu84, Pro49, Gly88, Ala74, Gys (half)4, Val62, Met15, Ile49, Leu75, Tyr34, and Phe47. Carboxypeptidase Sa was stable in the pH range from 4.5 to 6.5 and in the temperature range from 0 to 50°, but carboxypeptidase Sb was quickly denatured at pH values below 5.0 or over 6.0. They were completely inhibited by the detergents, sodium dodecyl sulfate and cetyltrimethylammonium bromide, but not by Tween 80 or Triton X-100. The Km and Vmax values of carboxypeptidase Sa for the hydrolysis of Z-Glu-Phe were 0.16 M and 0.29 μmol/min/·mg, respectively, and those of carboxypeptidase Sb were 0.053 M and 11.36 μmol/min·mg, respectively.
  • 坂野 俊行, 山地 章子, 平内 三政, 天野 為之
    1976 年 96 巻 12 号 p. 1426-1431
    発行日: 1976/12/25
    公開日: 2008/05/30
    ジャーナル フリー
    An in situ fluorometric method was developed for the quantitation of 1-methyl-2-(2-naphthyl) aziridine (I) in biological materials. Three-phase thin-layer plate (Silica gel G, cellulose powder, and talc) was effective for the separation and fluorescence measurement of I. I in rat muscle or in rat blood was extracted with AcOEt n-hexane, respectively, and then 2-10 μl of the extract was spotted on the silica gel phase of the three-phase thinlayer plate. The plate was developed for 40 min with MeOH·ether (7 : 1, v/v) mixture, dried, and then isopropyl myristate was sprayed. Rf-value of I was about 0.5 in the talc phase of the three-phase plate. The plate was heated for 20 min on a hot plate (180°) and cooled in N2 stream. Fluorescence intensity was determined by scanning with a spetrofluorodensitometer (excit, 340 nm, emission 480 nm) after the fluorescent spot was covered with a quartz plate. The linear dynamic range for the assay was found from 0.02 to 0.2 μg of I per spot. This method was applied for the determination of unchanged I in the rat blood and muscle, and 2-vinylnaphthalene was found as the metabolite of I in rat blood.
  • 岡野 定輔, 渡辺 善照, 吉村 敬治
    1976 年 96 巻 12 号 p. 1432-1439
    発行日: 1976/12/25
    公開日: 2008/05/30
    ジャーナル フリー
    Examinations on the effect of poly (vinylpyrrolidone) (PVP) on the gastrointestinal absorption of salicylic acid and related compounds in rats, and also on the intermolecular interaction between several compounds related to salicylic acid and PVP revealed that the absorption of small-molecule compounds from the stomach (absorption analysed by the loop method) and small intestine (by the circulation method) was inhibited by the presence of PVP and degree of inhibition decreased in the order of 2, 4-dihydroxybenzoic acid, p-aminosalicylic acid, salicylic acid, salicylamide, and o-anisic acid. This order of inhibition was independent of the easiness of absorption of these compounds in the absence of PVP. The inhibitory effect of PVP on the absorption was observed to be reflected on the blood level pattern of salicylic acid administered orally. Intermolecular interaction of 12 compounds related to salicylic acid with PVP was analysed by the equilibrium dialysis method. It was found that the degree of the interaction, expressed in terms of R-value, ran parallel with the degree of inhibition of the gastrointestinal absorption by PVP. From the relationship between the chemical structure and R, it was presumed that hydrogen bonding through the phenolic hydroxyl group of the small-molecule compounds played an important role in the interaction with PVP. Such a presumption was supported by the results of infrared spectroscopic examinations.
  • 三由 文久, 徳野 健次, 荒田 義雄, 広木 繁, 大橋 力
    1976 年 96 巻 12 号 p. 1440-1447
    発行日: 1976/12/25
    公開日: 2008/05/30
    ジャーナル フリー
    1-Thioniabicyclo [4.4.0] decane bromide (I) derived from 1, 9-diphenoxy-5-mercaptononane was found to be composed of isomers, Ia and Ib, in the ratio of 2 : 3, each of which was purified by column chromatography on silica gel. On heating at 260-270°, Ia was partially isomerized to the equilibrium mixture of Ia and Ib in 3 : 2 ratio, as did Ib. The structures of Ia and Ib were established as cis and trans isomers, respectively, on the basis of the carbon-13 neuclear magnetic resonance spectral studies. The reaction of Ia and Ib with sodium amalgam gave 2-butylthiane and thiecane. Heating of Ia and Ib with aqueous potassium hydroxide gave 2-(3'-butenyl) thiane, trans-3, 4, 7, 8, 9, 10-hexahydro-2H-thiecine and 2-(4'-hydroxybutyl) thiane.
  • 小林 茂, 木原 勝, 新宮 徹朗
    1976 年 96 巻 12 号 p. 1448-1452
    発行日: 1976/12/25
    公開日: 2008/05/30
    ジャーナル フリー
    The reaction of diphenides (IIa-f) with potassium cyanide in dimethyl sulfoxide was found to give 10-hydroxy-9-phenanthrenecarbonitriles (IIIa-f) in a reasonable yield via the intramolecular recyclization of a ring-opened intermediate (IV). However, the reaction of 1, 2, 10, 11-tetramethoxydiphenide (IIg) afforded 2'-cyanomethyl-5, 6, 5', 6'-tetramethoxy-2-biphenylcarboxylic acid (Ig), which could not be recyclized to IIIg because of steric hindrance of the methoxyl groups in Ig. The nuclear magnetic resonance spectra of III were discussed.
  • 福島 清吾, 上野 明, 野呂 和子, 野呂 忠敬, 森永 邦夫, 赤堀 幸男, 石原 広男, 斎木 保久
    1976 年 96 巻 12 号 p. 1453-1457
    発行日: 1976/12/25
    公開日: 2008/05/30
    ジャーナル フリー
    Two new pyrimido-1, 4-diazepine derivatives, 4-phenyl-6, 8-dimethyl-1H-pyrimido-[4, 5-b] [1, 4] diazepine-2, 7, 9 (3H, 6H, 8H) trione (VIII) and 2-phenyl-6, 8-dimethyl-3H-pyrimido [4, 5-b] [1, 4] diazepine-4, 7, 9 (5H, 6H, 8H) trione (X), were synthesized. 5, 6-Diamino-1, 3-dimethyluracil (I) was condensed with ethyl acetoacetate under elimination of ethanol by heating in xylene, to give N-(6-amino-1, 3-dimethyl-2, 4-dioxo-1, 2, 3, 4-tetrahydro-5-pyrimidyl)-3-phenyl-3-oxopropionamide (VI). When the two components were heated in butanol, I gave ethyl 3-phenyl-3-(6-amino-1, 3-dimethyl-2, 4-dioxo-1, 2, 3, 4-tetrahydro-5-pyrimidylamino) acrylate (IX) under elimination of water. Heating of VI at 230-240°for a few minutes under a reduced pressure gave VIII in a poor yield (17%), while heating of IX in ethanol with sodium ethoxide on a water bath for a few minutes gave X in a good yield (74%).
  • 石井 永, 石川 勉, 盧 盛徳, 陳 益昇
    1976 年 96 巻 12 号 p. 1458-1467
    発行日: 1976/12/25
    公開日: 2008/05/30
    ジャーナル フリー
    Chemical constituents of the wood and bark of Xanthoxylum cuspidatum CHAMP. (Fagara cuspidata ENGL.), a Formosan Rutaceous plant (Japanese name : Tsuru-Zansho), were examined. From the wood six alkaloids, nitridine (2) chloride, dictamine (6), γ-fagarine (7), skimmianine (8), robustine (12), and haplopine (13), β-sitosterol (9), and a new phenylpropanoid, cuspidio (11), mp 65-67°, were isolated. From the bark eight known alkaloids, 2 chloride, oxynitidine (4), des-N-methyl-chelerythrine (14), decarine (24), 7, 8, liriodenine (20), and 4-methoxy-1-methyl-2-quinolone (19), four new alkaloids, des-N-methylavicine (16), mp 290-295°, arnottianamide (18), mp 264-267°, isoarnottianamide (21), mp 254-257°, and base X-C-1 (23), mp 268-272°, 9, 11, and dihydro-p-coumaryl alcohol (22), were isolated.
  • 渡辺 康, 本橋 清, 三井 美澄, 米田 良蔵, 田中 美雄
    1976 年 96 巻 12 号 p. 1468-1477
    発行日: 1976/12/25
    公開日: 2008/05/30
    ジャーナル フリー
    Examinations were made on the possibility of an in vitro test for bioinequivalence of chloramphenicol tablets, previously found by the measurement of their level in human serum, using the dissolution tests as a marker. Dissolution tests were made by the Japanese Pharmacopoeia VIII disintegration test, USP XVIII dissolution test, Levy's beaker method and Erweka's method. Erweka's method, using water as the solvent, was found to give a result that correlated well with the area under a serum level-time curve. Serum level of 10 products selected from 24 kinds of commercial chloramphenicol tablets was measured in a total of 135 healthy women in the first and 129 healthy women in the second experiment. Dissolution rate of these 10 products was also measured. In addition, serum level and dissolution rate of the original powder for these chloramphenicol tablets were measured and the difference between tablets and their original powder of chloramphenicol was confirmed. Correlation between the human serum level and dissolution rate of commercial chloramphenicol tablets manufactured in Japan was examined and a regression formula for them was calculated. It was found from these experiments that chloramphenicol tablets with 50% dissolution time of over 64 min have a high probability to be bioinequivalent, and 3 out of 24 products of commercially available chloramphenicol tablets on Japanese market in 1974 were found to be bioinequivalent.
  • 酒井 清, 西畑 利明, 西野 隆雄, 高松 早基子
    1976 年 96 巻 12 号 p. 1478-1480
    発行日: 1976/12/25
    公開日: 2008/05/30
    ジャーナル フリー
    マウス, ラット, 家兎等の哺乳類実験動物は, プリン代謝の最終産物が尿酸であるヒトに比べ, その一部が異なり水に易溶性のアラントインにまで代謝されて排泄されるために痛風, Lesch-Nyhan症候群などのいわゆる高尿酸血症を認めることができないが, 現在これらの実験動物を用い高尿酸血症モデルを作成するためにウリカーゼ(EC1.7,3.3.Urate : oxygen oxidoreductase)活性を何んらかの方法で抑制しアラントイン排泄型から尿酸排泄型に変える試みが行なわれている.著者らは先にキサンチンオキシダーゼ(EC1.2.3.2.Xanthine : oxygen oxidoreductase)の作用を抑制するといわれる痛風治療剤4-hydroxypyrazolo[3,4-d]pyrimidine(H.P.P.)の各種剤形を家兎に経口投与し, その剤形が薬効におよぼす影響を検討したところ, いずれの剤形においても, その血中濃度, 排泄時間, 血清尿酸値などに性差があることを認めた.このためこれらの現象がH.P.P.のウリカーゼ活性に対する作用にも関連性を有するのではないかと考え, H.P.P.がウリカーゼ活性に及ぼす影響について検索を加えた.
  • 玉木 七八, 飯泉 久子, 益満 宜郎, 窪田 彬, 浜 堯夫
    1976 年 96 巻 12 号 p. 1481-1486
    発行日: 1976/12/25
    公開日: 2008/05/30
    ジャーナル フリー
    Anserine, carnosine, β-alanine, and methylhistidine contained in animal and vegetable tissues were measured with an amino acid autoanalyzer, and quantitative characteristic of their distribution was examined. Distribution of their content varied greatly with animal and vegetable species, but the variation was not related to taxonomy. Anserine and carnosine were not found in rice, wheat, soybean, and cow milk, and these constituents were recognized as not being a food nutrient and not affected by the intestinal bacteria. The striking feature in the animal kingdom was found in tuna (Thunnus thynnus (LINNE) in which a large quantity (89.43 μmol/g wet tissue) of anserine was detected but no carnosine. In the eel (Entosphenus japonicus (MARTENS)) 3.617μmol of carnosine was detected but not anserine. Some animal tissues contained one or both of these dipeptides. The human iliopsoas usually contained carnosine but anserine was detected in 3 of 58 cases examined, including a case that contained 8.984 μmol/g protein of anserine and 6.88 μmol/g protein of carnosine. In the case in which anserine was detected, an abnormally high (3.45 μmol/g protein) of free histidine was detected. β-Alanine was not detected in human hepatoma.
  • 栗原 藤三郎, 菊地 正雄
    1976 年 96 巻 12 号 p. 1486-1488
    発行日: 1976/12/25
    公開日: 2008/05/30
    ジャーナル フリー
    Biochanin A, formononetin, ononin, sissotorin, genistin, β-sitosterol, and β-sitosterol-3-O-β-D-glucoside were isolated from the methanolic extract of the fresh flower of Pueraria thunbergiana BENTH.
  • 小川 俊太郎, 吉田 昭義, 三谷 洋子
    1976 年 96 巻 12 号 p. 1488-1491
    発行日: 1976/12/25
    公開日: 2008/05/30
    ジャーナル フリー
    A rapid, simple, and accurate high-speed liquid chromatographic procedure was established for the quantitative determination of glycyrrhizin in pharmaceutical preparations including Glycyrrhiza radix. Glycyrrhizin, extracted from simple pharmaceutical preparations, was determined under the same conditions as previously. Glycyrrhizin in compound pharmaceutical preparations containing multiple components was separated on Permaphase AAX column (1 m×3 mm, internal diam.) with a mobile phase of 50% ethanol in phosphate buffer (pH 5.2)-0.005 M NaClO4 solution at 45°. In most of preparations, good recovery was obtained, but in a few, sufficient recovery was not obtained because of incomplete extraction.
  • 山内 盛, 滝戸 道夫, 三川 潮, 柴田 承二
    1976 年 96 巻 12 号 p. 1492-1493
    発行日: 1976/12/25
    公開日: 2008/05/30
    ジャーナル フリー
    From the fruits of Arctium lappa L. (Japanease name"goboshi, ""akujitsu, "or "dairikishi"), two new sesquilignan derivatives, AL-D and AL-F, were isolated along with arctin, arctigenin, and matairesinol. From spectroscopic and chemical investigations, the structure of AL-D was elucidated as 2-[2-(3-methoxy-4-hydroxy) phenyl-3-hydroxymethyl-7-methoxy-2, 3-dihydrobenzofuran-5-yl] methyl-3-(3-methoxy-4-hydroxy)-benzyl-buthyrolactone [I] or 2-(3-methoxy-4-hydroxy) benzyl-3-[2-(3-methoxy-4-hydroxy)-phenyl-3-hydroxymethyl-7-methoxy-2, 3-dihydrobenzofuran-5-yl] methyl-buthyrolactone [II]. AL-F was found to be a stereoisomer of AL-D.
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