YAKUGAKU ZASSHI
Online ISSN : 1347-5231
Print ISSN : 0031-6903
ISSN-L : 0031-6903
96 巻 , 7 号
選択された号の論文の18件中1~18を表示しています
  • 加藤 安之, 有馬 徳行, 西峯 秀夫
    1976 年 96 巻 7 号 p. 819-826
    発行日: 1976/07/25
    公開日: 2008/05/30
    ジャーナル フリー
    Absorption, excretion, distribution, and metabolism of 2-(5H-[1] benzopyrano [2, 3-b] pyridin-7-yl) propionic acid (Y-8004), a new anti-inflammatory agent, were investigated in rats and mice by the use of 14C-labeled compound (14C-Y-8004). When the radioactive compound was given to rats orally or intraperitoneally, about 50% of the given radio-activity (14C) was excreted in urine and 40% in feces during 72 hr, while about 80% in urine and 20% in feces after oral administration to mice. Approximately 55-60% was recovered in rat bile during 24 hr after oral administration. The highest blood level of 14C was obtained at 0.5-1 hr after oral administration to rats and mice. A good correlation was observed between blood level and dose level. However, apparent species difference in the blood 14C concentration and its disappearance rate were observed between rats and mice. When 14C-Y-8004 was orally administered to bileduct-cannulated rat, the blood 14C concentration and its disappearance rate came close to those of normal mice. The highest concentration of 14C was observed in the serum and relatively high levels in the liver and kidney of rats and mice after oral administration of 14C-Y-8004. In both animals, most of 14C in the serum existed as unchanged material bound to serum protein. Thin-layer chromatography after enzymic, acid, and alkaline hydrolysis experiments showed that the major metabolite in urine and bile of rats was Y-8004 acylglucuronide and in urine of mice Y-8004 acylglucoside. The present investigation provides the first evidence for the formation of an acylglucoside of a drug in mammals.
  • 奥本 武城, 今村 博
    1976 年 96 巻 7 号 p. 827-831
    発行日: 1976/07/25
    公開日: 2008/05/30
    ジャーナル フリー
    Improsulfan tosylateは実験腫瘍に対して特異な抗腫瘍スペクトルを示し, 従来のアルキル化剤に対して抵抗性を示すラット腹水肝癌AH-66あるいはAH-7974に対しても効果を示すことが知られている.Nitrogen mustardで耐性を誘導した吉田肉腫の耐性亜系に対してもimprosulfanは効果を示した.また, 本薬物は臨床的にbusulfan耐性白血病症例に対しても効果が認められている.一方, 静置浮遊培養細胞の増殖, 分裂期への移行, あるいは蛋白ならびに核酸合成に対しては, improsulfanとnitrogen mustardの作用間に本質的な差異は認められていない.現在, 本薬物が臨床的にも使用されていることから, この薬物の投与方法を検討するための知見を得る目的で, さらに培養細胞に対する作用について検討を加えた.本報告では, improsulfanの培養細胞のコロニー形成に対する作用, ならびにDNA鎖切断作用について報告する.
  • 川田 俊展, 原野 一誠, 田口 胤三
    1976 年 96 巻 7 号 p. 832-840
    発行日: 1976/07/25
    公開日: 2008/05/30
    ジャーナル フリー
    O, S-Dialkyl dithiocarbonate(I)は熱分解によりChugaev反応をうけるが, それに塩化アルミニウム(AlCl3)を加え二硫化炭素中で反応させると収率よくS, S-dialkyl dithiocarbonate(II)へ転位することを報告した.また一般のチオール酸エステルをエタノールアミンの存在下蒸留すると容易にメルカプタンが留出するというメルカプタン合成法も発表した.そしてこの2つの反応を組合せるとアルコールからメルカプタンを合成する有用な方法になることを明らかにした(Chart1).
  • 小宮 威彌, 津久井 誠, 大塩 春治
    1976 年 96 巻 7 号 p. 841-854
    発行日: 1976/07/25
    公開日: 2008/05/30
    ジャーナル フリー
    A new choleretic substance, capillarisin (I), was isolated from the herb of Artemisia capillaris Thunb. (Japanese name, "Inchinko" ?? 〓 ?? ) by tracing the activity in rats. By heating with 1% NaOH or H2SO4 in methanol, I was cleaved to p-hydroquinone and a compound (XI) or p-hydroquinone and the compound (XII). Infrared and ultraviolet spectra suggested that I and XI are chromone derivatives and XII is a coumarin derivative. Positions of the functional groups in XI and XII were determined by direct comparison with the synthetic samples, and the structure of I was established as 2-(p-hydroxy-phenoxy)-6-methoxy-5, 7-dihydroxychromone.
  • 小宮 威彌, 成瀬 義知, 大塩 春治
    1976 年 96 巻 7 号 p. 855-862
    発行日: 1976/07/25
    公開日: 2008/05/30
    ジャーナル フリー
    Four new 2-phenoxychromone derivatives were isolated from Artemisiae Capillaris Herba (Japanese name, "Inchinko" ?? 〓 ?? ). Their structures were established on the basis of chemical and spectroscopic evidences as 2-(p-methoxyphenoxy)-6-methoxy-5, 7-dihydroxychromone (4'-methylcapillarisin), 6, 7-dimethoxy-2-(p-hydroxyphenoxy)-5-hydroxychromone (7-methylcapillarisin) 2-(p-methoxyphenoxy)-5, 7-dihydroxychromone (6-demethoxy-4'-methylcapillarisin), and 2-(p-hydroxyphenoxy)-5, 7-dihydroxychromone (6-demethoxycapillarisin), respectively. Four flavonoids, cirsilineol, cirsimaritin, genkwanin, and rhamnocitrin, were also isolated from this herb.
  • 中島 重勝, 小中 隆盛, 武田 健一
    1976 年 96 巻 7 号 p. 863-879
    発行日: 1976/07/25
    公開日: 2008/05/30
    ジャーナル フリー
    In the oxidation reactions of 3-oxo-steroids with oxygen in a basic solution, the effect of various substituents in B and C rings was examined by product analyses and by ESR measurements. 3-Oxo-5α-steroids themselves produced only 2, 3-diketones although Δ3-semidiones were observed along with Δ2-semidiones in the ESR spectra. Introduction of 11-oxo, 11-methylene, 11β-methyl, Δ7 (8), or Δ9 (11) group into 3-oxo-5α-steroids gave 3, 4-diketones together with 2, 3-diketones, but the substituent effect of 11α-hydroxyl 11α-methyl-11β-hydroxyl, Δ9 (11)-11-methyl, Δ6 (7), Δ11 (12), Δ11 (12)-12-methyl, or 12-meth-ylene group was not observed significantly. 25D.5β-Spirostan-3-one (XLVIII) afforded only the 3, 4-diketone and no substituent effect was observed by introducing an oxo group into the C-11 position of (XLVIII). In the ESR measurements the concentrations of Δ2-semidiones and Δ3-semidiones changed with time and the ratios of the maximum concentration corresponded to the product ratios. The long range effect of these substituents can be interpreted in terms of"conformational transmission"based on the direction of enolation in the A rings.
  • 北村 桂介, 森 義雄, 堀井 通代, 穂積 啓一郎
    1976 年 96 巻 7 号 p. 880-885
    発行日: 1976/07/25
    公開日: 2008/05/30
    ジャーナル フリー
    Some aromatic hydrocarbons, such as benzene, toluene, ethylbenzene, p-xylene, and styrene, were polymerized by subjecting them to a radio-frequency glow discharge at a reduced pressure (plasma polymerization), resulting in any of three types of products : powder, oil, and solid film, under varied plasma conditions. The oily products soluble in chloroform and carbon tetrachloride exhibited an average molecular weight of 400-600. The infrared spectra of these materials showed similar characteristics and also similar to normal polystyrene having a linear backbone chain, whereas their nuclear magnetic resonance (NMR) spectra did not show resemblance to the latter. NMR spectra of these products showed the presence of aromatic protons, widely shifted aliphatic protons, and olefinic protons, and the comparison of signal intensities of the polymer products with that of monomers suggested the formation of aliphatic chains derived from the cleavage of the aromatic rings. Based on these spectral data, structure of the oily products is postulated to be a polystyrene type but to have longer and branched backbone chains involving some double bonds. By assuming 1.5 hydrogen atoms to be bonded to a chain carbon, as in the normal polystyrene, the number of backbone chain carbons per benzene ring should be about four. Values of H/C ratio calculated from this assumption agreed well with that obtained from elemental analysis.
  • 久野 拓造, 小路 清勝, 市川 正孝
    1976 年 96 巻 7 号 p. 886-890
    発行日: 1976/07/25
    公開日: 2008/05/30
    ジャーナル フリー
    Nitroanthranilic acids were reacted with picolinic acid, in the presence of phosphoryl chloride, to form 3-, 4-, and 5-nitro-2-picolinamidobenzoic acids which were used as the starting material for the application of anilines, with phosphorus trichloride as the condensation agent, to effect cyclization to 4 (3H)-quinazolinones. The yield of the cyclization product was very poor when the reaction was carried out with ortho-substituted anilines but the yield was raised 3-fold when polyphosphoric acid was used as the condensation agent. Examination of the nitration of 2-(2-pyridyl)-3-phenyl-4 (3H)-quinazolinone showed that the reaction progressed only with nitric acid in sulfuric acid to yield 2-(2-pyridyl)-3-(m-nitrophenyl)-6-nitro-4-(3H)-quinazolinone.
  • 岡野 定輔, 堀江 孝, 本橋 登
    1976 年 96 巻 7 号 p. 891-898
    発行日: 1976/07/25
    公開日: 2008/05/30
    ジャーナル フリー
    Studies were made on the intermolecular interaction of the oxazine dye Nile Blue A and calf-thymus deoxyribonucleic acid (DNA). It was concluded from these experimental results that two modes of interaction, ionic binding of the basic dye and the phosphate group of DNA, which leads to metachromasis of the dye, and intercalation of the dye between adjacent base-pairs of the macromolecule, are taking part in the binding of Nile Blue A and DNA : (1) When this dye was mixed with DNA at pH 7.0, intensity of its characteristic absorption bands (α and β bands) decreased, and new absorption bands appeared in the vicinity of 550 nm (γ band) and 668 nm (δ band). (2) The γ-band was produced when the molar ratio of [Dye]/[DNA-P] was greater than 1, while the δ-band was produced when this molar ratio was smaller than 1. (3) Flow dichroism spectrum of the δ-band indicated that the Nile Blue A molecule was oriented perpendicularly to the longer axis of the double helix of DNA ; dichroism was not observed with a mixture of this dye and heat-denatured DNA. (4) The γ absorption band was also produced by the mixed system of Nile Blue A and potassium poly (vinylsulfonate) : no spectral change was observed with a monomeric vinyl sulfonate. (5) Mixed systems of Nile Blue A and a high concentration of purine nucleosides or mononucleotides exhibited a larger δ band than the systems in which corresponding pyrimidine derivatives were involved. (6) Larger spectral changes were produced by the interaction systems of Nile Blue A and purine homopolynucleotides than by the systems in which pyrimidine homopolynucleotides were involved. (7) Viscosity and melting temperature of DNA increased with increasing concentration of this dye added.
  • 砂田 久一, 大塚 昭信
    1976 年 96 巻 7 号 p. 899-904
    発行日: 1976/07/25
    公開日: 2008/05/30
    ジャーナル フリー
    Compaction of a powder has been simulated on two-dimensional model by employing a digital computer. In the process of formation of the initial bed, 400 discs of equal size were dropped one by one into a container, introducing the probability P to make each two discs cohere in contact. Compaction of the beds by tapping was also simulated by shifting each disc into the hole present in the lower layer. In this process the coordination number of a disc and the cohesion probability P'were taken into consideration. Another probability P"was introduced in the step of insertion of a disc into the hole created by the transfer of the former disc. The relation between porosity and tapping number was fitted in Kawakita's equation when P'was relatively large and P"small. On the other hand, Kuno's equation was applicable when P'was small and P"large. It was also indicated that the cohesion probability P'is closely related to the rate constant in these equations.
  • 小嶋 正治, 渡辺 正純, 田口 胤三
    1976 年 96 巻 7 号 p. 905-911
    発行日: 1976/07/25
    公開日: 2008/05/30
    ジャーナル フリー
    Methyl 2, 3-dideoxy-2, 3-dithio-α-D-altropyranoside derivatives were synthesized by the thermal rearrangement of xanthate derivative of methyl 4, 6-O-benzylidene-3-S-benzyl-3-deoxy-3-thio-α-D-altropyranoside (III) or methyl 4, 6-O-benzylidene-2-S-benzyl-2-deoxy-2-thio-α-D-altropyranoside (IV).
  • 半田 哲郎, 中垣 正幸
    1976 年 96 巻 7 号 p. 912-918
    発行日: 1976/07/25
    公開日: 2008/05/30
    ジャーナル フリー
    モノヘキサデシルリン酸(HP)はリン酸とヘキサデシルアルコールのモノエステルであり, 2塩基酸である.また, これは生体膜に存在する酸性リン脂質, 例えば, フォスファチジン酸やフォスファチジルセリンのモデル物質として興味がある.HPは一種のモノアルキルリン酸であるが, これは単分子膜中でリン酸基同士が水素結合をして高い表面粘性や異常なpK値などを示す事が知られている.われわれは炭素数の異なるモノアルキルリン酸の2ナトリウム塩を合成し, その水溶液の界面化学的研究をおこなった.また, この水溶液表面においてコレステロールやそのエステのル不溶性単分子膜を展開し, 可溶性成分と不溶性成分の相互作用について検討した.今回は, 酸性水溶液表面において遊離のアルキルリン酸(モノヘキサデシルリン酸, HP)とコレステロール(CH)の混合単分子膜を展開し, その表面圧一面積曲線(F-A曲線)を測定した.同時にこれ等の平衡拡張圧(Fs)をも測定した.これ等の結果に基づき混合単分子膜中でのHPの分子会合とコレステロール分子との混合性について検討した.
  • 寺田 幸正, 中野 功一, 奥 照夫, 藤本 明, 岡田 寿太郎
    1976 年 96 巻 7 号 p. 919-922
    発行日: 1976/07/25
    公開日: 2008/05/30
    ジャーナル フリー
    Photochemical reaction of 2-(1-cyclohexenyl) cyclohexanone (II) with formamide in tert-butanol afforded two cyclization products ; 1, 2, 3, 4, 4a, 7, 8, 9, 10, 10b-decahydro-6 (5H)-phenanthridinone (III) and 1, 2, 3, 4, 7, 8, 9, 10-octahydro-6 (5H)-phenanthridinone (IV). These two products (III and IV) were further dehydrogenated with sulfur to give the known compounds V and VI, respectively. On irradiation of 1, 2-cyclohexanedione (VIII) in acidic solution under various conditions, several dimerization products were obtained ; 4, 4', 5, 5', 6, 6'-hexahydro-2, 2'-dihydroxybiphenyl-3, 3'-dione (IX), perhydro-4a, -9a-epoxydibenzo-p-dioxin-5a, 10a-diol (X), perhydro-2, 3'; 2', 3-diepoxybiphenyl-2, 3, 3'-triol (XI), and an unknown compound (XII).
  • 井上 正美, 榎本 三郎
    1976 年 96 巻 7 号 p. 923-926
    発行日: 1976/07/25
    公開日: 2008/05/30
    ジャーナル フリー
    フェノール類のメチルエーテル体は強アルカリ性の下でジメチル硫酸を作用させることにより高収率, 選択的に行なわれている.しかし, ジメチル硫酸の毒性が高いこと, 廃液中に未反応原料および副生硫酸ナトリウムが高濃度に含まれてくるので後処理がはん雑である.そこで, 理想的反応系としてフェノールとメタノールの触媒反応がもとめられている.メタノールをアルキル化剤として触媒の存在下, フェノール類のエーテル化を行なった例として, フェノールとメタノールからBF3を触媒とし, 170°でアニソールが得られていることを挙げることができる.著者らは, さらに取り扱いの容易な触媒系を探索し, 金属塩のうちFeおよびCrのリン酸塩が300-375°でフェノール類のエーテル化を選択的に行なうことを見い出した.一方, 硝酸塩を触媒とすればortho位核メチル体が得られた.そこで, アルキル化に対する金属塩の特性を反応条件に対する生成物の分布, 変換率の相違等から明らかにすることを目的とした.
  • 山口 達明, 斉藤 仁俊, 木曽 幸一, 竹下 優, 辻本 利雄, 由岐 英剛
    1976 年 96 巻 7 号 p. 927-931
    発行日: 1976/07/25
    公開日: 2008/05/30
    ジャーナル フリー
    The base-catalysed reaction of 3-acetyltetramanilide (II) with benzaldehyde in refluxing ethanol gave two isomeric condensation products. This indicates that both the ring methylene group (5-position) and the methyl group in α-phenylaminoethylidene group of II have the possibility of being attacked by the benzaldehyde molecule. Ratio of their yield varied with the nature of the base, the basicity and the steric requirement. Differences in the selective catalytic action between pyridine and piperidine are discussed on the basis of the results on the catalytic H-D exchange rate of the CH bonds of II susceptible to the condensation reaction.
  • 小沢 樹夫, 中村 好志, 木苗 直秀
    1976 年 96 巻 7 号 p. 932-935
    発行日: 1976/07/25
    公開日: 2008/05/30
    ジャーナル フリー
    The four pigments of isatin derivatives were separated from the browinng reaction of L-ascorbic acid (AAH2) with p-toluidine. These colors were identified as 2, 3-di-(p-tolylimino)-5-methylindoline (I) (reddish brown), 2-deoxy-2-(p-tolylimino)-5, 5'-dimethyl-isoindigo (II) (reddish orange), 5, 5'-dimethylindirubin (III) (violet), and 3-deoxy-3-(p-tolylimino)-5, 5'-dimethylindirubin (IV) (violet), which were found to be formed by the reaction of glucose and p-toluidine. The formation pathway of these pigments is different from those produced by the glucose-p-toluidine reaction, that is, the reaction of 14C1-AAH2, 5, 6-isopropylidene-AAH2, 5-phenyl-2, 3, 4 (5) furantrione, glycolaldehyde, and triose reductone with p-toluidine suggested that they are not formed from C1-C2 fragment of AAH2, but formed from its C5-C6 fragment.
  • 前田 稔, 小松 博史, 山元 より子, 下入佐 寛, 米谷 節子, 小嶋 正治
    1976 年 96 巻 7 号 p. 935-937
    発行日: 1976/07/25
    公開日: 2008/05/30
    ジャーナル フリー
    5α-Bromo-6, 19-epoxy-cholestan-3β-ol acetate was prepared in a good yield only by heating 5α-Bromo-cholestane-3β, 6β-diol 3-acetate in cyclohexane with I2-Pb (OAc)4 in the presence of calcium carbonate without ultraviolet ray irradiation.
  • 砂田 久一, 大塚 昭信
    1976 年 96 巻 7 号 p. 938-939
    発行日: 1976/07/25
    公開日: 2008/05/30
    ジャーナル フリー
    Comparison between two-dimensional porosity εa and three-dimensional porosity εv was made by a computer simulation study. In the formation of beds based on a random packing model, circles and spheres of equal size were used for the two- and three-dimen-sional systems, respectively. The porosity parameter P was introduced to decide whether the circles or spheres cohere or not when they came into contact with each other. εa and εv for the same P values were then compared. Porosities from the two-and threedimensional regular packing model were also examined. Results obtained by the random packing model were in good agreement with those by the regular packing model, as well as the two-dimensional"open-beam"packing model.
feedback
Top