Chemical and Pharmaceutical Bulletin
Online ISSN : 1347-5223
Print ISSN : 0009-2363
ISSN-L : 0009-2363
36 巻, 7 号
選択された号の論文の68件中1~50を表示しています
  • 尹 康子, 石田 寿昌, 土井 光暢, 井上 正敏, 柴田 健夫
    1988 年 36 巻 7 号 p. 2295-2302
    発行日: 1988/07/25
    公開日: 2008/03/31
    ジャーナル フリー
    As a part of studies aimed at elucidating the stereostructure-inhibitory activity relationship of histamine H2-receptor antagonists, the crystal structures of 2-acetoxy-N-[3-[m-(1-piperidinomethyl)phenoxy]propyl]acetamide (roxatidide acetate) and its hydrochloride salt have been analyzed by the X-ray diffraction method. The neutral and cationic molecules both have similar extended conformations, implying that the molecular conformation of roxatidine acetate is little affected by the hydrochloride salt formation. This is an important difference compared with other H2-antagonists such as cimetidine and famotidine, where a drastic change has been observed between the neutral and cationic molecular conformations. Based on the present X-ray and related data, the possibility of multiple binding sites on the H2-receptor is discussed.
  • 江口 正, 斎 洋之, 高津戸 秀, 原 典之, 池川 信夫
    1988 年 36 巻 7 号 p. 2303-2311
    発行日: 1988/07/25
    公開日: 2008/03/31
    ジャーナル フリー
    1α, 25-Dihydroxy-26, 27-dimethylvitamin D3 (5), 1α, 25-dihydroxy-26, 27-diethlvitamin D3 (6), 25-hydroxy-26, 27-dimethylvitamin D3 (7), and 1α-hydroxy-26, 27-dimethylvitamin D3 (8), as dialkyl analogues of 1α, 25-dihydroxyvitamin D3 (1), were synthesized starting from 3β-hydroxy-cholenic acid (9). When tested for ability to increase serum calcium concentration in rats, 5 was slightly less active than 1, whereas 6 was much less active. Compound 8 was less active than 1α-hydroxyvitamin D3. In test for ability to induce cell differentiation of HL-60, 5 was 2.5 times and 6 was 12.5 times more active than 1.
  • 原野 一誠, 内田 一哉, 伊妻 美加, 青木 孝司, 衛藤 仁, 久野 拓造
    1988 年 36 巻 7 号 p. 2312-2322
    発行日: 1988/07/25
    公開日: 2008/03/31
    ジャーナル フリー
    Pericyclic reactions of 2, 5-bis(methoxycarbonyl)-3, 4-diphenylcyclopentadienone (Ia) with nonconjugated dienes (IIa-g) were investigated. The cyclopentadienone (Ia) reacted readily with IIa-g to give [4+2]π cycloadducts (IIIa-g) that lost carbon monoxide to afford intramolecular double Diels-Alder adducts (Va-g) on heating above the melting points. The structures of these adducts were determined from spectral evidence. The stability of the cycloadducts between twistene and isotwistene type compounds is discussed on the basis of molecular mechanics calculation data.
  • 田中 邦喜, 松尾 圭造, 中西 愛, 片岡 洋介, 高瀬 加津子, 大槻 節子
    1988 年 36 巻 7 号 p. 2323-2330
    発行日: 1988/07/25
    公開日: 2008/03/31
    ジャーナル フリー
    Several kinds of cyclic hydroxamic acids were synthesized. They exhibited metal chelating abilities and analgesic activities, as expected. Besides these activities, some of these compounds inhibited the growth of microorganisms.
  • 小林 優, 近藤 和彦, 長部 克典, 三橋 博
    1988 年 36 巻 7 号 p. 2331-2341
    発行日: 1988/07/25
    公開日: 2008/03/31
    ジャーナル フリー
    Sarcophytol A (1a), a potent anti-tumor-promotor cembranoid from the soft coral Sarcophyton glaucum, was subjected to various oxidation reactions. m-Chloroperbenzoic acid oxidation of 1a gave two epoxides (2a, 2b) which were converted to the corresponding diols 6b, 11b, 12b, 12'b and triols 4b, 9b. Lithium aluminum deuteride reduction of 2a gave a C-7 monodeuterated diol; this was used as a model experiment for the tritiation of 1a. Chromic acid oxidation of 1a gave seco-cembranoids 13b-18, a dienone 19, and a dihydrofuran derivative 20a. Sarcophytol A acetate (1b) was less reactive in chromic acid oxidation and afforded a seco-aldehyde 22a and a dihydroxy derivative 23a in low yield. Hydrolysis of 22a followed by acid treatment afforded the furan 18. Hydrolysis of 23a gave a triol, which, on further oxidation, gave the aldehyde 16, the major product of the chromic acid oxidation of 1a.
  • 細見 彰, 高良 真也, 富永 義則, 稲葉 正宏, 櫻井 英樹
    1988 年 36 巻 7 号 p. 2342-2345
    発行日: 1988/07/25
    公開日: 2008/03/31
    ジャーナル フリー
    Potassium 2, 6-disilapiperidide, readily prepared from 2, 2, 6, 6-tetrametyly-2, 6-disilapiperidine and potassium hydride, can be smoothly N-alkylated with alkyl halides to give the corresponding primary amines after acid hydrolysis.
  • 西出 喜代治, 山村 真理子, 山崎 まゆみ, 小堀 武夫, 常本 大英, 近藤 聖, 佐藤 清
    1988 年 36 巻 7 号 p. 2346-2353
    発行日: 1988/07/25
    公開日: 2008/03/31
    ジャーナル フリー
    Three step transformations of α-formylation, chlorination and hydrolysis starting from ethyl 4-thiazoleacetate (1) afforded a new cephem 7-side chain acid, (E)-3-chloro-2-(thiazol-4-yl)propenoic acid (4-(E)). The presence of the corresponding 4-(Z) derived from photoisomerization of 4-(E) was confirmed by nuclear magnetic resonance analysis. Acylation of several 7-aminocephalosporins was conducted by two routes involving the photoisomerization of 4-(E) to 4-(Z) (method A) or the isomerization of the activated intermediate (formula III) of the carboxylic acid 4-(E) with Vilsmeier reagent by heating (method B). The synthesis and the antibacterial activities of a new series of geometrical isomers of 7-[3-chloro-2-(thiazol-4-yl)propenamido] cephalosporins (formula II) are described.
  • 西出 喜代治, 山村 真理子, 小堀 武夫, 常本 大英, 近藤 聖, 佐藤 清
    1988 年 36 巻 7 号 p. 2354-2361
    発行日: 1988/07/25
    公開日: 2008/03/31
    ジャーナル フリー
    The syntheses and the antibacterial activities of new 3-dimethoxyphosphinylmethyl and 3-dihydroxyphosphinylmethyl cephalosporins I-(Z), II-(Z), III-(Z) and III-(E), possessing the chloromethylene or methoxyimino substituent at the α-position to the 7-(2-aminothiazol-4-yl)acetamido or 7-(thiazol-4-yl)acetamido moiety of the cephem nucleus, are described. The key steps of these syntheses were the Michaelis-Arbusov reaction of the 3-halomethylcephem 1 with trimethyl phosphite and the dealkylation reactions of both the dimethoxyphosphinyl group and the p-methoxybenzyl ester of 7a, b-(Z) by treatment with bromotrimethylsilane to afford 9a, b-(Z).
  • 水谷 健二, 福永 裕一郎, 田中 治, 高杉 直之, 猿渡 雄一郎, 不破 亨, 山内 辰郎, 王 建, 賈 敏如, 李 〓〓, 凌 一揆
    1988 年 36 巻 7 号 p. 2362-2365
    発行日: 1988/07/25
    公開日: 2008/03/31
    ジャーナル フリー
    From Huajiao, the pericarps of Zanthoxylum bungeanum MAXIM. (Rutaceae), six unsaturated aliphatic acid amides (1-6) were isolated. Of these, three were identical with the known amides, hydroxy-α-, hydroxy-β- and hydroxy-γ-sanshools(1, 2 and 3). The other three are new compounds, and the structures were established as (2E, 4E, 8E, 10E, 12E)-2'-hydroxy-N-isobutyl-2, 4, 8, 10, 12-tetradecapentaenamide, and (2E, 4E, 8Z, 11Z)- and (2E, 4E, 8Z, 11E)-2'-hydroxy-N-isobutyl-2, 4, 8, 11-tetradecatetraenamide (4, 5 and 6, respectively).
  • 高橋 昭, 草野 源次郎, 太田 富久, 野副 重男
    1988 年 36 巻 7 号 p. 2366-2370
    発行日: 1988/07/25
    公開日: 2008/03/31
    ジャーナル フリー
    Three new geranylphenols, flavidulols A, B and C (I, II and III), were isolated from an edible mushroom, Lactarius flavidulus IMAI, and their structures were elucidated on the basis of chemical and spectral evidence. Flavidulol A (I) exhibited antimicrobial activity against Staphylococcus aureus and other bacteria.
  • 宮一 諭起範, 井本 吉隆, 富森 毅, 難波 恒雄
    1988 年 36 巻 7 号 p. 2371-2376
    発行日: 1988/07/25
    公開日: 2008/03/31
    ジャーナル フリー
    From the root of Scutellaria scandens BUCH.-HAM. ex D. DON, five new flavanones (I-V) were isolated, together with oroxylin A, dihydrooroxylin A, wogonin, chrysin, baicalein, dihydrobaicalein, norwogonin, wogonin 7-O-glucuronide, chrysin 7-O-glucuronide, baicalin and dihydrobaicalin. Compounds I-V were identified as (2S)-5, 7, 2', 5'-tetrahydroxy-6-methoxyflavanone, (2S)-5, 7, 2', 5'-tetrahydroxy-6-methoxyflavanone 2'-O-β-D-glucopyranoside, (2S)-5, 7, 2', 5'-tetrahydroxy-6-methoxyflavanone 2'-O-β-D-(2-O-feruloyl)glucopyranoside, (2S)-5, 7, 2', 5'-tetrahydroxy-6-methoxyflavanone 2'-O-β-D-(2-O-sinapoyl)glucopyranoside and (2S)-5, 7, 2', 5'-tetrahydroxy-6-methoxyflavanone 2'-O-β-D-(2-O-vanilloyl)glucopyranoside, respectively, based on spectral and chemical data.
  • 井藤 千裕, 呉 天賞, 古川 宏
    1988 年 36 巻 7 号 p. 2377-2380
    発行日: 1988/07/25
    公開日: 2008/03/31
    ジャーナル フリー
    Three new monomeric carbazole alkaloids, 3-formylcarbazole (1), N-methoxy-3-formyl-carbazole (2), and pyrayaquinone-C (3), and two new binary carbazoles, murrafoline-E (4) and murrafoline-F (5), were isolated from root bark of Murraya euchrestifolia HAYATA (Rutaceae) collected in Taiwan, and their structures were elucidated.
  • JEAN-CHARLES LANCELOT, MAX ROBBA
    1988 年 36 巻 7 号 p. 2381-2385
    発行日: 1988/07/25
    公開日: 2008/03/31
    ジャーナル フリー
    The synthesis of 6H- and 4H-pyrido[2, 3-c]pyrrolo[1, 2-e]1, 2, 5-triazepine derivatives was described starting from 2-chloro(pyrrolyl-1)-3-pyridine and 2, 6-dichloro(pyrrolyl-1)-3-pyridine. Proton nuclear magnetic resonance spectra were studied.
  • 日野 克彦, 永井 保嵩, 宇野 準
    1988 年 36 巻 7 号 p. 2386-2400
    発行日: 1988/07/25
    公開日: 2008/03/31
    ジャーナル フリー
    Three series of compounds, 3-phenyl-5, 6-dihydro-1-benzazocines (7-9), 3-methyl-5H-1-benzazepines. (15-20) and 3-phenyl-4, 5-dihydro-3H-1- benzazepines (24-35), having a 2-(1-piperazinyl) group, were synthesized, and their pharmacological effects on the central nervous system were evaluated in mice. Among them, 3-methyl- (15-18) and 3-phenyl-4, 5-dihydro-2-piperazinylbenzazepines (26 and 33-35) showed mild anti-reserpine activity. However, no significant anti-exploratory, anti-maximal electroshock seizure or anti-tremorine activity was generally found.Novel ring transformations of α-chlorolactams are also described. The reaction of the 3-chloro-3-phenyl-2, 3, 4, 5-tetrahydro-1H-1-benzazepin-2-ones (37a, b) and benzazocinone analogs (46a, b) with piperidine or various piperazines resulted in ring contraction to give the 2-phenyl-1, 2, 3, 4-tetrahydroquinoline-2-carbozamides (38-41) and the analogous benzazepine-2-carboxamides (47 and 48), respectively. The reaction of analogous 3-chloro-3-methylbenzazepinone (14a) with potassium carbonate in methanol also resulted in similar ring transformation to give methyl tetrahydroquinoline-2-carboxylate (50). These rearrangements were supposed to proceed via the azirinone intermediate.
  • 小川 英則, 玉田 重晴, 藤岡 孝文, 寺本 修二, 近藤 一見, 山下 修司, 薮内 洋一, 富永 道明, 中川 量之
    1988 年 36 巻 7 号 p. 2401-2409
    発行日: 1988/07/25
    公開日: 2008/03/31
    ジャーナル フリー
    A series of 1-aromatic ring substituted 4-(3, 4-dimethoxybenzoyl)piperazines were synthesized and examined for positive inotropic activity on the canine heart. Among them, 6-[4-(3, 4-dimethoxybenzoyl)-1-piperazinyl]-3-methyl-1H, 3H-quinazolin-2, 4-dione was found to have a potent activity.
  • 太田 裕子, 幸田 光復, 木本 博, 岡野 孝, 川添 豊
    1988 年 36 巻 7 号 p. 2410-2416
    発行日: 1988/07/25
    公開日: 2008/03/31
    ジャーナル フリー
    Ethyl esters of alkanesulfonic acids, isethionic acid, trifluoromethanesulfonic acid, and 2, 2, 2-trifluoroethanesulfonic acid were synthesized and tested for inhibitory activity toward the growth of cultured leukemia L1210 cells. A quantitative correlation with the rate of hydrolysis and the capacity factor (partition property) was demonstrated by a multiple linear regression analysis; the more reactive and more lipophilic, the more cytotoxic they are. Interestingly, fluorine substitution on the alcoholic moiety resulted in remarkable deviations of the toxicity from those expected from the correlation found for the ethyl esters without fluorine substitution. Then, some fluorine derivatives of busulfan, a clinically used bifunctional sulfonate, were synthesized and tested. 2, 2-Difluoroethyl 2, 2, 2-trifluoroethanesulfonate was several times more cytotoxic than busulfan.
  • 岩越 淳, 小西 天二, 清沢 脩, 嶋田 康男, 宮原 一元, 川崎 敏男
    1988 年 36 巻 7 号 p. 2417-2422
    発行日: 1988/07/25
    公開日: 2008/03/31
    ジャーナル フリー
    Three new phenylethylchromone derivatives, tentatively named AH7, AH8 and AH9, were isolated from acetone and pyridine extracts of agalwood (jinko) from Kalimantan. AH7 from the pyridine extract was characterized as 5, 8-dihydroxy-2-(2-phenylethyl)chromone, and AH8 from the acetone extract was elucidated to be 6, 7-dimethoxy-2-[2-(4-methoxyphenyl)chromone. AH9, acetylated in order to separate it from the mixture, was concluded to be (5S, 6S, 7R)-5a', 6a, 7a-triacetoxy-2-[2-(2-acetoxyphenyl)ethyl]-5, 6, 7, 8, 8-pentahydrochromone on the basis of the proton nuclear magnetic resonance (1H-NMR) spectrum, dihedral angle and circular dichroism (CD) spectral data.
  • 瀬戸 衛, 宮瀬 敏男, 梅原 薫, 上野 明, 平野 豊, 大谷 徳生
    1988 年 36 巻 7 号 p. 2423-2429
    発行日: 1988/07/25
    公開日: 2008/03/31
    ジャーナル フリー
    Four new sesquiterpene lactones, cichoriolide A and cichoriosides A, B and C, have been isolated from Cichorium endivia L. and C. intybus L., together with nine known sesquiterpene lactones. The structures of the new compounds were established on the basis of chemical and spectral data. Further, the cytotoxic activities of related glycosides and the aglycones were compared in the L-5178Y cultured cell system.
  • 下村 裕子, 指田 豊, 三巻 祥浩, 飯高 洋一
    1988 年 36 巻 7 号 p. 2430-2446
    発行日: 1988/07/25
    公開日: 2008/03/31
    ジャーナル フリー
    New bitter phenolic glycosides and a steroid glucoside have been isolated from the fresh bulbs of Lilium Henryi. On the basis of spectroscopic data, chemical evidence and X-ray crystallographic analysis, their structures have been elucidated as (2S)-1-O-p-methoxycinnamoyl-3-O-β-D-glucopyranosylglycerol (methylregaloside A), (2S)-1-O-caffeoyl-3-O-β-D-glucopyranosylglycerol (regaloside C), 3-O-feruloyl-6'-O-(4-O-β-D-glucopyranosylferuloyl)sucrose, and (25R)-3β, 26-dihydroxy-5α-cholestane-6, 22-dione 3-O-β-D-glucopyranoside. Several known components have also been isolated and identified.
  • 岩渕 久克, 吉倉 正博, 上硲 和輔
    1988 年 36 巻 7 号 p. 2447-2451
    発行日: 1988/07/25
    公開日: 2008/03/31
    ジャーナル フリー
    A novel sesquiterpene alcohol named ginsenol (1) has been isolated from the rootlets of Panax ginseng C. A. MEYER (Araliaceae). The structure of 1 was established on the basis of chemical reactions and spectral data.
  • 木内 文之, 中村 憲夫, 津田 喜典, 近藤 力王至, 吉村 裕之
    1988 年 36 巻 7 号 p. 2452-2465
    発行日: 1988/07/25
    公開日: 2008/03/31
    ジャーナル フリー
    Eight new amide constituents together with seven known amides were isolated from pepper and their structures were determined by spectroscopic means. They are piperamide-C5 : 1(2E) (2), -C7 : 1(6E) (3), -C7 : 2(2E, 6E) (4), -C9 : 1(8E) (5), -C9 : 3(2E, 4E, 8E) (7), 1-[(2E, 4E)-2, 4-decadienoyl]pyrrolidine (8), and 1-[(2E, 4E)-2, 4-dodecadienoly]pyrrolidine (9). Among all of the amides isolated, seven (3, 4, 5, 6, 8, 9, and 15) showed larvicidal activity against second-stage larva of Toxocara canis and the others were inactive. The assay results suggested that the strongest activity was exhibited by the tertiary amides (piperidin- and pyrrolidin-amides) possessing a nine-carbon chain between the aromatic group and the amine moiety [for example, piperamide-C9 : 1(8E), MLC : 0.05mM after 24h of incubation]. The aliphatic amides 8 and 9 were also larvicidal. Mass spectra of piperamides are also discussed.
  • 清水 繁, 石原 尚美, 梅原 薫, 宮瀬 敏男, 上野 明
    1988 年 36 巻 7 号 p. 2466-2474
    発行日: 1988/07/25
    公開日: 2008/03/31
    ジャーナル フリー
    A new guaiane-type sesquiterpene glycoside, cynaroside A, seven new ursane-type saponins, cynarasaponins A-G, and three new oleanase-type saponins, cynarasaponins H-J, have been isolated from Cynara cardunculus L., together with a known guaiane-type sesquiterpene glycoside, 11β, 13-dihydrodesacylcynaropicrin-8-β-D-glucoside, and a known oleanane-type saponin, chikusetsusaponin IVa. The structures of the new compounds were established on the basis of chemical and spectral data. This is the first isolation of saponin from Compositae plants.
  • 宮瀬 敏男, 上野 明, 滝沢 信夫, 小林 弘美, 小口 ひろ子
    1988 年 36 巻 7 号 p. 2475-2484
    発行日: 1988/07/25
    公開日: 2008/03/31
    ジャーナル フリー
    Ten new glycosides, icarisides A2-A4, B5-B7, E3, F1-F2 and G1, were isolated from the polar fraction of the water extract of Epimedium grandiflorum MORR. var. thunbergianum (MIQ.) NAKAI, together with three known glycosides, phenethyl glucoside, (Z)-3-hexenyl glucoside and blumenol C glucoside. Their structures were established on the basis of chemical evidence and spectral data.
  • 佐用 博照, 細川 幹夫, 李 英培, 仮家 公夫
    1988 年 36 巻 7 号 p. 2485-2489
    発行日: 1988/07/25
    公開日: 2008/03/31
    ジャーナル フリー
    The chloroperoxidase-catalyzed oxidation of 1, 4-diazabicyclo[2.2.2]octane (DABCO) by H2O2 or ethylhydroperoxide (EHP) in the presence of Cl- was investigated at pH 2.75, 5.0, and 7.0, and the results were compared with those of the chemical oxidation by HOCl. The oxidation of DABCO in the chloroperoxidase-EHP-Cl- system at pH 5.0 gave a fairly well-resolved electron spin resonance spectrum, which was identified as that of the radical cation of DABCO. The detection of the radical cation suggests that the first step of the chloroperoxidase-catalyzed oxidation of DABCO is the formation of the DABCO chloroammonium cation followed by the homolysis of the cation.
  • 湯田 康勝, 田中 淳子, 平野 文也, 北川 晴雄
    1988 年 36 巻 7 号 p. 2490-2498
    発行日: 1988/07/25
    公開日: 2008/03/31
    ジャーナル フリー
    The peroxidation of lipids and the activities of related enzymes, such as superoxide dismutase (SOD), and glutathione peroxidase (GSH-Px), the migration of leucocytes in the pleural space, and the release of superoxide by leucocytes were studied in a rat model of Bordetella pertussis vaccine pleurisy.A pleural injection of B. pertussis vaccine into sensitized rats was found to be associated with a transient increase of lipid peroxidation in the exudate and the serum, but the level of thiobarbituric acid-reactive substance rapidly diminished.The diminution of lipid peroxidation was not relatd to the activity of GSH-Px but was related to the activity of SOD. The migration of leucocytes into the pleural cavity increased gradually and reached the maximum value 96h after the intrapleural challenge, but the release of superoxide by leucocytes was not correlated with the number of leucocytes. The number of polymorphonuclear cells (PMN) reached the maximum value 24h later, then gradually decreased, and mononuclear cells replaced PMN. Mononuclear cells were more numerous than PMN in the leucocyte population of the exudate in vaccine-induced pleurisy. The release of superoxide by leucocytes reached the maximum value 24h later, then decreased gradually. Therefore, the production rate of supoxide by PMN was larger than that by mononuclear cells.A principal component analysis of these parameters was carried out. It has been suggested that the inflammatory process of pertussis vaccine pleurisy can be divided into three phases. The first response (0-24h) represents the acute phase response; this phase has the characteristic of a predominantly PMN population in the exudate and there is marked superoxide generation or lipid peroxidation. The second phase of the response (24-96h) represents the delayed-type reaction; this phase has the characteristic of a predominantly mononuclear cell population in the exudate. The third phase of the response (96-144h) represents the healing process of the inflammatory reaction.
  • 足立 博一, 古西 清司, 北 潔, 堀越 勇
    1988 年 36 巻 7 号 p. 2499-2505
    発行日: 1988/07/25
    公開日: 2008/03/31
    ジャーナル フリー
    The activity of glucose-dependent oxygen consumption of whole cells of Photobacterium phosphoreum was inhibi6ted by purified pentagalloylglucose (1, 2, 3, 4, 6-penta-O-galloyl-β-D-glucose). Sonicated membrane vesicles were used to study the effect of the inhibitor on the electron transport activity. The activity of reduced nicotinamide adenine dinucleotide (NADH) oxidase in sonicated membrane vesicles of P. phosphoreum decreased when pentagalloylglucose was added to the assay system. The results suggested that the targets of inhibitory action were NADH dehydrogenase and terminal oxidase.The effect of the inhibitor on the terminal oxidase was compared in the case of purified terminal oxidase (cytochrome bd complex) and sonicated membrane vesicles. The oxidase activities toward ubiquinol-1 and N, N, N', N'-tetramethyl-p-phenylenediamine dihydrochloride (TMPD) in the presence of ascorbate were both inhibited by pentagalloylglucose in sonicated membrane vesicles and purified cytochrome bd complex. The inhibition of ubiquinol-1 oxidase activity in sonicated membrane vesicles and purified enzyme was of noncompetitive type. On the other hand, the inhibitions of TMPD plus ascorbate oxidase in both membrane vesicles and purified enzyme were uncompetitive. Thus, the mechanisms of inhibition of the two kinds of oxidase activities by the inhibitor were different.The inhibitory effect of tetragalloylglucose (1, 2, 3, 6-tetra-O-galloyl-β-D-glucose) on the respiratory chain was similar to that of pentagalloylglucose in the case of membrane vesicles and purified enzyme.
  • 安孫子 敬, 関野 宏
    1988 年 36 巻 7 号 p. 2506-2516
    発行日: 1988/07/25
    公開日: 2008/03/31
    ジャーナル フリー
    The octatetracontapeptide corresponding to the entire amino acid seuence of human thymopoietin (hTP) was synthesized by assembling ten peptide fragments in solution followed by deprotection with 1 M trifluoromethanesulfonic acid-thioanisole (molar ratio, 1 : 1) in trifluoroacetic acid in the presence of dimethylselenide and m-cresol. Finally, the deprotected peptide was incubated with dithiothreitol to reduce sulfoxide on the methionine side chain. The synthetic peptide was found to have a restoring effect on the impaired blastogenic response of T-lymphocytes isolated from uremic patients.
  • 大槻 昌彦, 中西 義信, 関水 和久, 名取 俊二
    1988 年 36 巻 7 号 p. 2517-2522
    発行日: 1988/07/25
    公開日: 2008/03/31
    ジャーナル フリー
    A nuclear extract of Ehrlich ascites tumor cells was separated into three fractions that were essential for accurate transcription initiation. Studies with these fractions showed that the efficiency of transcription of supercoiled deoxyribonucleic acid (DNA) was better than that of linear DNA. A clear difference was found in the rates of formation of a preinitiation complex with these two templates. Consistent with this difference, the results of gel shift assay showed that the complex of supercoiled DNA with transcription factors is much more complicated than that of linear DNA.
  • 宮浦 修一, 堀江 貴代子, 磯野 秀夫
    1988 年 36 巻 7 号 p. 2523-2530
    発行日: 1988/07/25
    公開日: 2008/03/31
    ジャーナル フリー
    Glutathione peroxidase (GP EC 1.11.1.9) activity of glutathione S-transferse (GST, EC 2.5.1.18) in rabbit liver was investigated by using hydrogen peroxide (H2O2) and cumene hydroperoxide (C-OOH) as substrates for GP and 1-chloro-2, 4-dinitrobenzene (CDNB) as a substrate for GST.The crude extract from rabbit liver was applied to a diethylaminoethyl (DEAE)-cellulose column equilibrated with 10mM Tris-HCl (pH 8.0) and the absorbed proteins were eluted with the same buffer contaning 0.5 M KCl. The DEAE-non-adsorbed fraction showed 63-87% of the GST activity of the crude extract and 27-36% of the GP activity toward C-OOH, but no GP activity toward H2O2. The DEAE-adsorbed fraction showed 2-11% of the GST activity, 28-48% of the GP activity toward C-OOH and 54-87% of the GP activity toward H2O2. GST and GP in the DEAE-adsorbed fraction could be completely separated as two different activity peaks by gel filtration. This GP had a molecular weight of about 84000, a value similar to those of the well-known selenium-dependent GPs. However, activities of GST and GP in the DEAE-non-adsorbed fraction were eluted as a single peak on gel filtration. The proteins in the peak had a molecular weight of about 52000, a value corresponding to those of the rabbit hepatic GST forms in the previous study.The DEAE-non-adsorbed fraction was resolved into at least seven GST activity peaks (R0, R1, R2, Rx, R3, Rz, R4) by carboxymethyl (CM)-cellulose chromatography or at least eight GST activity peaks (I, II, III, IV, VI, VII, VIII, IX) by isoelectric focusing. These peaks, excepting R2 and VII-IX, showed a high GP activity toward C-OOH.The present study and the previous studies indicate that GST forms composed of Y1 and/or Y3 subunit have a high GP activity toward C-OOH and that these forms account for most of the non-selenium-dependent GP activity in rabbit liver.
  • 金庭 延慶, 今川 歓二, 市川 順一
    1988 年 36 巻 7 号 p. 2531-2537
    発行日: 1988/07/25
    公開日: 2008/03/31
    ジャーナル フリー
    The effect of particle size on compaction properties and compaction mechanism was investigated by using sulfadimethoxine (SD) and sulfaphenazole (SP) as model drugs. The plots of log(mean compaction pressure) against the thickness of the powder bed for SD and SP showed that the compaction proceeded biphasically (primary and secondary compaction) except in the case of the larger particle size fraction (42/48 mesh) for SD, and the compaction process of SD was much more markedly affected by particle size than that of SP. Analysis based on Janssen's equation suggested that the compaction proceeded by a repetitive process of structure formation and fracture. The tensile strength of SP tablets was higher than that of SD tablets, and the change in the fractional voidage indicated that all particle size fractions of SP gave tablets having the same structure. On the other hand, for SD, the larger particle size fractions showed higher tensile strength than the smaller particle size fractions in the intial compression pressure region, and measurement of the compaction energy indicated that the binding between the particles in the larger particle fractions was more effective than that of the smaller particle size fractions in that region. These results suggested that the compaction process of SD involves particle fragmentation, while that of SP involves mainly plastic deformation.
  • 山下 伸二, 高橋 政文, 政田 幹夫, 灘井 種一, 小林 亨, 黒崎 勇二, 中山 太二, 木村 聰城郎
    1988 年 36 巻 7 号 p. 2538-2543
    発行日: 1988/07/25
    公開日: 2008/03/31
    ジャーナル フリー
    The effect of experimental acute renal failure on the permeability and transport function of the intestinal membrane was analyzed in the isolated rat jejunum by using in vitro electrophysiogical methods. The mucosal-to-serosal flux rate sulfanilic acid (SA), which was used as a model of the polar drug, increased significantly in the membrane obtained from the rat with acute renal failure, indicating a reduction of the barrier function of the intestinal membrane. This effect of renal failure was neither dependent on the procedure used to induce the disease nor correlated with the extent of the disease state, shown by the level of blood urea nitrogen. Furthermore, it was clarified that the change in the permeability to SA occurred mainly in the transcellular pathway but not in the paracellular one. The electrical rezistance of the jejunal membrane did not change in rats with acute renal failure. Thus, it was suggested that the structure of the tight-junctional portion of the epithelial layer remained unchanged, while the permeability of the cellular membrane was altered by the disease state. The activity of the intestinal membrane to transport Na+ or glucose might not be influenced by the disease state since the transmembrane potential difference and the short-circuit current of the membrane showed no significant change from their normal values.
  • 西畑 利明, 斉藤 由紀子, 酒井 清
    1988 年 36 巻 7 号 p. 2544-2550
    発行日: 1988/07/25
    公開日: 2008/03/31
    ジャーナル フリー
    The intestinal absorption of N, N'-dimethylcarbamoylmethyl 4-(4-guanidnobenzoyloxy) phenylacetate methanesulfonate (FOY305[○!R]) in rats was investigated using a rat intestinal loop method. Plasma drug concentrations and the disappearance of the drug from the intestinal lumen were measured. The absorption of FOY305 after administration into a rectal loop was greater than those after administration into variously positioned small intestinal loops. The low absorption of FOY305 after administration into the small intstine was due to the rapid degradation of FOY305 by esterase activity in the small intestinal lumen.
  • 上能 伊公雄, 中村 敏明, 堀内 正, 灘井 雅行, 北澤 式文, 吉峯 徳, 葛谷 文男
    1988 年 36 巻 7 号 p. 2551-2556
    発行日: 1988/07/25
    公開日: 2008/03/31
    ジャーナル フリー
    The diurnal variation in pharmacokinetics of valproic acid (VPA) was studied at unequal dosing intervals, because patients generally take drugs with each meal or with poor compliance. Six healthy volunteers (22 to 32 years old) orally took 300 mg of sodium valproate at 9 : 00 and 18 : 00 each day for 6 d. On the sixth day, blood was drawn periodically for 24 h for pharmacokinetic analysis. Faster absorption and a shorter absorption lag-time were observed at morning dosing after a light meal, and this may be meal-related. The systemic clearance and the mean plasma level during day were in good agreement with those during the night, although VPA plasma levels showed large diurnal fluctuations. Plasma albumin concentration at night was significantly decreased and this seems consistent with the finding that the free fraction (FF) of VPA was higher during the night. A significant negative correlation between plasma albumin concentration and the FF was observed. These results suggest that the VPA dosing schedule used here is adequate for maintaining the mean plasma level in an appropriate range. Mealtimes and blood sampling times should the taken into account in routine plasma VPA level monitoring to minimize the influence of diurnal variation.
  • 砂田 久一, 山本 昭夫, 大塚 昭信, 米澤 頼信
    1988 年 36 巻 7 号 p. 2557-2561
    発行日: 1988/07/25
    公開日: 2008/03/31
    ジャーナル フリー
    A series of experiments was conducted to evaluate the changes of surface area during the dissolution process of sieved crystalline particles. The dissolution of some paraben derivatives was followed under the sink condition. Whole particles were collected at intervals during the dissolution measurements. The mean diameter and surface area of the gathered particles were estimated by geometrical and projected area measurements on photomicrographs, and with a LUZEX image analyzer. A fairly good correlation between the surface area (SH) estimated from Heywood's diameter and the projected area was obtained in spite of the gradual change of particle shape. The dissolution rate constants of sieved paraben crystals were very, even though the original particle sizes were different. Dissolution measurements of binary systems mixed at various ratios of the sieved samples were carried out. These dissolution profiles were simulated based on the changes of surface area in the dissolution process of the sieved components by the use of SH. The simulated dissolution curves estimated from SH coincided well with those measured over almost the whole dissolution process. The evaluation of dissolution behavior based on the measurement of particle size or particle surface area appears to be useful to estimate or predict the dissolution process.
  • 石坂 隆史, 本田 宏隆, 居川 賢一, 木津 典生, 矢野 行一, 小石 眞純
    1988 年 36 巻 7 号 p. 2562-2569
    発行日: 1988/07/25
    公開日: 2008/03/31
    ジャーナル フリー
    Dry mixing of aspirin with potato starch in a centrifugal rotating mixer produced a novel powder, composed of potato starch particles with an aspirin layer adhering on their surfaces. Friction and collision which occurred in the dry mixing process micronized and spread aspirin over the potato starch surfaces, forming a thin aspirin layer. The powder gave a higher rate of aspirin dissolution than a physical mixture. It was suggested from powder X-ray diffractometry, differential scanning calorimetry, and contact angle measurements that the improvement of dissolution rate was caused by an increase in wettability and an increase in the available surface area aspirin.
  • 武田 厚司, 五島 廉輔, 岡田 昌二
    1988 年 36 巻 7 号 p. 2570-2575
    発行日: 1988/07/25
    公開日: 2008/03/31
    ジャーナル フリー
    The mechanism of transport of 99mTc-DL-homocysteine (99mTc-Hcy), a possible tumor-imaging agent, was studied. In the blood of mice at 10 min after intravenous injection of 99m Tc-Hcy, most of the radioactivity was distributed in the plasma in both the protein-bound and free forms. The protein-bound form was not appreciably dissociated in physiological saline. Further, when the protein-bound form was injected into tumor-bearing mice, the tumor-distributed radioactivity was about twice that of free 99mTc-Hcy. The binding protein was considered to be albumin from the result of high performance liquid chromatography analysis. An in vitro experiment showed that the tumor uptake of 131I-albumin was much less than that of 99mTc-Hcy-albumin. On the other hand, the radioactivity in the tumor cells of 99mTc-Hcy-injected mice was found to be mostly that of free 99mTc-Hcy. These results suggest that a portion of the 99mTc-Hcy ingected was transported to the tumor tissue as an albumin complex in the blood, then released from the albumin and taken up by the cells.
  • 小川 泰亮, 岡田 弘晃, 山本 眞樹, 島本 次雄
    1988 年 36 巻 7 号 p. 2576-2581
    発行日: 1988/07/25
    公開日: 2008/03/31
    ジャーナル フリー
    To screen a suitable polymer for preparing a controlled-release dosage form effective for one month, square plates of polyactic acid (PLA) with average molecular weights of 6000 to 50000 and copoly(lactic/glycolic) acid (PLGA) with average molecular weights of 6000 to 13500 and a copolymer ratio of 90/10 to 55/45 were implanted in rats subcutaneously, and the weight losses were determined over 100 d. Typically the pattern of weight loss was biphasic with a lag time followed by a period when the weight fell exponentially. The lag times and the half lives of the degradation period increased with increase in the molecular weight or with decrease in glycolide content. Release of leuprolide acetate from PLA microcapsules at the injection site in rats (in vivo release) tended to be comparable to the bioerosion rate of the polymer used as the wall substance, and the in vivo release of the drug from PLGA microcapsules tended to be comparable to the biodegradation rate of the polymer. The in vivo release profile of the drug from microcapsules prepared with PLGA of average molecular weight 14000 and copolymer ratio 75/25 was ideal for one month's controlled release. The in vivo release profile from microcapsules injected subsutaneously in rats was comparable to the in vitro release.
  • 黒野 幸久, 神野 康弘, 桑山 知成, 八代 有, 池田 憲
    1988 年 36 巻 7 号 p. 2582-2586
    発行日: 1988/07/25
    公開日: 2008/03/31
    ジャーナル フリー
    Reversible hydrolyses of benzodiazepinooxazoles having an 11b-methyl group and of oxazolam having a 7-methyl group were investigated kinetically in buffers of various pH's and at 25°C, in the light of the light of the difference in the reversibility of the hydrolysis between 11b-methyl- and 11b-phenyl- (e.g., oxazolam itself) benzodiazepinooxazoles. The irreversibility of the hydrolysis of 11b-phenylbenzodiazepinooxazoles is considered to arise from the larger size of the phenyl group than the methyl group in addition to the intramolecular hydrogen bonding between carbonyl oxygen of benzophenone and amide hydrogen at the ortho position. Substituents at the 2-position of 11b-methylbenzodiazepinooxazole do not greatly affect the reversible hydrolysis.
  • 王 本祥, 趙 学慧, 斉 尚斌, 金子 周司, 服部 征雄, 難波 恒雄, 野村 靖幸
    1988 年 36 巻 7 号 p. 2587-2592
    発行日: 1988/07/25
    公開日: 2008/03/31
    ジャーナル フリー
    Several biochemical parameters related to aging were evaluated after a hot-water extract prepared from unossified pilose antler of Cervus nippon TEMMINCK var. mantchuricus Swinhoe (Rokujo) had been administered orally for 8 successive days to senescence-accelerated mice (SAM), a novel murine model of spontaneously promoted aging. It was found that the repeated oral administration of Rokujo had significant restoring effects on the physiological degenerations which were associated with the development of senile symptoms. These effects included (1) an increase in the plasma testosterone level in male mice; (2) a decrease in the contents of malondialdehyde in the liver and brain; (3) an increase in the liver protein contents; (4) an increase in the liver superoxide dismutase activity; and (5) a decrease in the activity of monoamine oxidase B in the liver and brain membranes. Most of these effects were selectively observed in the senile-prone strain of SAM (SAM-P) as compared to the normal, resistant strain (SAM-R). The present data suggest that Rokujo may exert an anti-aging action in male senile animals.
  • 王 本祥, 趙 学慧, 斉 尚斌, 楊 秀偉, 金子 周司, 服部 征雄, 難波 恒雄, 野村 靖幸
    1988 年 36 巻 7 号 p. 2593-2598
    発行日: 1988/07/25
    公開日: 2008/03/31
    ジャーナル フリー
    The effects of subchronic administration of Rokujo (Cervus nippon TEMMINCK var. mantchuricus Swinhoe) extract on protein, ribonucleic acid (RNA) and deoxyribonucleic acid (DNA) syntheses in vivo were investigated in male senescence-accelerated mice (SAM). At 20 min after intraperioneal injection of amino acid and nucleosides labeled with radioisotpes, the incorporation of [14C]leucine into the serum protein was increased in the Rokujo-treated mice, in a parallel manner to the elevation of the serum protein content. Increased incorporation of [14C]uridine into RNA as well as that of [14C]leucine into protein was found in the liver and kidney of the Rokujo-treated mice. Further experiments revealed that although a brief exposure to Rokujo extract in vitro did not directly affect the RNA polymerase activity, the activity of RNA polymerase II in solubilized liver nuclei of Rokujo-treated mice was markedly accelerated. These results suggest that enhancement of RNA polymerase II activity induced by long-term Rokujo treatment is responsible for the increase in protein synthesis in vivo in SAM.
  • 浄住 護雄, 島田 秀昭, 本田 俊哉, 児島 昭次
    1988 年 36 巻 7 号 p. 2599-2606
    発行日: 1988/07/25
    公開日: 2008/03/31
    ジャーナル フリー
    The effect of various chelating agents, sodium N-benzyl-D-glucamine dithiocarbamate (NBG-DTC), 2, 3-dimercaptopropanol (BAL), D-penicillamine (D-PEN), and sodium N-methyl-D-glucamine dithiocarbamate (NMG-DTC), on the distribution and excretion of inorganic mercury were compared in rats exposed to HgCl2. Rats were injected i.p. with 203HgCl2 (300 μg of Hg and 2 μCi of 203Hg/kg) and 30 min or 24 h later, were injected with a chelating agent (400 μmol/kg). NBG-DTC and BAL mainly promoted the biliary excretion of mercury, while D-PEN and NMG-DTC significantly promoted the urinary excretion of mercury. In rats pretreated with HgCl2 30 min earlier, the injection of NBG-DTC reduced the content of mercury in the pancreas. BAL significantly reduced the contents of the liver, kidney, and pancreas. D-PEN reduced the contents of mercury in the pancreas, lung, and heart. In rats pretreated with HgCl2 24 h earlier, NBG-DTC reduced the content of mercury in the kindey. BAL reduced the contents of mercury in the liver and kidney, although BAL caused the redistribution of mercury to the lung, heart, and brain. In rats injected with NBG-DTC at 30 min after pretreatment with HgCl2, the biliary excretion of mercury increased with increasing dose of NBG-DTC. In rats injected with NBG-DTC at 24 h after pretreatment with HgCl2, the biliary excetion of mercury increased with increasing dose of NBG-DTC at the doses of 400-1200 μmol/kg and ato the doses above 1200 μmol/kg the urinary excretion of this metal increased remarkably. A long time interval beween the administrations of mercury and NBG-DTC resulted in the decreased biliary excretion of mercury. The reduced stimulatory effect of NBG-DTC on the biliary excretion of mercury with time after the pretreatment with mercury may result from the decrease of tissue mercury concentration and labile mercury content in the rat body.
  • 久保 陽徳, 齋藤 直樹, 大和 秀一, 山内 玲子, 蛭間 和美, 井上 玲
    1988 年 36 巻 7 号 p. 2607-2614
    発行日: 1988/07/25
    公開日: 2008/03/31
    ジャーナル フリー
    An efficient synthesis of 4-methyl-3-(2, 4, 5-trimethoxy-3-methylphenylmethyl)-2, 5-piperazinedione 5 and 1-methyl-3-(2, 4, 5-trimethoxy-3-methylphenylmethyl)-2, 5-piperazinedione 10 from (Z)-1-acetyl-3-(2, 4, 5-trimethoxy-3-methylphenylmethyl)-2, 5-piperazinedione 2 is described.The 1-methyl-2, 5-piperazinedione 10 is shown to be a useful intermediate for preparation of the 1, 5-imino-3-benzazocine derivative 16, which is the skeleton of the "right half" of saframycins.
  • 松田 玲子, 久保 道徳
    1988 年 36 巻 7 号 p. 2615-2623
    発行日: 1988/07/25
    公開日: 2008/03/31
    ジャーナル フリー
    The hypoglycemic activity of extracts from muscles of pigs (Sus scrofa; P), chickens (Gallus domesticus; C) and mackerel (Scomber japonicus; M) was examined. P exhibited an insulin-like activity on conversion of glucose to total lipids in rat free fat cells and an insulin secretion-promoting effect on perfused rat pancreas. C showed an insulin-like activity, an insulin secretion-promoting effect and an inhibitory effect on hepatic glycogenolysis. M proved to have a weak insulin-like activity, and a weak insulin secretion-promoting effect, but its inhibitory effect on hepatic glycogenolysis was strong.After intraperioneal administration of P, C and M, the blood glucose levels decreased in both normal mice and alloxan-induced diabetic mice.
  • 佐藤 潔, 織田 寿久, 杉林 堅次, 森本 雍憲
    1988 年 36 巻 7 号 p. 2624-2632
    発行日: 1988/07/25
    公開日: 2008/03/31
    ジャーナル フリー
    In order to estimate the in vivo behavior (e.g., blood concentration) of drugs on percutaneous absorption from in vitro permeation data using excised skin and pharmacokinetic parameters at intravenous administration, two models, a diffusion model and a compartment model with or without shunt transport, were established and applied to the in vitro and in vivo skin permeation data of nicorandil in hairless rats. When water was employed as a donor solvent (water treatment), the plasma concentration-time curve, which was calculated by means of the diffusion model, was similar to the observed values without introduction of shunt transport. In the case of propylene glycol treatment, on the other hand, the calculated plasma levels were not necessarily similar to the observed values, but it was found that the calculated values were better fitted to the observed values by introduction of shunt transport in the in vitro skin diffusion model. Similar results were obtained with the compartment model. These results suggest that both models may be useful to predict the plasma concentration after application of topical formulations. The characteristics and usefulness of these models were compared with those of the previously reported convolution method.
  • 森本 雍憲, 関 俊暢, 杉林 堅次, 從二 和彦, 宮崎 正三
    1988 年 36 巻 7 号 p. 2633-2641
    発行日: 1988/07/25
    公開日: 2008/03/31
    ジャーナル フリー
    The permeability of a model drug, nicardipine hydrochloride (NC), through ethylene-vinyl acetate copolymer (EVAc) or ethylene-vinyl alcohol copolymer (EVAl) membrane as a rate controlling layer was examined as one step in the development of a well-designed membrane permeation-controlled transdermal therapeutic system (TTS). The membrane permeability of NC from various suspensions in ethanol (EtOH)-methyl ethyl ketone (MEK)-water mixed solvents was affected by the solvent composition as well as the membrane composition. The NC permeation through EVAc membrane increased with increase in the MEK content in the solvent, whereas that through the EVAl membrane showed a convex curve against MEK content. As solvent penetration into the membranes may be important for the NC permeation, the extent of swelling of EVAc or EVAl beads was determined as an index of solvent pentration. The relationship between the solvent composition and degree of swelling of the copolymer was similar to that between the solvent composition and the logarithm of the product of the steady-state permeation rate of NC through EVAc or EVAl membrane and thickness of the membrane. It was found from the results of the permeation and swelling experiments that the permeability of NC through EVAc or EVAl membrane is mainly affected by the solvent penetration into the membrane. Finally, the effect of EVAll membrane on the permeation of NC through the intact or damaged skin was measured. The NC permation through a piled layer of EVAl membrane and full-thickness skin was similar to that through a piled layer of EVAl membrane and damaged skin. This result suggests that the application of these membranes would be useful in making a well-designed TTS which shows little inter- and/or intra-subject variation in skin permeation of NC.
  • YUN-LIAN LIN, YUEH-HSIUNG KUO, MING-CHU CHENG, YU WANG
    1988 年 36 巻 7 号 p. 2642-2646
    発行日: 1988/07/25
    公開日: 2008/03/31
    ジャーナル フリー
    A new neoclerodane-type diterpenoid lactone, scutellone E, together with a known compound, scutellone D (scuterivulactone D), has been isolated from aerial parts of Scutellaria rivularis WALL. Their structures have been determined from X-ray diffraction, spectral and chemical evidence.
  • 中村 憲夫, 木内 文之, 津田 喜典
    1988 年 36 巻 7 号 p. 2647-2651
    発行日: 1988/07/25
    公開日: 2008/03/31
    ジャーナル フリー
    Inspections of the infrared spectra of more than twenty tertiaty and secondary amides and acid-induced shift experiments clarified that, in open chain amides, the carbonyl absorption shifts to lower frequency by 10-20 cm-1 when a conjugation is introduced and that, among the plural absorptions at 1600-1700 cm-1 in conjugated amides, the lowest absorption (usually the most intense one) should be attributable to the C=O and the higher absorptions are assignable to the C=C.
  • 上山 勉, 榎本 三郎, 井上 正美
    1988 年 36 巻 7 号 p. 2652-2653
    発行日: 1988/07/25
    公開日: 2008/03/31
    ジャーナル フリー
    Aromatic sulfinic acids were synthesized conveniently by the direct oxidation of thiols with 30% aqueous hydrogen peroxide at room temperature in good yield.
  • 黒川 弓, 竹田 忠紘, 荻原 幸夫, 清水 正樹, 高井 誠
    1988 年 36 巻 7 号 p. 2654-2660
    発行日: 1988/07/25
    公開日: 2008/03/31
    ジャーナル フリー
    A water-soluble polysaccharide, designated as CSP-I, was isolated from the bark of Melia azadirachta (Meliaceae) and its inhibiting effect on the growth of subcutaneously inoculated Sarcoma-180 was tested in mice. CSP-I gave a single peak on high-preformance liquid chromatography and gel filtration. Chemical and spectroscopic studies indicated that the structure is composed of a β-D-(1→3)-linked galactopyranosyl backbone possessing branching points at position O-6 to which α-L-arabinofuranose, β-D-galactopyranose and β-D-glucopyranose side chains are attached, on average to three of five galactosyl units.
  • 功刀 彰, 辻 千代美, 田部井 克己
    1988 年 36 巻 7 号 p. 2661-2664
    発行日: 1988/07/25
    公開日: 2008/03/31
    ジャーナル フリー
    On prolongation of the reaction time in the on-column nitration of phenol (1) with 19% nitric acid at room temperature, the yield of 2, 4-dinitrophenol (5) increased. The dinitro compound 5 was derived from p-nitrophenol (4) through catalysis by 1 and was not obtained from o-nitrophenol (3). The formation of 5 from 4 in the on-column nitration was also catalyzed by several kinds of phenol derivatives.
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