巻号一覧
38 巻, 1 号
選択された号の論文の69件中1～50を表示しています
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中島 和雄, 内海 英雄, 風間 成孔, 濱田 昭1990 年 38 巻 1 号 p. 1-4
発行日: 1990/01/25
公開日: 2008/03/31
ジャーナル フリーThe effect of α-tocopherol and its acetate on the membrane structure of egg yolk phosphaticdylcholine (egg PC) dispersions was investigated using phosphate-31 nuclear magnetic resonance (31P-NMR) and small-angle X-ray diffraction. The incorporation of α-tocopherol into egg PC dispersions induced a change in the 31P-NNR spectrum from a multilamellar bilayer line shape to a hexagonal HII one. The phase transition by α-tocopherol was also confirmed by small-angle X-ray diffraction analysis. The amount of hexagonal HII phase increased with increase in concentration of α-tocopherol. Egg PC dispersions containing a molar ration of 0.8 of α-tocopherol gave a 31P-NMR spectrum of an approximately hexagonal HII type at 37°C. The amount of hexagonal HII phase increased with increasing temperature, indicating that the α-tocopherol-induced phase transitin is thermotropic and that the transition temperature of egg PC membranes from the lamellar to the hexagonal HII phase is lowered by α-tocopherol. The incorporation of α-tocopherol acetate did not induce any phase transition. This fact indicates that the hydroxyl group of α-tocopherol may play an important role in the hexagonal HII phase formation of egg PC dispersions.抄録全体を表示PDF形式でダウンロード (648K) -
古川 淳, 五十嵐 順悦, 島 宏治, 渡辺 三明, 木下 敏夫1990 年 38 巻 1 号 p. 5-7
発行日: 1990/01/25
公開日: 2008/03/31
ジャーナル フリーDisilyloxydienes (2a-c) were easily obtained by treatment of stable sulfur yliders (1a-c) with chlorotrimethylsilane in the presence of triethylamine. Cycloaddition reaction of these dienes with some dienophiles was carried out.抄録全体を表示PDF形式でダウンロード (532K) -
堀 幹夫, 片岡 貞, 清水 洋, 今井 英治, 小出 徳雄, 岩田 憲之, 黒野 昌庸1990 年 38 巻 1 号 p. 8-12
発行日: 1990/01/25
公開日: 2008/03/31
ジャーナル フリー2, 6-Epithio-3-benzazocines (9-thiabenzomorphans) in which the carbon atom at the 11-position is replaced by a sulfur atom, were synthesized by treatment of 1-(2-ethoxycarbonylaminoethyl)isothiochroman asulfoxides (16) with acetic anhydride or by heating 3-acetoxyisothiochromans (17) in Dowtherm A.The hetero-acetal moiety of this novel heterocycle (15) was stable to lithium aluminum hydride and boron tribromide. Reduction of 15 with lithium aluminum hydride gave the N-methyl derivative (19) and demethylation of the 8-methoxy derivative (19b) with boron tribromide gave the 8-hydroxy derivative (20).抄録全体を表示PDF形式でダウンロード (873K) -
徳竹 昌一, 山次 信幸, 加藤 元彦1990 年 38 巻 1 号 p. 13-18
発行日: 1990/01/25
公開日: 2008/03/31
ジャーナル フリーFive new glucopyranosides, phenolindophenyl- (2a), phenolindo-3'-chlorophenyl-(2b), phenolindo-3', 5'-dichlorophenyl- (2c), 2, 5-dimethylphenolindophenyl- (2d), and phenolindo-3', 5'-dibromophenyl-β-D-glucopyranoside (2e), were synthesized through two routes. Compounds 2c and 2e were synthesized by direct glycosidation (route A) of the Na salt of dihalogenophenolindophenol (4c and 4e). The direction of glycosidation was controlled by the choice of free phenolindophenois or the Na salts. Compounds 2a-d were synthesized via the condensation reaction (route B) of 4-aminophenyl 2, 3, 4, 6-tetra-O-acetryl-β-D-glucopyranosides (9a-c) with quinones (10 and 11). When 1, 4-naphthoquinone (12) was used in this reaction, N-(2-naphthoquinonyl)-4-aminophenyl 2, 3, 4, 6-tetra-O-acetyl-β-D-glucopyranoside (13) was the major product. These glucopyranosides (2a-d) were hydrolyzed by β-glucosidase to give a blue product having high absorbance and they were concluded to be potential substrates for the assay of β-glucosidase.抄録全体を表示PDF形式でダウンロード (985K) -
植田 泰誠, 中矢 賢治, 永井 愼一, 榊原 仁作, 村田 充男1990 年 38 巻 1 号 p. 19-22
発行日: 1990/01/25
公開日: 2008/03/31
ジャーナル フリーNovel classes of heterocycles, [1, 4]-dioxepino[5, 6-c]pyridine, [1, 5]-dioxocino[2, 3-c]pyridine, [1, 4]-dioxepino[6, 5-b]pyridine and pyrido[4, 3-f][1, 4]oxazepine, were synthesized from pyridoxine and pyridoxamine.抄録全体を表示PDF形式でダウンロード (730K) -
藤原 英俊, 加藤 旭, 岡林 一蔵1990 年 38 巻 1 号 p. 23-27
発行日: 1990/01/25
公開日: 2008/03/31
ジャーナル フリーThe mas spectra of 3-piperidinocyclohexanol derivatives (1-6) were measured by electron impact ionization.Characteristic fragment ions were observerd at [M-43]+, m/z 182, m/z 164, m/z 140, 138, m/z 124, m/z 111, m/z 98, m/z 85 and m/z 84.The cis- and trans-configurations of 3-piperidinocyclohexanol derivatives could be distinguished by the peak intensities at m/z 140 and m/z 85. The difference between alkyl and phenyl substituents could be recognized from the peak intensities at m/z 182 and m/z 164.抄録全体を表示PDF形式でダウンロード (683K) -
西谷 潔, 磯崎 正史, 山川 浩司1990 年 38 巻 1 号 p. 28-35
発行日: 1990/01/25
公開日: 2008/03/31
ジャーナル フリーCarbocyclic rings fused to an α-methylene-γ-lactone unit were synthesized from ω-formylated β-ethoxycarbonylallyl halides (4a-g) through intramolecular cyclization by the use of a low-valent chromium reagent, prepared from CrCl3 and LiAlH4, in N, N-dimethylformamide. α-Methylene-γ-lactones fused to medium (eight-membered) or large (twelve-and fourteen-membered) ring system (5a, c and d) were synthesized by this method in good to fairly good yields. However, the formylated allyl halide (4b), expected to afford a ten-membered carbocyclic ring system, gave dilactones fused to a twenty-membered ring unit even under a high dilution reaction condition.抄録全体を表示PDF形式でダウンロード (1386K) -
佐野 武弘, 堀口 よし江, 田中 和彦, 津田 喜典1990 年 38 巻 1 号 p. 36-44
発行日: 1990/01/25
公開日: 2008/03/31
ジャーナル フリーThermolysis of 4-oxo-2-azabicyclo[3.2.0]hept-2-enes caused two reactions; one is the 1, 3-shift of the C1-C7 bond to the C3 carbon followed by cheletropic loss of CO from the intermediary formed 2-azanorborn-2-enes to yield the dihydropyridines, and the other is epimerization of the C7-substituent. These two reactions occurred competitively depending on the nature of the C7 substituent. Intermediary formation of the 2-azanorborn-2-enes in the rearrangement reaction was proved by trapping experiments with the use of 4-acetoxy derivatives. The mechanisms of the thermal 1, 3-shift and 7-epimerization are discussed.抄録全体を表示PDF形式でダウンロード (1327K) -
山崎 宏亮, 原田 秀範, 松崎 憲一, 吉岡 君友, 高瀬 宗章, 大木 英二1990 年 38 巻 1 号 p. 45-48
発行日: 1990/01/25
公開日: 2008/03/31
ジャーナル フリーReactions of-methyl-2(3H)-thiazolones (5) with various N-alkoxycarbonyl pyridinium salts (6a-f) led to (N-alkoxycarbonyl dihydropyridyl)thiazolones (7a-f), oxidation of which yielded a new class of 5-pyridylthiazolones (8a-f). These reactions were applied to the synthesis of other azaarylthiazolones. Some of these azaarylthiazolones, particualrly 5-(4-pyridyl)thiazolones (8b, c) and 5-(4-quinolyl)thiazolones (14a, b), showed positive inotropic activity with little chronotropic effect on guinea pig left atria.抄録全体を表示PDF形式でダウンロード (673K) -
丹野 雅幸, 末吉 祥子, 神谷 庄造1990 年 38 巻 1 号 p. 49-54
発行日: 1990/01/25
公開日: 2008/03/31
ジャーナル フリーThermolysis of 1-aryl-3-benzyl-1-nitrosoureas(1c, d) was carried out in CCL4 at 33°C under an atmosphere of air or argon, Decomposition of 1c, d under aerobic conditions gave mainly benzyl isocyanate (4b) via a diazoester intermediate, whereas under anaerobic conditions, decomposition gave 1-aryl-3-benzyl-3-nitrosoureas (5c, d) as 1, 3-shifted products, and 3-benzyl-1-(4-substituted 2-nitrophenyl)-3-nitrosoureas (8c, d) as transnitrosated products via N-NO bond cleavage, 3-Benzyl-1-(4-substituted 2-nitrophenyl)ureas (6c, d) were also produced by N-NO bond cleavage. The 1, 3-nitroso shift and transnitrosation under these conditions were assumed to involve a nitrosyl radical fission pathway. The nitrosated nitro compounds (8c, d) were also obtained together with 6c, d by nitration of the ureas (7c, d) with a mixture of fuming nitric acid and acetic acid. The N-nitrosourea (1c) acted as a nitrosating agent on 3-methyl-1-(4-tolyl)urea (7a) to convert it into nitrosoureas (1a and 5a).From our results, we presumed that the O-nitrosoisourea (11) or its isomer (12) was an intermediate in the 1, 3-nitroso shift and also an ultimate nitrosating agent in the transnitrosation reaction.抄録全体を表示PDF形式でダウンロード (857K) -
黒柳 正典, 上野 明, 小山 清隆, 名取 信策1990 年 38 巻 1 号 p. 55-58
発行日: 1990/01/25
公開日: 2008/03/31
ジャーナル フリーFurther study on the sesquiterpenes from Curcuma aromatica (Zngiberaceae) has resulted in the isolation of eleven minor sesquiterpenes, 1-11 having guaiane, seco-guaiane and germacrane skeletons, and their structures were elucidated by proton nuclear magnetic resonance (1H-NMR) and 13C-nuclear magnetic resonance (13C-NMR) spectroscopy, as well as chemical investigation. The stereochemistry of these sesquiterpenes was elucidated by 2D NMR techniques such as 1H-H correlation (COSY) and nuclear Overhauser effect correlation (NOESY), and circular dichroism (CD) spectroscopy.抄録全体を表示PDF形式でダウンロード (721K) -
日野 亨, 長谷川 敦, 劉 進軍, 中川 昌子1990 年 38 巻 1 号 p. 59-64
発行日: 1990/01/25
公開日: 2008/03/31
ジャーナル フリーThe Pictet-Spengler reaction of N-hydroxytryptamine (6) with various aldehydes was examined. Reduction of 3-(2-nitroethyl) indole (5) with aluminum amalgam gave 6, which was not so stable and was readily oxidized to the azoxy compound (10) in solution under an oxygen atmosphere. Reaction of 6 with saturated aldehydes gave the corresponding nitrones (11b, c) without an acid catalyst at room temperature, while the reaction with α, β-unsaturated aldehydes provided nitrones (11d, e, f) in the presence of trifluoroacetic acid. Cyclization of the nitrones with trifluoroacetic acid in methylene chloride gave the 2-hydroxy-1, 2, 3, 4-tetrahydro-β-carbolines (2) in good yields. The cyclization of the saturated nitrones proceeded rapidly, whereas the similar reaction of the unsaturated nitrones was slow. Direct Pictet-Spengler reaction of 6 with aldehydes in methylene chloride in the presence of trifluoroacetic acid gave 2a, b, c in excellent yields. Dehydration of the 2-hydroxy-β-carboline (2b) with trifluoroacetic anhydride in benzene gave the 3, 4-dihydro-β-carboline (15). 6-Bromo-5-methoxy-N-hydroxytryptamine (25) was prepared from 3-bromo-4-methyoxyaniline (17) via the indole (22). The Pictet-Spengler reaction of 25 with isovaleraldehyde gave the 2-hydroxy-tetrahydro-β-carboline (26).抄録全体を表示PDF形式でダウンロード (1027K) -
井口 和男, 金田 宗一郎, 長岡 博人, 山田 泰司1990 年 38 巻 1 号 p. 65-68
発行日: 1990/01/25
公開日: 2008/03/31
ジャーナル フリーSeveral clavulone derivatives were synthesized from clavulone I (1) and clavulone II (2). The carboxylic acid 3 and 4-O-deacetyl derivative 4 were synthesized by selective enzymatic hydrolysis of 2 using porcine liver esterase and orange peel acetylesterase, respectively. From the carboxylic acid 3, the benzyl ester 5, tert-butyl ester 6 and amide 7 were prepared. The 12-O-deacetyl derivative 9 was synthesized by organicuprate reduction of the epoxide 8 which was prepared from 2. The derivatives 13-15, which possess an elongated α-side chain, were synthesized from 1 via the hemiacetal 12.抄録全体を表示PDF形式でダウンロード (700K) -
片桐 信弥, 渡辺 信久, 金子 主税1990 年 38 巻 1 号 p. 69-72
発行日: 1990/01/25
公開日: 2008/03/31
ジャーナル フリーAsymmetric Diels-Alder reaction of di-l-menthyl acetoxymethylenemalonate with cyclopentadiene under high pressure was examined. The yield, proportion of exo isomer, and diastereomeric excess (d.e.) of the adduct increased with increase of pressure when the reactions were carried out without any catalyst. The absolute structure of the major diastereoisomer of the endo adduct corresponded to the natural configuration, which could be transformed to a precursor of aristeromycin, while the exo adduct had the unnatural configuration. The same diastereoselectivity was also observed when diethylaluminum chloride (capable of chelating with only one carbonyl group of the dienophile) was used as the catalyst. On the contrary, both endo and exo isomers obtaiend from the high-pressure-mediated Diels-Alder reaction in the presence of zinc chloride or tris(6, 6, 7, 7, 8, 8, 8-heptafluoro-2, 2-dimethyl-3, 5-octanedionato)ytterbium (capable of chelating with the two carbonyl groups of the dienophile at the same time) had the natural configuration. Possible mechanisms of these selectivities are proposed.抄録全体を表示PDF形式でダウンロード (670K) -
川原 信夫, 野沢 幸平, 山崎 幹夫, 仲嶋 正一, 河合 賢一1990 年 38 巻 1 号 p. 73-78
発行日: 1990/01/25
公開日: 2008/03/31
ジャーナル フリーNovel compounds designated emethallicins B (1), C (2), and D (3), along with emethallicin A (4), were isolated from the mycelium of the heterothallic fungus, Emericella heterothallica (mating type a). The structures of emethallicins B (1), C (2), and D (3) were determined on the basis of spectroscopic and chemical investigations. Emethallicins B (1) and C (2) are epitetrathiodioxopiperazines, which have the same basic carbon skeleton as apoaranotin (19) and acetylaranotin (17), respectively, whereas emethallicin D (3) is an epitrithiodioxopiperazine derivative, which has the same carbon skeleton as apoaranotin (19). It is very interesting that a large amount of the disulfide, emethallicin A (4), was isolated from the strain of mating type A and that the corresponding tetrasulfide, emethallicin B (1), and trisulfide, emethallicin D (3), were isolated from the other mating type strain, along with a small amount of the disulfide (4). Emethallicins B (1), C (2), and D (3) have potent inhibitory activity against compound 48/80-induced histamine release from mast cells, like emethallicin A (4).抄録全体を表示PDF形式でダウンロード (982K) -
塩島 憲治, 増田 和夫, 上田 博之1990 年 38 巻 1 号 p. 79-85
発行日: 1990/01/25
公開日: 2008/03/31
ジャーナル フリーThe ozone oxidation reaction of eleven triterpenoid monoenes belonging to the hopane and migrated hopane series was investigated. Under suitable reacftion conditions, various reaction products including three ozonides, seven epoxides and one ketone were obtained from the eight starting materials. The reaction of glutin-5-ene was also examined for comparison.抄録全体を表示PDF形式でダウンロード (920K) -
吉田 隆志, 難波 治, 陳 玲, 奥田 拓男1990 年 38 巻 1 号 p. 86-93
発行日: 1990/01/25
公開日: 2008/03/31
ジャーナル フリーEuphorbin C (5), a member of a new class of dimeric hydrolyzable tannins, has been isolated form Euphorbia hirta L. In its molecule, a monomeric hydrolyzable tannin unit having a 1C4 glucopyranose core which is esterified with an equilibrated dehydrohexahydroxydiphenoyl group, and another monomer unit having a 4C1 glucose core are bonded through ester linkages of a euphorbinoyl group, which is a new galloyl tetramer.抄録全体を表示PDF形式でダウンロード (1003K) -
佐藤 雅之, 榊 潤一, 高山 和久, 小林 聡, 鈴木 美和子, 金子 主税1990 年 38 巻 1 号 p. 94-98
発行日: 1990/01/25
公開日: 2008/03/31
ジャーナル フリーNovel synthetic routes to tetronic acid and its derivatives from 6-substituted 1, 3-dioxin-4-ones through cycloreversion to acylketenes followed by either intra- or intermolecular ketene trapping by a hydroxy function is described. While tetronic acid and its 5-substituted derivatives were synthesized directly from 6-(x-hydroxyalky)-1, 3-dioxin-4-ones by intramolecular trapping, 3-acyltetronic acids were prepared by Dieckmann reaction of the β-keto esters obtained from the 6-substituted dioxinones and an approptiate α-hydroxy ester by intermolecdular trapping.抄録全体を表示PDF形式でダウンロード (814K) -
藤井 澄三, 斎藤 徹, 中坂 剛志, 木津 京子1990 年 38 巻 1 号 p. 99-102
発行日: 1990/01/25
公開日: 2008/03/31
ジャーナル フリーThe 2-deuterated species XI-XIII of 3, 9-dimethyladenine salts (Ia, b) and of 3-benzyl-9-methyladenine perchlorate (Ie) have been synthesized from the alkylaminoimidazoles VII and VIII through deuterioformylation with formic-d acid-d, hydrogenolytic demethoxylation, adn amidine-formamido cyclization. Comparison of the proton nuclear magnetic resonance spectra of XI-XIII with those of the isotophically unmodified species Ia, b, e permitted a distinction between C(2)-and C(8)-proton signals observed for a series of 3, 9-dialkyladenine salts (Ia-I) : the C(2)-proton resonates at lower field than does the C(8)-proton by 0.04-0.52 ppm. The low electron density at C(2) of I was also exemplified by the NaBH4 reduction of 3, 9-dimethyladenine perchlorate (Ib) to give the 1, 2-dihydro derivatibe XIX. The structrue of XIX was confirmed by a similar reduction of the 2-deuterated species XII, leading to XX.抄録全体を表示PDF形式でダウンロード (800K) -
西 剛秀, 斉藤 冨士夫, 永堀 均, 片岡 満, 森沢 靖弘, 矢部 裕一郎, 桜井 満也, 東田 勧, 庄子 真知子, 松下 洋一, 飯 ...1990 年 38 巻 1 号 p. 103-109
発行日: 1990/01/25
公開日: 2008/03/31
ジャーナル フリーSyntheses and biological activities of dipeptide renin inhibitors that contain statine analogues are described. The key steps fo the synthetic approach to dipeptide renin inhibitors are the asymmetric synthesls of 2(R)-substituted-3-aminocarbonylpropionic acids and the diastereoselective syntheses of (3S, 4S)-statine analogues. These inhibitors (2, 14-40) inhibited human renin in the 3-140 nM range. Inhibitor ES 6864 (2) was found to be a highly potent inhibitor of human renin (IC50 : 4.6×10-9M) and showed high enzyme specificity. Oral administration of ES 6864 at 3 mg/kg to conscious, sodium-depleted marmosets inhibted plasma renin activity (PRA) more than 80% after 1h.抄録全体を表示PDF形式でダウンロード (1060K) -
澤山 忠弘, 塚本 正利, 笹川 隆, 西村 和也, 出口 貴司, 武山 邦彦, 細木 和1990 年 38 巻 1 号 p. 110-115
発行日: 1990/01/25
公開日: 2008/03/31
ジャーナル フリーA new series of highly potent angiotensin-converting enzyme (ACE) inhibitors, 1-(N2-substituted L-lysyl-γ-D-glutamyl)octahydro-1H-indole-2-carboxylic acids, was synthesized; various acyl groups were introduced at the α-amino group of the N-terminal P1 Lys. The effect of the N2-acyl groups on in vitro inhibitory activity and oral antihypertensive effect was examined. All of the synthesized N-acyl tripeptides were found to have in vitro inhibitory activity at an approximately nanomolar level, and showed antihypertensive potency in renal hypertensive rats at a dose of 10 mg/kg, when administered orally. Among them, compounds 7e, g adn 9f, i, m showed potent and long-lasting antihypertensive effects compared with eanlapril (2a). Their structure-activity relationships are also discussed.抄録全体を表示PDF形式でダウンロード (815K) -
田村 典一, 松下 義弘, 川野 泰彦, 吉岡 晃一1990 年 38 巻 1 号 p. 116-122
発行日: 1990/01/25
公開日: 2008/03/31
ジャーナル フリーThe chemical modification of the 4-acetylamino group on the cycloserine moiety of lactivicin (1a) was carried out.The lactivicin derivatives (1d, k-p and w) having heterocyclic acylamino groups which have been often utillized in β-lactam antibiotics showed potent antibacterial activities. Ester prodrugs (7a-d) of lactivicin derivatives were also prepared in order to improve the bioavailability on oral administration. The pivaloyloxymethyl (POM) esters (7a and 7b) and 1-ethoxycarbonyloxyethyl (EOE) ester (7c) were found to have slightly improved protective effect in vivo compared with their parent compounds 1c and 1k.抄録全体を表示PDF形式でダウンロード (1068K) -
倉持 浩, 茂手木 明子, 丸山 佐起子, 岡本 一也, 高橋 克俊, 粉川 治, 埜渡 裕義, 速水 宏1990 年 38 巻 1 号 p. 123-127
発行日: 1990/01/25
公開日: 2008/03/31
ジャーナル フリーFactor analysis was applied to the data matrix of in vitro growth inhibitory activities of 52 platinum complexes against 9 tumor cell lines, L1210, P388, Lewis lung, AH66, AH66F, HeLa S3, KB, HT-1197 and HT-1376 cell lines.Three factors were obtained by the principal factor analysis method. After the varimax rotation of these three factors, tumor cell lines cells lines were classified into four groups according to their factor loadings. The platinum complexes were characterized by the factor scores. Cisplatin was situated in an extreme position as compared with the other platinum complexes. In vivo antitumor activities of the platinum complexes were tested against L1210 and LL murine tumor models. The in vivo activity against L1210 showed a negative correlation with that against LL. Factor 2 scores of the complexes obtained by factor analysis of in vitro antitumor activities showed a good correlation with these in vivo antitumor activities. Then, the atructure-factor 2 score relationships among platinum complexes were analyzed by the Free-Wilson method. From this analysis, structure-activity relationships for carrier ligands and leaving groups are proposed. Factor analysis is suggested to be a useful method to establish an efficient screening system for platinum complexes.抄録全体を表示PDF形式でダウンロード (717K) -
高畠 亨, 長谷川 稔, 長野 哲雄, 広部 雅昭1990 年 38 巻 1 号 p. 128-132
発行日: 1990/01/25
公開日: 2008/03/31
ジャーナル フリーThe toxicities of some benzofurazans (BZs), benzofurazan (1), 4, 7-dimethylbenzofurazan (2), 4, 7-dibromobenzofurazan (3), 4-bromo-6-cyanobenzofurazan (4), 4, 7-dicyanobenzofurazan (5) and 4, 5-dicyanobenzofurazan (6), were examined on Escherichia coli. Compound 5 at 4 μM and compound 6 at 7 μM completely inhibited the growth of E. coli in a simple nutritionally restricted medium (GM medium). These compounds were more toxic in GM medium than in a nutritionally rich medium (YE medium), which contained yeast extract as an additive in GM medium. Compound 4 also inhibited the growth of E. coli at 300 μM in GM medium. The toxicities of BZs were in the order of 1≈2≈3<4«5≈6. Compounds 4, 5 and 6 induced manganese-superoxide dismutase (Mn-SOD) and catalase activities of E.coli in YE medium. The induced SOD and catalase provide a defense against the potential cytotoxicities of O2- and H2O2. The rate of dioxygen uptake in cyanide-resistant respiration of E. coli was dependent on the concentration of 5, and was correlated with the induction of SOD and catalase. The reduction potentials of BZs followed the order of 1≈2<3<4<5≈6. Compounds 5 and 6, which had redox potentials higher than those of the order BZs, are thought to be more readily reduced in the living system. The present results suggest that the toxicities of compounds 5 and 6 to E. coli are due to their reduction within the E. coli cell and their reoxidization by molecular dioxygen to form superoxide (O20-) and hydrogen peroxide (H2O2). Compound 4 was also suggested to damage E. coli through the same mechanism. though it was less toxic.抄録全体を表示PDF形式でダウンロード (905K) -
福山 愛保, 児玉 三明, 三浦 巖, 金城 順英, 森 英雄, 中山 康夫, 高橋 真行1990 年 38 巻 1 号 p. 133-135
発行日: 1990/01/25
公開日: 2008/03/31
ジャーナル フリーPhlorofucofuroeckol A (1), a novel phlorotannin with both dibenzo-1, 4-dioxin and dibenzofuran elements, has been isolated from the brown alga Ecklonia kurome OKAMURA as a potent anti-plasmin inhibitor. Its structure has been elucidated to be 1, 11-di(3, 5-dihydroxyphenoxy)-benzofuro[3, 2-a]dibenzo[b, e][1, 4]dioxin-2, 4, 8, 10, 14-pentaol on the basis of the spectral data, in particular, by means of negative nuclear Overhauser effect (NOE) and long-range carbon-proton couplings (2J<CH> and 3J<CH>). Phlorofucofuroeckol A inhibited the action of α2-macroglobulin (IC<50>=1.0μg/ml) and α2-plasmin inhibitor (IC<50>=0.3μg/ml), the main plasmin inhibitors in plasma.抄録全体を表示PDF形式でダウンロード (533K) -
池谷 幸信, 三橋 博, 佐々木 博美, 松崎 豊, 松崎 珠絵, 細谷 英吉1990 年 38 巻 1 号 p. 136-141
発行日: 1990/01/25
公開日: 2008/03/31
ジャーナル フリーAfter oral administration of gomisin A (1) to rats, the bile and urine were collected and treated with β-glucuronidase and arylsulfatase. Seven metabolites, met B (2), met A-III (3), met E (4), met D (5), met F (6), met G (7), and met H (8) were isolated from the bile treated with the enzymes. Eight metabolites 2-8, and met A-II (9) were isolated from the urine treated with the enzymes. A major metabolite 2, and two minor metabolites 3 and 9 were identified as met B, met A-III, and met A-II, respectively, which are oxidative products of 1 formed by rat liver S9 mix. The structures of five new metabolites 4-7, and 8 were determined on the basis of chamical and spectral studies.抄録全体を表示PDF形式でダウンロード (904K) -
浅田 善久, 上岡 健人, 古谷 力1990 年 38 巻 1 号 p. 142-149
発行日: 1990/01/25
公開日: 2008/03/31
ジャーナル フリーSix novel triterpenoid saponins, named crocosmiodsides C, D, E, F, G, and I, were isolated from the corms of montbretia (Crocosmia crocosmiiflora N.E.Br., Iridaceae). The structures of these saponins were determined on the basis of spectral and chemical evidence. They are 3, 28-di-O-glycosides of polygalacic acid, carrying hydroxylated palmitic acid derivatives at the C-4 position of the β-D-fucopyranosyl moiety. Namely, crocosmiosides C (1), D (2), E (3), F (4), and G (5) bear 3-O-[α-L-arabinopyranosyl-(1→ 6)-β-D-glucopyranosyl]-28-O-{2-O-[β-D-apio-D-furanosyl-(1→4)-β-D-xylopyranosyl-(1→4)-α-L-rhamnopyranosyl]-3-O-(β-D-glucopyranosyl)-β-D-fucopyranosyl}-polygalacic acid as as common structural unit of the desacylsaponin moiety, while the structures of the acyl moiety of crocosmiosides C (1), D (2), E (3), F (4), and G (5) are 9-oxo-16-hydroxy-2-β-D-xylopyranosyloxyhexadecanoic acid, 9, 16-dihydroxy-2-β-D-xylopyranosyloxyhexadecanoic acid, 2, 9, 16-trihydroxyhexadecanoic acid, 2, 9-dihydroxy-16-α-L-rhamnopyranosyloxyhexadecanoic acid, and 9-oxo-16-α-L-rhamnopyranosyloxy-2-β-D-xylopyranosyloxyhexadecanoic acid, respectively. In addition, the structure of crocosmioside I (6) which has a different desacylsaponin moiety was elucidated as 3-O-[α-L-arabinopyranosyl-(1→6)-β-D-glucopyranosyl]-28-O-{2-O-[β-D-xylopyranosyl-(1→4)-α-L-rhamnopyranosyl]-3-O-(β-D-glucopyranosyl)-4-O-(2, 9-dihydroxy-16-α-L-rhamnopyranosyloxyhexadecanoyl)-β-D-fucopyranosyl}-polygalacic acid.抄録全体を表示PDF形式でダウンロード (1258K) -
三宅 義徳, 重年 稔, 小嶋 正治1990 年 38 巻 1 号 p. 150-152
発行日: 1990/01/25
公開日: 2008/03/31
ジャーナル フリーAnti-testosterone antisera were produced by pretreatment of rabbits with 15α-carboxymethyl-5α-dihydrotestosterone linked to a copolymer of D-glutamic acid and D-lysine (D-GL) before immunization with the bovine serum albumin conjugate of 15α- and 15β-carboxymethyltestosterone. The specificity for 5α-dihydrotestosterone of the anti-testosterone antisera was considerably improved.抄録全体を表示PDF形式でダウンロード (615K) -
田上 昇一郎, 松田 和久1990 年 38 巻 1 号 p. 153-155
発行日: 1990/01/25
公開日: 2008/03/31
ジャーナル フリーA simple kinetic method to assay L-asparaginase and L-asparagine with an ammonia gas-sensing electrode is described. The method is based upon the de-amination of L-asparagine by L-asparaginase from Escherichia coli, resulting in the production of ammonia. The initial rate (mV/min) of ammonia release is proportional to the activity of L-asparaginase and also to the concentration of L-asparagine in the presence of a large amount of the enzyme. Optimal temperature, buffer composition and pH for the assays are specified. L-Asparaginase was determined in the range of 0.4-1.6U in a 0.1 ml sample; the recovery was 98.1-103.8% for 16 determinations and σn was 1.59. L-Asparagine was determined in the concentration range of 1×10-4-1×10-3M with σn-1 1.92. The method was applied to the determination of 1-5×10-4M asparagine added to human serum with σn-1 1.96 for 5 determinations.抄録全体を表示PDF形式でダウンロード (536K) -
野崎 誉士秀, 今村 順茂, 小田切 優樹1990 年 38 巻 1 号 p. 156-158
発行日: 1990/01/25
公開日: 2008/03/31
ジャーナル フリーThe kinetic mechanism for the reduction of befunolol catalyzed by befunolol reductase from rabbit liver was investigated. From the initial velocity analysis, product inhibition and coenzyme binding studies, the reduction of befunolol was found to proceed through an ordered Bi Bi mechanism, in which β-nicotinamide adenine dinucleotide phosphate, reduced form (NADPH) binds to the enzyme firstly and NADP+ leaves lastly. NADPH bound to the free enzyme at a molar ratio of 1 : 1. Furthermore, the result of dead-end inhibition by Cibacron blue F3GA, a nucleotide analogue which binds to many enzymes, was consistent with the ordered Bi Bi mechanism for the enzyme.抄録全体を表示PDF形式でダウンロード (580K) -
山口 正義, 森 聖一, 祐田 泰延1990 年 38 巻 1 号 p. 159-163
発行日: 1990/01/25
公開日: 2008/03/31
ジャーナル フリーThe effect of various metals on uridine diphosphate (UDP)-glucuronyltransferase and β-glucuronidase activities in rat liver microsomes was investigated. The presence of Mn2+, Cd2+, Zn2+, V5+, Ni2+, Co2+, Cu+ or Ca2+ (20μM) in the enzyme reaction mixture did not a significant alteration of UDP-glucuronyltransferase activity in hepatic microsomes. Of these metals, Zn2+ and Cd2+ (20μM) caused a remarkable increase in hepatic microsomal β-glucuronidase activity. Appreciable effects of Zn2+ and Cd2+ on β-glucuronidase activity were seen at 5.0 μM, and the effects were saturated at 50 μM. Ca2+ (5.0-50 μM) and/or the Ca2+-binding protein regucalcin (2.0μM) did not have an appreciable effect on UDP-glucuronyltransferase and β-glucuronidase activities in hepatic microsomes. Thus, Zn2+ and Cd2+ uniquely increased β-glucuronidase activity. The Zn2+-and Cd2+-induced increase in β-glucuronidase activity was completely reversed by the presence of an SH group-protecting reagent (dithiothreitl). The response of the microsomal enzyme to Zn2+ and Cd2+ (20 μM) was no longer seen after treatment with 0.2% Triton X-100 [polyoxyethylene(10) octylphenyl ether], indicating that the stimulation by these metals is dependent on membrane association. The present study suggests that, of various metals tested, Zn2+ and Cd2+ can uniquely increase hepatic microsomal β-glucuronidase actibity, and that their effect is based on binding to membranous SH groups, beside the enzyme protein.抄録全体を表示PDF形式でダウンロード (797K) -
守谷 智恵, 境 由妃, 津田 正明, 金沢 浩, 土屋 友房1990 年 38 巻 1 号 p. 164-167
発行日: 1990/01/25
公開日: 2008/03/31
ジャーナル フリーWe have characterized H+-translocating adenosine triphosphatase (ATPase) in membrane vesicles of Vibrio parahaemolyticus. The ATPase required high concentrations (about 0.5 M) of Na2SO4 (or other salts) for its maximum activity. Magnesium ion stimulated the ATPase activity, but Ca2+ did not. The activity of ATPase was inhibited by tetrachlorosalicylanilide, an H+ conductor, but not by another H+ conductor, carbonylcyanide-m-chlorophenylhydrazone. The activity was strongly inhibited by dicyclohexylcarbodiimide or Zn2+, and partially inhibited by azide, but not at all by vanadate.抄録全体を表示PDF形式でダウンロード (721K) -
藤岡 聡之, 井上 富美子, 栗山 雅行, 三浦 康司, 東島 勉1990 年 38 巻 1 号 p. 168-171
発行日: 1990/01/25
公開日: 2008/03/31
ジャーナル フリーDigitonin-solubilized opioid receptors from rat brain were purified with an affinity resin, AH-Sepharose coupled with [D-Ala2, D-Ler5]enkephalin (DADLE). Radioreceptor binding assay showed that the purified materials had specific opioid-binding activity of 310 pmol/mg protein on DADLE binding. Analyses by polyacrylamide gel electrophoresis in the presence of sodium dodecyl sulfate (SDS-PAGE) revealed that the materials were rich in two polypeptides; the major component had a molecular weight of 62000-64000. To establish the materials responsible for binding opiates, the purified materials were cross-linked with 125I-labeled β-endorphin using bis[2-(succinimidooxycarbonyloxy)-ethyl]sulfone aqs a cross-linker. The molecular weight of 62000-64000, the major band of the purified materials on SDS-PAGE, agreed closely with that determined by the cross-linking experiment. The results suggested that the purified materials contained opioid-binding materials (opioid receptors).抄録全体を表示PDF形式でダウンロード (692K) -
及川 勉, 茶山 和敏, 岩口 孝雄, 松沢 昭雄1990 年 38 巻 1 号 p. 172-175
発行日: 1990/01/25
公開日: 2008/03/31
ジャーナル フリーSome immunological properties of mouse kidney type IV collagen (MKIVC) were investigated. In enzyme-linked immunosorbent assay (ELISA), rabbit anti-MKIVC antiserum reacted strongly with MKIVC but not at all with type I collagen or laminin of mouse origin. Thus, the purified MKIVC preparation was not contaminated with detectable amounts of other constituents of the extracellular matrix and the basement membrane including interstitial collagens, as suggested previously (T. Oikawa et al., Chem. Pharm. Bull., 34, 789 (1986 )). In ELISA inhibition assay, human kidney type IV collagen (HKIVC) only partially inhibited the binding of MKIVC to anti-MKIVC antiserum. Similarly, HKIVC showed a far weaker binding capacity to the antiserum compared to MKIVC in ELISA direct binding assay.After the anti-MKIVC antiserum was absorbed with acetone powder of human kindney, the resulting antiserum still possessed a considerable binding activity to MKIVC but did not react with HKIVC. In accord with these findings, anti-MKIVC antiserum immunostained both mouse and human renal basement membranes, while it stained the former but not the latter after being absorbed with human kidney. Taken together, these results suggest that MKIVC possesses at least two antigenic determinants; one but not the other cross-reacts with human kidney basement membrane collagen.抄録全体を表示PDF形式でダウンロード (862K) -
吉岡 篤也, 山本 政信, 伊藤 隆弘, 入江 徹美, 平山 文俊, 上釜 兼人1990 年 38 巻 1 号 p. 176-179
発行日: 1990/01/25
公開日: 2008/03/31
ジャーナル フリーPossible utility of hydroxyalkylated β-cyclodextrin (β-CyD) derivatives as parenteral drug carriers was investigated, using nimodipine, a dihydropyridine derivative with calcium antagonistic action, as a model drug. The aqueous solubility of nimodipine increased linearly with increase in the concentration of hydroxyalkylated β-CyDs, showing as AL-type phase solubility diagram. The stability constant of nimodipine-hydroxyalkylated β-CyD complexes was in the order of 2, 3-dihydroxypropyl-β-CyD<β-CyD<2-hydroxyethyl-β-CyD<3-hydroxypropyl-β-CyD<2-hydroxypropyl-β-CyD, and the solubilizing ability of the β-CyDs was also taht order. The results of powder X-ray diffractometry and thermal analysis suggested 1 : 3 (guest : host) complex formation of nimodipine with 2-hydroxypropyl-β-CyD in the solid state. The dissolution rate of nimodipine-2-hydroxypropyl-β-CyD complex was much faster than that of the drug alone. Nimodipine-2-hydroxypropyl-β-CyD complex gave higher plasma levels of the drug after intramuscular administration to rabbits, i.e., the area under the plasma concentration-time curve and the maximum plasma concentration of the complex were about 2.5 times higher than those of the drug alone. The muscular damage after the injection of nimodipine was reduced by the administration of the complexed form.抄録全体を表示PDF形式でダウンロード (763K) -
阿曽 幸男, 吉岡 澄江, 武田 寧1990 年 38 巻 1 号 p. 180-184
発行日: 1990/01/25
公開日: 2008/03/31
ジャーナル フリーEpimerization and racemization of carbenicillin, ethiazide, etoposide and oxazepam acetate were examined kinetically in the presence of human serum albumin (HSA). The concentration of both optical isomers of each drug was determined by stereospecific high-performance liquid chromatography. The apparent rate constants of epimerization or racemization and hydrolysis were estimated from the concentration-time data. HSA retarded the racemization of ethiazide and the epimerization of etoposide. The binding of the drugs to HSA may inhibit the attack of hydroxy ion and/or water molecule and thus retard the epimerization and the racemization. HSA acelerated the epimerization of carbenicillin, which is charged at the pH studied. Ion-ion and ion-dipole interactions between carbenicillin and HSA activate the carbenicillin molecule favorable for the attack of hydroxy ion and/or water molecule. The hydrolysis rates of ethiazide, carbenicillin and oxazepam acetate were increased by the addition of HSA. The hydropysis rate of d-oxazepam acetate enantiomer bound to HSA was twice that of the l-enantiomer, which suggests that the esterase-like activity of HSA is enantioselective. Differences in the binding affinities of the drug's enantiomers to HSA may account for the selectivity.抄録全体を表示PDF形式でダウンロード (725K) -
白石 澄廣, 荒平 光利, 今井 輝子, 小田切 優樹1990 年 38 巻 1 号 p. 185-187
発行日: 1990/01/25
公開日: 2008/03/31
ジャーナル フリーThe dissolution behaviors of acidic, basic and neutral drugs from kneaded mixtures with low-molecular chitosan or alginate (LM chitosan or LM alginate) have been studied in comparison with that of the drug alone. The results revealed a significant increase of dissolution rate of drugs from kneaded mixtures. Although essentially no interaction of any drug with LM chitosan or LM alginate was observed in an aqueous solution, changes of drug crystals in the kneaded mixtures were apparent. In addition, the contact angle of kneaded mixtures was obviously reduced in comparison with that of the corresponding drug powder and physical mixture.Thus, the enhanced dissolution rate of kneaded mixtures may be due to improvement of wettability and to changes of the crystallinity, microcrystal size and shape.抄録全体を表示PDF形式でダウンロード (592K) -
杉森 健一, 川島 嘉明, 竹内 洋文, 日野 知証, 丹波 敏幸, 大野 早百合, 森 章一1990 年 38 巻 1 号 p. 188-192
発行日: 1990/01/25
公開日: 2008/03/31
ジャーナル フリーAcetaminophen and ascorbic acid, which are slightly and highly soluble in water, respectively, were granulated with a low viscosity grade of hydroxypropylcellulose (HPC-L) aqueous solution by high-speed mixing, fluidized bed granulation, and spray drying. The granules obtained were compacted into tablets and their strengths were evaluated.The binding strength of acetaminophen granules increased with increase in the amount of water used, irrespective of the granulation method. On the other hand, the binding strength of ascorbic acid granules depended greatly on the granulation method and decreased when an excessive amount of water was used. The ascorbic acid granules obtained by fluidized bed and spray drying granulation with the minimum amount of water exhibited high compressibitlity. In these granules, the surface of crystals was found to be entirely coated with the binder. It is considered that the high solubility of the drug in the binder solution enabled such coating to occur, though excessive dissolution of the drug led to a decrease in compressibility.抄録全体を表示PDF形式でダウンロード (1446K) -
黒野 幸久, 沢辺 博司, 桑山 知成, 八代 有, 池田 憲1990 年 38 巻 1 号 p. 193-196
発行日: 1990/01/25
公開日: 2008/03/31
ジャーナル フリーOxazolidine ring-opening and ring-closing reactions of 11b-hydrogen(11b-nonsubstituted)benzodiazepinooxazoles (HBDOZ) and the subsequent hydrolysis of the diazepine ring were studied kinetically. The difference in the reactivities of the oxazolidine ring between cis and trans isomers (referring to substitutents at the 2- and 11b-positions) for HBDOZs is small, compared with those for BDOZs having 11b-methyl (MBDOZ) and 11b-phenyl groups (PBDOZ) reported previously. The reactions of the oxazolidine ring for HBDOZ occur about 10 times faster than those for MBDOZ and PBDOZ. For HBDOZ, hydrolysis of the amide bodn of the diazepine ring takes place rather than that of the iminium bond, in contrast to the cases of MBDOZs and PBDOZs.抄録全体を表示PDF形式でダウンロード (544K) -
石井 康子, 谷澤 久之, 滝野 吉雄1990 年 38 巻 1 号 p. 197-200
発行日: 1990/01/25
公開日: 2008/03/31
ジャーナル フリーThe mechanism of action of aloe-emodin-9-anthrone, a decomposition product of barbaloin, in causing a significant increase in the water content of the rat large intestine, was investigated. Aloe-emodin-9-anthrone inhibited rat colonic Na+, K+-adenosine triphosphatase (ATPase) in vitro, and increased the paracellular permeability across the rat colonic mucosa in vivo. Therefore, it seemed that the increase in water content of the rat large intestine produced by aloe-emodin-9-anthrone was due to both inhibition of absorption and atimulation of secretion without stimulation of peristalsis.Furthermore, pretreatment with poperamide, an antidiarrheal agent, completely prevented the increase of paracellular permeability induced by aloe-emodin-9-anthrone but did not completely reduce the concomitant increase in residual fluid volume. These findings suggest that aloe-emodin-9-anthrone has multiple mechanisms of action involved in the increase of water content in the rat large intestine.抄録全体を表示PDF形式でダウンロード (674K) -
牧野 栄一, 岩崎 信彦, 八木 典幸, 大橋 徹生, 加藤 日出男, 伊藤 安夫, 東 洋1990 年 38 巻 1 号 p. 201-207
発行日: 1990/01/25
公開日: 2008/03/31
ジャーナル フリーVarious pyrazine derivatives were synthesized and their antiallergic activity was examined. The inhibitory activity on allergic histamine release of the compounds bearing a 5-tetrazolyl group was more potent than that of the corresponding carboxyl derivatives. The introduction of -CONH- or -NHCO- between the pyrazine ring and the 5-tetrazolyl group as a spacer greatly enhanced the activity. N-(1H-Tetrazol-5-yl)-2-pyrazinecarboxamide (I-3) was estimeted to exhibit nearly the same potency as disodium cromoglycate (DSCG). The structure-activity relationship among various derivatives modified by introducing some substituents onto the 3-, 5- or 6-position of the pyrazine ring of I-3 was investigated. The activity remained unchanged or was reduced when such substituents as methyl, chloro, methoxy, methylamino and dimethylamino were introduced at the 3- or 5-position. In contrast, 6-substitution with various alkylamino groups more or less increased the activity. Among them, the 6-dimethylamino (I-17c) and 6-(1-pyrrolidinyl) (I-34) derivative were proved to be most potent. The IC50 values (concentration which produces 50% inhibition of the allergic histamine release) of I-17c and I-34 were determined to be 4.7×10-10 and 4.6×10-10 M, respectively. These two compounds produced a potent inhibitory activity on passive cutaneous anaphylaxis (PCA) in rat, not only by the intravenous route (ED50=0.0096 mg/kg for both compounds) but also by the oral route (ES50=0.19 and 0.18 mg/kg, respectively). On the other hand, when the pyrazine ring of some representative compounds was replaced with a pyridine ring, the inhibitory activity on histamine release was significantly reduced.抄録全体を表示PDF形式でダウンロード (948K) -
阿部 健一, 井上 治, 弓岡 栄三郎1990 年 38 巻 1 号 p. 208-211
発行日: 1990/01/25
公開日: 2008/03/31
ジャーナル フリーBiliary excretion of metabolites of baicalin, present in Scutellariae Radix, was investigated using rats. The bile of rats administered baicalin orally was shown to montain five major metabolites, which were identified as baicalein 6-O-β-glucopyranuronoside (M1), 6-O-methyl-baicalein 7-O-β-glucopyranuronoside (oroxylin A 7-O-β-glucuronide (M2)), baicalein 7-O-β-glucopyranuronoside (M3), 6-O-β-glucopyranuronosyl-baicalein 7-O-sulfate (M4), and baicalein 6, 7-di-O-β-glucopyranuronoside (M5) on the basis of chemical and spectroscopic evidence.The bile of rats treated with baicalein also contained the above metabolites. Slower biliary excretion of the metabolites after baicalin administration suggested that it was absorbed as baicalein after hydrolysis in the gastrointestinal tract.The total cumulative amounts of the five metabolites excreted in the bile during 30 h after oral administration of baicalin and that of baicalein were approximately 54% and 40% of hte doses, respectively. In addition the bilary metabolites of both drugs were shown to be mainly composed of M5 and M4, which have high polarity and large molecular weight.抄録全体を表示PDF形式でダウンロード (666K) -
石田 志朗, 崎谷 陽子, 市川 勤, 平良 全栄, 粟津 荘司1990 年 38 巻 1 号 p. 212-218
発行日: 1990/01/25
公開日: 2008/03/31
ジャーナル フリーThree physiologically based pharmacokinetic models A-C, incorporating enterohepatic recycling, were developed to predict glycyrrhizin (GLZ) disposition in rat plasma and tissues, and human serum. Model A, which indluded fourteen compartments (artery, vein, tissues except brain, and gut lumen) with the assumption of direct excretion of GLZ from the liver into the gut lumen gave fairly good agreement between the observed and predicted disposition profiles in rat, but was unsuitable in man, where elimination is very rapid. Models B and C for man were obtained by adding a gallbladder compartment (drug storage organ) for the excretion from the liver into the gut lumen and by assuming continuous transfer from the storage compartment or instantaneous amptying from it during meal ingestion as the excretion process from the gallbladder into the gut lumen, respectively. The agreement between the observed and predicted serum concentration time-course profiles was better with model C than model B, especially in the terminal elimination phase, where secondary peaks appeared. However, it was thought that the observed serum disposition can be sufficiently well predicted by model B. In conclusion, prediction in rat was successful in all compartments except the brain, which shows a negligible distribution. Scale-up of the disposition kinetics of GLZ from rat to man was also successful.抄録全体を表示PDF形式でダウンロード (966K) -
上岡 龍一, 堂園 弘幸, 松本 陽子, 長 正徳, 北原 一太, 加藤 康夫1990 年 38 巻 1 号 p. 219-220
発行日: 1990/01/25
公開日: 2008/03/31
ジャーナル フリーRemakably high enantioselectivity (L/D=19) along with marked enhancement of the hydrolytic cleavage of the L-form enantiomer (L-S13) catalyzed by a tripeptide (Z-L-Phe-L-His-L-Leu) was attained by the use of specific coaggregates of 20 mol% dilauroylphosphatidylcholine and 80 mol% Triton X-100.抄録全体を表示PDF形式でダウンロード (385K) -
金岡 又雄, 加藤 弘巳, 矢野 三郎1990 年 38 巻 1 号 p. 221-224
発行日: 1990/01/25
公開日: 2008/03/31
ジャーナル フリーIn order to prepare an immunogen for enzyme immunoassay of 3β-(monoglucuron-1'-β-yl)-18β-glycyrrhetic acid (3MGA), which was isolated from a patient with glycyrrhizin-induced pseudoaldosteronisms, benzyl glycyrrhetate (3) was allowed to react with an acetobromosugar (2) in the presence of silver carbonate to give benzyl 3β-(methyl2', 3', 4'-triacetyl-glucuron-1'β-yl)-glycyrrhetate (5) and methyl 3', 4'-diacetyl-α-1', 2'-O-[1-(benzyl glycyrrhet-3β-yl)-ethylidene]-D-glucuronate (4). On the other hadn, this reaction was carried out in the presence of mercuric cyanide in nitromethane to give compound 5, benzyl 3β-acetryl glycyrrhetate (6) and benzyl 11-oxo-A-neooleana-3(5), 12-dien-3-oate (7). 4-Aminomethylcyclohexanecarboxylic acid and glycine were introduced as chemical bridges at C-30 of 3β-(tertbutylglucuron-1'β-yl)-glycyrrhetic acid (11) derived from compound 5. The former bridge was used to prepare an immunogenic conjugate with bovine serum albumin, and the latter bridge was used for antigen labelled with β-galactosidase.抄録全体を表示PDF形式でダウンロード (737K) -
余合 基, 石黒 小都子, 村田 弘之, 古川 宏1990 年 38 巻 1 号 p. 225-226
発行日: 1990/01/25
公開日: 2008/03/31
ジャーナル フリーCoclauril (1), a nonglucosidic 2-cyclohexen-1-ylideneacetonitrile, was isolated from the leaves of Cocculus lauriforius DC. (Menispermaceae) collected at Ishigaki Island (Okinawa, Japan), and the structure was elucidated by spectroscopic means. Two known bicyclic butenolides, menisdaurilide (8) adn aquilegiolide (9), were also characterized.抄録全体を表示PDF形式でダウンロード (448K) -
古川 淳, 五十嵐 順悦, 渡辺 三明, 木下 敏夫1990 年 38 巻 1 号 p. 227-229
発行日: 1990/01/25
公開日: 2008/03/31
ジャーナル フリーHighly stabilized sulfonium diacethylides (1a-c) reacted with acetyl chloride to give a mixture of the enol acetates (2a-c) and the enol diacetates (3a-c). Similarly, sulfonium acetylcarbomethoxymethylides (5a, b) gave the enol acetates (6a, b). These enol acetates were hydropyzed with HCl-MeOH to give 3-methylthio- (3-phenylthio-)2, 4-pentanediones (4a, b) or methyl 2-methylthio- (2-phenylthio-)acetoacetates (7a, b).抄録全体を表示PDF形式でダウンロード (519K) -
宮下 晶, 佐藤 進, 泰道 直方, 丹治 健一, 大石 悦男, 東野 武郎1990 年 38 巻 1 号 p. 230-233
発行日: 1990/01/25
公開日: 2008/03/31
ジャーナル フリーAcid hydrolysis of the 6-methylpyrazolopyrimidine Reissert compound (6) gave the ring-opened product (12) and the oxazole (13). Alkaline hydrolysis of 6 afforded the 6-methylpyrazolopyrimidine (7) and benzoic acid (15). The anion (1) of 6 mainly underwent both aromatization and rearrangement, resulting in the formation of the 6-methylpyrazolopyrimidinecarbonitrile (20) and the 4-benzoyl-6-methylpyrazolopyrimidine (21) together with by-products such as 7, the dimer (22), the benzoate (23a), and O-benzoylbenzoin (24a). The anion I added to the carbonyl carbon of aromatic aldehydes (8a-c), giving the benzoates (23a-c) together with 7, the O-benzoylaroins (24a-c), and the O-benzoylcyanohydrins (27a, c).抄録全体を表示PDF形式でダウンロード (665K) -
高田 大介, 末宗 洋, 酒井 浄1990 年 38 巻 1 号 p. 234-235
発行日: 1990/01/25
公開日: 2008/03/31
ジャーナル フリーReaction of alkanesulfonyl chloride with α-hydroxycyclopentanones in the presense of triethylamine in CH2Cl2 at room temperature afforded the sultones and α, β-unsaturated sultones; the usual alkanesulfonate was not obtained.抄録全体を表示PDF形式でダウンロード (383K) -
畑中 保丸, 吉田 栄一, 中山 仁, 金岡 祐一1990 年 38 巻 1 号 p. 236-238
発行日: 1990/01/25
公開日: 2008/03/31
ジャーナル フリーμ-Conotoxin GIIIA, a 22 amino acid peptide paralytic toxin which inhibits the muscle voltage-activated sodium channels, was synthesized by a solid phase method. No purification of intermediates was necessary for the synthesis, and a simple air oxidation of the deprotected crude peptide gave the desired toxin. By all criteria applied, the synthetic material was indistinguishable from the authentic natural toxin.抄録全体を表示PDF形式でダウンロード (541K)