巻号一覧
40 巻, 2 号
選択された号の論文の62件中1～50を表示しています
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角谷 重幸, 米田 照代, 北村 一泰, 村田 充男, 横尾 千尋, 玉井 正晴, 山元 淳, 井上 正敏, 石田 寿昌1992 年 40 巻 2 号 p. 299-303
発行日: 1992/02/25
公開日: 2008/03/31
ジャーナル フリーTo design a potent inhibitor specific for cathepsin B(rat liver), the tertiary structure was predicted based on the crystal structure of the papain complexed with(+)-(2S, 3S)-3-{1-[N-(3-methylbutyl)amino]leucylcarbonyl}oxirane-2-carbolylic acid(E-64-c), a thiol protease inhibitor. Taking advantage of the structural characteristics of the predicted active site, seventeen inhibitors were chemically synthesized by molecular modeling, and one of them, N-(L-3-trans-propylcarbamoyloxirane-2-carbonyl)-L-isoleucyl-L-proline(CA-074)was show to be the first potent inhibitor specific for cathepsin B. The relationship between the structure and inhibitory activity is discussed based on the model structure of the cathepsin B-inhibitor complex.抄録全体を表示PDF形式でダウンロード (813K) -
北河 修治, 藤沢 博子, 桜井 弘1992 年 40 巻 2 号 p. 304-307
発行日: 1992/02/25
公開日: 2008/03/31
ジャーナル フリーWe investigated the scavenging effects of dihydric, trihydric phenols and related polyphenols on superoxide anion radicals (O-2) generated form the hypoxanthine-xanthine oxidase system by ESR (electron spin resonance) spin trapping technique using 5, 5-dimethyl-1-pyrroline-N-oxide (DMPO) as a trapping reagent.The O-2 scavenging activities of non-substituted dihydric phenols were in the order of pyrocatechol»hydroquinone»resorcinol.Trihydric phenols, pyrogallol and gallic acid, which have phenolic OH groups at ortho positions, had stronger activities than pyrocatechol; phloroglucinol, on the other hand, which has phenolic OH groups at meta positions, had much weaker effect. Polyhydric phenols like quercetin and hematoxylin, which have catechol groups, had significant O-2 scavenging activities. In order to clarify the physico-chemical property of these phenolic compounds which determines their O-2 scavenging acivities, we investigated the effects of six 4-substituents of pyrocatechol on O-2 scavenging effects. The effects of these substituents were well correlated with their redox potentials, indicating that O-2 scavenging activities of catechol derivatives are controlled by their electron donor activities.We also observed the scavenging effects of these phenolic compounds on O-2 from a defferent source : potassium superoxide (KO2) solubilized in dimethyl sulfoxide by 18-crown-6. ESR analysis in this system revealed that one-electron oxidized products of these compounds were concomitantly formed accompanied by the reduction of O-2. The results revealed that phenolic compounds directly react with O-2 to form stable radicals, which account for the O-2 scavenging activities of the compounds.抄録全体を表示PDF形式でダウンロード (632K) -
石田 均司, 糠谷 東雄, 辻 邦郎, 全田 浩, 小菅 卓夫1992 年 40 巻 2 号 p. 308-313
発行日: 1992/02/25
公開日: 2008/03/31
ジャーナル フリーBy following the antifungal activity, four antifungal principles, acetovanillone(1), two new cyclic β-diketones, (2 and 3), and an unknown compound (4), were isolated from wood tar, Pix Pini, which has been used traditionally for the treatment of fungal diseases in Japan. The structures of 2 and 3 were established by synthesis to be 1, 1', 3, 3'-tetraoxo-2, 2'-bicyclopentyl and its 4-methyl derivative, respectively. Chemical reactivities and physical properties of 2 and 3 are also described.抄録全体を表示PDF形式でダウンロード (1003K) -
金岡 又雄, 加藤 弘巳, 島田 文恵, 矢野 三郎1992 年 40 巻 2 号 p. 314-317
発行日: 1992/02/25
公開日: 2008/03/31
ジャーナル フリーEnzyme immunoassay (EIA) of ginsenoside Rb1 (GRb1), one of the glucosides of protopanaxadiol from Panax ginseng, was explored. A carrier protein (bovine serum albumin (BSA)) was coupled to the C-26 position on the unsaturated side chain of the protopanaxadiol moiety to prepare the immunogen. In order to perform bridge heterologous EIA, a label (β-D-galactosidase) was introduced at C-26 of the saturated side chain to obtain labeled antigen. Anti-GRb1 antisera were elicited in rabbits by immunization with GRb1-BSA conjugate(9). The double antibody method (with goat anti-rabbit IgG antiserum) was used to separate the bound and free GRb1-β-Gal. A satisfactory standard curve for EIA of GRb1 was obtained in the range of 0.04-10ng/tube. In a comparison of the assay results obtained by EIA and HPLC, the linear regression equation and correlation coefficient for the two methods were y(EIA)=9.18x(HPLC)-0.033 and 0.98, respectively. The anti-GRb1 antiserum cross-reacted with GRb2 (21.8%) and GRc (10.6%), which are also constituents of Panax ginseng.抄録全体を表示PDF形式でダウンロード (722K) -
秋田 弘幸, 梅澤 勲, 松倉 弘子, 大石 武1992 年 40 巻 2 号 p. 318-324
発行日: 1992/02/25
公開日: 2008/03/31
ジャーナル フリーFor the purpose of carrying out smoothly enzymatic reaction of water-insoluble substrates in organic solvents, a new type of immobilized enzyme, a lipid-lipase aggregate, was developed. In order to prepare various kinds of lipid-lipase aggregates, 27 kinds of dialkyl ether-type phospholipid analogues were newly synthesized and used for the preparation of aggregates with lipase. Thus obtained lipid-lipase aggregates were found to catalyze the enantioselective hydrolysis of the (±)-α-acyloxy ester 2 much more efficiently than lipase immobilized with synthetic prepolymer (ENTP-4000) in water-saturated isopropyl ether. Namely. the reaction time became much shorter (2 to 3d for completion as compared with 21 d) and the chemical and optical yields of the reaction products were found to be high.抄録全体を表示PDF形式でダウンロード (1097K) -
杉山 正尚, 菊地 正雄1992 年 40 巻 2 号 p. 325-326
発行日: 1992/02/25
公開日: 2008/03/31
ジャーナル フリーThree new phenolic glucosides were isolated from the leaves of Osmanthus asiaticus NAKAI (Oleaceae). The structures of 1, 2 and 3 were determined to be 2-hydroxy-5-(2-hydroxyethyl)phenyl β-D-glucopyranoside, 4-(2, 3-dihydroxypropyl)-2, 6-dimethoxyphenyl β-D-glucopyranoside and D-threo-guaiacylglycerol 7-O-β-D-glucopyranoside, respectively, on the basis of chemical and spectral data.抄録全体を表示PDF形式でダウンロード (437K) -
棚瀬 隆宏, 村上 啓寿, 永井 慎一, 植田 泰誠, 榊原 仁作, 安藤 裕明, 堀田 芳弘, 竹谷 和視1992 年 40 巻 2 号 p. 327-332
発行日: 1992/02/25
公開日: 2008/03/31
ジャーナル フリーThree aromatic compounds (2-4) possessing a carbomethoxyl group or a dimethoxyphthaloyl group, prepared by the Diels-Alder reaction of the cardiac glycoside, proscillaridin (1), with dimethyl acetylenedicarboxylate and methyl propiolate, were transformed into alcohols, carboxylic acids and amides. The biological activities of hte resulting derivatives were evaluated by the use of Na+, K+-adenosine triphosphatase (Na+, K+-ATPase) from dog kidney and isolated guinea-pig papillary muscle. Although the biological activities of the resulting derivatives were less potent than that of 1, a para-substituted benzylalcohol (5), methylbenzamides (9a and 10a), and ethylbenzamides (9b and 10b) inhibited the activity of Na+, K+-ATPase almost as potently as naturally occurring cardiac glycosides such as digoxin and digitoxin.抄録全体を表示PDF形式でダウンロード (986K) -
小林 慶行, 石田 登, 荒井 雅巳, 汐崎 正生, 平岡 哲夫, 西島 正弘, 久下 小百合, 大塚 俊明, 赤松 穰1992 年 40 巻 2 号 p. 333-337
発行日: 1992/02/25
公開日: 2008/03/31
ジャーナル フリー2-Deoxy-2-[(2S, 3R)-(2-fluoro-3-hydroxytetradecanoyl)amino]3-O-[(3R)-3-tetradecanoyloxytetradecanoyl]-D-glucopyranose 4-(dihydrogen phosphate) and 2-deoxy-2-[(2R, 3S)-(2-fluoro-3-hydroxytetradecanoyl)amino]-3-O-[(3R)-3-tetradecanoyloxytetradecanoyl]-D-glucopyranose 4-(dihydrogen phosphate) were synthesized. The (2S, 3R)-compound (9a) was a little more active than GLA-60 in the prostaglandin D2 releasing test on macrophages, and the(2R, 3S)-compound (9b) was almost inactive.抄録全体を表示PDF形式でダウンロード (855K) -
吉田 隆志, 難波 治, 呂 車鳳, 楊 玲玲, 顔 焜〓, 奥田 拓男1992 年 40 巻 2 号 p. 338-342
発行日: 1992/02/25
公開日: 2008/03/31
ジャーナル フリーA new hydrolyzable tannin, antidesmes A (4), was isolated along with carpinusin (1) and geraniin (2) from dried leaves of Antidesma pentandrum MERR, var. barbatum MERR., and its dimeric structure, composed of devidiin (3) and geraniin (2), has been elucidated by spectral and chemical methods.抄録全体を表示PDF形式でダウンロード (712K) -
小川 和男, 西井 正廣, 稲垣 甚一郎, 野原 富士夫, 斎藤 徹, 板谷 泰助, 藤井 澄三1992 年 40 巻 2 号 p. 343-350
発行日: 1992/02/25
公開日: 2008/03/31
ジャーナル フリーA full account is given of the first chemical synthesis of the antitumor antibiotic guanine 7-oxide (5) and its 9-substituted derivatives (24a-k and 26). Coupling of appropriate primary amines (17a-e, g-k) with phanecyl bromide (16) produced, after treatment with HCl, the corresponding N-substituted phenacylamine hydrochlorides (18a-e, g-k). A similar phenacylation of 4-amino-1-butanol (21) failed to give the desired compound 18f, so that 21 was heated with 2-bromomethyl-2-phenyl-1, 3-dioxolane (20) at 150-155°C for 3h to furnish, after treatment with HCl, the amino ketal hydrochloride 22 in 40% yield. Deketalization of 22 with hot 2N aqueous HCl afforded 18f in 96% yield. Condensations of the free bases, generated in situ from the hydrochlorides 18a-l and 1N aqueous NaOH, with the chloropyrimidinone 6 were effected in aqueous EtOH at the boiling point for 20 min or at 25-30°C for 3-24h, giving the 6-phenacylamino-4-pyrimidinones 19a-l in 54-90% yields. On treatment with 2N aqueous NaOH at room temperature for 10-60 min, the nitropyrimidinones 19a-k cyclized to provide the 9-substituted guanine 7-oxides 24a-k in 61-98% yields. A similar alkali-treatment of 19l failed to yield guanine 7-oxide (5). However, removal of the 9-(arylmethyl) group from 24i-k was effected with conc, H2SO4 at room temperature for 1-3h in the presence of toluene, producing the target N-oxide 5 in 56-89% yields. In the in vitro bioassay of antileukemic activity against murine L5178Y cells, none of the 9-substituted guanine 7-oxides (24a-k and 26) was more effective than the parent, natural N-oxide 5. Within this series, however, the benzyl analogues 24g-k with or without alkoxy functions were more cytotoxic, with IC50's of 13.0-48.0μg/ml, than the alkyl analogues 24a-f.抄録全体を表示PDF形式でダウンロード (1426K) -
米島 伸泰, 大沢 立志, 西鳥羽 剛, 神野 康弘, 桐生 映美1992 年 40 巻 2 号 p. 351-356
発行日: 1992/02/25
公開日: 2008/03/31
ジャーナル フリーIn order to search for anti-inflammatory agents against autoimmune diseases, we synthesized 4-alkylthio-o-anisidine derivatives possessing antioxidant activity, and tested them for anti-inflammatory activity against the Arthus reaction in mice. Experimental inflammations, including the Arthus reaction, concanavalin A, phorbol ester and pyrophosphate-induced edemas in rats were inhibited by 4-propylthio-o-anisidine, which inhibited autoxidation of rat brain homogenate and suppressed the lipopolysaccharide-induced increase in the plasma malondialdehyde level in mice. An antioxidant may be an effective agent in immune complex type inflammation where active oxygen species play an important role.抄録全体を表示PDF形式でダウンロード (922K) -
鈴木 範夫, 三輪 保, 相原 俊三, 菅野 英幸, 高森 秀男, 坪川 政雄, 両川 祐一, 塚田 恒, 磯田 純郎1992 年 40 巻 2 号 p. 357-363
発行日: 1992/02/25
公開日: 2008/03/31
ジャーナル フリーA series of 6-substituted [1, 3, 4]thiadiazolo[3, 2-a]-1, 2, 3-triazolo[4, 5-d]pyrimidin-9(3H)-one derivatives 4a-z were synthesized from 5-substituted 1, 3, 4-thiadiazol-2-amines 5 by the following consecutive reactions : pyrimidine ring closure with bis(2, 4, 6-trichlorophenyl)malonate, nitration, chlorination, amination, hydrogenation and diazotization. The structure of 4 was confirmed by an alternate synthesis of 4, involving reaction of 5-subsituted 2-azido-1, 3, 4-thiadiazole 13 with ethyl cyanoacetate, followed by the Dimroth rearrangement and ring closure.The antiallergic activities (anti-passive peritoneal anaphylaxis, anti-passive cutaneous anaphylaxis and anti-slow reacting substance of anaphylaxis activities) of the products were evaluated.抄録全体を表示PDF形式でダウンロード (1055K) -
厚海 修吾, 中野 真人, 小池 隆, 田中 誠一, 松山 研治, 中野 麻喜子, 森島 甫1992 年 40 巻 2 号 p. 364-370
発行日: 1992/02/25
公開日: 2008/03/31
ジャーナル フリーThe synthesis and structure-activity relationships of transition-state renin inhibitors containing the homostatine analogues at the scissile bond are described. These inhibitors incorporate the amino acid side chains corresponding to positions 7-12 (P4-P2') of angiotensinogen. Ethyl, 2-hydroxyethyl and 3-hydroxypropyl groups at position 2 of the homostatine analogues (P1') are more effective for increasing potency than the isopropyl group. A combination of residues at P1, P3 and P4 is important for potency and this result auggests that S1, S3 and S4 form a huge hydrophobic core together in renin.抄録全体を表示PDF形式でダウンロード (1168K) -
桂 洋介, 西野 重孝, 井上 善一, 友井 正明, 高杉 寿1992 年 40 巻 2 号 p. 371-380
発行日: 1992/02/25
公開日: 2008/03/31
ジャーナル フリーA series of imidazo[1, 2-a]pyridinylbenzoxazoles (4) and 5, 6, 7, 8-tetrahydroimidazo[1, 2-a]pyridinylbenzoxazoles (5) were synthesized and tested for anti-stress ulcer activity in rats. Several compounds were found to be more active than the reference compounds, sucralfate, cimetidine and ranitidine. Some of them exhibited potent protective activity against ethanol-induced gastric lesion. The synthesis and structure-activity relationships of these compounds are discussed.抄録全体を表示PDF形式でダウンロード (1131K) -
田村 典一, 岩間 斗史, 伊藤 克己1992 年 40 巻 2 号 p. 381-386
発行日: 1992/02/25
公開日: 2008/03/31
ジャーナル フリー(S)-2-Amino-3-(2, 5-dihydro-5-oxo-3-isoxazolyl)propanoic acid, (3a) and its analogs (3b-h) were prepared and evaluated for glutamate receptor-agonistic and antifungal activities. Several(S)-and (R)-2-amino-3-isoxazolylpropanoic acid derivatives (3a-d) were synthesized starting with (S)-and (R)-N-tert-butoxycarbonyaspartic acid α-methyl esters (4, n=1) by means of Masamune's chain extension reaction followed by isoxazolone formation with hydroxylamine and subsequent deprotection reactions. Furthermore, (S)-and (R)-N-tert-butoxycarbonylglutamic acid α-methyl esters (4, n=2) were converted to (S)- and (R)-2-amino-4-isoxazolylbutyric acid derivatives (3e-h) via the same sequence of reactions.抄録全体を表示PDF形式でダウンロード (869K) -
木内 文之, 岩上 敏, 渋谷 雅明, 花岡 文雄, 三川 潮1992 年 40 巻 2 号 p. 387-391
発行日: 1992/02/25
公開日: 2008/03/31
ジャーナル フリーThe rhizomes of Zingiber officinale (ginger) and Alpinia officinarum contain potent inhibitors against prostaglandin biosynthesizing enzyme (PG synthetase). Gingerols and diarylhepatanoids were identified as active compounds. Their possible mechanism of action which was deduced from the structures of active compounds indicated that the inhibitors would also be active against arachidonate 5-lipoxygenase, an enzyme of leukotriene (LT) biosynthesis, This was verified by testing their inhibitory effects on 5-lopoxygenase prepared from RBL-1 cells. A diarylheptanoid with catechol group was the most active compound against 5-lipoxygenase, while yakuchinone A was the most active against PG synthetase.抄録全体を表示PDF形式でダウンロード (897K) -
出水 佐知緒, 梶山 喜一郎, 平賀 敬夫, 木下 薫, 小山 清隆, 高橋 邦夫, 田村 幸吉, 岡田 憲三, 木下 武司1992 年 40 巻 2 号 p. 392-395
発行日: 1992/02/25
公開日: 2008/03/31
ジャーナル フリーThree dibenzoylmethanes were isolated from licorice of Xinjiang origin (botanically assigned to Glycyrrhiza inflata), and their structures were elucidated spectroscopically as 1-(2, 4-dihydroxy-5-prenylphenyl)-3-(4-hydroxyphenyl)-1, 3-propanedione (I), 1-(2, 4-dihydroxy-5-prenylphenyl)-3-(4-hydroxy-3-prenylphenyl)-1, 3-propanedione (II) and 1-(2, 4-dihydroxy-5-prenylphenyl)-3-(2, 2-dimethyl-2H-1-benzopyren-6-yl)-1, 3-propanedione (III). The latter two constituents were new natural products, and were named glycyrdiones A and B, respectively.抄録全体を表示PDF形式でダウンロード (692K) -
曾 千芳, 岩上 敏, 三ヶ尻 昭宏, 渋谷 雅明, 花岡 文雄, 海老塚 豊, / 三川 潮, Ushio SANKAWA1992 年 40 巻 2 号 p. 396-400
発行日: 1992/02/25
公開日: 2008/03/31
ジャーナル フリーN-trans- and N-cis-Feruloyltyramines were isolated as the inhibitors of in vitro prostaglandin (PG) synthesis from an Indonesian medicinal plant, Ipomoea aquatica (Convolvulaceae). In order to clarify structure activity relationships, cinnamoyl-β-phenethylamines with possible combinations of naturally occurring cinnamic acids and β-phenethylamines were synthesized and tested for their inhibitory activities against PG synthetase and arachidonate 5-lipoxygenase. The compounds containing catechol groups such as N-caffeoyl-β-phenethylamine (CaP) showed higher inhibitory effects on PG synthetase. The catechol group was found to be essential for the inhibition of arachidonate 5-lipoxygenase. The investigation of concentration dependent effects on PG biosynthesis revealed that CaP enhanced PG biosynthesis at a lower concentration range, whereas it inhibited the reaction at a higher concentration. The effects of CaP on each reaction step were investigated with purified PG endoperoxide synthase and microsomal PG synthetase. CaP inhibited the cyclooxygenase reaction, while it enhanced the hydroperoxidase reaction. N-Acyldopamines which contain catechol and lipophylic group were synthesized from dopamine and fatty acids to test their inhibitory effects on arachidonate 5-lipoxygenase. N-Linoleoyldopamine was the most active compound and its IC50 value was 2.3nM in our assay system, in which an IC50 value of AA 861, a specific inhibitor of 5-lipoxygenase, was 8nM.抄録全体を表示PDF形式でダウンロード (935K) -
梅原 薫, 高木 理恵子, 黒柳 正典, 上野 明, 滝 孝雄, 陳 英杰1992 年 40 巻 2 号 p. 401-405
発行日: 1992/02/25
公開日: 2008/03/31
ジャーナル フリーDifferentiation-inducing activity of over 180 extracts of ctude drugs and plants was tested using mouse myeloid leukemia cell line (M1). The methanol extracts of clove (Syzygium aromaticum MERRILL et PERRY, Myrtaceae) showed remarkable induction of differentiation of M1 cells into macrophage-like cells. From the extract, oleanolic acid (1) and crategolic acid (2) were isolated as the active components. We also tested other triterpenes, such as oleananes, ursanes and dammaranes, to investigate the structure-activity relationship. Some triterpene aglycones showed differentiation-inducing activity, but triterpene glycosides showed little activity. Futhermore, the differentiation-inducing activity of these triterpene compounds was tested against human acute promyelocytic leukemia cell line (HL-60).抄録全体を表示PDF形式でダウンロード (646K) -
楊 秀偉, 服部 征雄, 難波 恒雄, 陳 道峰, 徐 国鈞1992 年 40 巻 2 号 p. 406-409
発行日: 1992/02/25
公開日: 2008/03/31
ジャーナル フリーThree-days successive p.o. administration of an EtOH extract of the stems of Kadsura heteroclita (Schizandreceae) or its major consituent, kadsurin, resulted in significant decreases of CCl4-induced lipid-peroxidation products, such as thiobarbituric acid reactive substances (TBA-RS), conjugated dienes and fluorescent products in the liver of mice. In contrast, a significant restoration of superoxide dismutase (SOD) activity reduced by CCl4-intoxication was observed in the administered groups, suggestin that the subchronic treatment of mice with the EtOH extract or kadsurin induce enzymes capable of scavenging oxygen radical species in the liver, though the extract and kadsurin themselves may have an anti-oxidant property.抄録全体を表示PDF形式でダウンロード (737K) -
Radioimmunoassay for the Determination of 2-Methoxyestriol Concentration in Plasma of Pregnent Women藤井 洋一, 寺西 正憲, 中田 啓二, 山崎 満, 岸田 繁, 宮保 進1992 年 40 巻 2 号 p. 410-413
発行日: 1992/02/25
公開日: 2008/03/31
ジャーナル フリーA specific assay method has been developed for the determination of 2-methoxyestriol in plasma of pregnant women. The quantitation was achieved by redioimmunoassay after extraction of the plasma with ethyl acetate and purification on a Sephadex LH-20 column. In order to obtain the immunogen for 2-methoxyestriol, 6-oxo-2-methoxyestriol was converted to its 6-(O-carboxymethyl)oxime derivative. The derivative was then coupled to bovine serum albumin by the mixed anhydride method, and rabbits were immunized with this conjugate. The antiserum obtained was partially purified by affinity chromatography on estrone 17-(O-carboxymethyl)oxime-aminohexyl Sepharose conjugate to eliminate the cross-reactive antibodies. Plasma 2-methoxyestriol concentrations in pregnancy were estimated to be mean values of 41.1pg/ml (12th-14th week), 85.3pg/ml (27th-29th week), and 97.5pg/ml (37th-41st week).抄録全体を表示PDF形式でダウンロード (776K) -
小濱 靖弘, 栢森 裕三, 片山 善章, 寺本 哲之, 村山 宣人, 辻川 和丈, 岡部 勝, 大谷 卓三, 松倉 武文, 三村 務1992 年 40 巻 2 号 p. 414-418
発行日: 1992/02/25
公開日: 2008/03/31
ジャーナル フリーWater soluble analogues of the anti-inflammatory compound, bis(2-aminopropyl)disulfide dihydrochloride (compd. I) with a butyl (II), phenyl (III), benzyl (IV) or pyrrolidinyl group (V) instead of the methyl group were synthesized, and their effects on the functions of cells related to inflammation were studied in vitro. Compounds II, III and IV showed much higher inhibitory activity than compd. I on formyl Met-Leu-Phe (FMLP)-induced O-2-generation of polymorphonuclear leukocytes (PMNs) and platelet aggregation. Compound II showed the strongest activity among the compounds (IC50 values : 2.6μM). The inhibition of O-2-generation of PMNs by compd. II was the most effective when FMLP was used as a stimulant rather than when phorbol myristate acetate, A-23187 and opsonized zymosan were used. However, compd. II was not an O-2-scavenger.Compounds II, III and IV significantly inhibited a series of activation processes in PMNs, chemotaxis, phagocytosis and lysosomal enzyme release at doses ranging from 10 to 100μM. Under these doses, compds II, III and IV did not affect the histamine release from mast cells or the hemolysis of erythrocytes. These results strongly suggest that the anti-inflammatory action caused by compd. II and its analogues was at least partly due to inhibition of several functions of PMNs and platelets.抄録全体を表示PDF形式でダウンロード (879K) -
高木 邦明, 阿江 章太郎, 祐田 泰延1992 年 40 巻 2 号 p. 419-422
発行日: 1992/02/25
公開日: 2008/03/31
ジャーナル フリーNitric oxide, nitrite and nitrate are released by activated macrophages in an immune response. We showed here that nitrite influenced cell growth and antibody production in mouse lipopolysaccharide (LPS)-stimulated splenic B cells and B cell hybridomas. The addition of 10-7 and 10-6M nitrite enhanced deoxyribonucleic acid (DNA) synthesis of LPS-stimulated splenic B cells. However, DNA synthesis and antibody production in the case of total spleen cells stimulated with LPS were suppressed by nitrite in a dose dependent-manner. These phenomena were also observed in a similar experiment involving mouse B cell hybridomas. Antibody production of all B cell hybridomas was significantly suppressed by the addition of nitrite. This suppressing effect could not be explained by changes in viable cell yields. This data suggests that the antibody production and cell proliferation of B cells may be influenced by nitrite from activated macrophages in the immune response.抄録全体を表示PDF形式でダウンロード (667K) -
吉村 好之, 近藤 薫, 西田 幹夫, 川田 純, 田中 亮1992 年 40 巻 2 号 p. 423-426
発行日: 1992/02/25
公開日: 2008/03/31
ジャーナル フリーThe Mg-adenosinetriphosphatase (ATPase) in the thyroidal NaI-treated microsome fraction was activated by treatment with basic polyamino acids or trypsin, but not with acidic polyamino acids and basic proteins such as lysozyme and ribonuclease.The enzyme kinetics showed that the activiation of trypsin or poly-L-lysine was due to an increase in the maximal velocity of the hydrolyzing reaction without a change in the affinity of the enzyme for its substrate.A break at about 25°C wasa observed in the Arrehenius plots of Mg-ATPase in the trypsin- or poly-L-lysine treated preparations, but there was no break in the control preparation.These results suggest that the activating effect of trypsin or poly-L-lysine on Mg-ATPase activity in the thvroidal NaI-treated microsome fraction is related to the lipid environment surrounding the enzyme molecule in the thyroid cell membrane.抄録全体を表示PDF形式でダウンロード (629K) -
足立 博一, 古西 清司, 足立 伊佐雄, 堀越 勇1992 年 40 巻 2 号 p. 427-431
発行日: 1992/02/25
公開日: 2008/03/31
ジャーナル フリーReduced nicotinamide adenine dinucleotide (NADH) dehydrogenase (EC 1.6.99.3) of Photobacterium phosphoreum was solubilized from membrane vesicles with 2% sucrose monolaurate, and was purified almost to homogeneity by use of diethylaminoethyl (DEAE)-Sephacel, hydroxylapatite, and Butyl-Toyopearl column chromatography in the presence of 0.5% sucrose monolaurate. About 100-fold purification was achieved, and the purified enzyme is composed of a single polypeptide with a molecular weight of 49000, as determined by gel electorophoresis in the presence of sodium dodecyl sulfate. The NADH dehydrogenase contains about one mol flavin adenine dinucleotide (FAD) as a prosthetic group per mol enzyme, but does not contain acid labile sulfide or non-heme iron. This NADH dehydrogenase can use ubiquinone-1, menadione, potassium ferricyanide, and cytochrome c as electron acceptors. The enzyme barely catalyzes the oxidation of reduced nicotinamide adenine dinucleotide phosphate (NADPH) as an electron donor. The enzyme is not susceptive to rotenone, 2-n-heptyl-4-hydroxyquinoline N-oxide, capsaicin, or N, N'-dicyclohexylcarbodiimide, which were reported as inhibitors of NADH dh I. On the other hand, flavone, reported as an inhibitor of NADH dh II of yeast and plant mitochondria, does inhibit the NADH dehydrogenase activity. These results indicate that the NADH dehydrogenase of P. phosphoreum belongs to NADH dh II.The NADH oxidase activity of the membrane vesicles of P. phosphoreum is remarkably stimulated by monovalent cations such as Na+ and K+, but is inhibited by divalent or trivalent cations. The NADH dehydrogenase activities (especially NADH-ferricyanide and NADH-ubiquinone-1 oxidoreductase) of the purified enzyme and membrane were also enhanced by Na+ and K+. However, the ubiquinol-1 oxidase activity of terminal oxidase complex (cytochrome bd complex) was not enhanced largely by the monovalent cations. These results suggest that in the respiratory chain of P. phosphoreum, NADH dehydrogenase contributes to the enhancement of electron transfer activity by monovalent cations.抄録全体を表示PDF形式でダウンロード (866K) -
桜井 光一, 羽賀 かおり, 小木曽 健人1992 年 40 巻 2 号 p. 432-435
発行日: 1992/02/25
公開日: 2008/03/31
ジャーナル フリーElectron spin resonance studies showed that addition of rat liver microsomes to the reaction system of alloxan with reduced nicotinamide adenine dinucleotide phosphate (NADPH) resulted in a marked increase in the generation of alloxan radicals (AH·), whereas heat-denatured microsomes were without such effect. Oxidation of NADPH by alloxan was also stimulated by microsomes. The microsomes from rats treated with phenobarbital, an inducer of cytochrome P-450 reductase, greatly stimulated both the AH· generation and the NADPH oxidation. However, the microsomes from rats treated with 3-methylcholanthrene, an inducer of DT-diaphorase, did not have stimulative effect greater than the control microsomes. These results suggest the possibility that NADPH-linked AH· generations in microsomal membranes is catalyzed by NADPH-cytochrome P-450 reductase.抄録全体を表示PDF形式でダウンロード (641K) -
長田 安史, 堀江 雅弘, 日高 裕介, 米本 麻里, 林 正弘, 渡辺 久子, 石田 史明, 亀井 敏夫1992 年 40 巻 2 号 p. 436-440
発行日: 1992/02/25
公開日: 2008/03/31
ジャーナル フリーNB-598, a potent inhibitor of squalene eposidase, inhibited cholesterol synthesis from [14C]acetate and induced intracellular squalene accumulation in Hep G2 cells. NB-598 inhibited cholesterol synthesis from [14C]acetate, [3H]mevalonate, and [3H]squalene, but not from [3H]2, 3-oxidosqualene in Hep G2 cells. It reduced cholesterol ester synthesis remarkably in the absence of exogenous cholesterol. This compound did not have any effect on the synthesis of ubiquinone and dolichol. When Hep G2 cells were prelabeled with micellar [3H]cholesterol, NB-598 did not affect the excretion of bile acid incorporated from [3H]cholesterol. However, NB-598 decreased the secretion of free and esterified cholesterol, triacylglycerol, and phospholipids, and increased the secretion of squalene. NB-598 is thought not only to inhibit cholesterol synthesis, but also to inhibit the secretion of lipids.抄録全体を表示PDF形式でダウンロード (900K) -
石黒 正恒, 中嶋 英美, 田邊 修一, 榊原 隆三1992 年 40 巻 2 号 p. 441-445
発行日: 1992/02/25
公開日: 2008/03/31
ジャーナル フリーTo clarify the mechanism of oral toxicity of ricin, the interaction of ricin with the epithelial cells isolated from rat small intstine was compared in vitro with those of other plant lectins by two different determinations, i.e., viability and cytotoxicity. After incubatino of the cells for 1h at 37°C with ricin, ricin B-chain, castor bean hemagglutinin (CBH), soybean agglutinin (SBA), wheat germ agglutinin (WGA), concanvalin A (Con A), and peanut agglutinin (PNA), respectively, followed by staining with tyrpan blue, ricin and ricin B-chain as well as CBH and SBA were found to have effectively reduced the number of viable cells. On the contrary, only ricin inhibited protein synthesis in the cells and the effect was blocked by D-galactose. Additional experiments employing [125I]-labeled ricin strongly suggested that ricin was first bound via its B-chain to the galactosyl residues on the cell surface followed by internalization into cells as the whole 62kDa molecule.These results infer first that ricin, as well as other lectins mentioned above, was able to reduced viability of the epithelial cells of rat small intestine by direct binding to the cell surface. The second effect, specific to ricin, was the inhibition of cellular protein synthesis.抄録全体を表示PDF形式でダウンロード (889K) -
鯉渕 康全, 山田 純司, 渡辺 隆史, 黒澤 隆夫, 藤間 貞彦, 須賀 哲弥1992 年 40 巻 2 号 p. 446-448
発行日: 1992/02/25
公開日: 2008/03/31
ジャーナル フリーWe examined stereoselectivities of enzymes related to bile acid formation in hepatic peroxisomes using two stereoisomers of 3α, 7α, 12α-trihydroxy-5β-cholestanoic acid (THCA) and its coenzyme A (CoA) derivatives. The activity of acyl-CoA synthetase for 25S-THCA was 1.4-times higher than that for 25R-THCA. The difference was also observed after clofibrate-treatment. This activity was located in microsomes, differing from palmitoyl-CoA synthetase located in mitochondria, peroxisomes and microsomes. There was no stereoselectivity in the reaction of peroxisomal fatty acyl-CoA oxidase for THCA isomers, and the activity was one tenth of that for acyl-CoA synthetase. Considering the overall raction of peroxisomal bile acid formation, the stereoselective difference observed in THCA-CoA synthesis should be denied. Thus, the previous finding that the overall formation of bile acid from THCA was not stereoselective was further confirmed. Furthermore, the activity for THCA oxidation was not induced by clofibric acid, suggesting that there would be different isozymes of peroxisomal acyl-CoA oxidase against THCA-CoA and palmitoyl-CoA.抄録全体を表示PDF形式でダウンロード (619K) -
田原 正義, 渡邉 一則1992 年 40 巻 2 号 p. 449-451
発行日: 1992/02/25
公開日: 2008/03/31
ジャーナル フリーInfluences of indomethacin, which has been known as an inhibitor of the production of prostaglandins, on the suppression of footpad reaction (FPR) of BALB/c mice against sheep red blood cells by the painting of 12-O-tetradecanoylphorbol 13-acetate (TPA, a typical tumor promoter) were studied. The temporary suppressive effect by the painting of TPA (8nmol) was abrogated by the painting of indomethacin (7-70nmol) 60min before TPA treatments. The lasting suppressive effect by TPA treatment (8nmol/d) for 7d following the painting of 7, 12-dimethylbenz[α]anthracene (DMIBA, 400nmol), which is a typical tumor initiator, also disappeared when indomethacin (7nmol) was painted 30-90min before each TPA treatment.Influences of some inhibitors of tumor promotion on the lasting suppressive effect of FPR by DMBA and TPA were also tested. Painting of 0.6μmol of 1-phenyl-2-pyrazolidone, 8.2nmol of salcophytol A, 17nmol of retinoic acid, 5.6μmol of 3(2)-tert-butyl-4-hydroxyanisol, and 3μmol of quercetin 45min before each TPA treatment decreased the suppressive effect on the footpad reaction.抄録全体を表示PDF形式でダウンロード (517K) -
林 勧生, 山本 格, 合田 栄一1992 年 40 巻 2 号 p. 452-455
発行日: 1992/02/25
公開日: 2008/03/31
ジャーナル フリーThe physicochemical and biological properties of a mouse hepatocyte growth-stimulating factor (mHGSF), whose amount in mouse serum increased markedly 24h after carbon tetrachloride administration (E. Gohda et al., Life Sci. 46, 1801 (1990)), were examined. This factor was a heat-labile protein with a molecular weight of 75000. Its activity was sensitive to disulfide reduction. Maximal stimulatino of deoxyribonucleic acid synthesis in cultured rat hepatocytes by this factor was greaster than that by acidic fibroblast growth factor (acidic FGF) or mouse epidermal growth factor (EGF) and was comparable to maximal stimulation by human hepatocyte growth factor (hHGF), a heterodimer with a molecular weight of about 85000. The effect of mHGSF was additive to the maximal effects of acidic FGF and EGF and was synergistic with the maximal effect of insulin, but was neither additive nor synergistic with the maximal effect of hHGF. The mHGSF activity was not inhibited by a neutralizing anti-hHGF antiserum, which recognized nonreduced hHGF but not reduced heavy and light chains of hHGF. mHGSF did not show any cross-reactivity to anti-hHGF monoclonal and/or polyclonal antibodies as measured by an enzyme-linked immunosorbent assay for hHGF. These results suggest that mHGSF is a hHGF-like factor with some structural difference from hHGF.抄録全体を表示PDF形式でダウンロード (787K) -
伊豆本 種野, 相生 章博, 上ノ山 智史, 栗山 澄, 東 正人1992 年 40 巻 2 号 p. 456-458
発行日: 1992/02/25
公開日: 2008/03/31
ジャーナル フリーThe transferred percentages of 13 drugs to rat skin from transdermal patches were studied to reveal the relationship to their physicochemical properties. The drugs to be tested had melting points of 13.5-234°C, lipophilic indices of 0.475-5.336, and molecular weights of 122.12-392.45. The transferred percentage of drug to intact skin was lower, the higher the melting point, lipophilic index and molecular weight. The same was true in stripped skin, where the transferred percentage of drug was markedly increased. The difference between transferred drug percentages to stripped and intact skin, which could be regarded as the regulatory contribution of the stratum corneum, tended to be larger, the lower the drug's melting point and lipophilic index.抄録全体を表示PDF形式でダウンロード (599K) -
渡邉 一則, 谷古宇 秀, 高山 幸三, 町田 良治, 永井 恒司1992 年 40 巻 2 号 p. 459-462
発行日: 1992/02/25
公開日: 2008/03/31
ジャーナル フリーThe release behavior of prednisolone from hydrogels prepared with xanthan and locust bean gums was investigated. Newly developed equipment was employed in order to increase the gum concentration in the hydrogels. The apparent release rate of prednisolone from the hydrogels decreased with increasing gum concentration, suggesting that the diffusion of drug molecules was mainly controlled by the density of the three-dimensional network structure in the matrix. The effect of additives such as glycerin and sucrose on the release behavior of prednisolone was also investigated in detail. Drug release was significantly lowered by the addition of these compounds to these hydrogels. A linear relation was observed between the apparent release rate of prednisolone and the microscopic viscosity of the hydrogels. these results indicated that the drug release could be controlled not only by the density of the network structure but also by the microscopic viscosity of the hydrogels.抄録全体を表示PDF形式でダウンロード (620K) -
内田 享弘, 安武 拓治, 後藤 茂1992 年 40 巻 2 号 p. 463-466
発行日: 1992/02/25
公開日: 2008/03/31
ジャーナル フリーHydroxy propyl methyl cellulose acetate succinate high grade (AS-HG) and ethyl cellulose (EC) mixture microcapsules containing cefadroxil or theophylline were prepared by a solvent evaporation method in liquid paraffin dissolved sorbitan tristearate as a dispersing agent, and their sustained-release properties were evaluated. The microcapsules prepared with AS-HG : EC (in a 2 : 5 weight ratio) mixture containing 20% of cefadroxil or theophylline exhibited apparent zero-order releasing pattern in pH 6 to 8, at 50rpm and 37°C (paddle method). These microcapsules were administered orally to beagle dogs and the plasma concentrations of cefadroxil or theophylline were measured periodically. As a result of in vivo investigation, a satisfactory sustained-release plasma pattern and an apparent zero-order process in the gastrointestinal absorption were confirmed by deconvolution analysis of both drugs.抄録全体を表示PDF形式でダウンロード (633K) -
/ 山本 恵司, / , 仲井 由宣, Fawzia Sayed HABIB, Yoshinobu NAKAI1992 年 40 巻 2 号 p. 467-471
発行日: 1992/02/25
公開日: 2008/03/31
ジャーナル フリーThe molecular interaction between benzoic acid and florite R (porous calcium silicate) in solid state was studied by using powder X-ray diffraction analysis, infrared (IR)-spectroscopy, differential sanning calorimetry and thermogravimetric analysis. It was found that the mixing ratio, relative humidity and heating significantly affected the molecular behavior of benzoic acid in the physical mixture. In low mixing ratios (up to 30% benzoic acid), benzoic acid was almost transformed to amorphous calcium benzoate within a few hours after mixing. Storage of the physical mixtures containing benzoic acid in the ratio of 40-60% at high relative humidity, or heating them in sealed ampules, accelerated the rate of transformation of benzoic acid to amorphous calcium benzoate and also allowed the formation of a crystalline complex of the following composition : (C6H5COO)2 Ca·C6H5COOH·H2O. The same complex was successfully prepared using benzoic acid and calcim benzoate trihydrate in a 1 : 1 molar ratio by coprecipitation from an aqueous solution, by mechanical grinding and by heating in sealed ampule at 100°C.抄録全体を表示PDF形式でダウンロード (755K) -
川島 嘉明, 日野 知証, 竹内 洋文, 丹羽 敏幸, 川勝 英次, 栢野 正則, 井田 勝三, 小沢 博, 坂本 浩1992 年 40 巻 2 号 p. 472-478
発行日: 1992/02/25
公開日: 2008/03/31
ジャーナル フリーPhospholipid nanosphere dispersions incorporating a lipophilic drug were prepared by the heating method. Prepared dispersions were powdered by depositing them on sugar nuclei in a fluidized-bed granulator in an aqueous system. Resultant free-flowing powders, which were agglomerates of sugar with phospholipid, reproduced phospholipid nanosphere dispersions when rehydrated with water. Incorporation of a lipophilic drug, e.g., tocopherol, into the nanospheres or increasing of phospholipid concentration in the formulation increased the sizes of rehydrated nanospheres compared to the original dispersion before powdering due to the fusion or aggregation of the nanospheres. Proper selection of sugar nuclei, decreasing the sizes of original phospholipid nanospheres for powdering and addition of polyhydric or sugar alcohols into the sprayed dispersion, however, significantly reduced the aggregation of rehydrated nanosphere. All procedures from the preparation of the original nanosphere dispersion to its powdering were performed in an aqueous system without use of any organic solvent. The procedures described here are recommended to produce stable powdered nanosphere which can be rehydrated to form phospholipid nanosphere dispersions when required.抄録全体を表示PDF形式でダウンロード (1716K) -
西沢 孝志, 稲川 裕之, 大島 治之, 奥冨 隆文, 月岡 大輔, 井口 誠, 杣 源一郎, 水野 伝一1992 年 40 巻 2 号 p. 479-483
発行日: 1992/02/25
公開日: 2008/03/31
ジャーナル フリーBased on our new concept of ontogenic inflammation, we have sought a substance which can prime macrophage in terms of the endogenous production of tumor necrosis factor (TNF). A lipopolysaccharide (LPSw) was found in wheat flour, purified and characterized. The molecular size of LPSw was about 5kDa sodum dodecyl sulfate-polyacrylamide gel electrophoresis, and it contained 3-deoxy-D-manno-octulosonic acid : 1, hexosamine : 4 and one phosphorus in a single molecule. LPSw can prime macrophage to release TNF when given intradermally, percutaneously or even orally in mice as well as in humans, in exactly the same way as intravenous administration of interferon γ.抄録全体を表示PDF形式でダウンロード (952K) -
竹内 由和, 安川 秀仁, 山岡 由美子, 森本 泰子, 中尾 智志, 福森 義信, 福田 友昭1992 年 40 巻 2 号 p. 484-487
発行日: 1992/02/25
公開日: 2008/03/31
ジャーナル フリーWhole skin lipid bio-liposomes (skin bio-liposomes), in size ranging from 2 to 8μm, were prepared by a reverse phase evaporation technique using rat full thickness skin. Leakage of an encapsulated fluorescence probe, ANTS (δ-amino-1, 3, 6-naphtalenetrisulfonate), was measured by adding transdermal penetration enhancers (penetrants) into the medium where the skin bio-liposomes were present. Oleylamine induced a fast release of ANTS from the liposomes compared to laurylamine which showed a weak action. With these penetrants, the degree of ANTS release from the prepared bio-liposomes was found to correlate well with the results of frequency changes in the CH-asymmetric stretching band near 2920cm-1 in the rat stratum corneum. The penetrant which caused relatively strong leakage of ANTS induced the significantly large shift of the peak toward the higher wavenumbers due to the perturbation in the structure of lipids of the stratum corneum. The skin bio-liposomes prepared from the rat full thickness skin could be useful in evaluating the penetrants.抄録全体を表示PDF形式でダウンロード (762K) -
前島 徹, 大沢 孝, 小林 征雄, 野田 和夫1992 年 40 巻 2 号 p. 488-492
発行日: 1992/02/25
公開日: 2008/03/31
ジャーナル フリーFactors effecting spherical beads granulation by using centrifugal fluidizing granulator were studied. Spherical beads were prepared by feeding powdered drugs on Non-pareil-103 while spraying a binder solution containing various sugars or polymers.Effect of binder species on the granulation was compared using nicotinamide as a model drug. Aqueous solutions of polyemrs commonly gave beads of high crushing strength, however, serious agglomeration of beads was observed. Aqueous sucrose solution produced beads of the highest strength with less agglomeration, while other sugars produced fairly fragile beads.Various drugs with different solubilities were granulated using aqueous sucrose solution as a binder to examine the effect of physicochemical properties of drugs on the granulatability. Water-soluble drugs such as nicotinamide or isoniazid produced spherical beads with a smooth surface, whereas slightly water-soluble drugs such as tipepidine hibenzate or bisbentiamine produced beads of irregular shape and rough surfaces. Dusting of powders was little in the former but was serious in the latter.The granulatability of these slightly water-soluble drugs was greatly improved by adding ethanol in the binder solution and the optimal ethanol concentration was around 30%. At this concentration, immersional wetting (Γ·cosθ) of the solvent to these drugs took the maximum value. On the basis of these findings, the granulatability of drugs using a CF granulator was discussed in relation to the solubility and wettability of drugs to the binder solvent.抄録全体を表示PDF形式でダウンロード (1078K) -
王 誠明, 太田 節子, 篠田 雅人1992 年 40 巻 2 号 p. 493-498
発行日: 1992/02/25
公開日: 2008/03/31
ジャーナル フリーThe fluctuation of lipid peroxidation (LP) in 9 tissues was investigated in mice for 7d after whole-body X-irradiation with a lethal dose of bone marrow death. LP increased significantly in bone marrow, thymus, spleen and liver following irradiation, and slightly in brain and testis, but not in blood plasma, submaxillary gland or kidney.The effects of 7 radioprotective Chinese traditional medicines (CTMs) and cysteamine (MEA) on the radiation-induced LP in 4 tissues were studied by i.p. injection before or after irradiation and their LP content in tissues was measured 2d after irradiaton. Most CTMs showed significant inhibition of radiation-induced LP in bone marrow and liver, especially when injected prior to irradiation. Some CTMs also showed such inhibition in spleen. MEA only inhibited the increase of LP in liver when injected before irradiation, but enhanced the increase of LP in spleen. None of these radioprotectors including MEA was recognized to inhibit radiation-induced LP in thymus.The in vitro experiments were carried out using mouse liver microsomal suspensions (MS). The MS were prepared from normal (non-irradiated) mice. Each of the 8 radioprotectors was added to MS before or after irradiation and then post-irradiation-incubated at 37°C. All markedly inhibited radiation-induced LP if added before irradiation, but were slightly less effective if added after.抄録全体を表示PDF形式でダウンロード (1129K) -
岡部 亘雄, 足立 薫1992 年 40 巻 2 号 p. 499-500
発行日: 1992/02/25
公開日: 2008/03/31
ジャーナル フリーThe interaction betwen tryptamine, 3-indoleacetic acid and 5-hydroxyindole-3-acetic acid and bovine serum albumin (BSA) was investigated using the equilibrium dialysis technique. The apparent binding constant was determined assuming the equivalence and independence of the binding sites on the BSA molecule. The binding constants of tryptamine, 3-indoleacetic acid and 5-hydroxyindole-3-acetic acid with a single binding site are 1.07 (0.14)×104M-1, 1.73 (0.15)×104M-1 and 2.02 (0.15)×104M-1 at 25°C at pH 6.5, respectively. The affinity of the tryptophan metabolites to BSA strengthened with progression of the metabolic process, and it reached a maximum at a relatively narrow pH region of 6 to 8.抄録全体を表示PDF形式でダウンロード (411K) -
邨次 誠, 黒沢 茂, 森 義仁, 加茂 直樹1992 年 40 巻 2 号 p. 501-503
発行日: 1992/02/25
公開日: 2008/03/31
ジャーナル フリーAllylamine (ALAM) film was plasma-polymerized on a flat glass (referred to as ALAM(GLA) : GLA refers to a flat glass plate). for use as a solid phase in two-site immunoradiometric assay (two-site IRMA). Adsorption of F(ab')2 anti-human immunogloblin G (referred to as F-__2hIgG) to ALAM(GLA) was larger than adsorption on a polyvinyl chloride plate (referred to as PVC). Contrary to the expectation that the dose response for human IgG (hIgG) on ALAM(GLA) was better than that on PVC, the dose responses on both solid phases were the same. This phenomenon was independent of molecular size of the antigen (Ag) (hIgG or Fc fragment of hIg G (hIgG-Fc)) and also of the reaction with protein A (pA). Because direct measurements of binding with 125I-labeled hIgG (hIgG⋆) or hIgG-Fc (hIgH-Fc⋆) showed no difference between ALAM(GLA) and PVC, the phenomenon was not due to the second step in the system of two-site IRMA (an Ag-Ab reaction (Ab refers to antibody)). These results indicated that the phenomenon was due to the first step (the adsorption of F-__ahIgG to a solid phase). When the concentration of F-__ahIgG immobilized on the solid phases was lowered, a significant increase in the dose response was observed for ALAM (GLA).抄録全体を表示PDF形式でダウンロード (548K) -
岡部 亘雄, 藤井 幹子1992 年 40 巻 2 号 p. 504-505
発行日: 1992/02/25
公開日: 2008/03/31
ジャーナル フリーThe denaturation of the 57kilodalton (kDa) rat liver nuclear thyroid hormone binding protein (NTHB) by pH and guanidine hydrochloride (GdnHCl) has been investigated with the fluorescence method. The acid and alkaline fluorescence quenching suggests that the structure of NTHB is invariant in the relatively narrow pH region of approximately pH 7-9. A cooperative conformational transition occured in GdnHCl concentrations of 1.5-2.5M. The apparent free energy of unfolding of NTHB, ΔGH2Oapp was evaluated as 6.31 (±0.12) kcal·mol-1 at pH 7.7, 25°C.抄録全体を表示PDF形式でダウンロード (418K) -
廣瀬 順造, 加納 浩之, 喜谷 喜徳, 岩本 博行, 廣海 啓太郎1992 年 40 巻 2 号 p. 506-508
発行日: 1992/02/25
公開日: 2008/03/31
ジャーナル フリーZinc deficient bovine superoxide dismutase (Cu2E2OSD(E=empty)) was prepared and purified by high performance liquid chromatography (HPLC). Each peak was characterized as to protein, copper content and specific activity. The Cu2E2SOD peak fractionated by HPLC has a low specific activity at pH 7.8 (about 10% of the native enzyme (Cu2Zn2SOD)). With the addition of zinc ions, the specific activity of Cu2E2SOD was quantitatively restored to that of the native enzyme. This behavior implies that the zinc ion is very important for the appearance of enzyme activity.抄録全体を表示PDF形式でダウンロード (498K) -
高野 悦1992 年 40 巻 2 号 p. 509-512
発行日: 1992/02/25
公開日: 2008/03/31
ジャーナル フリーPreferential formation of 1-(cholestan-3β-yl) N-CBZ-L-glutamate (3) or 5-(cholestan-3β-yl) N-CBZ-L-glutamate (4) was obtained when dicyclohexylamine or 4-(dimethylamino)pyridine was used as a basic catalyst for ester formation, respectively. Each glutamate was converted to an anomeric mixture of glucose derivatives : 1-(cholestan-3β-yl) 5-(2", 3", 4", 6"-tetra-O-benzyl-α- and -β-D-glucopyranosyl) N-CBZ-L-glutamates (7 and 8) or 5-(cholestan-3β-yl) 1-(2", 3", 4", 6"-tetra-O-benzyl-α- and -β-D-glucopyranosyl) N-CBZ-L-glutamates (9 and 10), using 2", 3", 4", 6"-tetra-O-benzyl-α-D-glucopyranose (11). After chromatographic separation of these isomers, their structures were determined by field desorption mass and nuclear magnetic resonance spectrometries.抄録全体を表示PDF形式でダウンロード (592K) -
丹治 健一, 佐藤 進, 金丸 喜彦, 飯島 千穂子, 宮下 晶, 東野 武郎1992 年 40 巻 2 号 p. 513-517
発行日: 1992/02/25
公開日: 2008/03/31
ジャーナル フリーIn the treatment of 6-benzoyl-6, 7-dihydro-3-phenyl-3H-1, 2, 3-triazolo[4, 5-d]pyrimidine-7-carbonitrile (1, triazolo-pyrimidine Reissert compound) and 6-benzoyl-6, 7-dihydro-5-methyl-3-phenyl-3H-1, 2, 3-triazolo[4, 5-d]pyrimidine-7-carbonitrile (2, 5-methyltriazolopyrimidine Reissert compound) with an acid, the ring fission of the pyrimidine ring proceeded to give the triazole derivatives (3-7). Alkaline hydrolysis of 2 and 1 gave 5-metyl-3-phenyl- (10) and 3-phenyl-3H-1, 2, 3-triazolo[4, 5-d]pyrimidines (9), respectively. The anions, generated from 1 and 2 with sodium hydride (NaH), underwent aromatization to give the 3H-1, 2, 3-triazolo[4, 5-d]pyrimidine-7-carbonitriles (12 and 14). Compounds 1 and 2 reacted with arylaldehydes in the presence of NaH to give corresponding 3H-1, 2, 3-triazolo[4, 5-d]pyrimidin-7-ylmethyl benzoates (15 and 17).抄録全体を表示PDF形式でダウンロード (696K) -
田中 哲也, 白井 直洋, 佐藤 義朗1992 年 40 巻 2 号 p. 518-520
発行日: 1992/02/25
公開日: 2008/03/31
ジャーナル フリーThe effects of substituents (MeO, Me, H, Br, CN, NO2) of the benzyl groups in the Sommelet-Hauser rearrangement of N, N-bis(substituted benzyl)-N-methyl(trimethylsilyl)methylammonium halides with cesium fluoride in N, N-dimethylformamide were examined.抄録全体を表示PDF形式でダウンロード (653K) -
宮澤 修平, 岡野 和夫, 下村 直之, 川原 哲也, 浅野 修, 吉村 寛幸, 河合 隆利, 左右田 茂, 吉田 豊, 里 忠, 町田 善 ...1992 年 40 巻 2 号 p. 521-523
発行日: 1992/02/25
公開日: 2008/03/31
ジャーナル フリーOptically active platelet-activating factor (PAF) receptor antagonist, (+)-6-(2-chlorophenyl)-3-cyclopropanecarbonyl-8, 11-dimethyl-2, 3, 4, 5-tetrahydro-8H-pyrido[4', 3' : 4, 5]thieno[3, 2-f][1, 2, 4]triazolo[4, 5-a][1, 4]diazepine (E6123), was synthesized on large-scale by optical resolution using (+)-dibenzoyl-D-tartaric acid. An X-ray crystallographic analysis clearly indicated that the absolute configuration of the synthesized E6123 was S.抄録全体を表示PDF形式でダウンロード (525K) -
松下 正行, 吉田 守宏, 張 勇, 宮下 正昭, 入江 寛, 上野 民夫, 鶴島 鉄1992 年 40 巻 2 号 p. 524-527
発行日: 1992/02/25
公開日: 2008/03/31
ジャーナル フリーSynthesis of (-)-gloeosporone (1a), isolated from spores of Colletotrichum gloeosporioides as a self-inhibitor for germination, and its three diastereomers was accomplished starting from (S)- and (R)-1-tridecen-8-ol obtained from their (S)-naphthyl ethylcarbamates (8a and 8b), both of which were isolated from the mixture of diastereoisomers derived from racemic 1-tridecen-8-ol (7) and the Pirkle reagent. Biological testing of the compounds showed weak self-inhibitor activity toward germination of the spores.抄録全体を表示PDF形式でダウンロード (734K) -
大和 正利, 竹内 靖雄, 張 明栄, 橋垣 国子1992 年 40 巻 2 号 p. 528-530
発行日: 1992/02/25
公開日: 2008/03/31
ジャーナル フリーNovel indolo[3, 2-b]quinoline derivatives (1c-f), which carried a methoxy or a hydroxy group at the 4- or 7-position of the lead compound 1a, were prepared and their antitumor activities against P388 in mice were examined. Except for the 4-hydroxy derivative (1d), these showed remarkably potent activity. Among these compounds, the 7-hydroxy derivative (1f) was the most potent one (optimal dose=50mg/kg, the median survival time of treated group/control group (T/C)>330%, cure=5/6).抄録全体を表示PDF形式でダウンロード (558K)