巻号一覧
34 巻, 10 号
選択された号の論文の76件中1～50を表示しています
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高橋 真一郎, 永嶋 伸也, 西村 善文, 坪井 正道1986 年 34 巻 10 号 p. 3987-3993
発行日: 1986/10/25
公開日: 2008/03/31
ジャーナル フリーTwo self-complementary deoxyribo-oligonucleotides, d(CCGG) and d(CCTAGG), were synthesized. Their 31P and ribose 1H nuclear magnetic resonance (NMR) assignments were achieved by the use of 31P-1H and 1H-1H shift correlated two-dimensional NMR techniques in low salt solution. One of the phosphorus atoms in each of these two origomers showed an anomalous behavior : its resonance was shifted to lower field instead of higher field on lowering the temperature in the range below the melting temperature. This "anomalous" 31P was assigned to CpG for d(CCGG), and TpA for d(CCTAGG). Among the four self-complementary G.C tetramers [d(CCGG), d(CGCG), d(GGCC), d(GCGC)], this anomalous behavior of 31P was found only in d(CCGG)[D.J.Patel, Biopolymers, 15, 533 (1976); ibid., 16, 1635 (1977); ibid., 18, 553 (1979)]. It was suggested from the results that a sequence 5'···(Py)p(Py)p(Pu)p(Pu)···3' always shows a conformational peculiarity at the (Py)p(Pu) portion, where Py=pyrimidine and Pu=purine nucleosides, and that the peculiarity involves the unusually low twist angle, tg, (i.e.the local residual rotation around the helix axis).The anomalous 31P behavior can be explained by postulating an intermediate form in the coil to helix transition.抄録全体を表示PDF形式でダウンロード (716K) -
野口 三千彦, 長田 聖士, 梶返 昭二1986 年 34 巻 10 号 p. 3994-4000
発行日: 1986/10/25
公開日: 2008/03/31
ジャーナル フリーPyrazolo[3', 4' : 4, 5]pyrido[2, 3-d]pyrimidine derivatives were obtained from the reaction of tosylhydrazones of 6-allylaminopyrimidine-2, 4(1H, 3H)-dione-5-carbaldehydes with lead tetraacetate in good yields. In this reaction, the nitrile imide intermediates underwent an intramolecular 1, 3-dipolar addition reaction to yield the tricyclic heterocycles. Pyrazolo[3, 4-d]pyrimido[4, 5-b]-azepine derivatives were also prepared by similar oxidation of tosylhydrazones of the corresponding 6-alkenylaminopyrimidine-2, 4(1H, 3H)-dione-5-carbaldehydes.抄録全体を表示PDF形式でダウンロード (759K) -
谷沢 和隆, 奥村 邦雄, 伊藤 博美, / 金岡 祐一, YUICHI KANAOKA1986 年 34 巻 10 号 p. 4001-4011
発行日: 1986/10/25
公開日: 2008/03/31
ジャーナル フリーA series of cyclic peptides varying in ring size and in amino acid constituents was synthesized. Cyclization reactions of linear peptides were carried out by the azide, p-nitrophenyl ester, N-hydroxysuccinimide ester and diethyl phosphorocyanidate methods. Intermolecular cyclodimerization was also applied for the preparation of a cyclic hexapeptide. The reaction yield in each cyclization method was found to be sufficient for preparative purposes. Conformational analysis of the cyclic peptides was carried out by using proton nuclear magnetic resonance. The temperature dependency of peptide NH signals revealed that hexapeptides with the cyclo(-Gly-Xxx-Gly-)2 sequence are stabilized by intramolecular hydrogen bonding and are resistant to temperatureinduced conformational change.抄録全体を表示PDF形式でダウンロード (980K) -
黒柳 正典, 塩津 道子, 海老原 毅, 河合 秀晃, 上野 明, 福島 清吾1986 年 34 巻 10 号 p. 4012-4017
発行日: 1986/10/25
公開日: 2008/03/31
ジャーナル フリーFrom Viburnum awabuki K. KOCH (Caprifoliaceae), four new acetyl glucosides of scopoletin, 2'6'-di-o-acetylscopolin (1), 3', 6'-di-O-acetylscopolin (2), 6'-O-acetylscopolin (3) and 2'-O-acetylscopolin (4), and two lupane-type triterpenes, 6α-hydroxylup-20(29)-en-3-on-28-oic acid (6) and its 6β-epimer (7), were isolated. Their structures were elucidated on the basis of physicochemical evidence, including proton and carbon-13 nuclear magnetic resonance spectrometry.抄録全体を表示PDF形式でダウンロード (582K) -
菊池 徹, 嘉ノ海(旧姓松田) 暁子, 村井 義洋, 門田 重利, 坪野 浩二, 荻田 善一1986 年 34 巻 10 号 p. 4018-4029
発行日: 1986/10/25
公開日: 2008/03/31
ジャーナル フリーSeven new triterpenes, ganoderic acids F, G, and H, lucidenic acids D2 and E2, compound C5', and compound C6, were isolated from the surface part of gills of Ganoderma lucidum. The structures 3a, 1a, 4a, 6a, 7a, 2b, and 5b were proposed for these compounds, respectively. Detailed analyses of the proton and carbon-13 nuclear magnetic resonance (1H-and 13C-NMR) spectra were performed by using two-dimensional (2-D) 1H-1H and 1H-13C shift correlation techniques.抄録全体を表示PDF形式でダウンロード (1004K) -
菊池 徹, 嘉ノ海(旧姓松田) 暁子, 村井 義洋, 門田 重利, 坪野 浩二, 荻田 善一1986 年 34 巻 10 号 p. 4030-4036
発行日: 1986/10/25
公開日: 2008/03/31
ジャーナル フリーThe structures of ganolucidic acids A and B, new lanostane-type triterpenoids isolated from the surface part of the gills of Ganoderma lucidum (Polypolaceae), ware determined to be 1a and 2a, respectively. Detailed analyses of proton and carbon-13 nuclear magnetic resonance (1H-and 13C-NMR) spectra were performed by using two-dimensional (2-D) 1H-1H and 1H-13C shift correlation NMR techniques.抄録全体を表示PDF形式でダウンロード (652K) -
森 雅美, 手島 節三, 丹羽 利充1986 年 34 巻 10 号 p. 4037-4044
発行日: 1986/10/25
公開日: 2008/03/31
ジャーナル フリーTreatment of methyl 2, 3, 4, -tri-O-benzoyl-6-deoxy-6-iodo-α-D-mannopyranoside (1) or methyl 4-O-acetyl-2, 3-di-O-benzoyl-6-deoxy-6-iodo-α-D-allopyranoside (11) with silver fiuoride in pyridine gave the corresponding D-lyxo- (2) or D-ribo-hex-5-enoside (12), respectively. Catalytic hydrogenation of these 5-enosides yielded preferentially the 6-deoxy-L-gulo derivative (4) from the D-lyxo-5-enoside (2) and the 6-deoxy-L-talo derivative (14) from the D-ribo-5-enoside (12). Zemplen deacylation followed by acid hydrolysis of the acylated glycosides afforded 6-deoxy-L-gulose and 6-deoxy-L-talose. The product ratios upon hydrogenation of the 5-enoside derivatives with several kinds of catalysts were measured by high-performance liquid chromatography and results are summarized in Tables I and II. The proton and carbon-13 nuclear magnetic resonance spectral data of the products are also discussed.抄録全体を表示PDF形式でダウンロード (824K) -
高津戸 秀, 池川 信夫1986 年 34 巻 10 号 p. 4045-4049
発行日: 1986/10/25
公開日: 2008/03/31
ジャーナル フリーSeveral deuterio-labelled brassinosteroids, [26, 28-2H6]brassinolide (1), [26, 28-2H6]castasterone (2), [26, 28-2H6]typhasterol (3), and [26, 28-2H6]teasterone (4), were synthesized from [26, 28-2H6]-crinosterol (5).抄録全体を表示PDF形式でダウンロード (663K) -
小林 茂, 徳元 俊弘, 木原 勝, 今倉 康宏, 新宮 徹朗, 小泉 淳二, 上尾 庄次郎1986 年 34 巻 10 号 p. 4050-4055
発行日: 1986/10/25
公開日: 2008/03/31
ジャーナル フリーThe structures of "acid B" and its monoethyl ester, which are stepwise oxidation products of lycoramine (2), an Amaryllidaceae alkaloid, and the structure of a nitro derivative of acid B, an oxidation product of oxolycoramine (5) with nitric acid, were established as 6, 10 and 12, respectively, on the basis of spectral and chemical evidence.抄録全体を表示PDF形式でダウンロード (638K) -
久保 陽徳, 中原 伸輔, 稲葉 勝利, 北原 嘉泰1986 年 34 巻 10 号 p. 4056-4068
発行日: 1986/10/25
公開日: 2008/03/31
ジャーナル フリーThree isoquinolinequinone antimicrobial metabolites, renierone (3), 7-methoxy-1, 6-dimethyl-5, 8-dihydroisoquinoline-5, 8-dione (4) and N-formyl-1, 2-dihydrorenierone (6), isolated from a marine sponge (Reniera sp.), were synthesized.抄録全体を表示PDF形式でダウンロード (1427K) -
小林 美幸, 島立 利貞1986 年 34 巻 10 号 p. 4069-4074
発行日: 1986/10/25
公開日: 2008/03/31
ジャーナル フリー2, 3, 4, 6-Tetra-O-acetyl-1-O-trifluoroacetyl-α-D-glucopyranose was prepared in a high yield by treating 1, 2, 3, 4, 6-penta-O-acetyl-α- or -β-D-glucopyranose with a mixture of trifluoroacetic acid and its anhydride in the presence of trifluoromethanesulfonic acid or antimony (V) fluoridegraphite catalyst. The reaction of the trifluoroacetate with some carboxylic acids afforded the corresponding 1-O-acyl-2, 3, 4, 6-tetra-O-acetyl-α-D-glucopyranoses. By a similar procedure, anomeric 1-O-trifluoroacetyl-2, 3, 5-tri-O-benzoyl- and -2, 3, 5-tri-O-acetyl-D-ribofuranose were obtained from 1-O-acetyl-2, 3, 5-tri-O-benzoyl- and 1, 2, 3, 5-tetra-O-acetyl-β-D-ribofuranose respectively, and these trifluoroacetates were allowed to react with some carboxylic acids to yield the corresponding 1-O-acyl-β-D-ribofuranose benzoates and acetates. These products were also prepared by direct fusion of 1-O-acetyl-β-D-ribofuranose benzoate and acetate with the carboxylic acids.抄録全体を表示PDF形式でダウンロード (585K) -
奥田 拓男, 吉田 隆志, 波多野 力, 池田 義孝, 新宮 徹朗, 井上 隆夫1986 年 34 巻 10 号 p. 4075-4082
発行日: 1986/10/25
公開日: 2008/03/31
ジャーナル フリーA highly water-soluble polyphenolic compound, geraniinic acid A, together with elaeocarpusin which is composed of equimolar geraniin and ascorbic acid, has been isolated from Geranium thubergii SIEB. et ZUCC. by means of centrifugal partition chromatography and gel chromatography, and the structure was elucidated on the basis of degradative and spectroscopic studies. One of these compounds, elaeocarpusin, was synthesized by condensation of geraniin and ascorbic acid; this route is considered to be biomimetic. The distribution of elaeocarpusin in various plants including Acer nikoense MAXIM. was also investigated.抄録全体を表示PDF形式でダウンロード (819K) -
柏田 良樹, 野中 源一郎, 西岡 五夫1986 年 34 巻 10 号 p. 4083-4091
発行日: 1986/10/25
公開日: 2008/03/31
ジャーナル フリーTogether with the known flavan-3-ols and procyanidins, a new procyanidin dimer (11) and several new trimers (14, 15, 16, 20, 22, 24 and 26) have been isolated from high-quality rhubarb ( ?? ?? ?? ). On the basis of chemical and spectroscopic data, the structures of these compounds were characterized as procyanidin B-5 3, 3'-di-O-gallate (11), procyanidin C-1 3', 3''-di-O-gallate (14), procyanidin C-1 3, 3', 3''-tri-O-gallate (15), 3-O-galloylepicatechin-(4β→6)-3-O-galloylepicatechin-(4β→8)-3-O-galloylepicatechin (20), 3-O-galloylepicatechin-(4β→6)-3-O-galloylepicatechin-(4β→6)-3-O-galloylepicatechin (22), 3-O-galloylepicatechin-(4β→6)-3-O-galloylepicatechin-(4β→8)-catechin (26), 3-O-galloylepicatechin-(4β→8)-3-O-galloylepicatechin-(4β→8)-catechin (16) and 3-O-galloylepicatechin-(4β→8)-3-O-galloylepicatechin-(4β→6)-catechin (24).抄録全体を表示PDF形式でダウンロード (893K) -
波多野 力, 服部 信, 奥田 拓男1986 年 34 巻 10 号 p. 4092-4097
発行日: 1986/10/25
公開日: 2008/03/31
ジャーナル フリーTwo new hydrolyzable tannins, named coriariins A and B, have been isolated from the leaves of Coriaria japonica A. GRAY along with 1, 2, 3-tri-O-galloyl-β-D-glucose, geraniin, tellimagrandins I (1) and II (2), and rugosins A, D and E. The structure 3 of coriariin A, which is a dimer of 2, and the structure 4 of coriariin B, a related monomer, have been established on the basis of spectroscopic and chemical evidence.抄録全体を表示PDF形式でダウンロード (645K) -
江川 宏, 宮本 皓之, 松本 純一1986 年 34 巻 10 号 p. 4098-4102
発行日: 1986/10/25
公開日: 2008/03/31
ジャーナル フリーA new method for the synthesis of 7H-pyrido[1, 2, 3-de][1, 4]benzoxazine derivatives was developed. The method is characterized by the intramolecular cyclization of 1-(1-hydroxyprop-2-yl)-8-fluoro-4-quinolones which are prepared in three or four steps from ethyl 2, 3, 4, 5-tetrafluoro-benzoylacetate. As an application of this method, ofloxacin, an antibacterial agent, was synthesized.抄録全体を表示PDF形式でダウンロード (578K) -
川添 豊, 二宮 眞一, 安達 孝浩, 幸田 光復1986 年 34 巻 10 号 p. 4103-4108
発行日: 1986/10/25
公開日: 2008/03/31
ジャーナル フリーThe chemoselectivities of 24 acylating and carbamoylating agents were evaluated in terms of the relative rate of aniline acylation versus the rate of hydrolysis in dioxane-phosphate buffer (pH 6). The chemoselectivity constant was defined as the logarithm of N[H2O]/(1-N)[aniline], where N is the molar fraction of the acylating agent consumed for the acylation of aniline, hence (1-N) is that for the hydrolysis. From these constants, the relative rates of nucleophilic attack of these acylating agents on aniline and water are estimated to range from 2 to 540000. These constants are linearly correlated with the substrate constants defined by Swain and Scott. Some structure-chemoselectivity relations are discussed.抄録全体を表示PDF形式でダウンロード (592K) -
染井 正徳1986 年 34 巻 10 号 p. 4109-4115
発行日: 1986/10/25
公開日: 2008/03/31
ジャーナル フリーTrivalent titanium ion can reduce arylaldehydes, and the reaction is controllable by selecting the pH of the reaction medium. Utilizing this new finding, 6-indolecarbaldehyde and 6-indolemethanol were convenienthy produced by the modified Leimgruber-Batcho method with titanium(III) chloride as the reducing agent. Syntheses of a natural alkaloid, (E)-6-(3-methylbuta-1, 3-dienyl)indole, and some new 6-substituted 1-hydroxyindoles are also reported.抄録全体を表示PDF形式でダウンロード (796K) -
染井 正徳, 斉田 義弘, 香村 尚子1986 年 34 巻 10 号 p. 4116-4125
発行日: 1986/10/25
公開日: 2008/03/31
ジャーナル フリーThe nature of a substituent on the pyrrole ring of 3-indolecarbaldehyde plays a significant role in governing the regioselectivity of metalation. To confirm the structures of the products, varios indoles carrying a carbon side chain at the 4-, 5-, 6-, or 7-position were prepared by other methods.Synthesis of 5-substituted 1-hydroxyindoles is also described.抄録全体を表示PDF形式でダウンロード (1129K) -
田中 俊樹, 藤野 憲一, 玉造 滋, 池原 森男1986 年 34 巻 10 号 p. 4126-4132
発行日: 1986/10/25
公開日: 2008/03/31
ジャーナル フリーFour ribonucleoside phosphoramidites bearing 5'-O-dimethoxytrityl and 2'-O-tetrahydrofuranyl groups were synthesized with the use of bis(diisopropylamino)-methoxyphosphine in yields of 68-92%. By the same procedure, the phosphoramidite derivatives of dimers were also prepared for block condensation.We measured the time course of the condensation reaction of ribonucleoside phosphoramidite and nucleoside linked to long-chain alkylamine-controlled pore glass (LCA-CPG) resin. It took 30 min for complete coupling if the nucleoside phosphoramidite was activated with 1-H-tetrazole. However, when 5-p-nitrophenyltetrazole was used for the activation, the condensation reaction was complete within 5 min. The behavior of the block condensation reaction using dimers was similar to that of monomers in the case of 5-p-nitrophenyltetrazole activation.We synthasized oligoribonucleotides UUUU, CUCUCUU and GGCGCGCC in yields of 51, 33 and 3%, respectively, by the phosphite-triester approach by means of either stepwise or block condensation on the LCA-CPG resin.抄録全体を表示PDF形式でダウンロード (765K) -
清水 訓子, 友田 正司, 足立 恵1986 年 34 巻 10 号 p. 4133-4138
発行日: 1986/10/25
公開日: 2008/03/31
ジャーナル フリーA representative mucilage, named Hibiscus-mucilage SL, was isolated from the leaves of Hibiscus syriacus L. It was homogeneous on electrophoresis and gel chromatography. Its intrinsic viscosity value in aqueous solution was 26.5. It was mainly composed of acidic polysaccharide, and its molecular weight was estimated to be about 2000000. The polysaccharide is composed of L-rhamnose : D-galactose : D-galacturonic acid : D-glucuronic acid in the molar ratio of 8.0 : 1.1 : 8.0 : 4.0. Methylation analysis of both the mucilage and the carboxyl-reduced derivative, and partial hydrolysis studies enabled elucidation of the structural features.抄録全体を表示PDF形式でダウンロード (697K) -
佐用 博照, 初村 広美, 道田 隆1986 年 34 巻 10 号 p. 4139-4143
発行日: 1986/10/25
公開日: 2008/03/31
ジャーナル フリーThe paramagnetic species formed by anodic oxidation of N-(o-nitrophenylthio)-1, 2, 3, 4-tetrahydroquinoline (3) in acetonitrile has been identified as the radical cation of 1, 1', 2, 2', 3, 3', 4, 4'-octahydro-1, 1'-di-(o-nitrophenylthio)-6, 6'-biquinoline by isolating the radical cation perchlorate. The perchlorate separated out from the electrolyzed solution and its structure was confirmed by converting it to 1, 1', 2, 2', 3, 3', 4, 4'-octahydro-6, 6'-biquinoline. Anodic oxidation of N-(o-nitrophenylthio)-1, 2, 3, 4-tetrahydroisoquinoline (4) in methanol gave an almost quantitative yield of 3, 4-dihydroisoquinoline (7) and a 56% yield of methyl 2-nitrobenzenesulfenate (9). In acetonitrile, electrolysis of 4 gave a 33% yield of 7 and no 9. These results were interpreted in terms of a much faster rate of deprotonation of the sulfenamide radical cation in methanol than in acetonitrile.抄録全体を表示PDF形式でダウンロード (522K) -
内藤 猛章, 宮田 興子, 多田 幸子, 西口 嘉乃, 木口 敏子, 二宮 一弥1986 年 34 巻 10 号 p. 4144-4149
発行日: 1986/10/25
公開日: 2008/03/31
ジャーナル フリーPhotocyclization of two enamides (2a and 2b) has provided a new entry for the construction of three yohimbans, yohimban (5a), epiyohimban (5b), and alloyohimban (5c), which are basic structures of yohimbine- and reserpine-type alkaloids.抄録全体を表示PDF形式でダウンロード (740K) -
大野 左千雄, 水越 清史, 小松 修, 久納 保夫, 中村 芳樹, 加藤 栄一, 長坂 光昭1986 年 34 巻 10 号 p. 4150-4165
発行日: 1986/10/25
公開日: 2008/03/31
ジャーナル フリーA series of 2-amino-7, 8-dihydro-4-piperazinyl- and 4-amino-7, 8-dihydro-2-piperazinyl-6H-thiopyrano[3, 2-d]pyrimidines and related compounds were synthesized and evaluated for hypoglycemic activity. Several compounds exhibited excellent activity, and 7, 8-dihydro-2-(4-methyl-piperazinyl)-4-(1-pyrrolidinyl)- (8c, dimaleate : MTP-1307) and 2-amino-7, 8-dihydro-4-piperazinyl-6H-thiopyrano[3, 2-d]pyrimidine (18a, dimaleate : MTP-1403) were selected for further investigation.Oral administration of 8c and 18a at 50 mg/kg markedly improved oral glucose tolerance in ob/ob mice. In this test, buformin also showed activity, whereas tolbutamide produced no significant improvement.抄録全体を表示PDF形式でダウンロード (1406K) -
宮原 一元, 川崎 敏男, 金城 順英, 下川 隆志, 山原 條二, 山崎 政城, 原野 一誠, 野原 稔弘1986 年 34 巻 10 号 p. 4166-4169
発行日: 1986/10/25
公開日: 2008/03/31
ジャーナル フリーThe chemical structure of caesalpin J (1) isolated from Sappan Lignum, the dried heartwood of Caesalpinia sappan L., was established by an X-ray crystallographic study of its triacetate.抄録全体を表示PDF形式でダウンロード (431K) -
瀬戸 衛, 宮瀬 敏男, 福島 清吾1986 年 34 巻 10 号 p. 4170-4176
発行日: 1986/10/25
公開日: 2008/03/31
ジャーナル フリーThree new sesquiterpene glycosides, ixerin U (III), ixerin V (IV), and ixerin W (XI), in addition to eight known sesquiterpenes, have been isolated from Ixeris dentata NAKAI. The structures of the new compounds were determined 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 (662K) -
細田 宏, 高崎 渉, 大江 知行, 塚本 玲子, 南原 利夫1986 年 34 巻 10 号 p. 4177-4182
発行日: 1986/10/25
公開日: 2008/03/31
ジャーナル フリーSix chromogenic substrates for horseradish peroxidase (HRP) as an enzyme label were compared with regard to the sensitivity obtainable with a testosterone enzyme immunoassay system. The chromogens tested were 2, 2'-azinobis(3-ethylbenzothiazoline-6-sulfonic acid)(ABTS), o-phenylenediamine (OPD), 5-aminosalicylic acid (5-AS), 3-amino-9-ethylcarbazole (AEC), 3, 3', 5, 5'-tetramethylbenzidine (TMB) and 3-methyl-2-benzothiazolinone hydrazone (MBTH); for comparison, a fluorimetric assay using 3-(p-hydroxyphenyl)propionic acid was also carried out. An HRP-labeled antigen was prepared by the N-succinimidyl ester method. The bound and free enzyme-labeled antigens were separated by a double antibody method. A dose-response curve with a satisfactory sensitivity was obtained in each system by the use of a minimum amount of the HRP label at an appropriate dilution of anti-testosterone antiserum (Ka=2×1010M-1). The amounts of testosterone needed to displace 50% of the bound label ranged from 9 to 150 pg. The sensitivity decreases in the order : TMB>OPD>ABTS>5-AS>MBTH>AEC. The assay using the non-mutagenic substrate, TMB, gave a high sensitivity, comparable to that of the fluorimetric method.抄録全体を表示PDF形式でダウンロード (618K) -
谷本 剛, 福田 秀男, 山羽 力, 田中 千秋1986 年 34 巻 10 号 p. 4183-4189
発行日: 1986/10/25
公開日: 2008/03/31
ジャーナル フリーThe reaction and inhibition kinetics of rabbit lens aldose reductase were investigated. The kinetic reaction mechanism of the enzyme is compatible with an ordered Bi Bi reaction mechanism in which reduced nicotinamide adenine dinucleotide phosphate (NADPH) binds first to the enzyme, before glyceraldehyde, and nicotinamide adenine dinucleotide phosphate (NADP+) is released last. The Michaelis constants for NADPH and glyceraldehyde were 1.7×10-5 and 8.9×10-5M, respectively, and the dissociation constant of NADPH was 7.5×10-6M. The inhibition constant for NADP+ as a product was 1.5×10-5M. Benzyl 4-isopropyl-5-phenyl-2-oxazolecarbamate (4-isopropyl-BPOC), a potent aldose reductase inhibitor, exhibited a linear un-competitive inhibition with respect to NADPH, and a linear non-competitive inhibition with respect to glyceraldehyde. It was suggested that 4-isopropyl-BPOC binds to the enzyme-NADPH binary complex but not to the free enzyme. The inhibition constants of the inhibitor for NADPH and glyceraldehyde were 4.3×10-7 and 3.6×10-7M, respectively. The inhibitory effect of 4-isopropyl-BPOC on aldose reductase was reduced when the enzyme was treated with pyridoxal 5-phosphate. From this fact, it may be speculated that 4-isopropyl-BPOC interacts with a lysine residue in the enzyme molecule.抄録全体を表示PDF形式でダウンロード (697K) -
三浦 一伸, 角地 淳二, 遠藤 恵理子, 上田 亨, 小林 邦彦, 中尾 ますみ, 石本 真1986 年 34 巻 10 号 p. 4190-4194
発行日: 1986/10/25
公開日: 2008/03/31
ジャーナル フリーThe 5S ribosomal ribonucleic acid (5S rRNA) isolated from Desulfovibrio vulgaris MK was sequenced by three different methods. A comparison of D. vulgaris 5S rRNA and 5S rRNAs from other microorganisms in terms of the primary and secondary structures showed that D. vulgaris 5S rRNA possessed higher homology with Bacillus 5S rRNAs than with other prokaryotic 5S rRNAs examined. This suggests that D. vulgaris is phylogenically related to gram-positive bacteria, such as Bacillus species.抄録全体を表示PDF形式でダウンロード (954K) -
与那覇 政憲, 丹保 好子1986 年 34 巻 10 号 p. 4195-4201
発行日: 1986/10/25
公開日: 2008/03/31
ジャーナル フリーThe effect of bromosulfophthalein (BSP), an inhibitor of cytosolic glutathione (GSH) S-transferases, on GSH-dependent protection against lipid peroxidation in rat liver microsomes was studied. Microsomal lipid peroxidation induced by ferrous-reduced incotinamide adenine dinucleotide phosphate (NADPH-Fe2+) or ascorbate was prevented by GSH, and addition of BSP abolished the protective effect of GSH in both peroxidation systems. The effect of BSP seemed to occur at concentrations which inhibited the activity of GSH S-transferase in microsomes.The liberation of free fatty acid hydroperoxides from microsomes during lipid peroxidation occurred at pH 7.5-8.0.The rate of NADPH oxidation in the system containing peroxidized microsomes, NADPH, GSH, and GSH reductase was significantly higher than that in the system containing normal microsomes, and was inhibited dramatically by BSP and moderately by phospholipase A2 inhibitors.The above findings suggest that microsomal GSH S-transferase may be responsible for GSH-dependent protection against peroxidation, probably via radical scavenging and the cooperative action of microsomal phospholipase A2 and GSH peroxidase activity, which is associated with GSH S-transferase.抄録全体を表示PDF形式でダウンロード (777K) -
坂元 弘子, 長田 いづみ, 小池 まりも, 入江 昌親1986 年 34 巻 10 号 p. 4202-4206
発行日: 1986/10/25
公開日: 2008/03/31
ジャーナル フリーIn order to establish the contribution of Tyr 411 of human serum album in (HSA) to specific drug binding, the effect to drug binding on the fluorescence spectrum of HSA in which Tyr 411 was modified with p-nitrophenyl anthranilate (ANT-HSA) was studied by using various drugs (diazepam, chlordiazepoxide, fluenamic acid, indomethacin, azapropazone, phenylbutazone, warfarin, salcylic acid, ibuprofen, L-tryptophan, tolbutamide and sulfadimethoxine). Among these durugs, indomethacin and flufenamic acid strongly quenched the fluorescence of the anthraniloyl group of ANT-HSA at a molar ratio of 1.0, indicating that these drugs bind near the Tyr 411 residue.抄録全体を表示PDF形式でダウンロード (554K) -
植木 寛, 元島 愛一郎, 世良 美佐紀, 十時 しんじ, 船越 崇行, 庄司 省三, 久保田 幸穂1986 年 34 巻 10 号 p. 4207-4214
発行日: 1986/10/25
公開日: 2008/03/31
ジャーナル フリーThe binding of an N-succinyl-L-trialanine p-nitroanilide-hydrolyzing protease (STA-protease) purified from pronase to equine α2-macroglobulin (α2M) was investigated in comparison with that of trypsin. The α2M subunits (about 90000 daltons), which were electrophoretically detected in the reaction mixture of α2M and trypsin, were undetectable in that of α2M and STA-protease. The binding molar ratios of enzyme to α2M were estimated from the inhibition curves of caseinolytic activity be 1.5 : 1 for native and acetylated STA-protease and 2 : 1 for native and acetylated trypsin. The finding of greater incorporation of monodansylcadaverine into α2M reacted with acetylated enzymes than into that reacted with the native enzymes suggests that free amino groups in the enzymes are involved at least partly in the formation of the α2M-proteinase complexes. The numbers of thiol groups generated in α2M bound to STA-protease and in α2M bound to trypsin were both estimated to be approximately 4 mol per mol of α2M by the use of thiol-directed fluorescent probes, though there were slight differences in the microenvironments of thiol groups generated in the two α2M-proteinase complexes. The values of Kcat/Km were one-half (α2M-STA-protease complex) and one-sixth (α2M-trypsin complex) of those of the uninhibited enzymes. These results suggest that STA-protease binds to α2M both covalently and noncovalently, as does trypsin, and its hydrolytic activities towards casein and low-molecular-weight substrates are inhibited to various extents.抄録全体を表示PDF形式でダウンロード (838K) -
城野 久美子, 高山 保, 久野 光造, 東出 栄治1986 年 34 巻 10 号 p. 4215-4224
発行日: 1986/10/25
公開日: 2008/03/31
ジャーナル フリーWe investigated the effect of chain length on the bactericidal activity of benzalkonium chloride during a short contact time by counting survivors. The C8 and C10homologues had very weak bactericidal activity. The bactericidal concentrations of the C12 and C14 homologues were 6-400μg/ml at 10 min of contact at 25°C against 15 strains of test bacteria. The C16 and C18homologues showed variable bactericidal activity towards the 15 strains tested.As the carbon chain was lengthened, the killing rate decreased and inhibition of the bactericidal activity by organic materials increased. The bactericidal concentrations of the C12 homologue at 1 min of contact at 25°C were 5000μg/ml in a suspension of 2.5% dried yeast, and 2500μg/ml in a 10% solution of human serum. Those of the C16 homologue were more than 10000μg/ml in both cases.We assayed unbound benzalkonium chloride in solutions of bovine serum albumin by high-performance liquid chromatography and found that the bactericidal activity in a solution of bovine serum albumin arose from it.These results show that from a practical point of view, C12-benzalkonium chloride is the most effective component of the homologues of benzalkonium chloride.抄録全体を表示PDF形式でダウンロード (868K) -
三輪 昌敬, / 石塚 秀夫, HIDEO ISHITSUKA1986 年 34 巻 10 号 p. 4225-4232
発行日: 1986/10/25
公開日: 2008/03/31
ジャーナル フリーThe antitumor agent 5'-deoxy-5-fluorouridine (5'-dFUrd) is a prodrug from which 5-fluorouracil (5-FUra) is generated mainly by uridine phosphorylase in mice and by thymidine phosphorylase in human tumors. In the present study varios derivatives related to 5'-dFUrd were examined to establish the relationship between their susceptibilities to these enzymes, and their in vitro antitumor activities against both human and murine tumor cells. These studies divided the compounds into four distinct groups. 1) Compounds (including 5'-dFUrd) which were phosphorolyzed to 5-FUra by extracts from both human tumors and murine sarcoma 180; these compounds inhibited the growth of both murine (sarcoma 180 and B16 melanoma) and human (HeLa and G361 melanoma) cells. 2) Compounds which were phosphorolyzed only by the extract from the murine tumor; these compounds inhibited the growth of only the murine tumor cells. 3)Compounds phosphorolyzed only by the human tumor extracts; these compounds showed activity against the tumor cells of both species, although the relative activity against the human tumor cells appeared to be higher than that of group 1 compounds. 4) Compounds which were not phosphorolyzed by the extracts from the human or murine tumors; these compounds showed no antitumor activity. These results suggest that phosphorolysis of the 5'-dFUrd analogs is essential for antitumor activity, and that the metabolism of pyrimidine nucleosides is different between human and mouse tumors. Future approaches towards the design of prodrugs of 5-FUra and 5'-dFUrd should be aimed at compounds which generate 5-FUra in human tumor cells, or which are substrates for the human enzyme.抄録全体を表示PDF形式でダウンロード (786K) -
横澤 隆子, 宮川 修治, 大浦 彦吉, 金子 光, 西岡 五夫1986 年 34 巻 10 号 p. 4233-4237
発行日: 1986/10/25
公開日: 2008/03/31
ジャーナル フリーAlthough rate fed on a high-protein diet of 70% casein showed hyperazotemia, administration of the extract from Rhei Rhizoma induced decreases of blood urea nitrogen, ammonia nitrogen in the portal vein, urea concentration in hepatic tissue, and Gln, Lys, Thr, Ala, Gly, Ser, Glu, Pro, Arg, Tyr, Cit, Asp, etc. in serum, while significant increases of Glu and Asp in hepatic tissue were observed. The modification of the nitrogen-processing mechanism by rhubarb extract is discussed on the basis of the present results.抄録全体を表示PDF形式でダウンロード (604K) -
浅野 剛資, 奥村 孝夫, 平野 和行, 足立 哲夫, 杉浦 衛1986 年 34 巻 10 号 p. 4238-4243
発行日: 1986/10/25
公開日: 2008/03/31
ジャーナル フリーAn enzyme immunoassay for an anti-ulcer agent, (-)-cis-2, 3-dihydro-3-(4-methylpiperazinyl-metyl)2-phenyl-1, 5-benzothiazepin-4(5H)-one hydrochloride (BTM-1086) was established. It was based on the double antibody solid phase procedure. The antisera to BTM-1086 were raised in rabbits by immunization with BTM-1086-ovalbumin conjugate. The formation of sulfoxide and the lack of a methyl group in the thiazepine ring and the piperazine ring, respectively, of the BTM-1086 skeleton markedly decreased the binding affinity for the antibody.Horseradish peroxidase was conjugated with hydrazinomethyl-BTM-1086 by the use of glutaraldehyde. The first and second immuno reactions require 20 min and 2.5h, respectively. The assay allows determination of 2.5-100pg of BTM-1086. This enzyme immunoassay has high sensitivity, and the results are reproducible. The time course of serum BTM-1086 level was also examined after a single intravenous administration in rats.抄録全体を表示PDF形式でダウンロード (586K) -
佐藤 恭史, 際田 弘志, 加藤 百合子1986 年 34 巻 10 号 p. 4244-4252
発行日: 1986/10/25
公開日: 2008/03/31
ジャーナル フリーThe blood concentration and urinary excretion after intravenous injection of liposomes containing 3H-inulin at three dose levels were examined in rats. A pharmacokinetic model for the dose dependency is postulated based on the results. The effects of vesicle size were also examined and the biological disposition was simulated. Factors affecting the liposomal disposition are discussed.Dose dependency of the disposition was observed at three dose levels (1.8, 14.9 and 70.3μmol total lipids/rat) of liposomes having a mean diameter of 0.22μm. The results suggest the existence of saturable processes in the uptake of liposomes by the reticuloendothelial system (RES) and leakage of inulin from liposomes, and a first-order rate process in the release of inulin from the cell after degradation of liposomes taken up by the RES. However, simulation of the data obtained after high-dose administration was unsuccessful with this model, the blood clearance of liposomes being faster than calculated. It is suggested that first-order processes may operate in parallel with the saturable processes of uptake and leakage.The effects of the size of liposomes (mean diameter : 0.15, 0.22 and 0.43μm) on the disposition were also examined. The patterns of the blood levels and urinary excretion of small liposomes and large liposomes were very similar to those of the high-dose and low-dose experiments, respectively, in spite of the very similar dose levels of total lipids administered.Simulation suggested that the dose expressed in terms of the number of vesicles was suitable for evaluation of the liposomal disposition. The results indicate that the size and number of liposomes are important variables affecting the disposition of liposomes and they should be controlled strictly in liposomes for in vivo use.抄録全体を表示PDF形式でダウンロード (824K) -
際田 弘志, 佐藤 純子, 山田 俊寿, 加藤 百合子1986 年 34 巻 10 号 p. 4253-4258
発行日: 1986/10/25
公開日: 2008/03/31
ジャーナル フリーLiposomes containing ultrafine magnetite were prepared and their transport characteristics in a magnetic field were examined in vitro and in vivo. About 15μg of magnetite (Fe3O4) could be entrapped in the liposomes per μmol of lipid without impairing the liposomal encapsulation capacity for the aqueous marker (3H-inulin). In in vitro experiments, when 0.1 ml of liposome suspension (0.86μmol of lipids and 13.3μg of magnetite) was applied to a glass capillary at a flow rate of the medium of 0.17 ml/min, about 35% of the liposomes was found in the region of the applied magnetic field (4000 G).It became apparent that the ability of the magnetic field to hold the liposomes was influenced by the flow rate of the medium and the magnitude of the magnetic field. The viscosity of the medium and diameter of the capillary where the magnet is applied for fixation of the liposomes may also affect the holding capacity.In vivo experiments were carried out with rats having Yoshida sarcoma implanted in a foot pad. The liposomes were injected from the branch of the femoral artery without impairing normal blood flow in the tumor tissue. A very small amount of the liposomes, but significantly more than the control, was trapped at the tumor tissue.The trapped amount of liposomes in the present expriments appeared to be insufficient for practical therapy, but a more powerful magnet may give better results.抄録全体を表示PDF形式でダウンロード (698K) -
山口 俊和, 老田 哲也, 池田 知左登, 関根 豊1986 年 34 巻 10 号 p. 4259-4264
発行日: 1986/10/25
公開日: 2008/03/31
ジャーナル フリーThe stable micellar complex formation between nadolol and sodium cholate was studied. The proton nuclear magnetic resonance spectroscopic study showed that the signals of protons in the hydrophobic site of cholic acid, i.e., the methine signals of C-7 and C-12, and the methyl signals of C-18 and C-19. exhibited rather larger shifts than those of the other protons. The longitudinal relaxation times of the aromatic ring protons (C-4, C-6, C-7 and C-8) of nadolol were shortened by about 10% in the presence of sodium cholate, indicating that the aromatic ring protons were more immobilized upon complex formation. These results suggest that the hydrophobic protons of sodium cholate and nadolol interact with each other, and complex formation with the hydrophobic protons inside and the hydrohilic protons outside may occur in aqueous solution. The intestinal absorption of four nadolol derivatives was examined by the in situ ligated loop method in rat jejunum in the presence of sodium cholate. The absorption of the trans-2, 3-diol isomer was inhibited as effectively as that of nadolol. The absorption of the 2-and 3-monohydroxy derivatives and cis-2, 3-dimethoxy derivative was inhibited by sodium cholate at 1 h after dosing, but no inhibition was observed at 4 h. This absorption behavior of nadolol derivatives was well correlated with the apparent dissociation constants of their micellar complexes with sodium cholate. It is concluded that the stability of the complexes of β-adrenergic blocking agents with sodium cholate depends upon the steric features of both hydrophobic and hydrophilic parts of the drug molecules. The hydrophilic cis-2, 3-diol moiety of nadolol plays an important role in stabilizing the micellar complex with sodium cholate.抄録全体を表示PDF形式でダウンロード (675K) -
佐々木 均, 中村 純三, 小西 良士, 柴崎 寿一郎1986 年 34 巻 10 号 p. 4265-4272
発行日: 1986/10/25
公開日: 2008/03/31
ジャーナル フリーThe absorption characteristics of three anticancer antimetabolites, 5-fluorouracil (5-FU), ftorafur and 6-mercaptopurine (6-MP), were investigated by in vitro and in situ absorption techniques in rats. Absorption of a nucleic acid, uracil, was also investigated. In the in situ experiment, the disappearance ratios of uracil, 5-FU and 6-MP from the lumen showed a dependency on initial concentration, although ftorafur was absorbed at a constant rate regardless of the initial concentration. At low concentrations, Michaelis-Menten type processes were involved in the disappearance of uracil, 5-FU and 6-MP as judged from reciprocal plots. No metabolite of uracil, 5-FU of ftorafur was detected in the experiments. Most of the 6-MP that was lost from the lumen appeared as its metabolite, 6-thiouric acid, in the lumen. The in vitro data supported the results of the in situ experiment. In particular, uracil and 5-FU showed the ability to permeate at low concentrations against a concentration gradient. A small serosal transfer of 6-MP and the selective appearance of 6-thiouric acid on the mucosal side were confirmed. Metabolic inhibitors, 2, 4-dinitrophenol and ouabain, strongly depressed the disappearance and transfer of uracil and 5-FU, but not ftorafur. The absorption and metabolism of 6-MP were affected by 2, 4-dinitrophenol, but not ouabain.抄録全体を表示PDF形式でダウンロード (781K) -
中島 毅, 名取 和一, 広橋 敏之, 青野 俊二1986 年 34 巻 10 号 p. 4273-4279
発行日: 1986/10/25
公開日: 2008/03/31
ジャーナル フリーThe inhibitory effect of melinamide, N-(α-methylbenzyl)-linoleamide, on cholesterol solubility in a mixed micellar solution of sodium taurocholate was investigated in vitro by the solubility method. At pH 7.4, melinamide decreased the amount of cholesterol by 30-40% without influencing the concentration of oleic acid in bile salt-rich micelles with a molar ratio of more than 10 : 10 : 5 of bile salt : oleic acid : monolein, while it had no effect on oleic acid-monolein-rich micelles. Further, the effect of melinamide was independent of the pH of the medium. Melinamide seems to exhibit its effect as a result of releasing cholesterol from the micellar phase. On the other hand, it is assumed that neomycin reduces the amount of cholesterol by destroying micellar structure, as it was shown to completely eliminate oleic acid as well as cholesterol from micellar solution.抄録全体を表示PDF形式でダウンロード (636K) -
吉岡 澄江, 阿曽 幸男, 柴崎 利雄, 内山 充1986 年 34 巻 10 号 p. 4280-4286
発行日: 1986/10/25
公開日: 2008/03/31
ジャーナル フリーThe stability of various dosage forms of pilocarpine ophthalmic formulations available on the Japanese market was studied. For opthalmic solutions, hydrolysis was found to be a main route of degradation, and the stability depended largely on the pH and the concentration of general bases. Nonlinear regression analysis allowed estimation of the rate constants of degradation, including reversible hydrolysis to pilocarpic acid and reversible epimerization to isopilocarpine. It was also found that an ointment formulation was stable, while a conjunctival insert preparation was susceptible to epimerization and hydrolysis. The factors affecting the stability of pilocarpine preparations are discussed.抄録全体を表示PDF形式でダウンロード (600K) -
今井 公江, 相本 太刀夫, 佐藤 正基, 渡辺 一弘, 木村 良平, 村田 敏郎1986 年 34 巻 10 号 p. 4287-4293
発行日: 1986/10/25
公開日: 2008/03/31
ジャーナル フリーSeveral sodium metallochlorophyllins (Me-Chl-Na), i.e., sodium copper chlorophyllin (Cu-Chl-Na), sodium cobalt chlorophyllin and sodium iron chlorophyllin, decreased the activities of aminopyrine N-demethylase and aniline hydroxylase and the content of cytochrome P-450 in liver microsomes when given intraperitoneally to rats. The lowest levels of these variables were observed 24h after dosing. Me-Chl-Na administration did not modify the substrate-induced spectral changes of cytochrome P-450. Of the kinetic parameters studied in aminopyrine N-demethylation and aniline hydroxylation, only the Vmax values were markedly decreased by Cu-Chl-Na, indicating that the enzyme inhibition was non-competitive. Me-Chl-Na also reduced cytochrome b5 and total heme contents and NADPH-cytochrome c reductase activity in microsomes. Preincubation of liver microsomes from control rats with Cu-Chl-Na did not cause any reduction in the aminopyrine-and aniline-metabolizing enzyme activities and in the cytochrome P-450 content.These findings strongly suggest that the decreases in the activities of the hepatic microsomal drug-metabolizing enzyme system caused by Me-Chl-Na are correlated with the reduction in the contents of microsomal cytochromes P-450 and b5, and are brought about by primary action(s) of Me-Chl-Na on the control mechanism of microsomal hemoprotein levels, not by direct action of Me-Chl-Na on the system.抄録全体を表示PDF形式でダウンロード (753K) -
LUCY SAI CHEONG WAN, P.P.KANNEGANTI PRASAD1986 年 34 巻 10 号 p. 4294-4300
発行日: 1986/10/25
公開日: 2008/03/31
ジャーナル フリーThe action of methylcelluloce (MC) of different viscosity on the properties of tablets was studied. The penetration of water into the tablets was retarded by the presence of MC. The disintegration time of tablets was reduced with increasing viscosity of MC and a high level of starch. This correlates with the water penetration data. Dissolution of tablets is governed to a lesser extent by water uptake into the tablets. It is more influenced by the gel formed by MC and the diffusion of drug through this layer. With higher concentration of methylcellulose the adhesiveness of MC becomes more significant in decreasing dissolution of the tablets. MC in contact with water hydrates, swells, gels and becomes adhesive. These actions are affected by starch, MC concentration and viscosity.抄録全体を表示PDF形式でダウンロード (677K) -
小木曽 太郎, 岩城 正宏, 城守 美佐, 塚脇 千穂1986 年 34 巻 10 号 p. 4301-4307
発行日: 1986/10/25
公開日: 2008/03/31
ジャーナル フリーTo clarify the relationship between hemolytic activity and membrane penetration of drugs, some tranquilizers and antihistaminics were compared with each other as regards the amount of drugs able to penetrate human erythrocyte membrane at 27 and 37°C, and the activation energy for penetration was calculated. The drugs exerting strong hemolytic action penetrated the membrane much more effectively than those with less activity. The relation between the amount (A) of drug penetrated vs. extracellular drug concentration (C) could be generally described by a linear equation : log A (10-8mol)=0.817·log C (10-4M)+b. With 8 phenothiazines, the correlation coefficient between A and the value of 1/C1 or 1/C50 (C1 is the initial concentration inducing hemolysis and C50 is the concentration inducing 50% hemolysis) was 0.916 (p<0.01) or 0.927 (p<0.01), respectively. The amount of drugs penetrated at the C50 was (0.7-4.1)×10-17mol/ghost and (1.7-10.6)×10-2mol/mol phospholipid. The drug penetration into the membrane could be approximately described by the Freundlich equation, but not the Scatchard equation. The activation energy for drug penetration was in the range from 1.07 to 6.16 kcal, and there was no clear-cut relationship between the energy and the above parameters.抄録全体を表示PDF形式でダウンロード (747K) -
砂田 久一, 大塚 昭信, 山田 誉春, 川島 嘉明1986 年 34 巻 10 号 p. 4308-4313
発行日: 1986/10/25
公開日: 2008/03/31
ジャーナル フリーThe process of Brownian flocculation of suspended particles has been simulated based on the random coalescence model for polydisperse systems by using a digital computer. The conformity between von Smoluchowski's and Muller's theories was examined. It was found that the simplifying assumption by which the concept of collision probability is introduced into the theories was adequate. Since no such assumption was necessary in the present model, the model can be applied to more complicated polydisperse systems. Moreover, this model can be used to obtain not only the total number of particles formed but also the particle size distribution at any period in the flocculation process. The results indicate that the process is governed by a layering mechanism such that the flocculation is promoted by a preferential cohesion of small particles to large aggregates.抄録全体を表示PDF形式でダウンロード (578K) -
福岡 英平, 牧田 みどり, 山村 重雄1986 年 34 巻 10 号 p. 4314-4321
発行日: 1986/10/25
公開日: 2008/03/31
ジャーナル フリーGlassy indomethacin was prepared by cooling the melt, and the glassy state was confirmed by the jump of heat capacity and the anomalous endothermic park (heat capacity maximum) in the differential scanning calorimetry (DSC) curve. The influences of the cooling rate of the melt and the heating rate of the glass formed on the glass transition temperature (Tg) were examined, and the apparent activation energy of glass transition was calculated to be 212.5kJ/mol. The relaxation process below Tg was traced in terms of the area under the anomalous endothermic park of the DSC curve and the rate of relaxation during annealing was found to reach the maximum at about 303 K. The rate of dissolution of glassy indomethacin was far greater than that of crystalline indomethacin. Although indomethacin remained as a glass for 2 years at room temperature, pulverized glassy indomethacin was found to crystallize, and the rate of crystallization was determined by the X-ray diffraction method. The degree of crystallization was determined by Hermans' method, and was found to reach a maximum of 60% after 2 months. The process of crystallization followed first-order kinetics.抄録全体を表示PDF形式でダウンロード (702K) -
坂野 俊行, 長岡 忠義, 森本 厚, 平内 三政1986 年 34 巻 10 号 p. 4322-4326
発行日: 1986/10/25
公開日: 2008/03/31
ジャーナル フリーA high-performance liquid chromatographic (HPLC) method was developed for measuring endogenous K vitamins in human and animal feces, and these vitamins in human feces were also identified by mass spectrometry (MS). K vitamins extracted from human and animal feces were purified by thin-layer chromatography (TLC) and then measured by reversed-phase HPLC with fluorometric detection. Vitamin K1 (VK1) and menaquinone (MK)-4 to MK-15 were found and their amounts were determined in human, monkey and rabbit feces. K vitamins extracted from human feces were purified succesively by column chromatography, TLC, reversed-phased HPLC and normal-phase HPLC, and then identified as VK1 and MK-4 to MK-15 by MS, confirming the validity of the HPLC method.抄録全体を表示PDF形式でダウンロード (563K) -
津田 益広, 平野 恵子, 山根 武, 根釜 務, 谷 勇, 樋口 富彦1986 年 34 巻 10 号 p. 4327-4330
発行日: 1986/10/25
公開日: 2008/03/31
ジャーナル フリーIt was shown that addition of L-malate to anaerobic mitochondria, like addition of adenosine triphosphate, caused a red shift of the absorbance maximum, and an increase in the fluorescence of ethidium. These responses of ethidium were sensitive to uncouplers and roteone. They were not inhibited by antimycin A, KCN or oligomycin.These results show that addition of L-malate to anaerobic, KCN-or antimycin A-inhibited mitochondria caused energization of the mitochondrial inner membranes. Furthermore, this energization of the membranes was reversed by succinate, malonate, and theoyltrifluoroacetone. Thus, the present results clearly show that L-malate-induced energization of anaerobic mitochondria was driven by energy derived from redox reactions at site I of phosphorylation.抄録全体を表示PDF形式でダウンロード (448K) -
樋口 富彦 /, HAGAI ROTTENBERG1986 年 34 巻 10 号 p. 4331-4334
発行日: 1986/10/25
公開日: 2008/03/31
ジャーナル フリーIsolated hepatocytes from euthyroid or hypothyroid (thyroidectomized) rats showed a 20 to 30% stimulation of respiratory activity when treated with triiodothyronine (T3). Maximal stimulation was obtained in the presence of the uncoupler carbonylcyanide m-chlorophenyl-hydrazone (CCCP) suggesting a direct effect on the respiratory chain. Physiological concentrations of T3 (10-11-10-9) induced maximal stimulation after a short incubation (75% of maximum in 3 min) and the effect persisted for over 1 h of incubation. Mitochondria, rapidly isolated from T3-treated hepatocytes, retained stimulated respiratory activity in both coupled and uncoupled states. These results are consistent with the hypothesis that the mitochondrion is a primary target for thyroid hormones, and the present system appears to be suitable for the systematic investigation of these effects.抄録全体を表示PDF形式でダウンロード (526K) -
野瀬 敦子, 工藤 忠宏1986 年 34 巻 10 号 p. 4335-4339
発行日: 1986/10/25
公開日: 2008/03/31
ジャーナル フリーThe reduction of anhydrides, lactones, esters, carboxylic acids and acyl chlorides with trialkylborane is described. Cyclic anhydrides were reduced with 4mol eq of trialkylborane at temperatures above 300°C to give diol derivatives via the lactones. Lactones, esters, carboxylic acids and acyl chlorides were reduced under similar conditions to give te corresponding alcohol derivatives.抄録全体を表示PDF形式でダウンロード (597K)