巻号一覧
94 巻, 11 号
選択された号の論文の21件中1～21を表示しています
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北澤 式文, 酒井 克美, 村崎 宏1974 年 94 巻 11 号 p. 1353-1357
発行日: 1974/11/25
公開日: 2008/05/30
ジャーナル フリーThe effect of magnesium aluminosilicate (MAS) on the absorption of aspirin was investigated with five young healthy volunteers. The volunteers were administered 1 g of the drug alone (control study) or with 300 mg (case-1 study) and/or 600 mg (case-2 study) of MAS, and the order of these studies was randomly designed. After each administration of the drug, the blood samples at a given time and the urine of up to 34 hr were collected, and the levels of the drug were determined. Because of almost the same results in the blood level and the excretion of the drug were obtained in each case of the control, the case-1 and case-2 studies, it would be possible to conclude from these data of such a balanced study that MAS did not affect the absorption of aspirin in man.抄録全体を表示PDF形式でダウンロード (694K) -
中垣 正幸, 近藤 明1974 年 94 巻 11 号 p. 1358-1367
発行日: 1974/11/25
公開日: 2008/05/30
ジャーナル フリーFollowing the previous work on the interaction between mitomycin derivatives and bovine serum albumin (BSA) at pH 7.0 and 8.0, by the membrane equiliblium method, which showed pH dependence of this interaction and association constants at pH 7.0 1.6-3.3 times larger than those at pH 8.0, effect of pH on the binding of mitomycins and BSA was examined in the pH region of 6.0 to 10.0 by the partition equilibrium method based on the distribution of mitomycins between heptanol and aqueous buffer solution. It was found that in the pH region of 6.0 to 8.0, the number of binding sites of mitomycins on a BSA molecule was about 9, as was revealed by membrane equilibrium method, and analysis of the data by the Scatchard method revealed that there existed, at least, two classes of binding sites. In the pH region of 9.0 to 10.0 the number of binding sites decreased to 4-6 with homogeneous binding sites. The apparent association constants k1 of the first binding class decreased with the increase of pH above 7.0, and linear relationship was observed between log k1 and pH. The difference in these results obtained by membrane equilibrium method and by partition equilibrium method was assumed to be due to the denaturation of BSA by heptanol.抄録全体を表示PDF形式でダウンロード (1092K) -
中西 美智夫, 後藤 一洋1974 年 94 巻 11 号 p. 1368-1376
発行日: 1974/11/25
公開日: 2008/05/30
ジャーナル フリーIn prophylactic experiments, steroidal and nonsteroidal acidic anti-inflammatory agents inhibited dose-dependently the local Shwartzman reaction, and the former also inhibited the leucocyte emigration. In therapeutic experiments, only steroidal antiinflammatory drugs were found to inhibit this reaction, when they were treated after the leucocyte accumulation. However, nonsteroidal acidic anti-inflammatory agents were found to inhibit the above reaction, when they were administered prior to leucocyte emigration. These results suggest that steroidal anti-inflammatory drugs have a membranestabilizing activity on both intact and unstable lysosomes of the emigrated leucocytes, and that nonsteroidal acidic anti-inflammatory agents have a protecting action merely on the intact lysosomes. Humoral factors such as p1asma inflammation units, erythrocyte sedimentation rate, A/G ratio, and lysocyme activity were influenced by the local Shwartzman reaction. However, it was concluded that the above inhibitory activities had no correlation with change in humoral factors.抄録全体を表示PDF形式でダウンロード (1407K) -
榊原 仁作, 伊奈 郊二, 安江 政一1974 年 94 巻 11 号 p. 1377-1383
発行日: 1974/11/25
公開日: 2008/05/30
ジャーナル フリーLyoniside, β-sitosteryl β-D-glucoside, and monotropein and its methyl ester were isolated from the benzene-insoluble portion of the methanol extract of the wood of Tripetaleia paniculata SIEB. et ZUCC. The steric structure of lyoniresinol, the aglycone of lyoniside, was determined as formula (II) from the optical rotatory dispersion (ORD) and circular dichroism curves of its various derivatives (I, III to VI). The sugar moiety of lyoniside was determined as D(+)-xylose from the ORD curve of the sugar and from the gas-liquid chromatography of its trimethylsilyl ether, and the bonding was determined as β-linkage from the nuclear magnetic resonance spectrum of completely methylated compound. The position of sugar linkage was concluded as the methylol in 3-position from the hydrolysis of the completely methylated compound, followed by oxidation of the aglycone.抄録全体を表示PDF形式でダウンロード (986K) -
田上 昇一郎, 松葉 綾子, 沢田 照子, 中野 琢, 志甫 伝逸1974 年 94 巻 11 号 p. 1384-1388
発行日: 1974/11/25
公開日: 2008/05/30
ジャーナル フリーAn acurate and rapid method has been developed for the determination of urea based on the measurement of the electric conductivity of ammonium carbonate produced from urea by urease in solution. The initial decomposition rates were followed by recording the response signal related to the change of electric conductivity as a function of time. This simple method is also applicable to samples containing NH4+ or other ions. It is well suited for routine analysis, such as determination of urea in urine and fertilizers.抄録全体を表示PDF形式でダウンロード (639K) -
丹野 慶紀, 今井 明子, 上村 和夫1974 年 94 巻 11 号 p. 1389-1392
発行日: 1974/11/25
公開日: 2008/05/30
ジャーナル フリーAn examination was made on the method for determination of the optimal melting temperature at which the mixture of main active ingredients and a base is poured into molds for preparing suppositories by the fusion method. The mixture was prepared by labeling zinc oxide with 113mIn·Fe(OH)3, and mixing it with cacao butter, and distribution of zinc oxide was determined from radioactivity. Distribution of the active ingredient in mixtures melted at 40 to 60° showed a coefficient of variation not higher than 1.0% immediately after cessation of stirring and about 2.5% 5 min later. Coefficient of variation of the active ingredient was higher 10 min after cessation of stirring and thereafter, when the melting temperature was higher. Further, the higher the melting temperature, the larger was the difference in the content of the active ingredient between the upper and bottom layer of the mixture. In the mixture melted at 40°, virtually no difference was noted in the content of the active ingredient between the upper and bottom layers even 50 min after cessation of stirring, but in the mixture melted at 60° there was about two-fold difference in the content between the two layers 30 min after cessation of stirring and about 3-fold difference 50 min later. From these data, a method was established which would permit rapid determination of the distribution of active ingredienst in a mixture of active ingredients and a base.抄録全体を表示PDF形式でダウンロード (546K) -
進藤 英世, 南部 公彦, 中島 栄一, 河合 賢司1974 年 94 巻 11 号 p. 1393-1403
発行日: 1974/11/25
公開日: 2008/05/30
ジャーナル フリーThe absorption, distribution, excretion and biotransformation of carbazilquinone [2, 5-bis(1-aziridinyl)-3-(2-carbamoyloxy-1-methoxyethyl)-6-methyl-1, 4-benzoquinone], a new antitumor agent, in mice were investigated after oral and intravenous administration of the drug labeled with 14C at the aziridinyl moiety. After intravenous and oral administration, about 50% of the dose was recovered in the urine during the first 24 hr, and about 25% and 40% in the feces, respectively. A high absorptivity of the drug from the intestine and a high participation of biliary excretion were demonstrated by in situ experiments with ligated loop of a rat small intestine and with rats cannulated at the bile duct, respectively. Whole-body autoradiography and radioassay revealed that a very high uptake of radioactivity occurs mainly in the excretory organs such as the liver, gall bladder, intestine, kidney, and urinary bladder, and a high uptake in the lung, salivary gland, and hypophysis. An appreciable uptake of radioactivity was also observed in the adrenal medulla, spleen, thymus, and bone marrow, wherein the concentration appears to increase gradually up to 3 hr after administration and retained for more than 24 hr. Carbazilquinone was found to be excreted in the urine as more than 15 kinds of metabolites, most of which are non-extractable with ethyl acetate and are thus polar metabolites. Two metabolites were identified as unchanged carbazilquinone and a compound in which one of the two aziridine rings is opened to form hydroxyethylamino group. After intravenous administration, the blood level of carbazilquinone declined rapidly with an approximate half-life of 13.5 min.抄録全体を表示PDF形式でダウンロード (1922K) -
山口 稽子, 森脇 千秋, 杉浦 衛1974 年 94 巻 11 号 p. 1404-1407
発行日: 1974/11/25
公開日: 2008/05/30
ジャーナル フリーIntestinal absorption of the semi-alkaline proteinase (SAP) from Aspergillus melleus was examined in the rat whose mesenteric vascular system was perfused in situ with Krebs-Ringer bicarbonate buffer containing 6% dextran. When the rat was given 0.25-4 mg of SAP and 125I-labeled SAP in each of the ligated jejunum, the perfusate contained non-diffusib1e 125I-binding macromolecule(s), and the amount recovered during 60 min corresponded to 0.8-1.7% of 125I-SAP administered. Immunochemical analysis of the perfusate obtained from rats given 10 mg of SAP revealed a precipitin band against the anti-SAP rabbit serum on an immunodiffusion plate. These results suggest that SAP may be transmitted into the mesenteric vascular system across the intestinal wall, retaining its immunoreactivity.抄録全体を表示PDF形式でダウンロード (697K) -
岸本 博, 上野 雅晴1974 年 94 巻 11 号 p. 1408-1413
発行日: 1974/11/25
公開日: 2008/05/30
ジャーナル フリーAerosol OT distribution between water and carbon tetrachloride was investigated at 25° and analyzed on the basis of its thermodynamic parameters in both phases. The standard chemical potential difference, △μ° (ca. 0.54kcal/mole), on transfer of the solute from water to carbon tetrachloride phase was determined by direct measurement of the solute concentration in the dilute region, where the solute is monomeric in both phases. Activity coefficient vs. concentration relationships were obtained from vapor pressure depression data up to relatively high concentration regions in both phases over c.m.c., and concentration terms of chemical potential of Aerosol OT, 2RT ln γ'm' (in water) and RT ln γ″m″ (in carbon tetrachloride), were determined. For the sake of the unified description of solute chemical potential, the relative chemical potential diagram of Aerosol OT in water and carbon tetrachloride, based on the standard chemical potential in water, was drawn from △μ°, 2RT ln γ′m′, and RT ln γ″m″. From this diagram, the actual distribution can be estimated approximately, even in the high concentration region, where the direct measurement of solute concentration is difficult.抄録全体を表示PDF形式でダウンロード (616K) -
栗原 藤三郎, 武田 秀雄, 伊藤 秀雄1974 年 94 巻 11 号 p. 1414-1418
発行日: 1974/11/25
公開日: 2008/05/30
ジャーナル フリーIn order to obtain better antibiotics than natural colistin, colistin derivatives were synthesized by replacing 6-methyloctanoic acid or 6-methylheptanoic acid in colistin with various organic acids or aromatic sulfonic acids. Twenty kinds of (2-acylamido-or -stlfonamido-4-aminobutyric acid)1'-colistin were obtainee by the condensation of organic acids with pentabenzyloxycarbonyldeacylcolistin1) by the dicyclohexylcarbodiimide method or with acyl chloride or sulfonyl chloride by the Schotten-Baumann reaction, followed by liberation of the benzyloxycarbonyl group. Among these derivatives of colistin, two of them showed antibacterial activity against gram-negative bacteria equal to that of colistin sulfate and two that showed an effect against gram-positive bacteria.抄録全体を表示PDF形式でダウンロード (614K) -
篠田 雅人, 太田 節子, 高木 良成, 赤星 三弥1974 年 94 巻 11 号 p. 1419-1424
発行日: 1974/11/25
公開日: 2008/05/30
ジャーナル フリーExaminations were made on the relationship between the chemical structure of 47 kinds of sulfur-containing compounds, both SH-type and non-SH-type and toxicity to male ddY mice, and the protective effect of their lethal dose against X-irradiation. Among the compounds tested, 22 compounds were found to prolong the survival of X-irradiated mice, but there was no definite evidence for a relation between chemical structure and survival effect, or between toxicity and survival effect. Thiourea, methylthiourea, ethylenethiourea, methylisothiourea, and ethylisothiourea were found to be radioprotectors with a low toxicity.抄録全体を表示PDF形式でダウンロード (643K) -
北條 博史, 内山 充1974 年 94 巻 11 号 p. 1425-1428
発行日: 1974/11/25
公開日: 2008/05/30
ジャーナル フリーThe structual integrity of radioactive substances in various tissues of mouse recovered after the administration of labeled baker's yeast mannan was examined by the immunological method. 1) Antiserum was prepared from rabbits immunized with the heat-killed whole cells of Saccharomyces cerevisiae. The agglutinin titer of the antiserum was in the range of 1 : 1280 to 1 : 2560 against the living cells of S. cerevisiae. 2) Upon quantitative analysis of the precipitin reaction of 3H-labeled mannan with the antiserum, 50% of the radioactivity was precipitated in the case of antibody excess and equivalence zone. 3) The radioactive substances in the reticuloendothelial tissues of the mouse after injection of 3H- or 14C-mannan had a precipitability similar to mannan for 1 week, and the activity decreased progressively, but dissapeared rapidly from the kidney.抄録全体を表示PDF形式でダウンロード (588K) -
堀 幹夫, 片岡 貞, 清水 洋, 吉村 昌治1974 年 94 巻 11 号 p. 1429-1444
発行日: 1974/11/25
公開日: 2008/05/30
ジャーナル フリーAs a fundamental experiment for the synthesis of 2-thiabulenes (10), syntheses of 2-thiaazulen-6-ones and 2-thiaazulenylium salts were attempted. For the synthesis of 2-thiaazulen-6-ones, a modified method was established for known compounds (12 and 15), and 1, 3-dihalogeno-5, 7-dimethyl-2-thiaazulen-6-ones (18 and 19) were successfully synthesized. Synthesis of 2, 5-dihalogeno-3, 4-diformylthiophenes, the starting materials for the synthesis of 1, 3-dihalogeno derivatives, by oxidation was accompanied by side reactions and their yield was generally poor. Therefore, 18 and 19 were synthesized by mercuration-halogenation of 5, 7-dimethyl-2-thiaazulen-6-one (14). For the synthesis of 2-thiaazulenylium salts, an attempt was first made to obtain 6-phenyl derivative by the application of phenyllithium to thiaazulenones (14 and 15). While 1, 2-addition product (47) was obtained from 14, 1, 2-additive (51) and 1, 4-additive (16) products were obtained from 15. Reaction of 1, 3-dibromo derivative (18) with phenyllithium resulted in halogen-metal interconversion of the bromine atom and the resultant lithio compound was yielded a compound (56) by the reaction of another molecule of 18. In the reaction of 18 with 2 moles of phenylmagnesium bromide, a normal addition product (58) was formed but the use of 11 moles resulted in the formation of an abnormal product (59) besides 58. Reduction of 18 with lithium aluminum hydride to obtain 64 ended in the liberation of bromine in 1-and 3-positions, and reduction without debromination was effected by the use of sodium borohydride. The alcohols (58 and 64) thereby obtained were isolated as their hexachloroantimonates (63 and 67) by treatment with hydrochloric acid and antimony pentachloride. 58 was also obtained as its perchlorate (60). Some discussions were made on the mechanism of the formation of 58 and 59.抄録全体を表示PDF形式でダウンロード (1742K) -
堀 幹夫, 片岡 貞, 清水 洋, 吉村 昌治1974 年 94 巻 11 号 p. 1445-1451
発行日: 1974/11/25
公開日: 2008/05/30
ジャーナル フリーReaction of 2-thiaazulen-6-ones with electrophilic reagents was examined, using 6-hydroxy-2-thiaazulenylium salts formed from the ketones with mineral acid. Nitration with mixed acid or fuming nitric acid resulted in nitration of 1- or 1- and 3-positions, except in compounds having substituents in 1, 3-positions. Bromination with equimolar amount of bromine and silver sulfate gave 1, 3-dibromo compound (18), accompanied by oxidation products (19 and 20), while only a trace of 18 was obtained and 19 was the main product by the use of 2 moles of bromine-silver sulfate. Iodination with iodinesilver sulfate failed to give iodinated product, and the compounds obtained were an oxidation product (21) and structurally unknown compound.(14). Sulfonation and chlorosulfonation also occurred in 1-position. Some discussions were made on the formation mechanism of the oxidation products (19-21).抄録全体を表示PDF形式でダウンロード (803K) -
堀 幹夫, 片岡 貞, 清水 洋, 吉村 昌治1974 年 94 巻 11 号 p. 1452-1458
発行日: 1974/11/25
公開日: 2008/05/30
ジャーナル フリーReduction of 2-thiaazulenylium salts (2, 3, 5) with lithium aluminum hydride in ether gave only 4H-cyclohepta[c]thiophenes (12, 14, 18) and not the 6H-isomer. Only 6H-cyclohepta[c]thiophene derivative (16) was obtained from 4, not having a phenyl group in 6-position. Reaction with phenylmagnesium bromide also gave 4H-cyclo-hepta[c]thiophenes (13, 15, 19) alone from 2, 3, and 5, and 6H-isomer (17) from 4. These results suggested that selectivity of this reaction was due to the formation of a bulky complex from the nucleophilic reagents, which reacted with 2-thiaazulenylium salts. Reaction of 6 with malononitrile also gave 4H-cyclohepta[c]thiophene derivative (20). 2-Phenyl-2-thiaazulenes (21-24) were synthesized by the reaction of 2-thiaazulenylium salts (1, 2, 3, 7) with phenyllithium. Various physical data of these compounds support the S-phenyl structure, rather than the corresponding 4H- or 6H-cyclohetta[c]thiophenes.抄録全体を表示PDF形式でダウンロード (706K) -
的場 勝英, 浜島 健二, 山崎 高応1974 年 94 巻 11 号 p. 1459-1467
発行日: 1974/11/25
公開日: 2008/05/30
ジャーナル フリー2-Ethoxy-3-methoxy-2-cyclohexenone (II) and 2, 3, 5-trimethoxy-2-cyclohexenone (III) were prepared from pyrogallol in a satisfactory yield. II was reduced with lithium aluminium hydride to 2-ethoxy-3-methoxy-2-cyclohexenol (XXV), which was not so stable. III was reduced under the same condition to 2, 5-dimethoxy-2-cyclohexenol (XXIX) and 2, 3, 5-trimethoxy-2-cyclohexenol (XXX). XXX was relatively stable but was not so stable as the reduced product of acutumine (I).抄録全体を表示PDF形式でダウンロード (1013K) -
安江 政一, 榊原 仁作, 貝谷 トヨ1974 年 94 巻 11 号 p. 1468-1474
発行日: 1974/11/25
公開日: 2008/05/30
ジャーナル フリーMethyl 3-aza-2-oxolup-20(29)-en-28-oate (VII) was synthesized from betulinic acid (Chart 1). When VII was boiled with TsCl in pyridine, it did not give seco-nitrile (VI) and the starting material was recovered. Seven N-substituted oleanolamides were synthesized and they were treated with LiAlH4. Only tertiary amides (IXe, IXf, IXg) were reduced to give the corresponding amines (Xe, Xf, Xg). Then two derivatives of oleanolic acid which contain nitrogens at both carbon-28 and A-ring were synthesized ; N-(3b-aza-A-homoolean-12-en-28-yl)morpholine (XVI) and N-(furazano[2, 3-c]olean-12-en-28-oyl)morpholine(XIX).抄録全体を表示PDF形式でダウンロード (867K) -
工藤 忠宏, 野瀬 敦子1974 年 94 巻 11 号 p. 1475-1483
発行日: 1974/11/25
公開日: 2008/05/30
ジャーナル フリーIn order to clarify the reactivity of enamines with diborane and sodium borohydride, exo-enamines and endo-enamines were examined. From these experiments, it was found that, in the reaction of exo-enamines with diborane, the hydroboration proceeds in aprotic solvents, except for a few lower aldehyde enamines, but the reduction proceeds in protic solvents, although in the reaction of endo-enamines with diborane, the reduction proceeds in either protic or aprotic solvents. Reduction of these enamines with sodium borohydride proceeds in protic solvents.抄録全体を表示PDF形式でダウンロード (832K) -
吉沢 逸雄, 渡部 喜久子, 羽賀 健一, 木村 道也1974 年 94 巻 11 号 p. 1484-1488
発行日: 1974/11/25
公開日: 2008/05/30
ジャーナル フリーThe tritium compound, 2-hydroxyestra-1, 3, 5(10)-trien-17β-ol[6, 7-3H], was prepared by catalytic hydrogenation of 2-methoxyestra-1, 3, 5(10), 6-tetaen-17β-ol acetate (IV) with tritium gas and palladium on charcoal in dioxane, followed by deacetylation and demethylation. Radioactivity and purity measurements of the stored highly labeled compound are described. About 99% of the isotopes in the labeled compound (VII) was found to be located at C6-and C7-positions of the molecule.抄録全体を表示PDF形式でダウンロード (737K) -
亀谷 哲治, 青山 豊彦1974 年 94 巻 11 号 p. 1489-1490
発行日: 1974/11/25
公開日: 2008/05/30
ジャーナル フリーIn order to obtain an effective analgetic, 1-substituted 3-(3-hydroxyphenyl)-3-phenyl-piperidine (3) was synthesized through several steps from 1-(3-methoxyphenyl)phenyl-acetonitrile (4), readily available by benzyne reaction of o-chloroanisole with phenyl-acetonitrile.抄録全体を表示PDF形式でダウンロード (364K) -
栗原 藤三郎, 武田 秀雄, 伊藤 秀雄, 佐藤 弘幸, 清水 昌寿, 黒沢 秋雄1974 年 94 巻 11 号 p. 1491-1494
発行日: 1974/11/25
公開日: 2008/05/30
ジャーナル フリーIn order to investigate the deacylation of colistin or colistin derivatives with the free amino group protected, these compounds were treated with various acids. De-acylcolistin was obtained by reaction of colistin with 6N formic acid for 7 hr at 70° or with 1N oxalic acid for 9 hr at 70°. Pentabenzyloxycarbonylcolistin gave its deacylated compound when treated with 11N formic acid for 4 hr at 70° or with 1N oxalic acid for 4 hr at 50°. Deacylation of penta-tert-butoxycarbonylcolistin was carried out by its reaction with 11N formic acid for 4 hr at 70° or with 1N oxalic acid for 4 hr at 50°.抄録全体を表示PDF形式でダウンロード (553K)
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