巻号一覧
103 巻, 6 号
選択された号の論文の16件中1～16を表示しています
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富取 恵美子, 岡本 敏彦, 井戸 達雄1983 年 103 巻 6 号 p. 601-606
発行日: 1983/06/25
公開日: 2008/05/30
ジャーナル フリーReaction of 6-nitroquinoline (1) with potassium cyanide in methanol was analyzed. The major products were 5-cyano-6-methoxyquinoline (2) and 1-aminoisoxazolo[4, 3-f]-quinoline (3). An acidic product, 4-oxo-3, 4-dihydro-1, 2, 3-triazino[4, 5-f]quinoline (8) was isolated. The structure of 8 was confirmed by synthesis from 6-aminoquinoline-5-carboxamide. Compound 8 was confirmed by synthesis from 6-aminoquinoline-5-carboxamide. Compound 8 could be prepared from 3 and hydroxylamine in alkaline solution : this suggested that NO- was eliminated from the primary intermediate, 5-cyano-6-nitrosoquinoline, by nucleophilic attack of methoxide anion perticipates. This also explains the formation of the major product, 2. The formation of the isoxazole derivative (3) is interpreted by the nucleophilic perticipation of cyanide anion. The mechanism proposed satisfies the observation obtained by isotope experiments.抄録全体を表示PDF形式でダウンロード (610K) -
富森 毅, 宮一 諭起範, 井本 吉隆, 木津 治久, 田辺 良久1983 年 103 巻 6 号 p. 607-611
発行日: 1983/06/25
公開日: 2008/05/30
ジャーナル フリーFrom the root of Scutellaria baicalensis GEORGI, two new flavonoids, III and IV, were isolated, together with 5-hydroxy-7, 8-dimethoxyflavone (I), norwogonin (II) and dihydrobaicalin (V). The structures of III and IV were established as 5, 7, 2'-trihydroxy-6-methoxyflavone and 5, 2'-dihydroxy-6, 7, 8-trimethoxyflavone, respectively.抄録全体を表示PDF形式でダウンロード (599K) -
北川 勲, 吉川 雅之, 吉原 実, 林 輝明, 谷山 登志男1983 年 103 巻 6 号 p. 612-622
発行日: 1983/06/25
公開日: 2008/05/30
ジャーナル フリーDuring the studies on the chemical characterization of crude drug precession, the constituents of Ginseng Radix Rubra were investigated by comparing with those of Ginseng Radix. Panaxynol (4), ginsenosides Ro, Rb1, Rb2, Rc, Rd, Re, Rf, Rg1, Rg2 (11), Rg3 (10a), and Rh1 (9) were identified as common constituents of both Ginseng, whereas panaxytriol (1), ginsenoside Rh2 (8), 20 (R)-ginsenoside Rh1 (9a), 20 (S)-ginsenoside Rg3 (10), and 20 (R)-ginsenoside Rg2 (11a) were elucidated as characteristic constituents of Ginseng Radix Rubra. It was also found that Ginseng Radix Rubra contained larger quantities of ginsenosides Rh1 (9), Rg3 (10a), and Rg2 (11) than Ginseng Radix. The less polar constituents of Ginseng Radix Rubra were shown to significantly differ from those of various samples of Ginseng Radix by means of the thin layer chromatographyprofile analysis.抄録全体を表示PDF形式でダウンロード (1089K) -
大石 悦男, 渡辺 裕美, 林 英作1983 年 103 巻 6 号 p. 623-630
発行日: 1983/06/25
公開日: 2008/05/30
ジャーナル フリー5, 8-Dichloropyrido[2, 3-d]pyridazine (I), in benzene in the presence of sodium amide, reacted with active methylene compounds ; ethyl cyanoacetate (IIa), ethyl acetoacetate (IIb), diethyl malonate (IIc), malononitrile (IId), phenylacetonitrile (IIe), to afford 5-substituted (R1)-8-chloropyrido[2, 3-d]pyridazine (III) or 8-substituted (R2)-5-chloropyrido[2, 3-d]pyridazine (IV) ; IIIa (R1=NC-C^^^〓H-CO2C2H5), IVa (R2=NC-C^^^〓H-CO2C2H5), IVb' (R2=-CH2CO2C2H5), IVc (R2=-CH(CO2C2H5)2), IIId (R1=-CH(CN)2), IVe (R2=NC-C^^^〓H-Ph). Compound I, in toluene in the presence of sodium hydride, also reacted with acetophenone (IIf), propiophenone (IIg) to afford 2-(5-chloro-8-pyrido[2, 3-d]pyridazinyl) acetophenone (VII), 2, 2'-(5, 8-pyrido[2, 3-d]pyridazinediyl) di-(1-phenylethanone) (VIII) ; 2-(5-chloro-8-pyrido[2, 3-d]pyridazinyl) propiophenone (XV) respectively. However, reaction of I with acetone (IIh), diethyl ketone (IIi) gave no 5 or 8-substituted pyrido[2, 3-d]-pyridazine der., but a mixture of structure-unknown products.抄録全体を表示PDF形式でダウンロード (754K) -
大石 悦男, 中村 克己, 林 英作1983 年 103 巻 6 号 p. 631-643
発行日: 1983/06/25
公開日: 2008/05/30
ジャーナル フリーChemical properties of 5-phenylpyrido[2, 3-d]pyridazine 7-oxide (II), obtained in the reaction of 5-phenylpyrido[2, 3-d]pyridazine (I) with m-chloroperbenzoic acid, were studied. Compound II reacted with nucleophiles to give 5-phenyl-8-substituted (R1)-pyrido[2, 3-d]pyridazine or 5-phenyl-8-substituted (R2)-pyrido[2, 3-d]pyridazine 7-oxide. Nucleophiles[Products] ; phosphoryl chloride, sulfuryl chloride, tosyl chloride and potassium carbonate [XVIII (R1=-C1)], benzoyl chloride and potassium cyanide [III (R1=-CN)], sodium hydroxide [XVII (R1=-OH) and I], methylmagnesium iodide, ethyl-(isopropyl) magnesium bromide [IVa, b, c (R2=-CH3, -C2H5, -CH(CH3)2], acetophenone [IVa, in the presence of NaOH ; IVa and VI (R1=-CH2COPh), in the presence of CH3ONa], ethyl cyanoacetate [IX (R1=NC-C^^^〓H-CO2C2H5), in Ac2O ; X (R1=NC-C^^^〓H-CO2CH3) and XI (R1=-OCH3), in the presence of CH3ONa]. Application of Reissert-Henze reaction to IVb gave α-methyl-5-phenyl-8-pyrido[2, 3-d]pyridazinylmethyl benzoate (VII). Reaction of II and dimethyl acethylenedicarboxylate afforded three products (XIIa, b, c), which showed the same molecular formula (C19H15NO5). The structures of XIIa and XIIb were presumed to be methyl 6-methoxycarbonyl-α-oxo-5-phenyl-6H-cyclopenta[b]pyridine-6-ethanoate (XIIa), methyl 5-phenylpyrido[3, 2-c]oxepine-7, 8-dicarboxylate (XIIb), respectively. It is considered that these products are formed by the liberation of nitrogen from 1, 3-dipolar cycloadducts. In these reactions, the poor yield of the expected product was accompanied in majority of cases with viscous substance with unknown structure.抄録全体を表示PDF形式でダウンロード (1225K) -
伊藤 隆之, 小川 弘, 前田 稔, 小嶋 正治1983 年 103 巻 6 号 p. 644-649
発行日: 1983/06/25
公開日: 2008/05/30
ジャーナル フリーAttempts to improve adrenal imaging with 131I-6β-iodomethyl-19-norcholest-5 (10)-en-3β-ol (NCL-6-131I) were made. Various NCL-6-131Is with higher specific activity than those used clinically were prepared. An increase in specific activity of NCL-6-131I had no significant effect on the rat adrenal uptake, but caused an increase in the liver concentration of radioactivity. Lipid extraction and radiochromatographic analysis showed the presence of unchanged NCL-6-131I in the liver, but in the adrenal the esterified form of NCL-6-131I was predominant. Autoradiochromatogram of faeces extract indicated the presence of a radioactive spot with an Rf value slightly lower than that of NCL-6-131I. Effects of N-(4-hydroxyphenyl) salicylamide and ursodeoxycholic acid on rat biodistribution of NCL-6-131I were also examined. No significant effect on the adrenal uptake and adrenal-liver ratio of NCL-6-131I was observed in either case.抄録全体を表示PDF形式でダウンロード (717K) -
佐野 敏幸, 庄山 正敏1983 年 103 巻 6 号 p. 650-654
発行日: 1983/06/25
公開日: 2008/05/30
ジャーナル フリーCartap could be determined colorimetrically and fluorometrically by use of ion pair extraction with calcon, which was used for fluorometric reagent of aluminium ion. Cartap (S, S'-[2-(dimethylamino) trimethylene]-bis (thiocarbamate)) was hydrolyzed to nereistoxin, and then 0.5 ml of 0.2% calcon and 4 ml of dichloromethane was added to 1 ml of the nereistoxin solution in acidic medium. The mixture was shaked mechanically for 1 min, followed by separation and centrifugation of the extracted solution. The solution showed max. absorbance at 530 nm, and that obeyed Beer's law in the range of 1 to 20μg/ml. Then, the solution was made to be fluorescence one by the addition of aluminium ion in acidic medium. Samples including lower content of cartap could be determined by the measurement of fluorescence intensity.抄録全体を表示PDF形式でダウンロード (550K) -
久保田 幸穂, 庄司 省三, 船越 崇行, 塩永 一寛, 植木 寛1983 年 103 巻 6 号 p. 655-661
発行日: 1983/06/25
公開日: 2008/05/30
ジャーナル フリーAn esterase was separated from the exocarp of Citrus natsudaidai HAYATA in a highly purified from. The enzyme hydrolyzes p-nitrophenyl esters of fatty acids, phenyl acetate, and tosylarginine methyl ester at varing rates. Of the substrates tested, p-nitrophenyl acetate, for which the specific activity was determined to be 18.60 units per mg of protein, was most rapidly hydrolyzed. The esterase was free from carboxypeptidase and other proteolytic activities. The esterase had a pH optimum at pH 5.5 for p-nitrophenyl acetate. It was strongly inhibited by HgCl2. The other metal ions or inorganic anions tested showed no significant effect on the enzymatic activity. The values of s20, w and D20, w were 1.8 S and 4.5×10-7cm2/s, respectively, and the molecular weight was calculated to be 40000 from these values. The enzyme was composed of 323 amino acid residues : Trp2, Lys21, His9, Arg10, Hyp23, Asp24, Thr18, Ser35, Glu22, Pro20, Gly40, Ala22, Cys(half)2, Val18, Met3, Ile12, Leu17, Tyr14, Phe11.抄録全体を表示PDF形式でダウンロード (746K) -
青沼 繁, 小浜 靖弘, 牧野 俊猛, 服部 有宏1983 年 103 巻 6 号 p. 662-666
発行日: 1983/06/25
公開日: 2008/05/30
ジャーナル フリーThe effect of an atrial peptide, Gly-Pro-4Hyp-Gly-Ala-Gly (AAP), on several druginduced arrhythmias in anesthetized dogs, rats and mice was investigated together with its effect on the related functions. AAP (10 mg/kg, i.v.) significantly reversed the persistent arrhythmias consisting of atrio-ventricular (A-V) block, ectopic beat and/or ventricular tachycardia induced by aconitine pretreatment, to normal sinus rhythm for a while, and evidently prevented development of ventricular fibrillation in dogs and rats. AAP (10, 25 mg/kg, i.v.) significantly prolonged the time until onset of A-V block or ectopic beat and the time until onset of ventricular tachycardia induced by aconitine infusion in mice. This peptide (10 mg/kg, i.v.) significantly prolonged the onset time of A-V block or ectopic beat induced by CaCl2 infusion and the time until ventricular fibrillation induced by ouabain infusion in mice, and significantly shortened the duration of arrhythmia induced by ADP in rats, but did not affect the mouse epinephrine-induced arrhythmia. The peptide (25 mg/kg, i.v.) was found to prolong significantly the QTc interval and to have no effect on the PQ interval, heart rate, respiratory rate and blood pressure in dogs. AAP (1 g/kg. i.v., i.p. and p.o.) did not show the acute toxicity in mice. AAP was a chemically new type of antiarrhythmic substance with very little side effect and low toxicity, possessing the action intensity almost equal to quinidine.抄録全体を表示PDF形式でダウンロード (626K) -
中村 秀雄, 元吉 悟, 世戸 康弘, 今津 千恵子, 門河 敏明, 清水 當尚1983 年 103 巻 6 号 p. 667-674
発行日: 1983/06/25
公開日: 2008/05/30
ジャーナル フリーTherapeutic effect of etofenamate gel (5% etofenamate), applied topically, on traumatic edema and mode of its anti-edema action were investigated in rats. Plasma flufenamic acid levels were 5.73 and 0.173μg/ml 2.5 h after oral administration of etofenamate (diethylene glycol ester of flufenamic acid, 8.5 mg/kg) and after topical application of etofenamate gel (33 mg/paw) equipotent to the oral etofenamate, respectively. Etofenamate gel (25 mg/paw) showed a significant therapeutic effect against traumatic edema of the hind paw, when the gel was applied to the inflamed paw 2 h after bruising but not to the non-inflamed paw. Vehicle gel lacked the activity. Etofenamate gel (25 mg/paw) inhibited both the early and delayed phases of hind paw edema produced by the mixed phlogistics (histamine, serotonin, kaolin, carrageenin), but vehicle gel inhibited only the early phase mediated by histamine and serotonin. Hind paw edema induced by carrageenin (1 mg) was potentiated by the concomitant administration of arachidonic acid (100μg) or PGE2 (1μg). Etofenamate gel (25 mg/paw) did not modify the edema produced by the combination of carrageenin and PGE2, but reduced the arachidonic acid potentiation of carrageenin-induced edema. Vehicle gel did not reduce the edema. From these results, it was suggested that etofenamate gel, applied topically, produced locally therapeutic activity against traumatic edema, and mode of its antiedema action was discussed.抄録全体を表示PDF形式でダウンロード (862K) -
中山 充, 堀江 徳愛, 林 忠男, 有沢 宗久, 清水 岑夫, 森田 直賢1983 年 103 巻 6 号 p. 675-678
発行日: 1983/06/25
公開日: 2008/05/30
ジャーナル フリー5, 7-Dihydroxy-4', 8-dimethoxyflavone (1) was synthesized for the structural confirmation of cirsitakaogenin. However, it was not identical with the natural pigment but it was found that cirsitakaogenin and cirsitakaoside should be read as cirsimaritin (3) and cirsimarin (4), respectively.抄録全体を表示PDF形式でダウンロード (447K) -
倉石 忠幸, 三田寺 洋二, 村上 孝夫, 田中 信寿, 斎木 保久, 陳 秋明1983 年 103 巻 6 号 p. 679-682
発行日: 1983/06/25
公開日: 2008/05/30
ジャーナル フリーFrom the fronds of Dicranopteris dichotoma (THUMB.) BERNH. protocathechuic acid, shikimic acid and two unknown glycosides, which were shown to be p-β-rutinosyloxystyrene (I) and 1-(1-hydroxyethyl)-4-β-rutinosyloxybenzene (II) mainly by spectroscopic methods, were isolated besides the already detected flavonoids (afzelin and quercitrin). The yield of shikimic acid referred to the dry fronds amounted to 3%. From the fronds of Microlepia obtusiloba HAYATA an unknown glycoside was isolated and identified as p-β-D-allosyloxystyrene (III) by spectroscopic methods.抄録全体を表示PDF形式でダウンロード (507K) -
小菅 卓夫, 糠谷 東雄, 山本 藤輔, 辻 邦郎1983 年 103 巻 6 号 p. 683-685
発行日: 1983/06/25
公開日: 2008/05/30
ジャーナル フリーTwo cardiac principles were isolated from nekombu (the basal part of the blade of a laminariaceous seaweed). Fatty acids of C14, C16 and C18 were found to stimulate the isolated frog heart, while histamine dihydroiodate to accelerate the isolated guinea pig atrium. Histamine and iodine contents of nekombu were 501 mg/kg and 3200 mg/kg, respectively, indicating that 36% of the total iodine present in nekombu is in the salt form of histamine. It was also found that a small amount of histamine improves the taste of glutamic acid.抄録全体を表示PDF形式でダウンロード (416K) -
寺井 忠正, 形井 雅昭, 廻 治雄1983 年 103 巻 6 号 p. 686-689
発行日: 1983/06/25
公開日: 2008/05/30
ジャーナル フリーA spectrophotometric method has been established for the determination of grayanotoxin (G)-I, G-II and G-III, toxic diterpenoids of Leucothoe grayana MAXIM., by using a color reaction with vanillin in perchloric acid. This method has been applied to the determination of these grayanoid compounds contained in toxic honey.抄録全体を表示PDF形式でダウンロード (461K) -
平川 善行, 原田 清1983 年 103 巻 6 号 p. 690-695
発行日: 1983/06/25
公開日: 2008/05/30
ジャーナル フリーIn the previous paper, a new technique for particle size reduction of oxolinic acid (OA), a slightly soluble model drug having an acidic group in a molecule, by the crystallization through the neutralization of its alkaline solution in the presence of certain surfactant or polymer was described. The wet sieving method by the use of polycarbonate membrane filter for the evaluation of size reduction effect was also described. Various factors affecting the size reduction of OA were investigated in this paper. The results obtained were as follows ; manners of participation in various factors affecting the size reduction varied with OA concentration at crystallization, and in the case of 5 w/v% OA concentration, the influences of addition rate of hydrochloric acid solution, stirring rate, reaction temperature and concentration of hydrochloric acid were relatively low. Size reduction effects of various surfactants and polymers were investigated. All of them were effective, though differences were recognized in the extent of size reduction. It has been found that the establishment of optimal conditions to obtain the finest particles is enabled and moreover, there is a possibility to prepare the particle that have an optional particle size by regulating the various factors.抄録全体を表示PDF形式でダウンロード (598K) -
労 愛娜, 藤本 康雄, 辰野 高司1983 年 103 巻 6 号 p. 696-699
発行日: 1983/06/25
公開日: 2008/05/30
ジャーナル フリーFrom Artemisia rubripes NAKAI (Compositae) collected in China were isolated ten compounds, eupatilin, 4'-demethyleupatilin, cirsilineol, dammaradienyl acetate, bauerenyl acetate, cycloartenyl acetate, cycloart-23-en-3β, 25-diol, cycloart-25-en-3β, 24-diol, trisnorcycloartanoloic acid acetate and caffeic acid. The isolation of trisnorcycloartanoloic acid acetate from a natural source is the first example.抄録全体を表示PDF形式でダウンロード (475K)
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