巻号一覧
106 巻, 9 号
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大村 智1986 年 106 巻 9 号 p. 729-757
発行日: 1986/09/25
公開日: 2011/01/31
ジャーナル フリーAfter structure elucidation of 16-membered macrolide antibiotic leucomycin, the structures of spiramycin, tylosin, megalomicin, irumamycin and virustomycin were determined by chemical degradation and nuclear magnetic resonance (NMR) spectroscopy. The studies on the chemical modification and structure activity correlation of macrolides led to the elaboration of clinically useful new derivatives.
The biosynthetic origin of the carbon skeletone of macrolide aglycone was investigated by means of 13C NMR and the feeding experiments of 13C labeled precursors. We found that an antifungal antibiotic cerulenin is a specific inhibitor of fatty acid and “polyketide” biosyntheses, and applied the antibiotic to the biosynthetic studies of macrolides after formation of the lactone ring and to the production of a new “hybrid” macrolide, chimeramycin. Furthermore, a strain which produces a new “hybrid” antibiotic mederrhodin was breaded from actinorhodin and medermycin producers by gene manipulation.
Sixty five or more new antibiotics have been discovered from secondary microbial metabolites using newly devised screening systems. Azureomycins and izupeptins were found as bacterial cell wall biosynthesis inhibitors. In combination with the above screening, several new antibiotics, nanaomycins, frenolicin B, cervinomycins, asukamycin and so on were discovered as antimycoplasmal substances. Diazaquinomycins as antifolate substance, hitachimycin and avermectin as anthelmintics, herbimycin, phosalacine and oxetin as herbicids have been found by the corresponding each screening system. The structure elucidation, biosynthesis and mode of action of these antibiotics have been studied. Among of them, nanaomycin A and avermectin (or ivermectin) have been employed as antifungal and antiparasitic therapeutics, respectively, for veterinary use.抄録全体を表示PDF形式でダウンロード (3517K) -
アマチャヅルのサポニン成分について その10吉川 和子, 竹本 常松, 在原 重信1986 年 106 巻 9 号 p. 758-763
発行日: 1986/09/25
公開日: 2011/01/31
ジャーナル フリーNew saponins, named gypenosides LXI (1), LXII (2), LXIII (3), LXIV (4) and LX VII (5) were isolated from the aerial parts of Gynostemma pentaphyllum MAKINO collected in Miyagi Pref. On the basis of chemical and physicochemical evidence, they were characterized as follows: 1, 2α, 3β, 12β, 20 (S), 26-pentahydroxydammar-24-ene 3-O-β-sophoroside-20-O-β-primeveroside; 2, 3β, 12β, 19, 20 (S)-tetrahydroxydammar-24-ene 3-O-β-sophoroside-20-O-β-primeveroside; 3, 3β, 19, 20 (S)-trihydroxydammar-24-ene 3-O-β-sophoroside-20-O-β-primeveroside; 4, 3β, 12β, 19, 20 (S)-tetrahydroxydammar-24-ene 3-O-β-D-glucopyranoside-20-O-β-primeveroside; 5, 2α, 3β, 19, 20 (S)-tetrahydroxydammar-24-ene 3-O-β-sophoroside-20-O-β-primeveroside.抄録全体を表示PDF形式でダウンロード (846K) -
室 富雄, 湯木 弘, 川北 武志, 千原 保昭, 安本 光由, 瀬戸口 信郎, 阿南 惟毅, 瀬戸口 通英1986 年 106 巻 9 号 p. 764-774
発行日: 1986/09/25
公開日: 2011/01/31
ジャーナル フリーSeventeen 2-(substituted phenoxymethyl) morpholines were synthesized by the reduction of 6-(substituted phenoxymethyl) morpholin-3-one or by the reaction of 1, 2-epoxy-3-(substituted phenoxy) propane, 2-aminoethyl hydrogen sulfate and sodium hydroxide in a mixture of water and ethanol. These compounds were tested for effectiveness in preventing reserpine-induced ptosis and in prolonging the survival time of mice subjected to hypobaric hypoxia. In the reserpine ptosis test, o-benzyl, o-(3-thenyl), o-(2-pyridylmethyl) and o-(2-thenyl) substituted 2-phenoxymethylmorpholine (VIn, VIl, VIe and VIh) were effective with RD30 values of 3, 9, 10 and 12 mg/kg (p.o.), respectively. In the antihypoxia test, p-(2-thenyl), o-(5-methyl-2-thenyl) and m-(2-thenyl) substituted 2-phenoxymethylmorpholine (VIj, VIk and VII) and VIh were effective with survival times of 515.0, 375.8, 346.7 and 406.7 s, respectively. From these results the two most promising compounds, VIh and VIn were tested for amelioration of CO2-induced amnesia. VIn but not VIn showed ameliorative activity.抄録全体を表示PDF形式でダウンロード (1675K) -
1-Aryl-6-(4-dimethylaminophenyl)-4-pyridone-3-carboxylic Acid類の合成と構造-活性相関成田 弘和, 小西 義憲, 新田 純, 長木 秀嘉, 北山 功, 渡辺 泰雄, 才川 勇1986 年 106 巻 9 号 p. 775-781
発行日: 1986/09/25
公開日: 2011/01/31
ジャーナル フリーA series of 1-aryl-6-(4-dimethylaminophenyl)-4-pyridone-3-carboxylic acids (7-33) has been prepared in order to evaluate antibacterial activity of N-aryl group within pyridonecarboxylic antibiotics. The in vitro minimum inhibitory concentration data as indicated in Table II, all compounds except four compounds (18, 20, 21 and 29) exhibit considerably higher activity against gram-positive S. aureus than the parent N-ethyl compound 1 and nalidixic acid. Among the compounds having substituted 1-phenyl groups, 4'-hydroxy compound 9 and its 2'-fluoro and 2'-methyl derivatives (25 and 27) are significantly active against both gram-positive and negative bacteria.抄録全体を表示PDF形式でダウンロード (911K) -
1-(4-Hydroxyphenyl)-6-substituted-4-pyridone-3-carboxylic Acid類の合成と構造-活性相関成田 弘和, 小西 義憲, 新田 純, 小林 順子, 渡辺 泰雄, 南 新三郎, 才川 勇1986 年 106 巻 9 号 p. 782-787
発行日: 1986/09/25
公開日: 2011/01/31
ジャーナル フリー1-(4-Hydroxyphenyl)-4-pyridone-3-carboxylic acid and its congener (2'-methyl- and 2'-fluoro-4'-hydroxyphenyl) bearing alkyl, cycloalkyl and aryl groups at C-6 have been prepared in order to verify and develop the structure-activity relationship obtained in the preceding paper. Excellent in vitro activity against gram-positive S. aureus FDA 209P (minimum inhibitory concentration<0.05μg/ml) was observed with 4''-(2-thienyl) phenyl, 2''-naphthyl, 2''-thianapthenyl and 1''-methyl-5''-indolyl derivatives. As expected, these compounds also showed broad and good effects on gram-negative bacteria. The origin of the observed low urinary recovery of this class of compounds in oral administration to mice has been investigated with 81 (2''-thianaphthenyl) through oral and intravenous administrations in rats, leading to the conclusion that low intestine absorption (ca. 20%) and glucuronate conjugation (predominantly at the phenolic hydroxyl group) are responsible for the in vivo result.抄録全体を表示PDF形式でダウンロード (773K) -
1-(4-Fluorophenyl)-and 1-(2, 4-Difluorophenyl)-6-substituted-4-pyridone-3-carboxylic Acid類の合成と構造-活性相関成田 弘和, 小西 義憲, 新田 純, 宮島 三香子, 渡辺 泰雄, 四辻 彰, 才川 勇1986 年 106 巻 9 号 p. 788-794
発行日: 1986/09/25
公開日: 2011/01/31
ジャーナル フリーA series of 1-(4-fluorophenyl)-and 1-(2, 4-difluorophenyl)-4-pyridone-3-carboxylic acid having a substituent at 6-position has been prepared, and their antibacterial activity and urinary recovery in mice were evaluated. Substituents at 6-position remarkably affected the antibacterial activity and urinary recovery. 1''-Methyl-5''-indolyl compounds (4c, 5c) and 4''-methylaminophenyl compound (5f) showed equal or better in vitro activity than 6-(4-dimethylaminophenyl)-1-(4-fluorophenyl)-4-pyridone-3-carboxylic acid (6) and good urinary recovery. However, no compounds showed better in vitro activity than 1-(4-hydroxyphenyl)-6-(2-thianaphthenyl)-4-pyridone-3-carboxylic acid (7). Structure-activity relationship focused on 1-and 6-substituents is also discussed.抄録全体を表示PDF形式でダウンロード (914K) -
7-Amino-1-aryl-6-Huoro-4-quinoione-3-carboxylic Acid類の合成と構造-活性相関成田 弘和, 小西 義憲, 新田 純, 長木 秀嘉, 小林 順子, 渡辺 泰雄, 南 新三郎, 才川 勇1986 年 106 巻 9 号 p. 795-801
発行日: 1986/09/25
公開日: 2011/01/31
ジャーナル フリーA series of unsubstituted and substituted cyclic amino derivatives at 7-position of 1-aryl-6-Huoro-4-quinolone-3-carboxylic acid (aryl=4-fluoro-, 2, 4-difluoro-, 4-fluoro-2-hydroxy-and 4-hydroxyphenyl) has been, prepared and their antibacterial activity was evaluated. The compounds 6b and 7b, 1-(4-Huorophenyl) and 1-(2, 4-difluorophenyl) variants of norfloxacin (NF), respectively, showed better in vitro activity than NF and good urinary recovery. 7-(3-Methyl-1-piperaziny1) and 7-(3-amino-1-pyrrolidiny1) derivatives of 1-(2, 4-difluoropheny1)-6-fluoro-4-quinolone-3-carboxylicacids (7c, f) exhibited comparable in vitro activity and excellent in vivo efficacy on systemic infections and practically no toxicity [ED 50 (mg/mouse, p. o.): vs.S.aureus SA-57, 7c=0.020, 7f=0.023;vs.S.marcescens IID 620, 7c=0.013, 7f=0.012].Structure-activity relationship focused on 7-substituents is also discussed.抄録全体を表示PDF形式でダウンロード (746K) -
7-Amino-6-fluoro-1-(fluorophenyl)-4-oxo-1, 8-naphthyridine-3-carboxylic Acid類の合成と構造-活性相関成田 弘和, 小西 義憲, 新田 純, 北山 功, 宮島 三香子, 渡辺 泰雄, 四辻 彰, 才川 勇1986 年 106 巻 9 号 p. 802-807
発行日: 1986/09/25
公開日: 2011/01/31
ジャーナル フリーA series of 7-amino derivatives (unsubstituted and substituted piperazine, pyrrolidine and piperidine) of 1-aryl-6-fluoro-4-oxo-1, 8-naphthyridine-3-carboxylic acid (aryl=4-fluoro-, 2, 4-difluoro-and 3, 4-difluorophenyl) has been prepared, and their antibacterial activity and urinary recovery in mice were evaluated. All compounds (6a-h, 7a-h, 8a) showed better in vitro antibacterial activity than the quinolone counterparts described in the preceding paper and especially 7-(3-amino-1-pyrrolidinyl)-1-(4-fluorophenyl) and -1-(2, 4-difluorophenyl) derivatives (6e and 7e) showed a noteworthy excellent activity against S. aureus (minimum inhibitory concentration<0.05μg/ml) as well as gram-negative bacteria. Among the four selected compounds (6a, e and 7a, e) for the estimation of in vivo efficacy on systemic infections and acute toxicity, 7e was the best compound [ED 50 (mg/mouse, p. o.): vs. S. aureus SA-57, 0.013; vs. S. marcescens IID 620, 0.008]. Structure-activity relationship concerning 7-amino groups is also discussed.抄録全体を表示PDF形式でダウンロード (871K) -
小柴胡湯, 大柴胡湯及びその配剤生薬の改善作用谿 忠人, 大野 智子, 井上 一美, 勝城 忠久, 有地 滋1986 年 106 巻 9 号 p. 808-817
発行日: 1986/09/25
公開日: 2011/01/31
ジャーナル フリーEffects of Sho-saiko-to, Dai-saiko-to and their constituent crude drugs on blood property in betamethasone-treated rats were biorheologically examined. Sho-saiko-to and Dai-saiko-to, famous Kampo-prescriptions used in traditional Chinese system of medicine were found to inhibit the increase of blood viscosity in betamethasone-treated rat. They were also found to improve the increase of serum lipids and decreases of thrombin time, antithrombin III activity and the serum level of endogenous corticosterone affected by betamethasone.
The activity of two Kampo-prescriptions may be explained by combined actions of prescribed crude drugs, such as Bupleuri Radix, Ginseng Radix, Glycyrrhizae Radix, Scutellariae Radix and Rhei Rhizoma.抄録全体を表示PDF形式でダウンロード (1745K) -
西村 清志, 高橋 雅行, 中陳 静男, 篠田 雅人1986 年 106 巻 9 号 p. 818-824
発行日: 1986/09/25
公開日: 2011/01/31
ジャーナル フリーBy the kinetic analysis of pig adrenal Δ5-3β-hydroxysteroid dehydrogenase and Δ4-Δ5-isomerase activities, the apparent Km values of pregnenolone, 17α-hydroxypregnenolone and dehydroepiandrosterone for the dehydrogenase activity were identified to be 1.2, 1.8 and 0.2μM (Vmax: 23, 26 and 26nmol/min/mg Protein); those of pregn-5-ene-3, 20-dione and androst-5-ene-3, 17-dione for the isomerase activity were 9.1 and 22μM (Vmax: 220 and 270 nmol/min/mg protein), respectively.
The inhibitory effect by various inhibitors of steroid metabolizing enzyme and steroids on the dehydrogenase activity and the 17α-hydroxylase activity were investigated using pregnenolone as substrate. The dehydrogenase activity was considerably inhibited by cyanoketone, SU 8000, o, P'DDD and SKF 525A. On the other hand, the hydroxylase activity was inhibited by SU 8000, SU 10603, cyanoketone, o, P'DDD and SKF 525A. Furthermore, various kinds of steroid, androgens, corticoids, estrogens, etc., inhibited the dehydrogenase activity. However, the hydroxylase activity was not inhibited by ail of those steroids except 5α-dihydrotestosterone and 20α-or 20β-hydroxyprogesterone.抄録全体を表示PDF形式でダウンロード (1062K) -
「日局10」収載結晶性薬品の分析, 同定及び厚さの測定などが同時にできるチャートの作成渡辺 厚1986 年 106 巻 9 号 p. 825-836
発行日: 1986/09/25
公開日: 2011/01/31
ジャーナル フリーThe combined charts by which about 85 group A crystals (lamellar, scales or plates) listed in the Japanese Pharmacopoeia X can be analyzed, identified and their thicknesses can be simultaneously measured, have been prepared by use of a graph of retardation plotting by log (n2-n1) as the abscissa and (n1, n2) as well as log (D) as the ordinate, where n1 and n2 are the key refractive indices (refractive indices measured at the natural position by the immersion method) and D denotes the thickness of the sample. As the charts are advantageous for the estimation of optical properties of anisotropic crystals, other about 85 drugs not belonging to group A were also tried to present in the charts by using their refractive indices measured at the position parallel to the microscope stage. These charts would be useful to apply for the quality testing of poorly soluble drugs.抄録全体を表示PDF形式でダウンロード (5277K) -
シャクヤク中ペオニフロリン分析への応用岡本 光美, 野口 衛1986 年 106 巻 9 号 p. 837-839
発行日: 1986/09/25
公開日: 2011/01/31
ジャーナル フリーPaeoniflorin contained in Paeony Root was analyzed by thin layer chromatography (TLC) by using a cyanoalkyl chemically bonded stationary phase, prepared by treated of pre-coated silica gel phase with 3-cyanopropyltrichlorosilane (CN). The CN-treated TLC plate was applied to the evaluation of the commercial “Paeony root”. By migration with methanol-water (10:90, v/v) on the CN-treated TLC plate, paeoniflorin spot on the chromatogram was measured with a TLC densitometer equipped with a dual-wave length TLC scanner at λS 233 nm (sample) and λR 350 nm (reference). By this method, the amount of paeoniflorin was measured within 3% error over the range of 0.5-10μg, and the limit of detection was 0.5 μg.抄録全体を表示PDF形式でダウンロード (379K)
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