著者

瀬川 純 数野 憲二 松岡 正人 白波瀬 一朗 尾崎 正邦 松田 真人 冨井 由文 北野 正彦 黄瀬 正博

出版者

公益社団法人日本薬学会

雑誌

Chemical & pharmaceutical bulletin (ISSN:00092363)

巻号頁・発行日

vol.43, no.1, pp.63-70, 1995-01-15

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A seried of 1,8-disubstituted 6-fluoro-4-oxo-7-piperazinyl-4H-[1,3]thiazeto[3,2-a]quinoline-3-carboxylic acid derivatives was prepared and evaluated for antibacterial activity. In the 7-piperazinyl series, addition of a fluorine at C-8,which increased the in vitro activity for the 1-hydrogen and 1-methyl analogues and decreased it for the 1-phenyl analogue, improved the in vivo activity of all the analogues. Introduction of a methoxy group at C-8 of the 1-methyl-7-piperazinyl analogue also improved its in vivo antibacterial activity. The effect of 8-substituents on the in vitro and in vivo antibacterial activity of the 1-methyl-7-(4-methyl-1-piperazinyl) series is also discussed.

著者

小林 資正 田中 淳一 香取 岳人 北川 勲

出版者

公益社団法人日本薬学会

雑誌

Chemical & pharmaceutical bulletin (ISSN:00092363)

巻号頁・発行日

vol.38, no.11, pp.2960-2966, 1990-11-25

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Following the characterization of swinholide A (1), the major cytotoxic dimeric macrolide, three new congeneric dimeric macrolides, named swinholide B (2), swinholide C (3), and isoswinholide A (10), have been isolated from the Okinawa marine sponge Theonella swinhoei. The structures of these dimeric macrolides have been elucidated on the basis of chemical and physiocochemical evidence. These dimeric macrolides were shown to exhiit potent cytotoxicities toward KB cell lines.

著者

Eri Segi-Nishida

出版者

公益社団法人日本薬学会

雑誌

Biological and Pharmaceutical Bulletin (ISSN:09186158)

巻号頁・発行日

vol.34, no.7, pp.939-944, 2011-07-01 (Released:2011-07-01)

参考文献数

58

被引用文献数

16 48

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Electroconvulsive seizure (ECS) therapy is a clinically proven treatment for depression and is often effective even in patients resistant to chemical antidepressants. However, the molecular mechanisms underlying the therapeutic efficacy of ECS are not fully understood. Here, I review studies that show molecular, cellular, and behavioral changes by ECS treatment, and discuss the functions of ECS to underlie the action of antidepressant effects. In hippocampus, these changes cover gene induction, increased adult neurogenesis, and electrophysiological reactivity. Especially, the role of vascular endothelial growth factor (VEGF) in neurogenesis is discussed. Among other gene expression changes in hippocampus, a role of cyclooxygenase (COX)-2, an inducible type of the rate-limiting enzyme of prostanoid synthesis, is focused. ECS-induced changes in other brain regions such as prefrontal cortex and hypothalamus, and ECS-induced behavioral changes are also reviewed. Understanding the molecular, cellular, and behavioral changes by ECS will provide a new view to find potential targets for novel antidepressant design that are highlighted by these findings.

著者

山中 宏 江戸 清人 今野 昌悦

出版者

公益社団法人日本薬学会

雑誌

薬学雑誌 (ISSN:00316903)

巻号頁・発行日

vol.97, no.7, pp.p726-730, 1977-07

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Reaction of 2-cyano-4-methoxy-6-methyl- (I), 4-cyano-6-methoxy-2-methyl- (II), 5-cyano-4-methoxy-2-methyl- (III), and 5-cyano-4,6-dimethoxy-2-methylpyrimidine (IV) with Grignard reagents is described. While 2-cyano and 4-cyano derivatives (I, II) were transformed to the corresponding pyrimidinyl ketones as expected, 5-cyano derivatives (III, IV) were converted to the addition products, 5-cyano-6-ethyl-1,6-dihydro-4-methoxy-2-methyl- (VIIa) and 5-cyano-2-ethyl-1,2-dihydro-4,6-dimethoxy-2-methylpyrimidine (XI), respectively.

著者

川崎 和幸 山田 一磨呂 大江 孝範 鶴田 峯生 寺澤 道夫 今吉 朋憲 安永 幸弘 後藤 一洋

出版者

公益社団法人日本薬学会

雑誌

藥學雜誌 (ISSN:00316903)

巻号頁・発行日

vol.109, no.11, pp.827-834, 1989-11-25

被引用文献数

3

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The pro-drugs of α, 2-dimethyl-5H-[1] benzopyrano [2,3-b] pyridine-7-acetic acid (I) with a potent anti-inflammatory activity were synthesized in order to reduce its gastrointestinal side effects. Various esters synthesized were evaluated for their anti-inflammatory activity and ulcerogenicity. Among the compounds maintaining a potent activity of I, N, N-dimethylcarbamoyl-methyl α, 2-dimethyl-5H-[1] benzopyrano [2,3-b] pyridine-7-acetate (II-18) showed excellent biopharmaceutical characteristics. The ulcerogenic effect of II-18 showed excellent biopharmaceutical characteristics. The ulcerogenic effect of II-18 on the rat gastric mucosa was about 3 times less than that of I. It was suggested that II-18 may be an useful biolabile pro-drug for I among the compounds tested.

著者

平原 敬三 安藤 直子 松石 哲郎 鈴木 信夫 寺尾 俊彦 倉田 宗司

出版者

公益社団法人日本薬学会

雑誌

薬学雑誌 (ISSN:00316903)

巻号頁・発行日

vol.108, no.9, pp.p860-866, 1988-09

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The addition of sodium oleate to antithrombin III (ATIII) produced complexes of ATIII and oleic acid by varying the acid concentration. During immunoelectrophoresis, ATIII shifted to the anode in the presence of sodium oleate. The reactivity of ATIII with anti human ATIII serum lowered as the sodium oleate level increased. However the reactivity with antibody obtained by immunization of rabbits with the mixture of sodium oleate and ATIII, was not lost on the immunoelectrophoresis. In acrylamide gel electrophoresis, ATIII separated into 6 bands with an increase in sodium oleate. The binding ratio of ATIII to heparin-Sepharose decresed in the presence of sodium oleate. In acrylamide gel isoelectrofocusing, the subtypes of ATIII having pI 5 showed high affinity to oleic acid. These high affinity subtypes also showed high affinity to heparin and thrombin. In fibrinogen agarose electrophoresis, ATIII lost its antithrombin activity depending on the increase of sodium oleate. By the determination of free fatty acids (FFA) in ATIII purified from normal plasma, we found that FFA would bind to ATIII in the normal plasma. Scatchard plot analysis indicated 7.6 binding sites of oleic acid per ATIII molecule. The results suggested that ATIII lost its activity by conformational change or interference in the thrombin binding site, and that the subtype of ATIII having pI 5 could be a significant carrier of plasma FFA.

著者

Wei He Li-Fang Fan Qing Du Bai Xiang Chun-Lei Li Min Bai Yong-Zhen Chang De-Ying Cao

出版者

公益社団法人日本薬学会

雑誌

Chemical and Pharmaceutical Bulletin (ISSN:00092363)

巻号頁・発行日

vol.57, no.2, pp.122-128, 2009-02-01 (Released:2009-02-01)

参考文献数

31

被引用文献数

7 17 9

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The purpose of the study is to perform the in vitro and in vivo evaluation of multi-layer film coatings for omeprazole. The system consists of drug-layered or drug-containing core pellets coated with salt (sodium chloride and disodium hydrogen phosphate), hydroxypropyl methyl cellulose (HPMC), and enteric film-coating layer, respectively. The drug-layered core pellets were prepared by a coating layer of omeprazole on inert pellet cores in fluidized bed coater. An in vitro/in vivo gastro-resistance study was conducted, and a dissolution study was performed in pH 7.4 phosphate buffer for omeprazole release. The multi-layer coated pellets were stable in gastric pH conditions and upper gastrointestinal (GI) tract in rats. Salt layer improved the drug stability, and its coating levels had little influence on the dissolution profiles of omeprazole. The rate of drug release was significantly delayed by HPMC layer. The salt layer could function as a separated layer, and substitute part of the HPMC layer and decrease the coating levels of HPMC. The bioavailability (AUC) of the multi-layer coated drug-layered and drug-containing pellets was 3.48±0.86 and 2.97±0.57 μg·h/ml, respectively. The drug-layered pellets with multi-layer film coatings not only provided delayed and rapid release of omeprazole, but also could provide a good stable property for omeprazole. It was confirmed that rapid in vitro drug release rate resulted in better absorption.

著者

袖岡 幹子

出版者

公益社団法人日本薬学会

雑誌

ファルマシア (ISSN:00148601)

巻号頁・発行日

vol.42, no.6, 2006-06-01

著者

井上 隆夫 石館 八重子 藤田 正雄 久保 正良 福島 美雪 永井 正博

出版者

公益社団法人日本薬学会

雑誌

藥學雜誌 (ISSN:00316903)

巻号頁・発行日

vol.98, no.1, pp.41-46, 1978-01-25

被引用文献数

1

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Chemical constituents of the leaves and stem bark of Acer nikoense MAXIM. (Aceraceae) were examined. β-Amyrin, β-sitosterol contaminated with campesterol and stigmasterol, and β-sitosterol glucoside were obtained from both parts of the plant. β-Amyrin acetate, quercetin, quercitrin, and ellagic acid were isolated from the leaves, and scopoletin, (+)-rhododendrol (VIII), (+)-catechin, and two new glycosides named aceroside I (XI), C_<25>H_<32>O_8,mp 170-171° (from acetone), [α] D-7.7°, and epi-rhododendrin (XII), C_<16>H_<24>O_7,mp 81-84°, [α] D -15.5°, from the stem bark. The absolute configuration of VIII was proposed to be S from empirical rule on optical rotation-chirality relationship. Hydrolysis of aceroside I (XI) afforded acerogenin A (XIII) as its aglycone, whose structure has already been reported. The structure of epi-rhododendrin (XII) was elucidated to be (S)-4-(p-hydroxyphenyl) butan-2-ol 2-β-D-glucopyranoside from chemical and spectral evidences.

著者

伊藤 勇一郎

出版者

公益社団法人日本薬学会

雑誌

ファルマシア (ISSN:00148601)

巻号頁・発行日

vol.27, no.10, 1991-10-01

著者

野副 鉄男 村瀬 雅之

出版者

公益社団法人日本薬学会

雑誌

ファルマシア (ISSN:00148601)

巻号頁・発行日

vol.31, no.8, pp.857-860, 1995-08-01

著者

柳澤 秀吉 高島 則一

出版者

公益社団法人日本薬学会

雑誌

藥學雜誌 (ISSN:00316903)

巻号頁・発行日

no.481, pp.179-189, 1922-03-26

著者

Sasaki Yohei Komatsu Katsuko Takido Michio TAKESHITA Kazuo KASHIWAGI Harutsugu NAGUMO Seiji

出版者

公益社団法人日本薬学会

雑誌

Biological & pharmaceutical bulletin (ISSN:09186158)

巻号頁・発行日

vol.30, no.8, pp.1511-1515, 2007-08-01

参考文献数

13

被引用文献数

1 4

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Kuma-zasa is Japanese folk medicine derived from plants of genus Sasa, family Bambusaceae. Although the plants of origin of Kuma-zasa were reported to be Sasa palmata, S. senanensis, S. yahikoensis, and S. kurilensis, authentication of those plants was difficult because of similarity in morphology. Several methods for the classification of genus Sasa are available, but none involve a genetic approach. Here, we performed the genetic profiling of genus Sasa, including the four species used medicinally. Thirteen sequences were observed in chloroplast DNA intron between rbcL and ORF106 and partial ORF106 regions of 34 specimens of 16 Sasa species and one specimen of Phyllostachys pubescens. We observed differences in alignment in this region among the specimens. The analyzed lengths varied from 759 to 821 bp depending on the specimen. There were nine base substitutions, eight successive thymines or adenines, and one to three repeat units of 31 bp. Moreover, we could not find species-specific alignment: different alignments were observed in specimens of the same species, while the same alignment was observed in specimens of different species. In the phylogenetic tree reconstructed by maximum parsimony analysis, medicinally used species did not form a cluster, although most of them were positioned close to each other. The genetic profiling of Sasa species would be of use in determining the botanical origin of the herbal medicine derived from the leaves of Sasa plants.

著者

大谷 道輝 川端 志津 假家 悟 内野 克喜 伊藤 敬 小瀧 一 籾山 邦男 森川 亜紀 瀬尾 巖 西田 紀子

出版者

公益社団法人日本薬学会

雑誌

藥學雜誌 (ISSN:00316903)

巻号頁・発行日

vol.122, no.5, pp.323-329, 2002-05-01

被引用文献数

1 13

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The effect of the intake of 200g of grapefruit pulp (corresponding to one grapefruit) on the pharmacokinetics of the calcium antagonists nifedipine (NF) and nisoldipine (NS) were investigated in 8 healthy Japanese male volunteers. A crossover design was used for the study: group I did not ingest any grapefruit (control group); group II ingested grapefruit 1 h after drug administration; and group III ingested grapefruit 1 h before drug administration. The intake of grapefruit pulp increased the plasma concentrations of both NF and NS, an effect that has previously been reported with grapefruit juice. The increase was most marked when grapefruit was eaten before drug administration. For both NF and NS, subjects who ingested grapefruit 1 h before drug administration exhibited a greater C_<max> and AUC_<0-24> than did subjects in the control group. For NF, the C_<max> was 1.4 times higher and the AUC_<0-24> 1.3 times larger in group III than in group I. For NS, the C_<max> was 1.5 times higher and the AUC_<0-24> 1.3 times larger in group III than in group I. The increase in the AUC_<0-24> was significant for both drugs (p<0.05). The finding that the ratios of C_<max> and AUC_<0-24> for unchanged drug and metabolites did not vary greatly among the three groups for either drug suggests that the increase in serum concentration produced by grapefruit intake may be due to other factors than an inhibitory effect on drug metabolism. Also, the increases in C_<max> and AUC_<0-24> of NS produced by grapefruit intake were smaller than those produced by grapefruit juice intake, indicating that grapefruit pulp and juice have different effects on the pharmacokinetics.

著者

三井 利幸 藤村 義和

出版者

公益社団法人日本薬学会

雑誌

衛生化学 (ISSN:0013273X)

巻号頁・発行日

vol.21, no.4, pp.183-187, 1975-08-31

被引用文献数

3

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The concentration of hydrochloric acid and potassium iodide in Dragendorff's reagent was examined in order to obtain high sensitivity in the detection of alkaloids. As the samples, caffeine, morphine, procaine, cocaine, methamphetamine, ephedrine, chloroephedrine, methylephedrine, codeine, and dihydrocodeine were used. The optimum concentrations of hydrochloric acid and potassium iodide were determined by measuring the unreacted amount of bismuth in the reaction mixture of an alkaloid and the Dragendorff's reagent containing a definite amount of these two components when using caffeine, cocaine, procaine, codeine, and dihydrocodeine. For other alkaloids, however, the optimum concentration of the two components could not be determined.

著者

岡田 寿太郎 川島 嘉明

出版者

公益社団法人日本薬学会

雑誌

藥學雜誌 (ISSN:00316903)

巻号頁・発行日

vol.89, no.10, pp.1345-1351, 1969-10-25

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Strychnine and brucine were extracted from slices of strychni seeds, cut into various sizes (#1-#4), in water at 27,37,and 47°. Results of analysis of extraction rate showed that the mechanism of extraction consists of washing, diffusion, and capillary extraction, but the capillary extraction occupies a small part. Mass transfer coefficients of these three mechanisms, which depend distinctly on temperature of the solvent, were determined.

著者

早川 順子 野田 直希 山田 貞二 宇野 圭一

出版者

公益社団法人日本薬学会

雑誌

藥學雜誌 (ISSN:00316903)

巻号頁・発行日

vol.104, no.1, pp.57-61, 1984-01-25

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Nux Vomica contains strychnine and brucine which showed a strong pharmacological activity. Therefore, an improved method of analyzing these compounds is of value. For determination of these compounds in Nux Vomica, titrimetry is employed on JPX. Then strychnine and brucine in Nux Vomica and commercial pharmaceutical preparations including Nux Vomica extracts were identified by thin layer chromatography (TLC) and determined using high performance liquid chromatography (HPLC). Samples were extracted with CHCl_3-MeOH (2 : 1). The extracts were passed through Sep Pak C_<18> cartridge and applied to TLC and HPLC. HPLCs of strychnine and brucine were carried out on Shodex ODS column and CH_3CN-H_2O (25 : 75) to which 1-heptanesulfonic acid was added as a counter ion for the solvent system. Recoveries from model preparations were more than 98%. This method was considered to be useful for the determination of strychnine and brucine in commercial preparations including Nux Vomica extracts.

著者

内山 充 鈴木 康男 福沢 健治

出版者

公益社団法人日本薬学会

雑誌

藥學雜誌 (ISSN:00316903)

巻号頁・発行日

vol.88, no.6, pp.678-683, 1968-06-25

被引用文献数

33

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Mechanism of antioxidation of tocopheronolactone, isolated as the quinonoid metabolic product of α-tocopherol, was examined. Tocopheronolactone was as effective as α-tocopherol in inhibiting the increase of TBA value during the in vitro incubation of α-tocopherol-deficient mouse liver homogenate, but the production of peroxide from unsaturated fatty acids irradiated with ultraviolet ray was not depressed by the sole addition of tocopheronolactone. Reduced tocopheronolactone depressed TBA value during the irradiation of unsaturated fatty acid with ultraviolet ray and reacted with the stable free radical α, α-diphenyl-β-picrylhydrazyl, but tocopheronolactone was not active. Reduced tocopheronolactone was oxidized to tocopheronolactone by free radical products of heme-catalyzed decomposition of cumene hydroperoxide. Tocopheronloactone in cytoplasm was reduced in 9000×g supernatant fraction but not in mitochondria, so that mitochondrial peroxidation was not inhibited by tocopheronolactone itself. Antioxidativeeffect of tocopheronolactone seems to appear after the biochemical reduction of the tocopheronolactone in vivo, followed by the reaction with free radicals and peroxides.

著者

安江 政一 加藤 義成 林 玉美 榊原 仁作

出版者

公益社団法人日本薬学会

雑誌

藥學雜誌 (ISSN:00316903)

巻号頁・発行日

vol.88, no.6, pp.738-741, 1968-06-25

被引用文献数

1

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Dried leaves of Acanthopanax sciadophylloides FRANCH. et SAV. were extracted with methanol and the water-soluble part of the extract was treated successively with solutions of lead acetate, basic lead acetate, and ammoniacal alkaline lead salt, as shown in Chart 1. myo-inositol, scyllitol, kaempferitrin, and antoside were isolated and identified. The constituents of these leaves were somewhat different according to the district where the materials came from. Utkin had suggested the structure of antoside as quercetin 3 (7)-glucosido-7 (3)-rhamnoside. Relative positions of glucose and rhamnose in the antoside molecule were now determined by enzymatic cleavage of rhamnose to give quercetin 3-glucoside (isoquercitrin) (Chart 2).

著者

北島 潤一 高森 靖 田中 靖子

出版者

公益社団法人日本薬学会

雑誌

藥學雜誌 (ISSN:00316903)

巻号頁・発行日

vol.109, no.3, pp.188-191, 1989-03-25

被引用文献数

1

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In fresh leaves of Acanthopanax sciadophylloides FR. et SAV. collected in June, the following substances were identified : (-)-β-caryophyllene, trans-β-farnesene, phytol, 1-dotriacontanol, taraxerol, a mixture of stigmasterol and β-sitosterol, trans-p-coumaric acid, trans-p-coumaric acid methylester, afzerin, kaemferitrin, kaempferol 7-O-α-L-rhamnopyranoside, 3-O-β-D-galactopyranosyl kaempferol 7-O-α-L-rhamnopyranoside and quercetin 3,7-O-bis-α-L-rhamnopyranoside. On the other hand, from the fresh leaves collected in August, trans-p-coumaric acid and kaempferol were obtained as aromatic compounds, but flavonoid glycosides were not detected. It is interesting that the constituents of these leaves were quite different between June and August.