著者
大谷 靖 川瀬 勝凡 林 敬一郎 龝本 晃 平山 宏 中村 勝一 小倉 勲
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.89, no.8, pp.1115-1118, 1969-08

Formation of azulene from hydronaphthalene by the application of Lang's method was observed when using decalin as the starting material, with single metal such as iron and Raney nickel or activated carbon as a catalyst, and the amount of the product was greater when using trans-decalin rather than cis-decalin. This is considered to be due to the difference in the distance between hydrogen atoms at 5- and 9-positions. A part of the cis isomer was found to change into the trans type when heated. There was no formation of azulene when using tetralin as the starting material. The spectra of azulene solution after irradiation of ultraviolet or γ-rays showed smaller change in absorption intensity than that of guaiazulene. Irradiation of γ-rays on azulene solution was found to produce reduction and polymerization, as in the case of guaiazulene, from the result of gas chromatographic analysis. In the case of oxygen-containing compounds, irradiation with ultraviolet or γ-rays was found to produce turbidity but isolation and identification of this product were not possible due to the minute amount formed. These irradiation experiments indicated that azulenes without a side chain were more stable than guaiazulenes.
著者
小林 和弘 織田 範一 榊原 仁作
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.103, no.2, pp.p165-172, 1983-02

Ethyl 5-hydroxybenzo [α] phenazine-6-carboxylates (IIa, b) were prepared by the condensation of ethyl 1,4-dihydro-1,4-dioxo-3-methoxy-2-naphthoate (I) with o-phenylene-diamines. Acylations and alkylations of IIa, b gave the corresponding o-acyl and alkyl compounds (IIIa-k). The reaction of IIa, b with ethanolamine gave β-hydroxyethyl-carboxamides (Va, b). Compound Va was converted into β-chlorinated compound (VIa), whose chlorine was substituted by dialkylamines to give ethylenediamine-type amides (VIIa, b, c). Compounds VIId and VIIe were obtained by the reaction of IIb with dialkylalkylenediamines. Oxidation of IIa, b afforded N-oxides (IXa, b). The antimicrobial activities of all synthetic compounds were tested by paper discagar diffusion assay. Compounds IIId, e, g, VIIa and IXa showed inhibitory activities to T. interdigitale and IXa to C. albicans.
著者
川島 嘉明
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.89, no.10, pp.1386-1391, 1969-10

Berberine was extracted from slices of Berberis thunbergii, cut into various sizes (#1-#4), with water and methanol at 37°. Results of analysis of extraction rate, indicated that the mechanism of extraction consists of washing, diffusion, and capillary extraction, and mass transfer coefficients for each mechanism were determined. Comparing with the extraction of berberine from the cortex of phellodendron, ^<3)> mass transfer coefficients were distinctly larger.
著者
山口 秀夫 有本 正生 山本 起巳子 沼田 敦
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.99, no.6, pp.p674-677, 1979-06
被引用文献数
1

Four kinds of lignans were isolated from the seeds of Hernandia ovigera L. collected in Okinawa besides the previously reported desoxypodophyllotoxin (I). Oily substance II, named bursehernin, C_<21>H_<22>O_6,was confirmed to be lignan-2 isolated from Bursera schlechtendalii. III, mp 171-173°, and IV, mp 125-126°, were determined as desoxypicropodophyllin and podorhizol obtained from Podophyllum emodi WALL. respectively. V, mp 270-275°, could not be clarified due to its small amount.
著者
安永 峻五 下村 脩
出版者
日本薬学会
雑誌
薬学雑誌 (ISSN:00316903)
巻号頁・発行日
vol.74, no.7, pp.778-780, 1954-07

In electrochromatography, five kinds of different filter paper holders were used and the velocity of migration, area of colored band, and migration distance of each position on the filter paper were measured under identical conditions so as to examine the separatory ability and equality of rate of each apparatus. It was thereby found that the best separation is effected by placing the paper in a convex form, with the middle higher, while for uniform mobility, the filter paper should be cooled directly by closely adhering the lower surface on a cooling vat.
著者
奥田 拓男 毛利 和子 寺山 香代子 樋口 恵子 波多野 力
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.99, no.5, pp.p543-545, 1979-05

Geraniin was isolated from herbs of Geranium carolinianum, G. wilfordii, G. wilfordii var. hastatum, G. sibiricum var. glabrius, G. tripartitum, and G. yoshinoi, and also from root bark of Triadica sebifera. The isolations were improved by application of droplet counter-current chromatography. Hyperin was isolated from G. carolinianum, and quercetin from G. yoshinoi.
著者
才川 勇 桃井 海秀 酒井 広志 高下 寛 大橋 俊則 南 尚 山本 芳子 福岡 義和
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.99, no.12, pp.p1207-1218, 1979-12

The stability, degradation pattern and structure of degradation products of sodium 7-[D (-)-α-(4-ethyl-2,3-dioxo-1-piperazinecarboxamido)-α-(4-hydroxyphenyl) acetamido]-3-[(1-methyl-1H-tetrazol-5-yl) thiomethyl]-3-cephem-4-carboxylate (T-1551) in aqueous solution were investigated. T-1551 was kept in various solutions in pH and μ=0.5 at 35°, its degradation was followed by HPLC. T-1551 was stable at the range of pH 4.0-7.0,slightly unstable at acid and markedly unstable at alkaline. It was confirmed that in alkaline solution, 7-[D (-)-α-[3-[2-(N-ethyl-N-oxaloamino)-ethyl] ureido]-α-(4-hydroxyphenyl) acetamido]-3-(1-methyl-1H-tetrazol-5-yl) thiomethyl-3-cephem-4-carboxylic acid (T-1551A) was produced, and that in acidic solution, 7-[D (-)-α-(4-ethyl-2,3-dioxo-1-piperazinecarboxamido)-α-(4-hydroxyphenyl) acetamido]-3-hydroxy-methyl-3-cephem-4-carboxylic acid γ-lactone (T-1551B), 7-[D (-)-α-(4-ethyl-2,3-dioxo-1-piperazinecarboxamido)-α-(4-hydroxyphenyl) acetamido]-3-hydroxymethyl-3-cephem-4-carboxylic acid (T-1551C), 5-mercapto-1-methyl-1H-tetrazole (T-1551F), 2-[2-(4-ethyl-2,3-dioxo-1-piperazinecarboxamido)-2-(4-hydroxyphenyl) acetamido]-2-[1,2,5,7-tetrahydro-7-oxo-4H-furo [3,4-d] [1,3] thiazin-2-yl] acetic acid (T-1551G), 2-[α-(4-ethyl-2,3-dioxo-1-piperazinecarboxamido)-α-(4-hydroxyphenyl) acetamidomethyl]-2,3-dihydro-5-hydroxy-methyl-6H-thiazine-4-carboxylic acid γ-lactone (T-1551H) and N-formylmethyl-D-(-)-α-(4-ethyl-2,3-dioxo-1-piperazinecarboxamido)-α-(4-hydroxyphenyl) acetamide (T-1551D) were produced, respectively.
著者
山田 敏広 山下 武彦 中村 正則 嶋村 浩 山口 東 高谷 昌弘
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.100, no.8, pp.p799-806, 1980-08

In order to obtain more hydrophylic and more potent hemostatics, 2-semicarbazono-1,2-naphthoquinone analogs with or without sulfonic acid or its salts at 4,5,6,7 or 8 position (III and IV) and 4-semicarbazido-1,2-naphthoquinone analogs (V) were prepared and their hemostatic activities and acute toxicities were examined. Among these compounds, more hydrophilic 2-semicarbazono-1,2-naphthoquinone analogs with sulfonic acid group (IIIj and IIIr) as well as less hydrophilic 2-semicarbazono-1,2-naphthoquinones without sulfonic acid group (IVa and IVh) and 4-semicarbazido-1,2-naphthoquinone analogs (Ve) showed the activity comparable to that of 2-semicarbazono-1,2-naphthoquinone (II) or carbazochrome sodium sulfonate (I) in shortening the bleeding time.
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

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
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

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
小菅 卓夫 横田 正実 長沢 道男
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.98, no.10, pp.p1370-1375, 1978-10
被引用文献数
3

Aconite root (Bushi in Japanese) from Aconitum japonicum THUMB. has long been used as one of the most important herbs as a heart stimulant, diuretic agent ; and anodyne in Chinese medichine. Isolation and identification of the cardiac principle predicted by Yakazu are described. In the isolation process, the Yagi-Hartung method using frog heart was found to be useful for pharmacological measurement of cardiac activity of the material. The material was water soluble and was fairly unstable, especilly in a basic medium, and was tightly adsorbed on charcoal, alumina, silica gel, and cellulose powder, indicating that these agents are not useful for the separation. Isolation of the material was finally achieved by the limited combination of gel filtration through Sephadex LH-20 and counter current distribution, and colorless plates, mp 260°, were obtained as HCl salt. This principle stimulates frog heart even 1 : 10^<-9> dilution, and it was designated as Higenamine. Higenamine was identified as dl-demethylcoclaurine (II) from the spectral data and by comparison with synthesized authentic sample.
著者
亀岡 弘 鄭 玉珍 宮沢 三雄
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.96, no.3, pp.p293-298, 1976-03

An essential oil was obtained in 0.11% yield by steam distillation from the fresh fruit of Canarium album RAEUSCH The oil was treated successively with 5% sodium carbonate and 5% sodium hydroxide solution, and separated into neutral, sodium carbonate-soluble, and sodium hydroxide-soluble fractions. α-Pinene, camphene, β-pinene, myrcene, limonene, 1,8-cineole, p-cymene, linalool, α-copaene, linalyl acetate, cis-p-2-menthen-1-ol, 1-terpinen-4-ol, trans-p-2-menthen-1-ol, β-caryophylene, citronellyl acetate, β-terpineol, α-terpineol, terpinyl acetate, neryl acetate, geranyl acetate, nerol, δ-cadinene, geraniol, δ-cadinol, elemol, 14 kinds of carboxylic acid, 6 kinds of phenolic compound, and alkane of C_<10> to C_<32> were identified from their infrared, mass, and nuclear magnetic resonance spectra, and by chemical methods.
著者
西岡 五夫 松尾 律子 大倉 洋甫 百瀬 勉
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.88, no.10, pp.1281-1285, 1968-10

A new colorimetric method for microdetermination of isothiocyanates was established, using 3,6-dinitrophthalic acid as a color developing agent in a potassium carbonatesodium thiosulfate solution. The reaction conditions were examined with allyl isothiocyanate as a model compound. The outline of the procedure is as follows : To 2.0 ml of allyl isothiocyanate solution (10-150 μg/ml), (dissolved in 50% ethylene glycol solution, 1.0 ml of 3,6-dinitrophthalic acid monopyridinium salt solution (0.1%), and 1.0 ml of alkaline solution (40% potassium carbonate and 30% sodium thiosulfate) are added and mixed well. The mixture is heated in a boiling water bath for exactly 10 minutes, cooled in running water, and diluted to 20.0 ml with water. The absorbance of the developed color is read at 400 mμ against the reagent blank. In this color reaction, 3,6-dinitrophthalic acid was assumed to be reduced to 3-amino-6-nitrophthalic acid by S^<2->, which was liberated from allyl isothiocyanate in the alkaline medium.
著者
井上 博之 上田 伸一 下川 徳明
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.86, no.12, pp.1202-1204, 1966-12

The detailed investigation on the bases of Swertia japonica MAKINO was carried out. Extraction of the plant with chloroform using ammonia as usual gave, gentianine and a base of m.p. 129.5〜130°. The structure of the latter was now elucidated. On the other hand, however, the extraction with methanol in the absence of ammonia as well as the treatment with methylamine gave none of these compounds. Thus, an evidence that both substances must be the artifacts produced during the extraction process was presented.
著者
永谷 康典 武藤 〓章 佐藤 宏 飯島 昌夫
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.106, no.1, pp.p41-46, 1986-01
被引用文献数
5

An improved method for the determination of hydroxyproline (Hyp) in animal tissues has been established by modifying Kivirikko's and KISO methods. This method consists of the oxidation of Hyp by the addition of chloramine T at 0°C for 2 h in 0.5 M borate buffer (pH 8.2) containing 1 M KCl. It was confirmed that Hyp was satisfactorily oxidized to an oxidation intermediate, which was stable throughout the process of the oxidation at 0°C for 2 h. The degree of color development with the colorimetric reagent in this method was 2-3 times higher than that in conventional methods, and the reproducibility was invariably good. The present method is very useful for the microanalytical determination (0.05-4 μg/tube) of Hyp.
著者
松田 秀秋 久保 道徳
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.103, no.12, pp.p1269-1277, 1983-12
被引用文献数
4

The antithrombic activities of 70% methanol extract (I) obtained from Korean red ginseng (root of Panax ginseng C.A. MEYER) were evaluated in the models of experimental disseminated intravascular coagulation (DIC) induced by endotoxin or thrombin in rats, and in the in vitro models of blood platelet aggregation, agglutination of fibrinogen and activation of fibrinolytic system. In the coagulative system, I prevented the exchanges of values of clinical examination (blood platelet, fibrinogen and prothrombin time) at a dose of 500 mg/kg in rats on DIC induced by endotoxin or thrombin. I also inhibited the formation of fibrin thrombi in the renal glomeruli on the thrombin-induced DIC in rats. In the fibrinolytic system, I was found to show fibrinolytic activity in rats as determined by the euglobulin lysis time (ELT) assay. In the in vitro experiments, incubation of I in the plasminogen-containing fibrin plate promoted activation of urokinase action.
著者
上尾 庄次郎 上田 寛一 山本 義公
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.86, no.12, pp.1172-1184, 1966-12

The structure of anhydrotaxininol, C_<20>H_<28>O_4,obtained by treatment of taxinine, a constituent of Taxus cuspidata SIEB. et ZUCC., with alcoholic sodium hydroxide, has been briefly reported in a preliminary communication.^<8)> In this paper, details of experimental results and the discussion which led to the assignment of structure III to anhydrotaxininol are presented.