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塚本 豊久, 森田 修之, 岡田 壽太郎
1982 年 30 巻 5 号 p.
1539-1549
発行日: 1982/05/25
公開日: 2008/03/31
ジャーナル
フリー
Oxidation of glucose to gluconic acid using a catalyst consisting of glucose oxidase and catalase both immobilized on activated carbon was employed to study the liquid-solid contacting efficiency (f) in a trickle-bed reactor. The global rates of reaction were measured at 25°C and at atmospheric pressure, as a function of catalyst loading (1.0 to 9.0 g), catalyst partiole size (0.055 and 0.110 cm), superficial liquid velocity (0.044 to 0.337 cm/s), and superficial gas velocity (1.63 to 7.35 cm/s). The measured rate was considered to be the sum of the rates at the liquid-covered and gas-covered outer surfaces of catalyst particles. The value of f was determined by integrating numerically the mass balance equations for oxygen and the equation for the intrinsic rate of reaction simultaneously. The estimated value of f did not vary with catalyst loading. While f was independent of gas flow rates, it was influenced by both liquid flow rates and particle sizes. The effects of these operating parameters on f are discussed on the basis of the static and/or dynamic holdup.
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田中 均, 村田 礼子, 吉田 昭義, 林 信一
1982 年 30 巻 5 号 p.
1550-1556
発行日: 1982/05/25
公開日: 2008/03/31
ジャーナル
フリー
A new glucoside, sennoside G, was isolated from the leaves of Cassia angustifolia (Senna) in crystalline form and shown by chemical and physical means to be the optical antipode of sennoside A with respect to the sennidin moiety. The optical rotatory dispersion spectrum of sennidin G showed a pattern exactly opposite to that of sennidin A. Sennosides A, B and G were isomerized to each other reversibly, and were oxidized to give 8-glucosylrhein.
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佐藤 和恵, 宮坂 貞, 荒川 基一
1982 年 30 巻 5 号 p.
1557-1566
発行日: 1982/05/25
公開日: 2008/03/31
ジャーナル
フリー
On treatment with hydrazine hydrate (80%) and methylhydrazine, oxazolo [3, 2-b] pyridazinium perchlorates (I) furnish hemi-perchlorates of 4H-pyridazino [6, 1-c] [1, 2, 4] triazines (VI) and 1-methyl-4H-pyridazino [6, 1-c] [1, 2, 4] triazinium perchlorates (VIII), respectively. On reaction with phenylhydrazine by refluxing in acetonitrile, I affords an osazone (XII), a phenylazopyridazine (XIII) and its hydrazo derivative (XIV), which are also formed from N-phenylamino-6-chloro-2-phenacyl-2, 3-dihydropyridazin-3-ylideneimine phenylhydrazone (XV) by refluxing with phenylhydrazine in acetonitrile. In the reaction of I with hydrazines, it has been shown that the initial attack of the reagent always occurs at the C
8a-position to furnish various condensed pyridazine derivatives.
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小林 茂, 沖本 和人, 今倉 康宏
1982 年 30 巻 5 号 p.
1567-1573
発行日: 1982/05/25
公開日: 2008/03/31
ジャーナル
フリー
Cleavage of the methylenedioxy ring in aromatic formyl (1-3), nitro (4 and 5), and acetyl (30) compounds with N-sodium benzyloxide-benzyl alcohol in dimethyl sulfoxide gave 3-hydroxybenzene derivatives (19, 22-24, 26, 27, and 33). In the case of the acetyl compound 30, the 4-hydroxybenzene derivative (34) was also obtained as a minor product. Regioselective cleavage of the ring in aromatic compounds having electron-withdrawing groups with nucleophilic oxide anions is discussed. Cleavage of the ring in 1-5 and 30 with 2N sodium methoxide in dimethyl sulfoxide-dimethylformamide was found to be useful for the praotical preparation of 3-hydroxybenzene derivatives (6-10 and 31).
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大川 原正, 松田 隆至, 野口 芳秀, 古川 潮
1982 年 30 巻 5 号 p.
1574-1578
発行日: 1982/05/25
公開日: 2008/03/31
ジャーナル
フリー
A one-pot synthesis of β-lactams (4) was successfully achieved by the reaction of β-haloacyl chlorides (1) with α-amino acids (2) in aqueous 5% sodium hydroxide solution in the absence of phase transfer catalyst in yields of 43-91%.
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町田 実, 武智 春子, 金岡 祐一
1982 年 30 巻 5 号 p.
1579-1587
発行日: 1982/05/25
公開日: 2008/03/31
ジャーナル
フリー
Upon irradiation, a homologous series of N-[ω-(methylanilino) alkyl] phthalimides 5, having a nonconjugated bichromopholic system, undergoes regioselective remote photooyclization to give medium- to large-sized (up to twenty-two-membered) diazacyclols 6.
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山田 幸一郎, 武田 幹男, 伊藤 信夫, 海野 徳英, 池沢 一郎, 清本 昭夫, 青江 啓一, 小寺 啓司, 岩隈 建男
1982 年 30 巻 5 号 p.
1588-1593
発行日: 1982/05/25
公開日: 2008/03/31
ジャーナル
フリー
Racemic 5, 7-dihydroxy-1-(3, 4, 5-trimethoxybenzyl)-1, 2, 3, 4-tetrahydroisoquinoline [(±) -1], a positional isomer of trimetoquinol (TMQ) with respect to its dihydroxy moiety, has been optically resolved. The bronchodilating activity in anesthetized cats (i.v. administration) was found to reside in the levorotatory enantiomer [(-) -1]. The absolute stereochemistry of the active enantiomer [(-) -1] was determined to be S by X-ray crystallographic analysis.
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石川 忠興, 大和 正利
1982 年 30 巻 5 号 p.
1594-1601
発行日: 1982/05/25
公開日: 2008/03/31
ジャーナル
フリー
Active methylene compounds, diethyl malonate, α-tetralone, dimedone, acetyl-acetone, malononitrile, and diketene, were reacted with 1-ethoxyisochroman (1) to give the corresponding 1-substituted isochroman derivatives, 4, 5, 6, 7, 8, 9, 10, and 11, respectively. When 4 was treated with sodium ethoxide or potassium tert-butoxide, ethyl 1, 4-dihydro-2-naphthoate (14a), ethyl 1, 2-dihydro-2-naphthoate (14b), and ethyl 2-naphthoate (13) were obtained. On the other hand, the reaction of 2-(1-isochromanyl) cyclohexanone (3) with potassium tert-butoxide afforded 9-formyl-1, 2, 3, 4-tetrahydroanthracene (20) and 1, 2, 3, 4, 9, 10-hexahydroanthracene (21). The conversion mechanisms of 1-substituted isochromans (2, 3, 4, and 7) into naphthalenes (13, 14a, b, and 18) and 1, 2, 3, 4-tetrahydroanthracenes (20 and 21) are proposed.
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黒柳 正典, 山本 容子, 福島 清吾, 上野 明, 野呂 忠敬, 宮瀬 敏男
1982 年 30 巻 5 号 p.
1602-1608
発行日: 1982/05/25
公開日: 2008/03/31
ジャーナル
フリー
A new cyclobutane derivative, which may be formed from dehydrokawain by [2+2] cycloaddition, named compound B (8a), mp 226-227°C, C
28H
24O
6, and a new flavanonol, named compound C (10a), mp 142-143°C, C
17H
14O
6, together with pinobanksin (1a), taxifolin (2a), quercetin-3β-D-glucopyranoside 2"-gallate (3), pinosylvin (4a), methyl gallate (5a), dehydrokawain (6) and compound A (7a) were isolated from Polygonum nodosum (Polygonaceae). The structures of the new compounds, 8a and 10a, were established to be rel-1, trans-3-bis-(4-methoxy-2-oxopyran-6-yl)-cis-2, trans-4-diphenyl cyclobutane and (2R, 3R)-3-hydroxy-5-methoxy-6, 7-methylenedioxy-flavanone, respectively, on the basis of physicochemical evidence. The structure of 7a was also established to be rel-(1R, 6S, 7S, 8S)-5-methoxy-7-phenyl-8-(4-methoxy-2-oxopyran-6-yl)-1-(E) styryl-2-oxabicyclo-[4, 2, 0]-oct-4-en-3-one and this compound was found to be identical with aniba-dimer-A.
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関田 節子, 義平 邦利, 名取 信策, 宇田川 俊一, 坂部 フミ, 倉田 浩, 梅田 誠
1982 年 30 巻 5 号 p.
1609-1617
発行日: 1982/05/25
公開日: 2008/03/31
ジャーナル
フリー
Bioproduction of chaetoglobosins, novel type cytochalasans, by Chaetomium spp. was examined. Details of the culture conditions and methods for separation of the metabolites of Chaetomium globosum are presented. Some cytological effects of chaetoglobosins were also mentioned.
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関田 節子, 義平 邦利, 名取 信策, 桑野 晴光
1982 年 30 巻 5 号 p.
1618-1628
発行日: 1982/05/25
公開日: 2008/03/31
ジャーナル
フリー
The structures (Chart 7) of chaetoglobosins A, B, and D, 10-(indol-3-yl)-[13] cytochalasans, were elucidated by isomerization reactions and physical method including precise
1H-NMR decoupling experiments.
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関田 節子, 義平 邦利, 名取 信策, 桑野 晴光
1982 年 30 巻 5 号 p.
1629-1638
発行日: 1982/05/25
公開日: 2008/03/31
ジャーナル
フリー
The structures (Chart 1) of chaetoglobosins C, E, F, G, and J, 10-(indol-3-yl)-[13] cytochalasans, were established on the basis of physical data, especially
1H-NMR, and chemical correlations. The stereo-structural features of chaetoglobosins are discussed.
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佐藤 [やす]彦, 仲井 英雄, 和田 征夫, 荻原 弘, 溝口 富茂, 右田 能尋, 畑中 保丸, 金岡 祐一
1982 年 30 巻 5 号 p.
1639-1645
発行日: 1982/05/25
公開日: 2008/03/31
ジャーナル
フリー
Photolysis of N-ω-alkoxyalkylphthalimides 1 gave the intramolecularly cyclized compounds, oxazolo [4, 3-a] isoindoles 2a-g, pyrrolo [2, 1-a] isoindoles 6i-j, oxazolo [4, 3-a]-isoindole-1-spiro-1'-cycloalkanes 2k-n and 3, 4-dihydro-2-benzazepine-1, 5 (2H)-dione 3, via δ-hydrogen abstraction and/or two-fold Norrish type II processes.
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野口 芳秀, 磯田 匡宣, 黒木 研吉, 古川 潮
1982 年 30 巻 5 号 p.
1646-1652
発行日: 1982/05/25
公開日: 2008/03/31
ジャーナル
フリー
One-pot syntheses of sulfinates, sulfinamides, and thiosulfinates by O-, N-, and S-sulfinylations of alcohols, amines, and thiols with p-toluenesulfinic acid in the presence of various activating reagents, phenyl phosphorodichloridate (1), diphenyl phosphoro-chloridate (2), triphenylphosphine N-chlorosuccinimide (NCS) (3), and 3-(phthalimidoxy)-1, 2-benzoisothiazole 1, 1-dioxide (4), were investigated. All of these reagents were reasonably effective for O-and S-sulfinylation, but ineffective for N-sulfinylation. Among them, the reagents 1 and 2 were slightly more efficient than the others.
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浪越 通夫, 佐崎 敬三, 小磯 邦子, 福島 和貴, 岩崎 成夫, 野副 重男, 奥田 重信
1982 年 30 巻 5 号 p.
1653-1657
発行日: 1982/05/25
公開日: 2008/03/31
ジャーナル
フリー
Azalomycin F
4a (C
56H
95N
3O
17), an antibiotic produced by Streptomyces hygroscopicus var. azalomyceticus, was purified and its physicochemical properties were determined. Partial strutures of this compound were elucidated from its spectral data.
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浪越 通夫, 岩崎 成夫, 佐崎 敬三, 矢野 美弦, 福島 和貴, 野副 重男, 奥田 重信
1982 年 30 巻 5 号 p.
1658-1668
発行日: 1982/05/25
公開日: 2008/03/31
ジャーナル
フリー
Degradations of azalomycin F
4a were carried out, and the structures of the products were determined.
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岩崎 成夫, 浪越 通夫, 佐崎 敬三, 矢野 美弦, 福島 和貴, 野副 重男, 奥田 重信
1982 年 30 巻 5 号 p.
1669-1673
発行日: 1982/05/25
公開日: 2008/03/31
ジャーナル
フリー
The skeletal structure of azalomycin F
4a (1) was determined on the basis of available data about the physicochemical properties of F
4a and about the structures of the degradation products of this compound and of its derivatives. The structure was found to consist of a 36-membered lactone ring bearing multiple hydroxy functions, a diene and a dienoic ester group, as well as a side chain with an N-methylguanidine moiety as its terminal. One of the hydroxyl groups on the lactone ring forms a hemiketal ring with the keto group on a ring carbon, and another hydroxyl group forms a hemiester with a malonic acid moiety.
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JEAN-CHARLES LANCELOT, JEAN-MARIE GAZENGEL, SYLVAIN RAULT, MAX ROBBA
1982 年 30 巻 5 号 p.
1674-1679
発行日: 1982/05/25
公開日: 2008/03/31
ジャーナル
フリー
Synthesis of pyrrolo [1', 2' : 1, 2] pyrazino [6, 5-c] carbazole derivatives is described starting from 3-amino-4, 6-dinitro-9-ethylcarbazole (1). The pyrrole ring is obtained by reaction with 2, 5-dimethoxytetrahydrofuran. Cyclization of the pyrazine ring is achieved after reduction of the nitro grouping by intramolecular cyclization of 4, 6-diamino-9-ethyl-3-(1-pyrrolyl) carbazole derivatives.
1H nuclear magnetic resonance spectra are studied.
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/ , 佐伯 清太郎, 浜名 政和, MASATOMO HAMANA
1982 年 30 巻 5 号 p.
1680-1691
発行日: 1982/05/25
公開日: 2008/03/31
ジャーナル
フリー
Reactions of quinoline, lepidine, 4-chloro-, 4-methoxy- and 4-morpholino-quinoline 1-oxides (1a-e) with Meldrum's acid (2) in acetic anhydride smoothly occurred at room temperature to afford the corresponding 5-(2-quinolyl)-Meldrum's aoids (3a-e) in good yields. On the other hand, when the reactions were carried out in dimethylformamide containing 1.2 eq acetic anhydride the N-ylides (4a-e) were produced ; while the reactions of 1a, d, e yielded only N-ylides 4a, d, e, 4b, c were formed along with smaller amounts of 3b, c in the reactions of 1b, c. 3-Bromoquinoline 1-oxide (1f) gave only the N-ylide (4f) and isoquinoline 2-oxide (6) gave the 1-substituted isoquinoline (7) independently of the reaction conditions. Further, 5-alkyl-Meldrum's acids (8a-c) also reacted readily with 1a in acetic anhydride to give the corresponding 2-substituted quinolines (9a-c) in good yields. Heating of 3a, b with conc. hydrochloric acid, 10% hydrochloric acid or methanol containing 10% hydrogen chloride gave 2-methylquinolines (10a, b), 2-quinolineacetic acids (11a, b) or their methyl esters (12a, b), respectively. Similarly, 9a-c afforded 2-alkylquinolines (14a-c) in good yields upon being refluxed with conc. hydrochloric acid.
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田村 恭光, 福森 敏, 和田 昭盛, 奥山 繁広, 安立 順子, 北 泰行
1982 年 30 巻 5 号 p.
1692-1696
発行日: 1982/05/25
公開日: 2008/03/31
ジャーナル
フリー
The photochemical behavior of a number of 2-acyl-3-alkylamino-5, 5-dimethyl-2-cyclohexen-1-ones has been investigated. Irradiation of these systems resulted in δ-hydrogen abstraction by the excited carbonyl oxygen to form a biradical intermediate, which produces the dealkylation product.
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船越 奨, 矢島 治明
1982 年 30 巻 5 号 p.
1697-1705
発行日: 1982/05/25
公開日: 2008/03/31
ジャーナル
フリー
As a starting material for the synthesis of human parathyroid hormone (1-38), a C-terminal-protected eicosapeptide ester (positions 19-38) was synthesized by successive condensation of four peptide fragments; (positions 29-38), (25-28), (22-24) and (19-21).
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船越 奨, 藤井 信孝, 矢島 治明, 滋野 長平, 山本 逸雄, 森田 陸司, 鳥塚 完爾
1982 年 30 巻 5 号 p.
1706-1717
発行日: 1982/05/25
公開日: 2008/03/31
ジャーナル
フリー
The octatriacontapeptide corresponding to positions 1 to 38 of human parathyroid hormone (hPTH), a half of the whole molecule, was synthesized by assembling 9 peptide fragments in a conventional manner. Arg (mesitylene-2-sulfonyl), a new arginine derivative bearing an acid-labile protecting group, was employed in combination with a new deprotecting procedure with 1 M trifluoromethanesulfonic acid-thioanisole in TFA. The synthetic peptide exhibited an activity of 1400 IU/mg when assayed by the mouse bone adenyl cyclase activity assay.
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的場 勝英, 柴田 美穂子, 山崎 高應
1982 年 30 巻 5 号 p.
1718-1721
発行日: 1982/05/25
公開日: 2008/03/31
ジャーナル
フリー
Quinoline N-oxide was treated with 1H-pyrrole in the presence of acetic anhydride to give 2-(2 [1H] pyrrolyl) quinoline (Ib) in 37.4% yield. In the reaction of Ib and 2-chloroethyl tosylate (V) in acetone catalyzed by potassium hydroxide, 2-(1-(2-tosyloxyethyl)-2 [1H]-pyrrolyl) quinoline (Ic) was obtained. Ic was unstable and cyclized gradually to a quaternary tosylate (VIa), which was reduced with sodium borohydride in methanol to 9, 13-diazagona-1, 3, 5 (10), 14, 16-pentaene (VII), which was identified as its picrolonate.
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本庄 紀子, 新矢 時寛, 後藤 良宣
1982 年 30 巻 5 号 p.
1722-1730
発行日: 1982/05/25
公開日: 2008/03/31
ジャーナル
フリー
The reactions of 2, 4- (Ia-d) and 2, 5-disubstituted thiazole 3-oxides (Ie-f) with aryl isocyanates (II) were studied. While the reactions of Ia-d with II proceeded smoothly to give bis (5-imidazolyl) disulfides (IV), those of Ie-f with II did not take place. The structures of IV were deduced from their chemical behavior and spectral data. The reaction mechanism of Ia-d with II is discussed.
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山本 豊, 柳 顕彦
1982 年 30 巻 5 号 p.
1731-1737
発行日: 1982/05/25
公開日: 2008/03/31
ジャーナル
フリー
Trimethylstannyl and bis (trimethylstannyl) derivatives of pyridine, quinoline, and isoquinoline were prepared from the corresponding halo and dihalo (chloro or bromo) derivatives and trimethylstannyl sodium, which was generated in situ from chlorotrimethyl-stannane and sodium. These stannyl derivatives readily underwent iododestannation on treatment with iodine to produce the corresponding iodo and diiodo derivatives of pyridine, quinoline, and isoquinoline, respectively, in good yields.
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船越 奨, 矢島 治明, 滋野 長平, 山本 逸雄, 森田 陸司, 鳥塚 完爾
1982 年 30 巻 5 号 p.
1738-1746
発行日: 1982/05/25
公開日: 2008/03/31
ジャーナル
フリー
The tetratriacontapeptide amide corresponding to positions 1 to 34 of human parathyroid hormone, H-(hPTH 1-34)-NH
2, was synthesized by the solution method. As a deprotecting reagent, 1M trifluoromethanesulfonic acid-thioanisole in trifluoroacetic acid was employed. When mouse bone adenyl cyclase activity was measured, our synthetic active fragment of human PTH exhibited an activity of 3380-4400 IU/mg.
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粕谷 浩次, 神田 昭一, 岬 哲夫
1982 年 30 巻 5 号 p.
1747-1752
発行日: 1982/05/25
公開日: 2008/03/31
ジャーナル
フリー
A study on the determination of sodium liothyronine in tablets by colorimetry is described. The method is based on the iodine-starch (potato) reaction after ignition of the sample with potassium carbonate. For the ignition procedure, effeotive mixing of the sample and potassium carbonate, each previously pulverized, in an agate mortar was essential if reproducible results were to be obtained. The conditions of the iodine-starch reaction were optimized for application to a dosage level as low as 5 μg of sodium liothyronine in a tablet. The accuracy and recovery of the proposed method are satisfactory for practical pharmaceutical analysis.
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金木 弘之, 田中 光也
1982 年 30 巻 5 号 p.
1753-1759
発行日: 1982/05/25
公開日: 2008/03/31
ジャーナル
フリー
Adsorption of β-galactosidase (EC 3. 2. 1. 23), β-glucosidase (EC 3. 2. 1. 21) and β-acetyl-glucosaminidase (EC 3. 2. 1. 30) on agarose substituted with N-(ε-aminohexanoyl)-β-D-galactosylamine, -β-D-glucosylamine, -2-acetamido-2-deoxy-β-D-glucosylamine and -β-D-mannosylamine was studied. All the glycosidases were adsorbed only at low buffer concentration. Although the adsorptions of Taka-diastase and Sanactase glycosidases were non-biospecific, the adsorption required the presence of the glycone as a ligand and the elution patterns in column chromatography were affected by variation of the glycone moiety of the adsorbent. The adsorptions of the enzymes on galactosylamine-agarose were prevented by low concentrations of hexoses and pentoses. The adsorption and desorption of emulsin glycosidase were apparently biospecific considering that the enzyme protein has one binding site for glucoside and one for galactoside, although the biospecificity was inexplicable in view of the large K
1 values of the spacerligand compounds.
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川野 博子, 尾谷 三枝子, 竹山 恵子, 河合 裕一, 真弓 忠範, 濱 尭夫
1982 年 30 巻 5 号 p.
1760-1765
発行日: 1982/05/25
公開日: 2008/03/31
ジャーナル
フリー
(1) Ergothioneine is contained as a component of the organella membranes in the rat liver, and is liberated by heat treatment or dithiothreitol treatment. The amount of bound form increases with aging up to 11 weeks of age, and then decreases. All of the ergothioneine measured by the normal determination procedures can be considered to be free form. (2) Ergothioneine is bound to proteins in the blood plasma, but is present in free form in erythrocytes. (3) Biosynthesis of ergothioneine from amino acids in rats was not detectable. Ergothioneine is ingested from the diet and accumulated in the body. (4) When dietary ergothioneine is restricted for 18 weeks, the amount in the liver falls to a threshold value but apparently does not fall further, and no deficiency symptoms are observed. (5) Experimental ergothioneine-free rats were successfully produced in the second generation (born to parent rats fed on ergothioneine-free diet).
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有地 英子, 木村 善行, 奥田 拓道, 馬場 きみ江, 小澤 貢, 有地 滋
1982 年 30 巻 5 号 p.
1766-1770
発行日: 1982/05/25
公開日: 2008/03/31
ジャーナル
フリー
The effects of the roots of Polygonum cuspidatum SIEB. et ZUCC. ("Kojo-kon" or "Itadori-kon" in Japanese) and its stilbene components (resveratrol and piceid) on lipid metabolism in rats and mice (higher animals) were investigated. Resveratrol and piceid inhibited the deposition of triglyceride and cholesterol in the liver of rats fed corn oil-cholesterol-cholic acid mixture. Piceid reduced the serum triglyceride and low density lipoprotein-cholesterol (LDL-ch) levels, and atherogenic index [total cholesterolhigh density lipoprotein-cholesterol (HDL-ch)/HDL-ch] in the oil mixture-fed rats. It was found that intraperitoneal or oral administration of resveratrol or piceid reduced triglyceride synthesis from
14C-palmitate in the liver of mice. In contrast, these stilbene components did not affect hormone-induced lipolysis in fat cells from rat eqididymal adipose tissue.
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松田 兆史, 宮崎 匡輔, 藤本 幸男, 法島 義男, 守屋 寛
1982 年 30 巻 5 号 p.
1771-1775
発行日: 1982/05/25
公開日: 2008/03/31
ジャーナル
フリー
The substrate specifioities of some glandular and plasma kallikreins, bovine trypsin and plasmin, and boar acrosin were investigated using five tripeptidyl-p-nitroanilides and ten arginine and lysine ester derivatives as substrates. Of the substrates examined, N-α-benzoyl-L-arginine methyl and ethyl esters (Bz-Arg-Me and Bz-Arg-Et) and N-α-acetyl-L-arginine methyl ester (Ac-Arg-Me) were the most effective for the pancreatic and intestinal kallikreins, while N-α-tosyl-L-arginine methyl ester (Tos-Arg-Me) and Bz-Arg-Me were effectives as substrates for the human salivary and guinea-pig coagulating gland kallikreins, respectively. Ac-Arg-Me and N-α-acetyl-glycyl-L-lysine methyl ester (Ac-Gly-Lys-Me) were also good substrates for the boar acrosin. All of the tripeptidyl-p-nitroanilide substrates examined were hydrolyzed relatively ineffeotively by glandular kallikreins and boar acrosin. However, D-valyl-L-leucyl-L-arginine-p-nitroanilide (Val-Leu-Arg-pNA) and D-prolyl-L-phenylalanyl-L-arginine-p-nitroanilide (Pro-Phe-Arg-pNA) were found to be moderately useful substrates for various kallikreins and related enzymes.
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安孫子 敬, 関野 宏
1982 年 30 巻 5 号 p.
1776-1783
発行日: 1982/05/25
公開日: 2008/03/31
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フリー
We have replaced the Ac-Ser residue of bovine thymosin α
1 (position 1) with Ser in order to examine the resulting change in immunological effect on the low resette-forming capacity with sheep erythrocytes of cells from a lipoid nephrosis patient. The deacetyl-thymosin α
1 was synthesized by the solution method. For the synthesis of the protected octaeicosapeptide, five peptide fragments were prepared by the stepwise elongation method with N-ethoxycarbonyl-2-ethoxy-1, 2-dihydroquinoline as a coupling reagent. The condensations of the fragments were achieved by Rudinger's azide procedure. Finally, all protecting groups were removed by HF treatment followed by catalytic hydrogenation. The in vitro addition of the synthetic deacetyl-thymosin α
1 at a dose of 100 μg/ml was able to restore the rosette-forming capaoity with sheep erythrocytes of lipoid nephrosis cells to normal levels. Our preparations of deacetyl-thymosin α
1 and thymosin α
1 were found to be equally active in cases of lipoid nephrosis.
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山田 陽城, 大島 赴夫, 宮崎 利夫
1982 年 30 巻 5 号 p.
1784-1791
発行日: 1982/05/25
公開日: 2008/03/31
ジャーナル
フリー
The extracellular polysaccharide fraction of Absidia cylindrospora (ACE), which has been used as an immunogen in immunochemical studies of Mucorales polysaccharide, showed marked heterogeneity of its mannoheteroglycans. ACE was classified into mannantype and fucomannan-type fraotions of sequential separation using affinity chromatography on concanavalin-A (con-A) Sepharose, ion exchange chromatography on diethylaminoethyl Sephadex, zone electrophoresis and gel filtration on Sephadex G-100. Serological reactivity to anti-ACE appeared in the con-A bound and high-mannose content fraction. By methylation analysis and proton magnetic resonanoe studies of each polysaccharide, it was confirmed that the fucomannan-type fraction mainly consisted of α (1→6) linked mannopyranosyl residues and fucopyranosyl non-reducing ends, whereas the mannan-type fraction consisted of (1→2) linked mannopyranosyl residues and mannopyranosyl non-reducing ends. These results were similar to those for mannoheteroglycans from A. cylindrospora mycelium. These results indicated that ACE of the immunogen contained serologically active mannan and fucomannan.
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木村 善行, 奥田 拓道, 谿 忠人, 有地 滋
1982 年 30 巻 5 号 p.
1792-1795
発行日: 1982/05/25
公開日: 2008/03/31
ジャーナル
フリー
Compounds (I and II) which inhibited lipid peroxides formation (in in vitro experiments) were isolated together with various flavonoids from the roots of Scutellaria baicalensis GEORGI. From the analytical and physical data, compounds I and II were identified as (2S)-2', 5, 6', 7-tetrahydroxy-flavanone and (2R, 3R)-2', 3, 5, 6', 7-pentahydroxy-flavanone, respectively. Compound II inhibited the lipid peroxide formation by Fe
2+ and ascorbic acid. Compounds I and II inhibited the lipid peroxide formation induced by adenosine diphosphate and reduced nicotinamide adenine dinucleotide phosphate in rat liver homogenate.
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仲井 由宣, 山本 恵司, 寺田 勝英, 堀部 秀俊
1982 年 30 巻 5 号 p.
1796-1802
発行日: 1982/05/25
公開日: 2008/03/31
ジャーナル
フリー
The partition coefficients of p-nitrophenol between 0.05N HCl and CHCl
3 were measured with or without tri-O-methyl-β-cyclodextrin (methyl-β-CD) at 15.5, 20.0, and 25.0°C. The partition coefficients increased linearly with methyl-β-CD concentration. In the presence of 3.00×10
-2M methyl-β-CD, the value was about 2.5 times larger than that measured in the absence of methyl-β-CD. Methyl-β-CD was not detected in the aqueous phase by polarimetry, and most of the methyl-β-CD molecules were present in the CHCl
3 phase. The increase of the partition coefficients can be interpreted in terms of 1 : 1 complex formation between methyl-β-CD and p-nitrophenol. The complexes of methyl-β-CD and p-nitrophenol in the aqueous solution and the CHCl
3 solution were studied quantitatively by ultraviolet absorption measurements. The formation of inclusion complex in D
2O was also investigated by proton magnetic resonance spectroscopy.
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佐藤 幸夫, 横尾 三千子, 高橋 秀一, 高橋 威夫
1982 年 30 巻 5 号 p.
1803-1810
発行日: 1982/05/25
公開日: 2008/03/31
ジャーナル
フリー
The photolysis of riboflavine with a low-intensity light source was investigated. Biphasic rate curves were obtained ; that is, an induction period was observed before the reaction rate reached its maximum value. The duration of the initial phase depended on the temperature and the concentration of riboflavine. The molecular associations of isoalloxazine nuclei may be responsible for such biphasic photolysis. The addition of xanthine derivatives to an aqueous solution of riboflavine reduced the rate of photolysis. Although the rate was reduced most effectively by theophylline, it appears that the interaction between riboflavine and theophylline differs considerably from that in other systems, i.e., caffeine, theobromine, and hypoxanthine systems.
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仲井 由宣, 福岡 英平, 中島 新一郎, 森田 正美
1982 年 30 巻 5 号 p.
1811-1818
発行日: 1982/05/25
公開日: 2008/03/31
ジャーナル
フリー
A computer program for the determination of the degree of crystallinity and the disorder parameter in lactose based on Ruland's method, one of the X-ray diffraction methods, was written. The correctness of the program was confirmed by comparing the computed results with those caloulated by the usual Ruland's method and Herman's method using several samples of lactose with different crystallinities. A series of integral upper limits was determined by rearranging the equation presented by Ruland. The degree of crystallinity and the disorder parameter in crystalline lactose which was used as the 100% crystalline standard in the other methods were estimated as ca. 70% and ca. 3.5 A
2, respectively. The effects of the normalization constant on the calculated results were rather small. However, the effects of integral upper limits on those results were large. A series of integral upper limits seems to be a very important factor for crystallinity determination by Ruland's method.
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今村 順茂, 有森 和彦, 園田 正信, 一番ヶ瀬 尚
1982 年 30 巻 5 号 p.
1819-1823
発行日: 1982/05/25
公開日: 2008/03/31
ジャーナル
フリー
The effect of salicylic acid on the hypoglycemic activity and blood carbutamide concentration after oral administration of carbutamide was investigated in rabbits. Salicylic acid was found to enhance the hypoglycemic activity, while on the other hand, it was found to deorease the blood carbutamide concentration. Salicylic acid markedly decreased the in vivo binding of carbutamide to rabbit plasma proteins, and caused a significant increase in the plasma concentration of unbound carbutamide, despite a significant decrease in the plasma concentration of total carbutamide. These results lead us to conclude that the displacement of carbutamide from its plasma protein binding sites by salicylic acid produces both the enhanced hypoglycemic activity and the decreased blood carbutamide concentration.
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小島 宏之, 際田 弘志, 加藤 百合子
1982 年 30 巻 5 号 p.
1824-1830
発行日: 1982/05/25
公開日: 2008/03/31
ジャーナル
フリー
The dissolution properties and physico-chemical properties of three polymorphic forms of (α-bromoisovaleryl) urea are reported. Form II transformed to form I repidly in water at 37°C, but this transition was delayed by 0.25% gelatin. The solubility of form II was 50% higher than that form I. The transition temperatures of form II to form I, and form III to form I were 70.2°C and 11.4°C, respectively, as determined by measurements of dissolution rates and solubilities. The enthalpy values, ΔH
sol and ΔH
diss, of the polymorphs were calculated. The thermodynamic values of form II and form III for the conversion to form I were calculated from these values, i.e. heats of transition (ΔH
trans), differences of free energy at 37°C (ΔG
T), differences of entropy at 37°C (ΔS
T), and entropy changes at transition temperatures (ΔS
trans). The differences of free energy, which may affect the bioavaliabilities of polymorphs, and the ΔS
trans values were found to be fairly small.
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小島 宏之, 新村 均, 際田 弘志, 加藤 百合子
1982 年 30 巻 5 号 p.
1831-1836
発行日: 1982/05/25
公開日: 2008/03/31
ジャーナル
フリー
A simple and sensitive determination method for (α-bromoisovaleryl) urea in plasma was developed by using gas-liquid chromatography with an electron capture detector, (α-Bromoisovaleryl) urea was extracted from plasma with ethyl ether and ethanol in a ratio of 5 : 1 (volume); the recovery was 97.5%. The plasma concentrations were determined by the internal standard GLC-ECD method without further clean-up by column chromatography. The detection limit was about 0.5 μg/ml in 0.1 ml plasma. In order to determine the effect of polymorphism (form I, form II, and form III) of (α-bromoisovaleryl)-urea on the bioavailiabilities, plasma levels in rats after intraduodenal administration were investigated. The areas under the blood concentration curves (AUC) and the mean dissolution times (MDT) were calculated to determine the extent of bioavailability and the rate of bioavailability, respectively. The results indicated that the polymorphic states of (α-bromoisovaleryl) urea did not show significantly different bioavailabilities.
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川島 嘉明, / 内藤 雅文, 竹中 英雄, HIDEO TAKENAKA
1982 年 30 巻 5 号 p.
1837-1843
発行日: 1982/05/25
公開日: 2008/03/31
ジャーナル
フリー
Sodium theophylline monohydrate was precipitated from ethylene diamine solution of theophylline by adding aqueous sodium chloride solution to the system with or without ethanol. The dried precipitates were redispersed in the filtrate without ethanol and were agglomerated with water liberated from the system by adding chloroform and ethanol to the filtrate with agitation. The sedimentation velocity of the agglomerated precipitates and their sedimentation volume at equilibrium were investigated to identify a suitable composition of the medium for agglomeration by gradually increasing the chloroform fraction in the medium. The sedimentation volume slightly increased before dropping drastically at 41% chloroform fraction, at which the precipitates were microagglomerated after passing through a flock stage of high bulk volume. At 56% chloroform fraction, the sedimentation volume sharply decreased again because of secondary agglomeration of the microagglomerates. The sedimentation velocity of the agglomerated precipitates increased with increasing chloroform fraction of the medium in the range above 41%. The agglomerate size increased drastically when the secondary agglomeration occurred. No changes in the sizes and shapes of the elemental crystals were found even after agglomeration. A triangular phase diagram was obtained to described a suitable composition of the medium for agglomeration. It was also proved that simultaneous agglomeration with crystallization was possible in a mixture of four liquids, i.e. ethylenediamine solution of theophylline, aqueous solution of sodium chloride, ethanol and chloroform, with a suitable composition.
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斎藤 洋, 上山 敬司, 中 信子, 八木 純, 岡本 敏彦
1982 年 30 巻 5 号 p.
1844-1850
発行日: 1982/05/25
公開日: 2008/03/31
ジャーナル
フリー
Pharmacological properties, especially, analgesic, antipyretio, antiinflammatory, sedative and antidiuretic activities, of ignavine, one of the main alkaloids in Aconite root, are discussed on the basis of the results of blind screening. Ignavine showed antiinflammatory activity in the acetic acid-induced writhing and carrageenin paw edema tests at doses of 50 and 100 mg/kg p.o., which did not produce undesirable effects such as sedation, motor incoordination, muscle relaxation, hypothermia, ulceration or antidiuresis. Pharmacological properties of mesaconitine are also discussed; mesaconitine showed antiinflammatory, antipyretic and weak sedative activities.
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野原 稔弘, 伊藤 淑子, 清家 治子, 古森 徹哉, 森山 峰博, 五味田 裕, 川崎 敏男
1982 年 30 巻 5 号 p.
1851-1856
発行日: 1982/05/25
公開日: 2008/03/31
ジャーナル
フリー
Seven compounds have been isolated from whole plants of Paris quadriforia L. and their chemical structures characterized as follows ; pennogenin (1), pennogenin 3-O-α-L-rhamnopyranosyl-(1→2)-[α-L-rhamnopyranosyl-(1→4)]-β-D-glucopyranoside (2), pennogenin 3-O-α-L-rhamnopyranosyl-(1→4)-α-L-rhamnopyranosyl-(1→4)-[α-L-rhamno-pyranosyl-(1→2)]-β-D-glucopyranoside (3), 22-hydroxyfurostanol 3, 26-O-bisglycoside corresponding to 3 (4), 1-dehydrotrillenogenin (5), ecdysterone (10) and kaempferol 3-O-β-D-glucopyranosyl-(1→4)-β-D-glucopyranoside (11). In addition, a stimulative effect of 3, one of the major components, on isolated bull frog heart was observed.
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/ 橋本 祐一, 首藤 紘一, 岡本 敏彦, TOSHIHIKO OKAMOTO
1982 年 30 巻 5 号 p.
1857-1859
発行日: 1982/05/25
公開日: 2008/03/31
ジャーナル
フリー
Two potent mutagens, 2-amino-3-methylimidazo [4, 5-f] quinoline and 2-amino-3, 4-dimethylimidazo [4, 5-f] quinoline, were synthesized.
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宮下 修, 松村 興一, 島津 浩, 橋本 直人
1982 年 30 巻 5 号 p.
1860-1864
発行日: 1982/05/25
公開日: 2008/03/31
ジャーナル
フリー
1-Acyl- and 1, 3-diacyl-5-alkoxycarbonyl-5-fluoro-6-substituted-5, 6-dihydrouracils were synthesized for study as a class of pro-drugs of 5-fluorouracil (5-FU).
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丹治 健一, 坂本 尚夫, 山中 宏
1982 年 30 巻 5 号 p.
1865-1867
発行日: 1982/05/25
公開日: 2008/03/31
ジャーナル
フリー
In the palladium-catalyzed cross-coupling reaction of halopyrimidines with terminal acetylenes, 2- and 4-chloropyrimidines can be used as starting compounds, though their reactivity is inferior to that of 2- and 4-iodopyrimidines. The conversion of the 2- and 4-alkynylpyrimidines thus obtained into the corresponding pyrimidinylmethyl ketones was successfully achieved by consecutive treatment with piperidine and oxalic acid dihydrate.
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丸中 照義, 梅野 幸彦
1982 年 30 巻 5 号 p.
1868-1871
発行日: 1982/05/25
公開日: 2008/03/31
ジャーナル
フリー
5-Fluoro-5'-deoxyuridine and ethyl (±)-6-n-butoxy-5-fluoro-5, 6-dihydrouracil-γ-5-carboxylate are new pro-drug forms of 5-fluorouracil that have been developed as antitumor agents. A gas chromatographic-mass fragmentographic determination of the active substance 5-fluorouracil in biological materials following administration of each compound was established. The detection limit for 5-fluorouracil was 1 ng/ml of plasma and 1-5 ng/g of wet weight of visceral tissues.
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田和 理市, 広瀬 信吾, 安達 健蔵
1982 年 30 巻 5 号 p.
1872-1875
発行日: 1982/05/25
公開日: 2008/03/31
ジャーナル
フリー
A method has been developed for the determination of the fraction of a single species in a binary mixture of tertiary amines, by measurement of the pseudo first-order reaction rates for decomposition of the π-complexes with tetracyanoethylene. The initial absorbances at three wavelengths (u, v and w) and their sum in a simplified complementary tristimulus colorimetry were calculated by a numerical method. The color points of the reaction solution at the initial time were calculated, so that the fraction of as single species in a mixture of tertiary amines could be evaluated.
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宇野 豊三, 奥村 一夫, 黒田 義弘
1982 年 30 巻 5 号 p.
1876-1879
発行日: 1982/05/25
公開日: 2008/03/31
ジャーナル
フリー
The structure of the red product of the Fujiwara reaction was investigated by using chloroform as a gem-polyhalogen compound. Isolation of the product followed by nuclear magnetic resonance and mass spectroscopic analysis revealed the red chromophore to be the sodium salt of N
1, N
2-bis [(1E, 3E)-4-formyl-1, 3-butadien-1-yl] formamidine. The structure of the red products formed from trichloroacetic acid and chloral hydrate were also investigated. High-performance liquid chromatography analysis and mass spectra showed that both products have the same structure as that from chloroform. Since the red product from benzotrichloride has an analogous spectrum, it is concluded that the structure of the red produots formed from the series of trichloroalkyl compounds (RCCl
3) is the nitrogenated polyene produced by the ring cleavage of two pyridine rings.
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水谷 隆治, 木村 仁美, 和木 薫子, 岡山 球美
1982 年 30 巻 5 号 p.
1880-1883
発行日: 1982/05/25
公開日: 2008/03/31
ジャーナル
フリー
The primary immune response in young adult mice to sheep red blood cells was studied by following the effects of anti-IgM or anti-Fc sera on the number of plaqueforming cells for IgM (dPFC) and IgG (iPFC) in the spleen. The number of dPFC in the case of administration of anti-IgM serum at 1 h before antigen injection was significantly decreased to 3.7±0.9/10
6 spleen cells in comparison with the value of control serum (69.0±15.7/10
6 spleen cells). However, the numbers of iPFC in the cases of both anti-IgM or control sera were similar. From these results, we suppose that progenitors of IgM-producing cells are different from progenitors of IgG-producing cells in adult mice.
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