巻号一覧
101 巻, 10 号
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上釜 兼人1981 年 101 巻 10 号 p. 857-873
発行日: 1981/10/25
公開日: 2008/05/30
ジャーナル フリーCyclodextrins are homologous series of cyclic oligosaccharides consisting of glucose units joined by α-1, 4 linkages. One of the important characteristics of cyclodextrins is the formation of inclusion complexes with various guest molecules in solid phase and in solution, in which the guest molecules are included in the relatively hydrophobic cavity of cyclodextrins. The present review is mainly concerned with the possible utilities of cyclodextrins in pharmaceutical fields. A number of examples such as improvements of solubility, chemical stability, bioavailability, etc. are presented. These informations will provide a rational basis for design of formulation and a means for improving efficacy of drug activity.抄録全体を表示PDF形式でダウンロード (1502K) -
大内 力男, 神戸川 明, 森 弘1981 年 101 巻 10 号 p. 874-882
発行日: 1981/10/25
公開日: 2008/05/30
ジャーナル フリーIn order to obtain specific antisera used for radioimmunoassay, 11α-succinoyloxy derivatives of 3β-hydroxy-5-androsten-17-one, 5-androstene-3β, 17β-diol, 17β-hydroxy-5α-androstan-3-one, and 3β-hydroxy-5-pregnen-20-one (13, 14, 23, and 33) were synthesized. Each compound was coupled with bovine serum albumin by mixed anhydride technique, and the complex was immunized in rabbits. The antisera thus obtained were found to be specific for the respective parent compound, except anti-17β-hydroxy-5α-androstan-3-one antiserum which showed relatively high cross reactivity to testosterone (55.1%).抄録全体を表示PDF形式でダウンロード (870K) -
大塚 紘司, 藤村 一, 沢田 徳之助, 後藤 實1981 年 101 巻 10 号 p. 883-890
発行日: 1981/10/25
公開日: 2008/05/30
ジャーナル フリーBerberine-containing plants are fairly widely distributed in the plant kingdom. From old times, they have been used for Chinese medicine or folk medicine. The Coptidis Rhizoma is especially prescribed in Chinese medicine for the purpose of antiphlogistic, analgesic, sedative, antidotal, hemostatic, and stomachic effects. Among efficacies of the medicine, the antiphlogistic effect has not been evidenced pharmacologically. We have investigated the anti-inflammatory active constituents in the rhizomes of Coptis japonica MAKINO by tracing the activity by means of the fertile egg method. Consequently, the active principles have been proved to be berberine, coptisine, jateorrhizine, and palmatine. Activity of berberine was also confirmed by means of cotton-pellet method, croton oil-granuloma pouch method, and punch method.抄録全体を表示PDF形式でダウンロード (833K) -
三由 文久1981 年 101 巻 10 号 p. 891-898
発行日: 1981/10/25
公開日: 2008/05/30
ジャーナル フリーThe phase transition, thermal isomerization and formation of a novel crystal structure out of cis-1-thioniabicyclo [4. 4. 0] decane bromide (cis-TBD-Br) and its trans isomer (trans-TBD-Br) were investigated by means of differential thermal analysis, X-ray diffraction and infrared absorption spectrometry. The cis-TBD-Br having a monoclinic C-lattice at room temperature is transformed into an orthorhombic F-lattice at 126°C. With continuous heating up to 180°C, the cis-TBD cations in this lattice are gradually isomerized into the cis and trans equilibrium state. This equilibrated compound forms a novel α-TBD-Br crystal, in which the ratio of the cis-and trans-TBD cations are approximately 3 : 2. The trans-TBD-Br having an orthorhombic C-lattice at room temperature is transformed into an orthorhombic F-lattice at 108°C, and then also isomerized into the α-TBD-Br. At room temperature, the α-TBD-Br can be kept for several days in a desiccator over silica gel. After that it gradually decomposes into its component crystals, cis-and trans-TBD-Br. As the α-TBD-Br lattice contains four formular units, C9H11SBr, the space group is restricted to one of Fmmm, Fmm2 and F222. It is concluded that, since the isomeric cis-and trans-TBD cations are distributed statistically around four equivalent positions having a site symmetry (mmm, mm2 or 222) given by the space group, these cations should have statistical orientations.抄録全体を表示PDF形式でダウンロード (806K) -
高木 修造, 山木 正枝, 井上 けい子1981 年 101 巻 10 号 p. 899-903
発行日: 1981/10/25
公開日: 2008/05/30
ジャーナル フリーThree compounds, S-III, S-IV and VI were isolated from the roots of Scutellaria baicalensis GEORGI. On the basis of chemical and spectral evidence, they were identified to be wogonin-5-β-D-glucoside, 2-(3-hydroxy-4-methoxyphenyl) ethyl 1-O-α-L-rhamnosyl-(1→3)-β-D-(4-feruloyl) glucoside and 2', 3, 5, 6', 7-pentahydroxyflavanone, respectively.抄録全体を表示PDF形式でダウンロード (547K) -
杉山 和明, 小川 孝子, 平野 弘1981 年 101 巻 10 号 p. 904-911
発行日: 1981/10/25
公開日: 2008/05/30
ジャーナル フリーIt has been found that 2-acyl-4-alkyl-4H-1, 4-thiazine derivatives (1a-f) were oxidized to their sulfoxides (2a-f) by treatment with sodium nitrite in acetic acid under mild conditions. However, this reaction was unable to be applied to thiazine derivatives such as 3a, 3b, and 4, lacking an acyl group at the 2-position and 2-acylthiophens being partially analogous with 2-acylthiazine. Alkali treatment of the sulfoxides (2a and 2b) gave 3, 4-dimethyl-4H-1, 4-benzothiazine-1-oxide (9a) and 4-methyl-3-phenyl-4H-1, 4-benzothiazine-1-oxide (9b), respectively. The fact that 3-hydroxy-2, 3-dihydro-4H-1, 4-benzothiazine derivative (8b) was isolated as an intermediate in transformation from 2b to 9b suggests that 9a and 9b may be formed via the reaction process shown in Chart 2. When 9b was treated with acid such as hydrochloric acid or p-toluenesulfonic acid, reductive dimerization of 9b proceeded to give benzothiazinylbenzothiazine derivative (14) in poor yield (below 15%), while the acid treatment of an equimolecular mixture of 9b and 3a elevated the yield from 14 to 64%. From these observations, it was suggested that the process from 9b to 14 might be as shown in Chart 3. Finally, Pummerer reaction of 9b with acetic anhydride was examined.抄録全体を表示PDF形式でダウンロード (854K) -
川鍋 康治, 丸山 幸三1981 年 101 巻 10 号 p. 912-917
発行日: 1981/10/25
公開日: 2008/05/30
ジャーナル フリーA new and simple technique for thin-layer chromatography (TLC) was devised by use of thin-layer stick in place of thin-layer stick in place of thin-layer plate. The glass sticks used were slim glass tubes of 2.5 mm in diameter and 13 cm in length. The separation and identification of 20 common anions were examined on a thin-layer stick of silica gel containing 2% of soluble starch by using 3 kinds of developing solvent. The separation of CNS-, I-, Br-, Cl-, Fe (CN)4-5, Fe (CN)3-6, ClO-3, BrO-3, IO-3 and NO-3 by acetone : H2O (10 : 1), F-, NO-2, S2O2-3, SO24, CrO24, PO3-4, AsO3-3 and AsO3-4 by methanol : n-butanol : H2O (3 : 1 : 1), C2O2-4 and BO-2 by n-butanol saturated with 2N HNO3 were successfully carried out. Thin-layer sticks developed for anions with respective solvent mixtures were allowed to dry in air and then immersed for a short time in color reagent. The tests yielded gratifying results with respect to the efficiency of detection and to the simplicity of the procedure.抄録全体を表示PDF形式でダウンロード (624K) -
榊原 房夫, 高柳 義一, 川内 廣明1981 年 101 巻 10 号 p. 918-925
発行日: 1981/10/25
公開日: 2008/05/30
ジャーナル フリーLoach egg lectin was extracted from the eggs of the fish, Misgurnus anguillicaudatus and purified by ion exchange chromatography on DEAE-and CM-cellulose, and affinity chromatography on a column by using L-rhamnose coupled to epoxy-activated Sepharose 6B. The lectin was eluated from the affinity column with L-rhamnose. The lectin purified by affinity chromatography was shown to be homogenous by polyacrylamide gel electrophoresis and identified as a glycoprotein of 50000 mol. wt. with an isoelectric point of pH 6.6. This lectin has potent agglutinating activity towards human B type erythrocytes as well as Ehrlich ascites tumor cells and ascites hepatoma, AH 109 A cells and exhibited the agglutinability at a concentration of 1 μg/0.05 ml. The agglutinating activity was inhibited best by L-rhamnose, L-mannose and L-lyxose but suitably by D-galactose, D-fucose and L-arabinose, and other monosaccharides failed to inhibit its agglutinating reaction. Among the glycosides of D-galactose tested, the α-anomers of methyl and phenyl D-galactose were more potent than the corresponding β-anomers. Of the oligosaccharides with a terminal α-linked D-galactose, melibiose, raffinose and stachyose were as potent as α-methyl and phenyl α-galactose. These findings indicate that the specificity of loach egg lectin is different from that of Bandeiraea simplicifolia and Sophora japonica lectin.抄録全体を表示PDF形式でダウンロード (887K) -
吉富 博則, 中山 太二, 後藤 茂1981 年 101 巻 10 号 p. 926-931
発行日: 1981/10/25
公開日: 2008/05/30
ジャーナル フリーThe hypoglycemic activity of 20 sulfonylurea related compounds (SU) was examined after oral administration by the use of rat. Two calculated values, (1) decreasing percentage of blood sugar concentration at 2 hours compared with that at 0 time and (2) area of the blood sugar concentration curve from 0 to 7 hours (S-value) were used to evaluate the hypoglycemic effect of SU. The relationship between the primary binding constant for bovine serum albumin-SU (K1) related to the hydrophobicity of SU molecule and the S value was investigated. No linear relationship was obtained and a parabola type relationship could be applied between log K1 and log S. It was concluded that the hypoglycemic activity of SU was influenced considerably by its binding ability to bovine serum albumin and an appropriate binding constant (K1) of SU may be required to obtain most efficient activity.抄録全体を表示PDF形式でダウンロード (577K) -
佐々木 健一, 斎藤 正明, 高柳 義一1981 年 101 巻 10 号 p. 932-938
発行日: 1981/10/25
公開日: 2008/05/30
ジャーナル フリーEffects of lipopolysaccharide (E. coli, LPS) and OK-432 (a Streptococcus preparation) on the activity of hepatic drug-metabolizing enzyme and on the blood concentration of aminopyrine, cyclophosphamide, or pentobarbital were studied in mice. LPS (5 mg/kg, i.v.) or OK-432 (50 KE/kg, i.v.) decreased the activity of drug-metabolizing enzymes in liver microsomes, and the greatest decrease of the enzyme activity was observed 24 h after the administration of LPS or OK-432. The levels of cytochrome P-450 and cytochrome b5 and the activities of aminopyrine N-demethylase and aniline hydroxylase in microsome decreased progressively for 24 h after the administration of LPS and then increased to the normal level within 4 days. Effect of OK-432 on the activity of these enzymes was weaker than that of LPS. The blood concentrations of aminopyrine and pentobarbital in mice treated with LPS were higher than those in untreated mice. On the other hand, the blood concentration of normustard relating to the active metabolite of cyclophosphamide was lower in mice treated with LPS. It is possible that the blood concentration of combined drugs was affected by LPS and OK-432 as a result of the depression of the hepatic drug-metabolism with a decrease in heme protein content and with an inhibition of electron transport system in liver microsomes.抄録全体を表示PDF形式でダウンロード (754K) -
米田 道明, 大川 泰, 渡辺 洋治, 小川 典之, 長井 秀隆1981 年 101 巻 10 号 p. 939-944
発行日: 1981/10/25
公開日: 2008/05/30
ジャーナル フリーSix different crystalline modifications of acemetacin, a carboxymethyl ester of indomethacin, were obtained and characterized through the studies on X-ray diffractometry, IR spectroscopy, differential scanning calorimetry, thermogravimetry and solubility measurement. The polymorphs obtained were classified into four anhydrous forms (designated as α, β, γ and δ forms) and two monohydrous forms (designated as A and D forms). Among the anhydrous forms, α, β and γ forms gave a similar melting point of 151-153°C and were not transformed to one another. On the other hand, the δ form melting at 132-134°C was transformed slowly to α form at this temperature. As for the hydrous forms, A form as well as D form were changed to the corresponding anhydrous forms, namely α form and δ form, when heated up to around 80°C. The molecular structure of each crystalline form was investigated by comparing the wave number of carbonyl groups on infrared spectra. The stability of six different crystalline forms when exposed to ultraviolet light as well as elevated temperature (130°C) was investigated and compared with that of indomethacin (stable form, mp 160-162°C).抄録全体を表示PDF形式でダウンロード (588K) -
竹内 久米司, 向後 博司, 相澤 義雄1981 年 101 巻 10 号 p. 945-950
発行日: 1981/10/25
公開日: 2008/05/30
ジャーナル フリーEffect of theophylline on intrarenal prostaglandin (PG) content and the PGE release from renal medulla was studied by using male Wistar rats. PG was assayed biologically by use of rat stomach fundus. The PGE content in the renal medulla increased 2 hours after oral administration of theophylline (50 mg/kg p.o.). The PGE release from renal medullary slices into Krebs-Ringer bicarbonate buffer was increased by the administration of theophylline both in vivo (50 mg/kg) and in vitro (10-5M). The effect of theophylline in vitro on PGE release from renal medulla into the Krebs-Ringer bicarbonate buffer was completely inhibited by the addition of indomethacin (10-5M) or aspirin (10-3M). The urinary cyclic AMP excretion and urine volume were increased by the oral administration of theophylline. On the other hand, addition of dibutyryl cyclic AMP (10-2M) increased the PGE release from renal medullary tissue. These results suggest that the increase of renal PGE induced by theophylline plays an important role in the mechanism of theophylline diuresis. Moreover, it is thought that intrarenal cyclic AMP may participate, at least in part, in the stimulation of PGE release from renal medullary tissue by theophylline.抄録全体を表示PDF形式でダウンロード (705K) -
國友 順一, 押方 恵, 赤須 通範1981 年 101 巻 10 号 p. 951-955
発行日: 1981/10/25
公開日: 2008/05/30
ジャーナル フリーFrom the alkaloids of the seeds of Stephania cepharantha HAYATA (Japanese name"tamasaki-tsuzurafuji") cultivated in Japan, a new dehydroaporphine type alkaloid, dehydrostephanine was isolated together with dehydrocrebanine (2), stephanine (3), crebanine (4), isotetrandrine (5), O-nornuciferine (6), stesakine (7) and berbamine (8). The structure of dehydrostephanine was established as 1 from various spectral data and identified to be a compound derived from stephanine (3) by iodine-oxidation. The 1, 2, 8, 9-substituted [(7), (4), (2)] and the 1, 2, 8-substituted [(3), (1)] aporphine type alkaloids in this plant were assumed to be formed from dienone-phenol rearrangement of orientalinone (9) and dienol-benzene rearrangement of orientalinol (10), respectively.抄録全体を表示PDF形式でダウンロード (591K) -
松田 りえ子, 仁木 喜治, 立沢 政義, 江島 昭1981 年 101 巻 10 号 p. 955-959
発行日: 1981/10/25
公開日: 2008/05/30
ジャーナル フリーHigh performance liquid chromatographic method for the determination of theophylline in biological fluids (serum, saliva and urine) was developed. Theophylline in biological fluids was adsorbed on a diatom earth column, followed by elution with a mixture of chloroform-isopropanol (95 : 5). After evaporation of the solvent, the residue was dissolved in water, injected onto a HPLC column packed with an ODS stationary phase eluted at 40°C with a mixture of 0.1M phosphate buffer (pH 5.3)-acetonitrile (9 : 1) and detected at 273 nm. 8-Chlorotheophylline was used as an internal standard. The recovery of theophylline from serum by this method was 100.1%±1.76% (SD ; n=5), Other xanthine derivatives (theobromine and caffeine) were seperated under the same conditions.抄録全体を表示PDF形式でダウンロード (550K) -
松尾 俊康, 高木 隆, 斎藤 仁俊, 由岐 英剛, 山口 達明1981 年 101 巻 10 号 p. 960-964
発行日: 1981/10/25
公開日: 2008/05/30
ジャーナル フリーThirty-two derivatives of indane-1, 3-dione were synthesized and screened for the growth inhibition activity on sarcoma 180 cells in vitro and the antitumor activity against solid tumor in vivo. Among them, one compound, 2-(α-anilinobenzylidene)-indane-1, 3-dione, was ineffective in vitro, whereas it was effective in vivo not only by intraperitoneal injection but also by oral administration.抄録全体を表示PDF形式でダウンロード (488K)
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