巻号一覧
108 巻, 7 号
選択された号の論文の11件中1～11を表示しています
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國枝 武久1988 年 108 巻 7 号 p. 593-603
発行日: 1988/07/25
公開日: 2008/05/30
ジャーナル フリーSynthetic potential of 4, 5-unsubstituted 2-oxazolone heterocycle has been reviewed as a versatile building block for vic-amino alcohol structures found in a number of bioactive compounds as well as a promising leaving moiety in carboxyl and phosphoryl activation processes. Good versatile strategy from such a simple heterocycle to a wide variety of 1, 2-amino alcohols is described and successfully applied to the efficient preparation of biologically significant hydroxy amino acids such as statine and hydroxyglutamic acid. The oxazolone-based compounds are introduced as excellent reagents for phosphorylation of alcohols and for β-lactam formation from β-amino acids.抄録全体を表示PDF形式でダウンロード (770K) -
北川 隆之1988 年 108 巻 7 号 p. 604-612
発行日: 1988/07/25
公開日: 2008/05/30
ジャーナル フリーExternal adenosine triphosphate (ATP) has been shown to induce permeability changes in a variety of animal cells. This review is mainly concerned with the effect of external ATP on passive permeability of transformed cells in culture. Brief exposure of several transformed cells to ATP causes a striking increase in passive permeability, allowing passage through the plasma membrane of phosphorylated metabolites and ions. Untransformed fibroblasts do not respond to the ATP. Although the molecular mechanisms of this permeability change in transformed cells are largely unknown, it has been demonstrated that the permeability change is modulated by cellular ATP, cytoskeleton and calmodulin. These characteristics and the recent studies with an isolated ATP-resistant variant designed to gain some insight into the biochemistry and regulation of the ATP effect are summarized. By considering a selective effect of external ATP on membrane permeability of transformed cells, possible application of this method to cancer chemotherapy has been examined. The results obtained mainly with in vitro systems are also described.抄録全体を表示PDF形式でダウンロード (862K) -
永井 恒司1988 年 108 巻 7 号 p. 613-624
発行日: 1988/07/25
公開日: 2008/05/30
ジャーナル フリーWith a view to finding an advanced technology of control of bioavailability, drug delivery systems have been investigated by controlled release, which are for (1) intrauterine, (2) buccal/gingival, (3) nasal, and (4) percutaneous administration. First the general concept of drug delivery systems by controlled release and then our results of trials are described. Among our trials, the productive ones are concerned with bioadhesive drug delivery systems and now their three commercial products are on the market, which have been developed on the basis of our investigations : (a) adhesive tablet of triamcinolone acetonide for aphthous stomatitis; (b) adhesive powder spray for extensive stomatitis; and (c) adhesive powder spray for nasal allergy. The others are : (d) a topical dosage form for carcinoma colli, which has been investigated in cooperation with gynecologists; (e) an oral mucosal dosage form for the absorption of insulin (f) a powder dosage form of nasal absorption of insulin; (g) a powder dosage form of nasal absorption of -interferone; (h) transdermal therapeutic systems of ionizable water-soluble drugs; (i) cyclohexane derivatives as percutaneous absorption enhancers.抄録全体を表示PDF形式でダウンロード (1220K) -
藤田 勇三郎, 駒越 圭子, 上原 郁恵, 森本 泰子, 原 令子1988 年 108 巻 7 号 p. 625-634
発行日: 1988/07/25
公開日: 2008/05/30
ジャーナル フリーAs reported previously, tannins inhibited efficiently the Cu (II)-catalyzed autoxidation of ascorbic acid and the peroxidation of methyl linoleate by the radical scavenging mechanism. However, the latter reaction was found to be accelerated remarkably in the presence of Cu (II) ion and tannin; that is, tannin was able to initiate the peroxidation of methyl linoleate in the presence of Cu (II) ion. The peroxidation of methyl linoleate induced under the coexistence of Cu (II) ion and tannin was kinetically investigated. The rate of oxidation, V, was represented as follows : V∝[methyl linoleate]1.0[Cu(II)]0.5[tannin]0.0 An acceleration mechanism by tannin was proposed to explain the above kinetics. It was found that tannin participates in both initiation and inhibition processes. The autoxidation was initiated by the superoxide radical, (O2)-·, which was produced by the reaction between reduced Cu (I) and dissolved oxygen, where the Cu (I) ion was produced through the reduction by tannin. This was proved by the fact that the removal of Cu (I) ions by the addition of cuproin in the reaction system completely diminished the peroxidation. Moreover, the participation of (O2)-· radical in the initiation reaction was confirmed by the use of ·OH and (O2)-· radical scavengers, respectively. Initiation efficiency of peroxidation by the Cu (II)-tannin couple was rather weak compared with that by the Cu (II)-ascorbic acid couple, and, therefore, the acceleration of peroxidation by tannin was observed only under conditions of remarkably high relative concentration of Cu (II) against tannin. A similar acceleration effect by tannin was found to occur by a metal ion such as Fe (III) whose redox potential is low.抄録全体を表示PDF形式でダウンロード (785K) -
原山 尚, 桜井 修, 曽根原 聡, 篠田 昌信, 手塚 康弘, 米田 文郎1988 年 108 巻 7 号 p. 635-640
発行日: 1988/07/25
公開日: 2008/05/30
ジャーナル フリーOxidation of sulfide (4) derived from tosylate (7), with m-chloroperbenzoic acid gave sulfoxide (5). Diels-Alder reaction of 5 with E-2-trimethylsiloxy-1, 3-pentadiene gave a mixture of 6b and 6c, which were successively treated with MeCu-TMSCl-TMEDA and Pd(OAc)2 to give enones (11a) and (11b). Enone (11b) was converted to the key intermediate (3) for the synthesis of spirovetivane sesquiterpenes via dithioacetal (14).抄録全体を表示PDF形式でダウンロード (703K) -
桑山 知成, 加藤 節子, 黒野 幸久, 八代 有, 池田 憲1988 年 108 巻 7 号 p. 641-646
発行日: 1988/07/25
公開日: 2008/05/30
ジャーナル フリー11b-Methyl-2, 3, 7, 11b-tetrahydrooxazolo[3, 2-d][1, 4]benzodiazepin-6(5H)-one (Ic) and its 2-methyl derivative (Id) were synthesized as model compounds of benzodiazepinooxazole drugs. In methanol-d4 solution at room temperature, the 11b-methyl protons of Ic and Id underwent exchange reaction with deuterium, and the reactions were investigated kinetically. The reaction was rationalized in terms of an iminium type intermediate which is formed via ring opening of an oxazolidine. The methyl substituent at the 2-position of Id affects markedly the proton exchange rate. The results suggest that the isomerization of oxazolam (Ia) proceeds via a similar intermediate.抄録全体を表示PDF形式でダウンロード (599K) -
菊地 正雄, 山内 洋子, 長岡 一郎, 杉山 正尚, 高橋 由香1988 年 108 巻 7 号 p. 647-652
発行日: 1988/07/25
公開日: 2008/05/30
ジャーナル フリーThree phenylethanoid glycosides, named neosyringalide, des-p-coumaroylibotanolide and ibotanolide, have been isolated together with desrhamnosylisoacetoside and other components from the leaves of Ligustrum obtusifolium SIEB. et ZUCC., and the structures were elucidated on the basis nuclear magnetic resonance spectra, circular dichroism spectra and other physicochemical evidence.抄録全体を表示PDF形式でダウンロード (534K) -
中澤 一治, 田中 晴美1988 年 108 巻 7 号 p. 653-658
発行日: 1988/07/25
公開日: 2008/05/30
ジャーナル フリーThe concentrations of caffeine and its metabolites, dimethylxanthines, in the plasma and saliva were determined in order to clarify the metabolic capacity of caffeine in pregnant women. After taking caffeine-free diet for 3 d, caffeine (3 mg/kg) was orally administered to 6 healthy volunteers. The concentrations of caffeine and dimethylxanthines, i.e. theobromine, paraxanthine and theophylline in the plasma and saliva were measured. The concentrations in the saliva showed positive relationships to those in the plasma for both caffeine and paraxanthine. There was a linear relationship between the plasma clearance of caffeine and the molar concentration ratio of paraxanthine to caffeine in the saliva at 6 h after oral administration of caffeine. The concentration of caffeine in the saliva from pregnant women was higher than 1.3 μg/ml at 1 h after taking one or three cups of coffee or green tea without restriction. These results indicate that the plasma levels of caffeine and paraxanthine can be predicted from the saliva levels of caffeine and paraxanthine. Moreover, it would be possible to estimate the plasma clearance or metabolic capacity of caffeine from the molar concentration ratio of paraxanthine to caffeine in the saliva.抄録全体を表示PDF形式でダウンロード (578K) -
渡辺 厚, 大沼 惟子1988 年 108 巻 7 号 p. 659-664
発行日: 1988/07/25
公開日: 2008/05/30
ジャーナル フリーParticle size distributions of 2 kinds of phenytoin were studied using a polarizing microscope by the immersion method. Both phenytoins, a commercial JPX product, (A), and a special grade reagent, (B), had the same key refractive indices and similar habits of plates, though sizes of particles were quite different. Using a polarizing microscope the shapes of larger crystals and the patterns of their retardation colors, from which the thicknesses were to be measured, were quantitatively sketched. Then the habit parameters a, b and c (thickness) were determined from the sketched crystals, and the habit coefficients, K=√(ab)/c, L=b/a, were calculated. The habit parameters of the other smaller crystal grains, which had similar habits as the sketched crystals, were calculated from the measured parameter b using the habit coefficients. Finally, an approximate volume of an each particle, V=abc, and the total weight of all the crystal grains belonging to the limitted range of log V were calculated. The particle size distribution was shown as the correlation between the value of log V (abscissa) and the weight percent of the crystal grains belonging to an each limitted range of log V (ordinate).抄録全体を表示PDF形式でダウンロード (623K) -
藤野 博之, 合屋 周次郎1988 年 108 巻 7 号 p. 665-668
発行日: 1988/07/25
公開日: 2008/05/30
ジャーナル フリーThe present paper deals with the preparation of stable 1-(dichloro-1, 3, 5-triazinyl)-2-methylisoindole having N-methylisoindole as a fluorophore together with dichloro-1, 3, 5-triazinyl group as a reacting group and its applicability as a precolumn fluorescence derivatization reagent for estrogens in high-performance liquid chromatography. The reagent reacts with phenolic hydroxyl group of estrogens under alkaline conditions to yield the corresponding fluorescent products, which can be separated on reversed-phase column TSKgel ODS-120A with aqueous methanol as eluent. The fluorescence intensity of estrogen derivatives excited at 380 nm was measured at 430 nm. The calibration curve for 17α-estradiol derivative was rectilinear over the range of 3-125 pmol, the limit of detection was 3 pmol per 10 μl injection.抄録全体を表示PDF形式でダウンロード (416K) -
中川 久, 西山 要, 松本 純子, 濱野 和子, 福井 義雄, 後藤 茂1988 年 108 巻 7 号 p. 669-673
発行日: 1988/07/25
公開日: 2008/05/30
ジャーナル フリーIn order to examine the effect of various absorption-promoters on gastrointestinal absorption of pirenzepine dihydrochloride (PRZ), a weak basic and very soluble compound in water, PRZ was orally given to rats in combination with them and the percentages of cumulative urinary excretion of PRZ were measured. Marked PRZ absorption-promoting effect was found for esters of fatty acids with long chains and monohydric alcohols, ester type nonionic surface active agents with less than 11 HLB values and triglycerides of fatty acids with long chains, while the promoting effect on PRZ absorption was less potent for triglycerides of fatty acids with chains of medium length, fatty acids with long chains and monoglycerides of fatty acids with long chains. PRZ was suspended in sorbitan trioleate, an ester type nonionic surface active agent, and in triolein, a triglyceride of fatty acids with a long chain, and the resulting suspensions were orally given to rats. About 4 times increase in area under the blood concentrationtime curve as compared with that obtained after administration of aqueous solution of PRZ was observed in both suspensions.抄録全体を表示PDF形式でダウンロード (580K)
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