巻号一覧
106 巻, 8 号
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桜井 弘1986 年 106 巻 8 号 p. 619-637
発行日: 1986/08/25
公開日: 2011/01/31
ジャーナル フリーRedox reactions are involved in some fundamental biological processes such as molecular oxygen activation and oxidation of organic compounds by mono-and dioxygenases, electron transfer and enzyme reactions by metalloproteins and biometal ions. To clarify the active site structure and functions of cytochrome P-450, several hydrophilic and lipophilic model compounds were constructed by using metalloporphyrins (Fe-and Coprotoheme or tetraphenylporphyrin) and various types of thiolcontaining ligands. The active site structure of P-450 in the ferric low-spin state was proposed to have a cysteinate thiolate in the 5th position and an oxygen of H2O in the 6th position. Aromatic, aliphatic and olefin oxidation activities were found in the metalloporphyrin-thiol ligand systems under oxygen and the active oxygen species was proposed.
Behaviors of biometal ions such as Mn and V in the living systems were studied on the conversion of the valence states by electron spin resonance spectrometry. Functional and active site models for Mnenzymes such as Mndioxygenase and superoxide dismutase or catalase, respectively, were proposed. In addition, redox and complex reactions of vanadate ion with biomolecules such as cysteine, glutathione, ascorbate, adenosine triphosphate, heme proteins as well as some drugs studied.
This review has been discussed on structure and functions of metalloenzymes and significance of biometal ions.抄録全体を表示PDF形式でダウンロード (2504K) -
橋本 祐一1986 年 106 巻 8 号 p. 638-652
発行日: 1986/08/25
公開日: 2011/01/31
ジャーナル フリーInitial chemical events caused by carcinogenic 2-amino-6-methyldipyrido [1, 2 -a: 3', 2'-d]-imidazole (Glu-P-1) and molecular design of antitumor agents on the basis of the intercalative ability of Glu-P-1 skeleton are reviewed.
Glu-P-1 binds to deoxyribonucleic acid (DNA) at the 8-position of guanine residues after metabolic activations. Structures of modified nucleic acid base and the activated metabolites were confirmed by alternative synthesis. The pathway of chemical modification of DNA with Glu-P-1 is established chemicaly, and found to occur in vivo. The chemical modification of oncogene proto-ras caused transforming activity of the gene toward NIH3T3 cells. In other words, chemical modification of DNA with Glu-P-1 results in cell transformation. The established pathway of the DNA modification provides a fundamental standpoint in the study of chemical carcinogenesis caused by Glu-P-1.
Glu-P-1 possesses intercalative ability toward double stranded DNA. We designed and synthesized polyamino-Glu-P derivatives and Hemin-Glu-P-1 derivatives. Polyamino-Glu-P derivatives were found to possess extremely high affinity toward DNA. Hemin-Glu-P-1 derivatives cleaved DNA efficiently. Hemin-Glu-P-1 derivatives were suggested to cleave DNA in the same mode of reaction as bleomycin: Hemin-Glu-P-1's are functional analogs of bleomycin. The results suggested the possibility of the method of molecular design described might be served for the development of new antitumor agents.抄録全体を表示PDF形式でダウンロード (2137K) -
四方田 千佳子, 岡田 敏史, 中垣 正幸1986 年 106 巻 8 号 p. 653-658
発行日: 1986/08/25
公開日: 2011/01/31
ジャーナル フリーThe interaction of arabic acid and counterions under electric field was studied by measuring the transference number and the specific conductivity. The transference number was determined by Wall's method. From these data, the fraction of free counterion, f, was calculated for the concentration range from 0.003 to 0.025 (eq/kg), and at some different degrees of neutralization. The values of f for sodium arabate slightly increased with increasing concentration, but there appeared no distinct change in the case of calcium arabate. At infinite dilution, f for sodium arabate and calcium arabate were 0.70 and 0.34, respectively. These results suggest that Manning's theory for cylindrical polyelectrolytes seems to be applicable not only to γ+ and ∅ but also to f of arabate, if the intercharge distance b can be assumed to be spatial intercharge distance.抄録全体を表示PDF形式でダウンロード (887K) -
dl-(3α, 4ξ, 6aα, 10aα)-Octahydro-4-hydroxy-7, 7-dimethyl-8H-3, 10a-methano-1H-2-benzoxocin-8-oneの合成原山 尚, 新海 豊, 犬伏 康夫1986 年 106 巻 8 号 p. 659-663
発行日: 1986/08/25
公開日: 2011/01/31
ジャーナル フリーSynthesis of a tricyclic compound (3), a key intermediate for the synthesis of dllaspterric acid (1), was investigated.
Robinson annulation of a keto ester (2), which was prepared from a diester (4) by Dieckmann condensation, gave an enone ester (5). Reduction of 5 with LiAlH4, followed by MnO2 oxidation afforded an enone alcohol (6), which was converted to hydroxy-ether (8) via three steps (I2-Ag2O, AgOAc, and alkaline hydrolysis). Reduction of 8 with Li in liq. NH3 and methylation gave alcohol A (12) and a key intermediate, alcohol B (3), stereostructure of which was determined by nuclear Overhauser effect measurement of its acetate (14).
On the other hand, reductive methylation of 6 gave 16, which was proven to be an undesired cis product by conversion to 12.抄録全体を表示PDF形式でダウンロード (889K) -
アマチャヅルのサポニン成分について その9竹本 常松, 在原 重信, 吉川 和子1986 年 106 巻 8 号 p. 664-670
発行日: 1986/08/25
公開日: 2011/01/31
ジャーナル フリーNew saponins, named gypenosides LVI (1), LVII (2), LVIII (3), LIX (4) and LX (5) besides the known gypenosides V (11), IX (12), XLIII (13), XLV (14) and ginsenoside-Rb3 (15) were isolated from the aerial parts of Gynostemma pentaphyllum MAKINO collected in Miyagi Pref. On the basis of chemical and physicochemical evidence, they were characterized as follows: 1, 2α, 3β, 12β, 20 (S)-tetrahydroxydammar-24-ene 3-O-β-sophoroside-20-O-β-primeveroside: 2, 2α, 3β, 12β, 20 (S)-tetrahydroxydammar-24-ene 3-O-β-D-glucopylanoside-20-O-β-primeveroside: 3, 3β, 12β, 20 (S)-trihydroxydammar-24-ene 3-O-[β-D-glucopyranosyl-(1→2)-α-L-arabinopyranoside]-20-O-β-primeveroside; 4, 2α, 3β, 12β, 20 (S), 26-pentahydroxydammar-24-ene 20-O-β-primeveroside: 5, 2α, 3β, 12β, 20 (S), 25-pentahydroxydammar-23-ene 20-O-β-primeveroside.抄録全体を表示PDF形式でダウンロード (966K) -
牡丹皮, 甘草及び柴胡田中 悟, 高橋 惇, 小野田 欽一, 川島 邦夫, 中浦 槇介, 長尾 重之, 大野 泰雄, 川西 徹, 中路 幸男, 小林 和雄, 鈴木 ...1986 年 106 巻 8 号 p. 671-686
発行日: 1986/08/25
公開日: 2011/01/31
ジャーナル フリーIn order to investigate adverse effects of herbal drugs, we performed toxicological studies on the methanolic extract from Moutan bark (botanpi) and on the aqueous extracts from Glycyrrhiza (kanzou) and Bupleurum root (saiko) in rats and mice. In the single administration study, these extracts were given orally or intraperitoneally to male Wistar rats and ddY mice at a dose of 6g/kg, and acute toxic effects of the extracts were investigated. In the repeated administration study, these extracts were given orally by intubation to male Wistar rats once a day for 21d at daily doses of 1.5g/kg and 3g/kg. General appearance and body weight of the rats were checked daily, and behavioral, hematological, biochemical and pathological examinations were performed. The results obtained are as follows.
1) Single administration stud
Moutan bark, Glycyrrhiza and Bupleurum root did not show any toxic effect in rats and mice by an oral administration, whereas these herbal drugs showed potent toxic effects by an intraperitoneal injection. No species difference in the toxic effects of these herbal drugs was found between the rat and mouse.
2) Repeated administration study
Moutan bark: The erythrocyte count, hemoglobin level and hematocrit value in the blood decreased, the total bilirubin level in the serum increased, and a moderate deposition of hemosiderin in the spleen was evidenced in the pathological observation. These results indicate a weak hemolytic effect of Moutan bark, though no abnormal changes in the size, shape and osmotic fragility of the erythrocytes were found. And also, increases in the liver ALP, GPDAP and LAP activities indicate the possibility of weak influence of Moutan bark on the liver function.
Glycyrrhiza: Increases in the kidney weight and urinary protein level and an induction of the renal drug metabolizing enzyme system indicate the possibility of weak influence of Glycyrrhiza on the renal function. The erythrocyte count and hematocrit value decreased slightly.
Bupleurum root: The erythrocyte count decreased slightly. The liver weight and the serum γ-GTP activity increased slightly.
It is considered that these results should be useful for the safety evaluation of the herbal drugs for human use.抄録全体を表示PDF形式でダウンロード (3355K) -
橋本 清澄1986 年 106 巻 8 号 p. 687-693
発行日: 1986/08/25
公開日: 2011/01/31
ジャーナル フリーBy the use of Sep-Pak C18 cartridge, a simple and rapid cleanup method was established for the quantitative determination of pheophorbide a (PB-a) and pyropheophorbide a (PyPB-a) in chlorella tablets. PB-a and PyPB-a were extracted with methanol from chlorella tablets, then the extract was adjusted to methanol-1% acetic acid (7: 3, v/v) and centrifuged. The supernatant was cleaned up by the use of Sep-Pak C18 cartridge, eluted with methanol-0.025M ammonium acetate (88: 12, v/v) and applied to high performance liquid chromatography. They were separated on Radial PAK NOVA-PAK C18 column with the same solvent as a mobile phase. The average recoveries of PB-a and PyPB-a added to chlorella tablets were 88.9% and 96.3%, respectively.
In order to estimate chlorophyllase activity in chlorella tablets, the proposed method was used to determine the amount of PB-a increased by incubation for 4h. As PB-a was separated from other chlorophyll degradative products derived during incubation, the proposed method was more specific and accurate than the official one (spectrophotometric determination).抄録全体を表示PDF形式でダウンロード (1142K) -
早瀬 幸俊, 村上 美穂, 高木 良成1986 年 106 巻 8 号 p. 694-697
発行日: 1986/08/25
公開日: 2011/01/31
ジャーナル フリーO-Phosphoethanolamine (PEA) content of various tissues of ddY mice was determined by high-performance liquid chromatography. PEA in tissues was extracted with trichloroacetic acid, and then chromatographed on a cation exchange column (Shimadze, ISC-07/S 1504) by using pH 2.00 sodium citrate-perchloric acid buffer (Na+, 0.2M) as a mobile phase. The eluate was monitored by an in-stream fluorometric detection system with o-phthalaldehyde.
Tissue and sex differences in PEA concentration were detected: concentration of PEA was significantly higher in the spleen and thymus than in all other tissues studied, and significantly higher in the submaxillary salivary gland and kidney of female mice than in those of male mice.抄録全体を表示PDF形式でダウンロード (609K) -
黒岩 信, 猪爪 信夫, 中野 眞汎1986 年 106 巻 8 号 p. 698-702
発行日: 1986/08/25
公開日: 2011/01/31
ジャーナル フリーSince very low bioavailability of the drug had been observed, the possibility of degradation of nicardipine in the presence of faecal flora was investigated. After the addition of nicardipine to sterilized broth, 1% or 8% sterilized stool culture without further anaerobic precautions, the drug did not degrade in the incubation mixture. This indicates that the drug did not react with the components of broth and stool cultures and was stable. On the other hand, after the addition of the drug to 1% or 8% human faecal contents in a broth, the drug disappeared rapidly in the incubation mixture depending on stool concentrations. The metabolite was identified to be aminonicardipine by high performance liquid chromatography (HPLC) and thin-layer chromatography (TLC). The disappearace of nicardipine and the appearance of a metabolite, aminonicardipine in the incubation mixture were followed by HPLC and TLC.抄録全体を表示PDF形式でダウンロード (672K) -
伊藤 雅之, 相沢 一雅, 小宮 泉, 宮城 克己, 藤田 正敬, 梅村 甲子郎1986 年 106 巻 8 号 p. 703-708
発行日: 1986/08/25
公開日: 2011/01/31
ジャーナル フリーA linear pharmacokinetic model was developed in order to calculate separately the plasma (or blood) concentrations of CM6913 and CM7116, major metabolites of ethyl loflazepate (CM6912), from the total concentrations of CM6913 and CM7116 (CM6913+CM7116) after the oral administration of CM6912 to dogs and humans. The plasma (or blood) concentrations of CM6913 and CM7116 were elaborately determined by the addition of alkaline solution to inhibit CM6913 degradation. The CM6913 concentration was well simulated by this calculation except for the deviation from one-compartment model in later time after the administration to dogs. The calculated CM7116 concentration was also comparable to the observed concentration. In an early period after the administration, however, the plasma (or blood) concentration of CM7116 was underestimated, especially in humans. The total plasma concentrations of CM6913 and CM7116 are measured routinely because of the rapid degradation of CM6913 in biological samples, hence this model approach will be useful for the separate estimation of the concentrations of the metabolites. In humans, the elimination half-life of CM7116, the most active metabolite of CM6912, was long (132h), which suggests the prolonged effects of CM6912.抄録全体を表示PDF形式でダウンロード (944K) -
鴨川 旭, 太田 節子, 立木 朱美, 熊坂 昌子, 篠田 雅人1986 年 106 巻 8 号 p. 709-714
発行日: 1986/08/25
公開日: 2011/01/31
ジャーナル フリーThe conditions of cholestasis induced by the administration of α-naphthylisothiocyanate (ANIT), thioacetamide (TAA) and carbon tetrachloride (CCl4) were investigated by examining bile flow and bile acids excretion.
Cholestasis generated by ANIT was caused from parasecretion of bile acids while CCl4 brought about parasecretion of components other than bile acids in bile. TAA was presumed to be a combined type of these two kinds of injuries. By various kinds of combination of dosage time and doses of the substances for hepatic injuries it might be possible to prepare three kinds of models concerning cholestasis with different generation mechanisms of injury.
Cysteamine (MEA) showed a significant protective effect on these three kinds of cholestasis and a correlation between the conditions of cholestasis and the amount of doses was observed. Therefore, it could be applicable to the use of MEA as a standard substance in case of tests for effectiveness by using these models.抄録全体を表示PDF形式でダウンロード (1649K) -
松尾 圭造, 高田 卯, 井上 淳, 田中 邦喜1986 年 106 巻 8 号 p. 715-720
発行日: 1986/08/25
公開日: 2011/01/31
ジャーナル フリー10-(4-Nitrophenyl)-and 10-(2-pyridyl)-3, 3-dimethyl-3, 4, 9, 10-tetrahydro-1H-furo [3, 4-b]-[1, 5] benzodiazepin-1-ones, and 10-(2-chlorophenyl)-3, 3-dimethyl-3, 4, 9, 10-tetrahydro-1H-pyrrolo [3, 4-b][1, 5] benzodiazepin-1-one showed considerable analgesic activity. 10-Substituted 3, 3-dimethyl-3, 4-dihydro-1H-furo [3, 4-b][1, 5] benzodiazepin-1-ones and their pyrrolo analogs were prepared by dehydrative cyclization of 3-(2-acylaminoanilino)-4, 4-dimethyl-2-buten-4-olide or 4-lactam with polyphosphoric acid. Analgesic activity of the dihydro derivatives were less effective than the corresponding tetrahydro derivatives.抄録全体を表示PDF形式でダウンロード (765K) -
新フェニルエ夕ノイド配糖体Cistanoside Gの単離と構造唐沢 ひろ子, 小林 弘美, 滝沢 信夫, 宮瀬 敏男, 福島 清吾1986 年 106 巻 8 号 p. 721-724
発行日: 1986/08/25
公開日: 2011/01/31
ジャーナル フリーA new phenylethanoid glycoside, cistanoside G (I), was isolated from Cistanchis Herba, the whole plant of Cistanche salsa (C. A. MEY.) G. BECK (Orobanchaceae), along with salidroside (p-hydroxyphenethyl, β-D-glucoside), syringin and (+)-pinoresinol.The structure of cistanoside G was determined to be 2-(4-hydroxyphenyl) ethyl O-α-L-rhamnopyranosyl-(1-, 3)-β-D-glucopyranoside (I) on the basis of chemical and spectral data.抄録全体を表示PDF形式でダウンロード (553K) -
矢原 正治, 野原 稔弘, 神田 博史, 下村 講一郎, 佐竹 元吉1986 年 106 巻 8 号 p. 725-728
発行日: 1986/08/25
公開日: 2011/01/31
ジャーナル フリーTwo new iridoid glucosides, tentatively named MS-5 (5) and MS-6 (6), along with three iridoid glucosides, catalpol, bartsioside and aucubin, and two phenolic glycosides, acteoside and dehydroacteoside, have been isolated from Monochasma savatieri FRANCH. ex MAXIM. These structures were established on the basis of chemical and spectroscopic evidence.抄録全体を表示PDF形式でダウンロード (574K)
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