巻号一覧
36 巻, 3 号
選択された号の論文の60件中1～50を表示しています
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黒田 義弘, 藤原 靖弘, 斉藤 雅子, 新宮 徹朗1988 年 36 巻 3 号 p. 849-856
発行日: 1988/03/25
公開日: 2008/03/31
ジャーナル フリーAdvantages and disadvantages of a Lorentzian to Gaussian trans formation function, which has been commonly employed in enhancing the resolution of two-timensional nuclear magnetic resonance (2D NMR) spectra, were investigated by applying this function to the 2D nuclear Overhauser effect (NOE) NMR spectrum of a drug-phosphatidylcholine vesicles solution. It was found that, although this function is known to be useful in enhancing the resolution of an NMR spectrum of a low-molecular-weight molecule which can afford relatively narrow NMR resonance peaks, the function often fails to yield a good line shape or contour map in the case where there exist broad resonance peaks having various line widths as in the presently tested sample solution. A careful choice of the parameters relevant to the function is required. In conclusion, the Lorentzian to Gaussian transformation function is less superior to a sine-bell function which has also been employed as an alternative function to process 2D NMR spectra. Some examples are presented in this paper.抄録全体を表示PDF形式でダウンロード (768K) -
野中 源一郎, 石丸 幹二, 三橋 国英, 岩瀬 由紀子, 上田 雅之, 西岡 五夫1988 年 36 巻 3 号 p. 857-869
発行日: 1988/03/25
公開日: 2008/03/31
ジャーナル フリーContinuing chemical examinations on tannins have led to the isolation of two new tannins, mongolicains A (3) and B (4), from five Quercus and one Castanopsis species. The structures of 3 and 4 have been characterized on the basis of chemical and spectroscopic data as novel flavanoellagitannins, in which hydrolyzable tannin and flavan-3-ol moieties are connected through a carbon-carbon linkage. Their structural features suggest that 3 and 4 are biosynthetically formed by oxidation of accompanying acutissimins A (1) and B (2).抄録全体を表示PDF形式でダウンロード (1157K) -
上田 雅之, 石丸 幹二, 野中 源一郎, 西岡 五夫1988 年 36 巻 3 号 p. 870-876
発行日: 1988/03/25
公開日: 2008/03/31
ジャーナル フリーSix new phenol glucoside gallates (3-5, 7, 9 and 10) have been isolated from Castanopsis cuspidata var. sieboldii NAKAI (Fagaceae), together with the known compounds, dehydrodigallic acid (1), cretanin (2), chesnatin (11) and chestanin (8). On the basis of spectroscopic evidence and the result of tannase hydrolysis, the structures of compounds 3-5 have been established to be the mono- (3) and digallates (4 and 5) of crenatin (6). Similarly, compounds 7, 9 and 10 have been characterized as the monogallate (7) of 3, 4-dihydroxyphenethyl alcohol 4-O-β-D-glucopyranoside and the monogallates (9 and 10) of 8. In addition, the structure of chesnatin (11), in which the orientation of the dehydrodigalloyl group had been unknown, was determined by detailed carbon-13 nuclear magnetic resonance examination.抄録全体を表示PDF形式でダウンロード (707K) -
大崎 勉, 栗木 武男, 植田 泰誠, 榊原 仁作, 浅野 正久1988 年 36 巻 3 号 p. 877-892
発行日: 1988/03/25
公開日: 2008/03/31
ジャーナル フリーNovel 1, 3, 6, 7-tetrahydro-7-oxoimidazo[4, 5-c][1, 2, 6]thiadiazine 2-oxide derivatives (2a-q) were synthesized by the reaction of imidazole derivatives (1), obtained by alkaline hydrolysis of 1, 3, 7-trisubstituted xanthines (3), with SOCl2 in 42-93% yields. Chlorination of 2 with SO2Cl2 gave the 5-chloro derivatives (10a, d, i-q), though in low yields. The reaction of 2 with benzoyl chloride derivatives (14) gave 3, 7-dihydro-6H-purin-6-one derivatives (15a-d).Among 2 and 10, compounds having the phenoxyalkyl group at the l-position exhibited potent vasodilating activity on the mesenteric artery of spontaneously hypertensive rats. In particular, ED50 values of the order of 10-7 M were obtained with those having a 1-[6-(4-chlorophenoxy)hexyl]-6-propyl (2o), 6-hexyl-1-[6-(4-methoxyphenoxy)hexyl] (2p), 1-[6-(4-chlorophenoxy)hexyl]-6-hexyl (2q), 5-chloro-1-[6-(4-chlorophenoxy)hexyl]-6-methyl (101), 5-chloro-1-[4-(4-methoxyphenoxy)-butyl]-6-propyl (10m), 5-chloro-1-[6-(4-methoxyphenoxy)hexyl]-6-propyl (10n), or 5-chloro-1-[6-(4-chlorophenoxy)hexyl]-6-propyl (10o) substituent.抄録全体を表示PDF形式でダウンロード (1339K) -
田代 孝司, 伏谷 眞二, 野副 重男1988 年 36 巻 3 号 p. 893-901
発行日: 1988/03/25
公開日: 2008/03/31
ジャーナル フリー2'-epi-Distichonic acid A (4b), an iron-chelating amino acid derivative was synthesized starting from L-vinylglycine epoxide (6b). Reaction of 6b with glycine ester 17 afforded a β-hydroxy amino acid derivative (18). Reductive coupling of 21 derived from 18 with L-malic-β-semialdehyde (25) gave 2'-epi-distichonic acid A (4b) after deprotection.抄録全体を表示PDF形式でダウンロード (925K) -
淀 光昭, 松下 至博, 大杉 栄一, 原田 紘1988 年 36 巻 3 号 p. 902-913
発行日: 1988/03/25
公開日: 2008/03/31
ジャーナル フリーOptical isomers of methyl 6, 7-dichloro-2, 3-dihydrobenzo[b]furan-2-carboxylate (2) were prepared by means of both optical resolution and chiral synthesis. The resolution of the carboxylic acid 3 was achieved in a practical and efficient way via the l-and d-menthyl esters, which were directly converted to enantiomers of 2. Chiral synthesis of 2 was attained with high optical yield via acidcatalyzed cyclization of the β-hydroxysulfide 10 derived from optically active glycidyl phenyl sulfide 13. The optical resolution method was considered to be better for large-scale preparation from the economical and operational viewpoints.抄録全体を表示PDF形式でダウンロード (1301K) -
佐藤 慎吾, 古畑 公夫, 伊藤 正善, 志鳥 善保, 小倉 治夫1988 年 36 巻 3 号 p. 914-919
発行日: 1988/03/25
公開日: 2008/03/31
ジャーナル フリーThe reactions of methyl N-acetyl-4, 7, 8, 9-tetra-O-acetyl-2-chloro-2-deoxy-β-D-neuraminate (2) with 2', 3'-di-O-acetylinosine (1) and with 2', 3'-di-O-acetyl-N-benzoylcytidine (8) under Koenigs-KOnorr-like reaction conditions geve the corresponding (2→5) linked disaccharide uncleoside analogues, in yields of 31% and 23% respectively. These nucleoside 5'-N-acetylneuraminic acid analogues were converted via saponification or ammonolysis into the final target compounds. The stereochemistry of these. compounds was confirmed by analysis. of the proton nuclear magnetic resonance (1H-NMR) spectra and measurement of the rate of hydrolysis of the (2→5) glycosidic linkage.抄録全体を表示PDF形式でダウンロード (681K) -
野田 直希, 小林 博恭, 宮原 一元, 川崎 敏男1988 年 36 巻 3 号 p. 920-929
発行日: 1988/03/25
公開日: 2008/03/31
ジャーナル フリーSix kinds of so-called resin glycoside, muricatins I-VI, were isolated from the seeds of Ipomoea muricata JACQ. (Convolvulaceae). Their structures including the stereochemistry have been determined on the basis of chemical and spectral data. Similar to the resin glycosides previously isolated from the roots of I. orizabensis (PELLET) LEDAN., all of them were monomers of a jalapinolic acid tetraglycoside in which the sugar moiety is partially acylated by organic acids and also combined with the carboxy group of the aglycone to form a macrocyclic ester structure.抄録全体を表示PDF形式でダウンロード (937K) -
東野 武郎, 佐藤 進, 菅 浩貴, 丹治 健一, 宮下 晶, 香取 達彦1988 年 36 巻 3 号 p. 930-939
発行日: 1988/03/25
公開日: 2008/03/31
ジャーナル フリーAcid hydrolysis of 3-benzoyl-3, 4-dihydro-2-methyl-4-quinazolinecarbonitrile (11, 2-methyl-quinazoline Reissert compound) resulted in the formation of the oxazole (13). Alkaline hydrolysis gave 2-methylquinazoline (12) and benzoic aicd (8). The anion (D1), generated from 11 and NaH in dimethylformamide (DMF), underwent decomposition to give the ketone (14) and the cyanoquinazoline (15) together with by-products 12 and O-benzoylbenzoin (9). Compound 11 reacted with aromatic aldehydes (10a-c) in the presence of NaH to give the benzoates (16a-c) and by-products 12 and 15. Alkylation (or arylation) with alkyl (or aryl) halides (11a, b) afforded the corresponding 4-substituted derivatives (19a, b) and a by-product 14.The reactivities of 11. and 3-benzoyl-3, 4-dihydro-4-quinazolinecarbonitrile (21, quinazoline Reissert compound) are compared.抄録全体を表示PDF形式でダウンロード (829K) -
関 興一, 大倉 一枝, 寺嶋 正直, 金岡 祐一1988 年 36 巻 3 号 p. 940-944
発行日: 1988/03/25
公開日: 2008/03/31
ジャーナル フリーPhotolysis of 2-halopyridine with indole afforded the (2-pyridyl)indoles as a regioisomeric mixture. On the basis of the isomer distributions, an electron tansfer mechanism is suggested for the present reaction. The regioselectivity was found to be fairly dependent on the solvent polarity.抄録全体を表示PDF形式でダウンロード (576K) -
松田 彰, 伊藤 弘子, 竹貫 健二, 佐々木 琢磨, 上田 亨1988 年 36 巻 3 号 p. 945-953
発行日: 1988/03/25
公開日: 2008/03/31
ジャーナル フリーThe reaction of 4-ethoxy-1-(3, 5-O-tetraisopropyldisiloxanyl-1, 3-diyl-β-D-erythro-pentofuran-2-ulosyl)-2(1H)-pyrimidinone (11) with various organometallic reagents yielded corresponding 2'-branched-chain sugar pyrimidine nucleosides. Only in the reactions with MeMgBr and EtMgBr was the more hindered β-attack observed to afford and 2'-alkyl ribofuranosides (13a, b). In the reaction of 11 with MeLi, Me3, Al, or PhMgBr, 2'-methyl or phenyl arabinosides (12a, b, c)were obtained stereoselectively. Conversion of these pyrimidine nucleosides into cytosine derivatives is also described and their antileukemic and antiviral activities are discussed.抄録全体を表示PDF形式でダウンロード (1027K) -
藪下 安紀, 陶山 勝彦, 高木 邦彦1988 年 36 巻 3 号 p. 954-958
発行日: 1988/03/25
公開日: 2008/03/31
ジャーナル フリーThe stability of immobilized human urokinase (UK; EC 3.4.21.31) is an important factor for the clinical application of the enzyme as an antithrombotic material. The stabilities of human UK immobilized on a polymeric support to heat and enzyme inhibitors were compared with those of the original soluble UK.UK was immobilized on an ethylene vinyl acetate copolymer (EVA) tube which has maleic anhydride as a functional group on its surface. Immobilized UK showed greater stability to thermal degradation than soluble UK. Comparative kinetic studies of these two forms of UK toward enzyme inhibitors revealed that immobilization of the enzyme did not result in any change of Michaelis constants (Km), though a significant increase of inhibition constans (Ki) was observed.Furthermore, UK immobilized on the EVA tube showed resistance to thermal denaturation. Therefore, an EVA tube carrying immobilized UK represents a stable and easy-to-handle material for clinical use.抄録全体を表示PDF形式でダウンロード (535K) -
井内 浤二, 新田 昌宏, 伊藤 敬三, 森元 康夫, 塚本 悟郎1988 年 36 巻 3 号 p. 959-965
発行日: 1988/03/25
公開日: 2008/03/31
ジャーナル フリーAnalogs of Cholecystokinin-heptapeptide (CCK-7), i.e., two epimers of 3-(-sulfooxyphenyl)-2-methylpropanoyl-Met-Gly-Trp-Met-Asp-Phe-NH2, two epimers of 3-(4-sulfooxyphenyl)-2-methylpropanoyl-Nle-Gly-Trp-Met-Asp-Phe-NH2 and [D-Try(SO3H)1]-CCK-7, were prepared by the solution method. The analgesic effects of these analogs were measured by means of the writhing test. These analogs produced analgesic effects after subcutaneous injection in mice. The replacement of the tyrosine(O-sulfate) residue at position 1 by a 3(4-sulfooxyphenyl)-2-methyl-propanoyl group enhanced the analgesic effect, and the configuration of these residues hardly influenced the effect. On the other hand, the replacement of the L-methionine residue at position 2 by an L-norleucine residue in addition to the exchange of the tyrosine(O-sulfate) residue at position 1 for a 3-(4-sulfooxyphenyl)-2-methylpropanoyl group reduced the activity.抄録全体を表示PDF形式でダウンロード (839K) -
園田 よし子, 関川 善夫, 佐藤 良博1988 年 36 巻 3 号 p. 966-973
発行日: 1988/03/25
公開日: 2008/03/31
ジャーナル フリーThe effects of oxygenated lanosterol derivatives (1-27, 5μM) including 32-oxygenated lanosterol derivatives on cholesterol biosyntheiss from [24, 25-3H2]-24, 25-dihydrolanosterol (18μM) were tested in 10000×g supernatant (S-10) fraction of rat liver homogenate. Among the derivatives, 7-oxolanost-8-en-3β-ol (7-oxo-DHL), 3β-acetoxylanost-8-en-7-one (7-oxo-DHL-3-OAc), and 7-oxolanosta-5, 8, 11-trien-3β-ol were highly active in depression cholesterol biosynthesis from 24, 25-dyhydrolanosterol. The inhibitory activities of these derivatives on cholesterol synthesis are discussed on the basis of the position and stereochemistry of the oxygen functional groups on the sterol nucleus. The effect of aphidicolin on cholesterol synthesis was also compared with that of 7-oxo-DHL.抄録全体を表示PDF形式でダウンロード (776K) -
白石 忠義, 亀山 啓司, 今井 直博, 堂本 剛史, 勝見 郁男, 渡辺 清1988 年 36 巻 3 号 p. 974-981
発行日: 1988/03/25
公開日: 2008/03/31
ジャーナル フリーA series of α-cyanocinnamamide derivatives was synthesized and evaluated for inhibitory activity against tyrosine-specific protein kinase using intact plasma membrane fractions from an epidermoid carcinoma cell line, A-431 cells. Among these compounds, several novel α-cyano-4-hydroxy-3, 5-disubstituted cinnamamide derivatives, e.g., α-cyano-3-ethoxy-4-gtdrixt-5-phenyl-thiomethylcinnamamide (ST 638), showed potent inhibitory activity. The studies on the structure-activity relationship revealed that the presence of the hydroxy group at the 4 position and the double bond in the α-cyano-4-hydroxycinnamamide skeleton was important for potent inhibitory activity, and that the presence of hydrophobic groups at the 3 and 5 positions on the benzene ring also enhanced the inhibitory activity of α-cyano-4-hydroxycinnamamide derivatives.抄録全体を表示PDF形式でダウンロード (751K) -
糸川 秀治, 徐 俊平, 竹谷 孝一, 渡辺 謹三, 庄司 順三1988 年 36 巻 3 号 p. 982-987
発行日: 1988/03/25
公開日: 2008/03/31
ジャーナル フリーThree new pregnane glycosides, named periplocosides A, B and C, have been isolated from the antitumor fraction, which was obtained by subjecting the CHCl3 extract of Periploca sepium to column chromatography over silica gel and eluting with CHCl3-MeOh (10 : 1). Their structures were established by various nuclear magnetic resonance techniques and chemical evidence. The major constituents, periplocoside A, showed significant antitumor activity against Sarcoma 180 ascites in mice.抄録全体を表示PDF形式でダウンロード (679K) -
中澤 宏1988 年 36 巻 3 号 p. 988-993
発行日: 1988/03/25
公開日: 2008/03/31
ジャーナル フリーFast atom bombardment mass spectrometric (FAB-MS) analysis of tryptic digest of human growth hormone (hGH) was caried out to verify the primary structures of two kinds of hGHs expressed in Escherichia coli; native type (r-hGH) and N-terminal methionine-containing type of hGH (met-hGH. Both structures were confirmed by comparing the mass spectra of the tryptic digest mixtures with that of authentic hGH extracted from human pituitary (p-hGH). The signals detected in the mass spectura accounted for 82% of the sequence of hGH. In order to determine the location of disulfide bonds, a method was designd for selective preparation of peptide fragments containing a disulfide bond from the tryptic digest. The selection was performed by comparison with high-performance liquid chromatograms before and after the reduction of the digest mixtures with dithiothreitol (DTT). From the mass spectra of two disulfide-containing peptide fragments, the locations of two disulfide bonds in the hGH sequence were confirmed to be the same among the three types of hGHs. The present study indicates that the FAB-MS provides an excellent method for the rapid verification of the primary structure of proteins, and the combination of high-performance liquid chromatography (HPLC) with this method facilitates and analysis of disulfide bonds.抄録全体を表示PDF形式でダウンロード (566K) -
池川 繁男, 小野寺 弘幸, 木下 純子, 藤間 貞彦1988 年 36 巻 3 号 p. 994-999
発行日: 1988/03/25
公開日: 2008/03/31
ジャーナル フリーThe preparation and antigenic properties of lithocholic aicd-bovine serum albumin conjugates in which the haptes are coupled to the carrier protein through a 6α-hemisuccinoyl, 6-O-carboxymethyloximino or 1β-hemisuccinoyl bridge are described. The antisera elcited by both the former conjugates showed relatively poor ability to discriminate lithocholic acid from ursodeoxycholic and chenodeoxycholic acids, whereas that from the latter revealed a high affinity constant (Ka=6.4×107M-1) and excellent specificity to lithocholic acid, exhibiting no significant crossreactivity with any of the major human bile acids.抄録全体を表示PDF形式でダウンロード (708K) -
足立 香子, 難波 宏彰, 大塚 正彦, 黒田 久寅1988 年 36 巻 3 号 p. 1000-1006
発行日: 1988/03/25
公開日: 2008/03/31
ジャーナル フリーThe fruit body of Grifola frondosa (maitake), Basidiomycetes, was confirmed to contain a substance with blood pressure-lowering activity. When powdered fruit body of maitake was given orally to spontaneously hypertensive rats (SHR), blood pressure reduction was observed, in contrast to the control group in which the blood pressure increased with ageing. Ether-soluble (ES) and hot water-soluble (WS) fractions were prepared from the fruit body and their hypertensive action was examined. Blood pressure-lowering activity was found when the dried ES fraction was administered orally at 30mg/kg, but the WS fraction was inactive. Thus, the ES fraction was further separated into setone-soluble (ES-AS) and insoluble (ES-AP) fractions. Administration of 20mg/kg dried material caused a blood pressure reduction of about 45mmHg in the former case and 65mmHg in the latter as compared with the control (about 220mmHg). When the EA-AP fraction was separated to 5 subfractions by thin layer chromatographic analysis, the most potent activity was observed in the subfraction which was detected on the spot of Rf=55.3. When authentic antihypertensive agents were examined in combination with maitake, a hypotensive effect was observed on administration of reserpine. This suggests that the blood pressure-lowering effect of maitake was brought about by a mechanism other than sympatholytic action.抄録全体を表示PDF形式でダウンロード (696K) -
大野 尚仁, 後藤 百合子, 橋本 好和, 宿前 利郎1988 年 36 巻 3 号 p. 1007-1015
発行日: 1988/03/25
公開日: 2008/03/31
ジャーナル フリーZymolyase is a commercially available endo-(1→3)-β-D-glucanase preparation, and is widely used to lyse fungal cell walls. In this paper, the active center of this enzyme preparation was examined by using chemical modification of functional groups of amino acid residues, ultraviolet (UV) spectroscopy, optical rotation measurement ant analysis of the enzymic products. First of all, chemical modifications of the amino acid residues of Zymolyase, by using 1-ethyl-3-(3-dimethyl-aminopropyl)-carbodiimide-HCl or 1-cyclohexyl-3-(2-morpholinyl-4-ethyl)carbodiimide metho-p-toluenesulforate for carboxyl, and N-bromosuccinimide (NBS) for tryptophan residues, caused the loss of (1→3)-β-D-glucanase activity. These inactivations were prevented by the addition of substrate to the reaction mixture. In the presence of the substrate analogues, e.g. laminarabiose or laminaratriitol, a UV difference spectrum attributed to tryptophan residues was observed. This difference spectrum disappeared after NBS oxidation. Secondly, when the specific rotation of carboxymethylated curdlan, a linear (1→3)-β-D-glucan obtained from Alcaligenes faecalis, was measured during the enzymic reaction, the value was more negative than that after mutarotation. These results suggest that carboxyl and tryptophan residues are essential to the enzyme activity and the anomeric specificity of the reducing end of the product is β.抄録全体を表示PDF形式でダウンロード (876K) -
大野 尚仁, 倉知 一也, 宿前 利郎1988 年 36 巻 3 号 p. 1016-1025
発行日: 1988/03/25
公開日: 2008/03/31
ジャーナル フリーA highly branced antitumor (1→3)-β-D-glucan, SSG, obtained from the culture filtrate of Sclerotinia sclerotiorum IFO 9395, is hardly soluble in water. To increase the solubility of SSG, carboxymethylated derivatives were prepared by reaction with monochloroacetic acid, and the antitumor activity and physicochemical properties of the products were comnared. Carboxymethylated derivatives of SSG (CM-SSG) having DS 0.04-0.49 (DS : degree of substitution with carboxymethyl groups per anhydro glucose unit) and CM-culdlan having DS 0.04-0.38 were obtained. As assessed by viscosity, optical rotation and carbon-13 nuclear magnetic resonance (NMR) measurements, CM-SSG and CM-curdlan having DS below ca. 0.1 and ca. 0.2, respectively, formed a gel in neutral aqueous media, but derivatives having higher DS values did not. CM-SSG having DS 0-0.14 showed potent antitumor activity, but higher DS derivatives did not show the activity. On the other hand, CM-curdlan having DS 0.08-0.38 showed antitumor activity. It is suggested that 1) the DS values corresponding to the gel-to-sol transition and the antitumor activity were affected by the existence of side chains and 2) the critical DS values for antitumor activity were higher than those for gel formation.抄録全体を表示PDF形式でダウンロード (907K) -
太田 洋子, 原田 真宏, 中林 利克, 池沢 宏郎1988 年 36 巻 3 号 p. 1026-1034
発行日: 1988/03/25
公開日: 2008/03/31
ジャーナル フリーA metal ion-activated acid adenosine triphosphatase (ATPase) of chicken liver lysosomes was purified from the 100000×g supernatant of lysosomal extract, by fractionation with (NH4)2SO4, column chromatographies on Phenyl-Separose CL-4B, Sephacryl S-300 and Affi-Gel 501, isoelectric focusing, and gel filtration on Sepharose 6B, with a recovery of 0.38% and a 19-fold increase in specific activity.Although the purified enzyme had a molecular weight ranging from 700000 to 800000 according to Sephacryl S-300 gel filtration, the enzyme was dissociated into several subunits having molecular weights ranging from 26000 to 93000 on sodium dodecyl sulfate (SDS)-polyacrylamide gel electrophoresis. By isoelectric focusing, the pI of the enzyme was found to be 4.12. The percentage activity rations of acid phosphatase and phosphodiesterase to ATPase in the enzyme preparations became lower with the progress of purification, those in the finally purified preparation being much lower than reported previously.The enzyme preparation mainly hydrolyzed nucleoside triphosphates, but also acted weakly on adenosine diphosphate (ADP), adenosine monophosphate (AMP), p-nitrophenylphosphate or bis(p-nitophenyl)phosphate. In terms of Km values, adenosine triphoshate (ATP) was the most accessible to the enzyme of all the nucleoside triphosphates tested. At 0.1 mM, nucleoside triphosphates were hydrolyzed in the absence of metal ions in the following order : ATP>GTP>CTP, UTP>dTTP. IN the presence of metal ions, the order of nucleotide preference was only slightly affected.The ATPase activity was markedly inhibited by HgCl2, but other reagents including several SH-blockers and ATPase inhibitors were without effect.抄録全体を表示PDF形式でダウンロード (893K) -
八柳 潤, 小木曽 健人1988 年 36 巻 3 号 p. 1035-1040
発行日: 1988/03/25
公開日: 2008/03/31
ジャーナル フリーThe effect of Zn2+ on the respiratory burst of rat pleural neutrophils was studiesd. Serum treated zymosan (STZ)-stimulated O2 consumption was inhibited by Zn2+ depending on hte Zn2+ concentration and time of cell incubation. Addition of Zn2+ after the stimulation of cells with STZ did not inhibit the O2 consumption Zn2+ failed to affect the cell viability or the opsonizing process of STZ, indicating that the inhibition of O2 consumption was not due to te direct cytotoxic action of Zn2+ or to the interaction of Zn2+ with STZ. In addition, the activity of reduced nicotinamide adenine dinucleotide phosphate (NADPH) oxidase, an enzyme responsile for the respiratory burst of neutrophils, was not inhibited by Zn2+. These results suggested that Zn2+ may inhibit some process of the activation of NADPH oxidase.Equimolar Zn2+ 8-hydroxyquinoline complex (Zn-8HQ), which is known to be unable to penetrate the cell membrane, inhibited the O2 consumption more drastically than did Zn2+ alone. 8-Hydroxyquinoline alone did not cause significant inhibition of O2 consumption, indicating that the inhibitory effect of Zn2+ is potentiated by complexing with 8-hydrozyquinoline. The inhibition of O2 consumption Zn2+ was almost completely restored by washing and reincubating the Zn2+-treated cells in Zn2+-free medium. On the other hand, in the cells treated with Zn-8HQ, the same treatment of cell washing and reincubation only partially restored the O2 consumption. These results suggested that Zn2+ may be acting on the cell membrane of neutrophils.抄録全体を表示PDF形式でダウンロード (726K) -
栗田 昌裕, 杉山 雄一, 伊賀 立二, 花野 学, 杉本 恒明1988 年 36 巻 3 号 p. 1041-1052
発行日: 1988/03/25
公開日: 2008/03/31
ジャーナル フリーWe have developed a systematic method of pharmacokinetic parameter estimation based on the "law of product" and the "law of sum, " just as in the theory of probability. We named this method the "combinatorial approach, " for this approach plays an essential role in the handing of our "combinatorial model scheme" (Kurita et al., J. Pharm. Sci., submitted). First we defined the concept of "conformation" and "subconformation." In any complicated system, simple relations hold among the transfer function or the availability for subconformations. For example we have proved that for any conformation, F(C1)+F(C2)=F(C1+C2) and F(C1*C2)=F(C1)×F(C2) hold, when F(C) stands for the availability of conformation C and C1+C2 is the combination in parallel and C1*C2 is the combination in series. We have introduced the "principle of replacement" and the "principle of substitution" as a concrete method of calculation, and explained how they work using several examples. In steady-state kinetics we have defined the concepts of "upstream" conformation and "downstream" conformation for each compartment. By these availabilities, the concentration ratio between the concentration of the inlet and that of the outlet is determined and these concentrations satisfy additive relations in a log scale just as in a cascade. The combinatorial approach in pharmacokinetics is available to estimate the pharmacokinetic parameters in an intuitive and straightforward manner in a complicated multicompartment model system.抄録全体を表示PDF形式でダウンロード (916K) -
木谷 真実, 尾崎 由紀子, 片山 和憲, 掛見 正郎, 小泉 保1988 年 36 巻 3 号 p. 1053-1062
発行日: 1988/03/25
公開日: 2008/03/31
ジャーナル フリーTo rationalize the observed time courses of furosemide distribution in arbitrarily selected tissues of rats, a phaarmacokinetic analysis based on the perfusion rate-limited model was carried out. Anatomical compartments include liver, kidneys, intestine, muscle and plasma. Required parameters were estimated on the basis of physiological principles for rats.抄録全体を表示PDF形式でダウンロード (731K) -
金庭 延慶, 市川 順一, 松本 崇弘1988 年 36 巻 3 号 p. 1063-1073
発行日: 1988/03/25
公開日: 2008/03/31
ジャーナル フリーPolymorphism of phenylbutazone was investigated in detail. Pure α form of phenylbutazone could not be obtained by conventional methods, but it was found that the β form was transformed to the stable α form in ethanol solution at 4°C. At 15 and 25°C, the β form was transformed to a mixture of the α and δ forms, while at 35°C, tha α form in the mixture was converted to the δ form. These results showed that the preparation of a pure polymorphic form by means of recrystallization in solution is not necessarily straightforward. The dissolution bethavior of each form in buffer solution was examined next. The transition temperatures of the pairs of α and δ forms and of α and β forms were 29.0 and 61.6°C, respectively, in buffer solution as determined by means of the non linear van't Hoff model proposed by Grant et al. The heats of fusion of the α, β and δ forms were 8.74, 6.48 and 6.85 kcal/mol, and their melting points were 91.2, 93.3 and 101.4°C, respectively. These results suggested that the pair of β and δ forms is in a monotropic relation and the pairs of a α and β forms and of α and β forms are in enantiotropic relationships.抄録全体を表示PDF形式でダウンロード (1208K) -
松本 崇弘, 市川 順一, 金庭 延慶, 大塚 誠1988 年 36 巻 3 号 p. 1074-1085
発行日: 1988/03/25
公開日: 2008/03/31
ジャーナル フリーThe transformation behavior of phenybutazone polymorphs during grinding at 4 and 35°C and the solid-state stability and dissoluiton behavior of the ground crystals were investigated kinetically. The α, β and δ forms were transformed to a new polymorphic ζ form, which in turn was transformed to the ε form, which was stable at 4°C. On the other hand, during grinding at 35°C, the δ form was not changed, while the α form was transformed to the δ form by was of the ζ form. The β form was apparently transformed directly to the δ form. The ε form, obtained by grinding, was transformed to the δ form under 0% relative humidity at various storage temperatures after an induction time of a few hours. The mechanism of solid-state transformation of the ε form to the δ form was fond to be random nucleation with two-dimensional growth of nuclei (Avrami-Erofeev model) by means of the Hancock and Sharp method, and the activation energy of this transformation was calculated to be 44.5 kcal/mol. The dissolution rate of the ε form was faster than those of other forms in buffer solution, but the ε form was transformed to the δ form during dissolution.抄録全体を表示PDF形式でダウンロード (2157K) -
GLAGASIGIJ USA, 佐藤 幸夫, 鈴木 康男1988 年 36 巻 3 号 p. 1086-1094
発行日: 1988/03/25
公開日: 2008/03/31
ジャーナル フリーA highly sensitive and reproducible immunoassy method for determination of theophylline was developed by using large unilamellar liposomes. Vesicles incorporating theophylline-phosphatidylethanolamine conjugate on the membrane surface as a sensitizer and including a fluorescent marker, calcein, were prepared by the reverse-phase evaporation method from mixtures of phosphatidylcholines containing various fatty acids and cholesterol. Competitive binding of specific antibody to the analyte drug and the sensitizer on the liposomal membrane resulted in lysis of liposomes, and consequently the amount of entrapped calcein that leaked out was inversely proportional to the concentration of the analyte. From studies of various parameters influencing liposome lysis, it was concluded that the chain length of fatty acid most strongly affected the calcein release. The proposed system is simple, rapid, precise, and sensitive to nanomolar concentrations of theophylline. Furthermore, the sensitized liposomes were stable and gave reproducible results. The principle of this assay should be applicable to routine analysis of a wide variety of drugs in biological samples for the purpose of clinical diagnosis or monitoring.抄録全体を表示PDF形式でダウンロード (979K) -
小川 泰亮, 山本 真樹, 岡田 弘晃, 矢敷 孝司, 島本 次雄1988 年 36 巻 3 号 p. 1095-1103
発行日: 1988/03/25
公開日: 2008/03/31
ジャーナル フリーThe aim of this work was to develop injectable microcapsules containing leuprolide acetate, that would deliver that drug at a zero-order rate over a period of about one month. A large amount of leuprolide acetate, a hydrophilic drug, was entrapped into polylactic aicd (PLA) and copoly-(lactic/glycolic) acid (PLGA) microcapsules prepared by an in-water dring method using a (w/o)/w emulsion. The basic techniques were designed to increase the viwcosities of the inner water phase and w/o emulsion. Under the conditions used, it was possible for the drug to be completely entrapped by the microcapsules in the range of 10 to 20% on the basis of the polymer. However, the release profiles of the drug in vitro were inadequate for controlled release for one month.抄録全体を表示PDF形式でダウンロード (913K) -
今井 公江, 相本 太刀夫, 佐藤 正基, 加藤 善久, 木村 良平, 村田 敏郎1988 年 36 巻 3 号 p. 1104-1109
発行日: 1988/03/25
公開日: 2008/03/31
ジャーナル フリーThe effect of protoporphyrin IX (PP) on lipid peroxidation was investigated in rat liver homogenates, in hepatic subcellular organelles such as mitochondria and microsomes, and in a mixture of unsaturated fatty acids. PP inhibited both the Fe2+ and ascorbic acid (AsA)-stimulated lipid peroxidation and the concomitant increase of oxygen consumption in the homogenates. PP failed to inhibit auto-oxidation in the mixture of unsaturated fatty acids. PP inhibited the lipid peroxidation both in mitochondria stimulated by AsA and in microsomes stimulated by AsA or a reduced nicotinamide adenine dinucleotide phosphate-generating system. Its antioxidative effects were less pronounced in the heat-denatured subcellular fractions. Soluble fraction (SF) enhanced the antioxidative action of PP on the lipid peroxidation in boiled microsomes, but boilde SF lessened the action of PP.These findings indicate that PP has an antioxidative effect on lipid peroxidation in liver, and that the antioxidative effect of PP is mediated by factors present in liver, some of which are heat-labile and some heat-stable.抄録全体を表示PDF形式でダウンロード (636K) -
三村 務, 小浜 靖弘, 桑原 栄樹, 山本 浩二, 小宮山 豊, 佐竹 幹雄, 千葉 義行, 宮下 和之, 田中 徹明, 今西 武, 岩田 ...1988 年 36 巻 3 号 p. 1110-1116
発行日: 1988/03/25
公開日: 2008/03/31
ジャーナル フリーThe characteristics of platelet anti-aggregant activity of 2, 2-dimethylthiazolidine hydrochloride (I) and 2-(4-hydroxy-3-methoxyphenyl)thiazolidin (II) have been evaluated. Compounds I and II were potent inhibitors of collagen- and arachidonic acid-induced aggregation of rat and rabbit platelets (IC50 or IC100 values : 10-5-10-4 M), while they were less effective in the cases of adenosine 5'-diphosphate 2Na, A-23187 and labile aggregation-stimulating substance. Also, both compounds inhibited platelet shape change induced by a low concentation of arachidonic acid. Compounds I (100μM) and II (25μM) significantly inhibited serotonin release and thromboxane B2 formation induced by arachidonic acid in rabbit platelets. Compound I (100μM) inhibited prostaglandin I2 formation in rat aorta, but II (100μM) did not. In contrast, neither compound had any effect on platelet adhesiveness. These results strongly suggest that I and II prevented platelet aggregation, shape change and serotonin release reaction via their inhibitory effects on arachidonic acid metabolism of platelets, and the inhibiting potency of II was higher than that of I.抄録全体を表示PDF形式でダウンロード (738K) -
釈 邦夫, 渡辺 隆史, 須賀 哲弥1988 年 36 巻 3 号 p. 1117-1121
発行日: 1988/03/25
公開日: 2008/03/31
ジャーナル フリーIn order to clarify the inhibitory mechanism of 5-tridecylpyrazole-3-carboxylic acid (TDPC) on the absorptive process of cholesterol, the effects of this agent on micelle in vitro and intestinal uptake of cholesterol in rats as measured by the ligated-loop method in situ were investigated using β-sitosterol as a reference agent.TDPC did not affect the micellar formation of distribution of micellar size, both of which are important determinants in the process of cholesterol uptake, but β-sitosterol increased the distribution of large-size micelles (>450nm).TDPC significantly decreased the intestinal cholesterol uptake by 27%, 44% and 59% at the dose levels of 0.25, 0.50 and 1.0mg, respectively. Similarly, β-sitosterol significantly decreased the cholesterol uptake by 79% at the dose of 1.0mg.It is apparent from the above data that the hypocholesterolemic activity of TDPC and β-sitosterol partly depends on interference with intestinal cholesterol uptake, though there is a difference between the two agents in terms of the effect on micellar size. It can be assumed that both energy-dependent and -independent systems are involved in the process of the intestinal cholesterol uptake, and hte inhibitory effect of TDPC might berelated to the energy-independent system rather than the energy-dependent system.抄録全体を表示PDF形式でダウンロード (605K) -
長友 孝文, 青野 遵一郎, 田尻 明, 中村 隆志, 土橋 洋史1988 年 36 巻 3 号 p. 1122-1127
発行日: 1988/03/25
公開日: 2008/03/31
ジャーナル フリーIn order to assess the antihypertensive activities of SGB-1534, 3-[2-[4-(o-methoxyphenyl)-1-piperazinyl]ethyl]-2, 4-(1H, 3H)-quinazolinedione monohydrochloride, the effect of this drug on the 3H-prazosin, 3H-p-aminoclonidine and 3H-dihydroalprenolol (3H-DHA) bindings to α1-, α2-and β-adrenoceptors in dog brain and aorta was determined by means of radioligand binding assay and compared with that of prazosin. Potent inhibition of 3H-prazosin binding to α1-adrenoceptor sites in the brain and the aorta by SGB-1534 was observed (the potency in the brain was almost the same as that prazosin), but the inhibition of 3H-p-aminoclonidine and 3H-DHA bindings to α2-and β-adrenergic binding sites by both SGB-1534 and prazosin was very weak. In addition, a high pA2 value of α1-blocking action by SGB-1534 was fornd in a pharmacological experiment. Thus, these results suggest that the inhibitory effect of SGB-1534 at α1-adrenoceptor binding sites, but not at α2-or β-adrenozeptor sites, may contribute to the hyprotensive effect.抄録全体を表示PDF形式でダウンロード (651K) -
井口 貞彦, 宮田 康行, 奥山 繁広, 三宅 八二六, 桶川 忠夫1988 年 36 巻 3 号 p. 1128-1134
発行日: 1988/03/25
公開日: 2008/03/31
ジャーナル フリーSynthesized was 15-cis-(4-n-propylcyclohexyl)-16, 17, 18, 19, 20-pentanor-9-deoxy-6, 9α-nitrilo-prostaglandin F1 methyl ester (OP-2507), a novel, promising anti-cerebral ischemic agent. A key intermediate, methyl cis-4-n-propylcyclohexanecarboxylate, was prepared stereoselectively by the hydrogenation of methyl 4-n-propylbenzoate with commercially available dimer of chloro(1, 5-cyclooctadiene)rhodium as a catalyst. Stereoselective reduction of C15-ketone to C15α-alcohol was achieved with diisobutylaluminum 2, 6-di-tert-butyl-4-methylphenoxide.抄録全体を表示PDF形式でダウンロード (742K) -
森田 岩男, 畳開 庄一, 津田 正己, 黄瀬 正博, 杉山 信1988 年 36 巻 3 号 p. 1135-1138
発行日: 1988/03/25
公開日: 2008/03/31
ジャーナル フリーThe reaction of cyclic silyl phosphites (2) with haloacetones (3) was in vestigated. When oxirane compounds were used as scavengers of trimethylsily halides, cyclic acetonylphosphonates (4) were obtained directly. Treatment of 2-trimethylsilyloxy-1, 3, 2-dioxaphosphorinane (2a) with bromoacetone (3b) or iodoacetone (3c) in propylene oxide gave 4a in 24% and 41% yields, respectively. With cyclohexane oxide, the reaction of 2a with 3c in MeCN at reflux gave 4a in 50% yield. Treatment of 5, 5-dimethyl-2-trimethylsilyloxy-1, 3, 2-dioxaphosphorinane (2b) with 3c in the same manner gave 4b in 43% yield.抄録全体を表示PDF形式でダウンロード (456K) -
森田 岩男, 津田 正己, 黄瀬 正博, 杉山 信1988 年 36 巻 3 号 p. 1139-1142
発行日: 1988/03/25
公開日: 2008/03/31
ジャーナル フリーAttempts were made to improve the synthesis of methyl 2, 6-dimethyl-4-(2-nitrophenyl)-5-(2-oxo-1, 3, 2-dioxaphosphorinan-2-yl)-1, 4-dihydropyridine-3-carboxylate (DHP-218), a new calcium antagonist. 2-Acetonyl-2-oxo-1, 3, 2-dioxaphosphosphorinane (5a), the key intermediate, was prepared from the allenylphosphonate (2) via the enaminophosphonate (4) in a good yield. Subsequently, the Knoevenagel condensation using 5a and the imine (6a) gave the benzylideneacetonylphosphonate (7a) in a good yield without the use of the Horner-Emons reaction. This condensation also gave good results for other acetonylphopshonates. The final step gave DHP-218 in a good yield through a modified Hantzsch synthesis with the use of a dehydrating agent. The overall yield was increased from 1.7% to 22%.抄録全体を表示PDF形式でダウンロード (517K) -
伊古田 暢夫, 花木 昭1988 年 36 巻 3 号 p. 1143-1146
発行日: 1988/03/25
公開日: 2008/03/31
ジャーナル フリーAn improved and facile synthesis of (2R, 3S, 4R)-2-hydroxymethyl-3, 4-dihydroxypyrrolidine derivatives (11 and 15), which are important intermendiates for the synthesis of (-)-swainsonine, from D-ribonolactone was developed.抄録全体を表示PDF形式でダウンロード (526K) -
杉山 直和, 菅井 啓, 山田 宣之, 後藤 元彰, 伴 千恵子, 古畑 公夫, 高柳 弘明, 小倉 治夫1988 年 36 巻 3 号 p. 1147-1152
発行日: 1988/03/25
公開日: 2008/03/31
ジャーナル フリーA new lactone compound was isolated as a minor by-product from the reaction mixture of N-acetylneuraminic acid with acetic anhydride in pyridine, in addition to the major product, 2, 4, 7, 8, 9-penta-O-acetyl-N-acetylneuraminic acid. The structure of the new compound was elucidated to be 5-acetamido-2, 4, 8, 9-tetra-O-acetyl-3, 5-dideoxy-β-D-glycero-D-galacto-2-nonulopyranosono-1, 7-lactone by nuclear magnetic resonance, mass spectroscopy and X-ray crystal analysis. It was revealed that the absolute configurations of the asymmetric centers of the new compound were consistent with those for the original N-acetylneuraminic acid with the conversion of the pyranose ring conformation from 2C5(D) to 5C2(D).抄録全体を表示PDF形式でダウンロード (590K) -
松本 広淳, 金子 千里, 山田 敬子, 竹内 惟雄, 森 武雄, 水野 義久1988 年 36 巻 3 号 p. 1153-1157
発行日: 1988/03/25
公開日: 2008/03/31
ジャーナル フリーA convenient and economical synthesis of 9-(2-hydroxyethoxymethyl)guanine (1, acyclovir, Zovirax, or acyclic guanosine : an antiherpetic agent)from guanine was developed via N2, O-diacetylacyclovir. Two closely related compounds, N2-acetylacyclovir (7) and O-acetylacyclovir (8), were also prepared by selective deacetylation.抄録全体を表示PDF形式でダウンロード (515K) -
丹羽 正武, 岩垂 安彦, 呉 永昌, 平田 義正1988 年 36 巻 3 号 p. 1158-1161
発行日: 1988/03/25
公開日: 2008/03/31
ジャーナル フリーTwo new phenylpropanoid diglucosides named syringinoside and coniferinoside have been isolated from the water-soluble fraction of Wikstroemia sikokiana FRANCE. et SAV. (Thymelaeaceae). Their structures have been characterized on the basis of spectral and chemical evidence.抄録全体を表示PDF形式でダウンロード (481K) -
染井 正徳, 脇田 真之, 太田 敏晴1988 年 36 巻 3 号 p. 1162-1168
発行日: 1988/03/25
公開日: 2008/03/31
ジャーナル フリーA simple synthetic metho which can provide 3, 4, 5, 6-tetrahydro-1H-azepinol[5, 4, 3-cd]indole derivatives having a carbon side chain at any desired position of the nucleus was developed. The method was applied to the preparation of 4- and 5-alkyl-3, 4, 5, 6-tetrahydro-1H-azepino[5, 4, 3-cd]indoles.抄録全体を表示PDF形式でダウンロード (824K) -
佐藤 毅, 本橋 重康, 山川 浩司1988 年 36 巻 3 号 p. 1169-1173
発行日: 1988/03/25
公開日: 2008/03/31
ジャーナル フリーThe alkylation of 4-(phenylthio)butanal with 1-chloroalkyl phenyl sulfoxides gave chlorohydrins, which were tereated with excess thiophenolate in tert-butanol to afford α, δ-bis(phenylthio)ketones in good overall yield. On treatment with m-chloroperbenzoic acid followed by pyrolysis in refluxing toluene, the bis(phenylthio)ketones gave 1-acylbutadienes in moderate yield with high E-stereoselectivity.抄録全体を表示PDF形式でダウンロード (576K) -
金城 順英, 竹下 尚, 安部 洋子, 寺田 尚子, 山下 博己, 山崎 政城, 竹内 一男, 村上 光太郎, 富松 利明, 野原 稔弘1988 年 36 巻 3 号 p. 1174-1179
発行日: 1988/03/25
公開日: 2008/03/31
ジャーナル フリーA new triterpenoidal saponin, 3-O-[α-L-rhamnopyanosyl(1→2)-α-L-arabinopyranosyl(1→2)-β-D-glucuronopyranosyl]sophoradio (I), was isolated from the flowers of Pueraria lobata (WILLD.) OHWI (Leguminosae). Its structure was elucidated on the basis of chemical and physicochemical evidence. In addition, a known oligoglycoside kaikasaponin III (II) was isolated from both flowers and leaves of this plant, together with several known aromatic compounds.抄録全体を表示PDF形式でダウンロード (648K) -
福永 武彦, 西谷 公一, 梶河 郁子, 渡辺 好邦, 鈴木 信夫, 竹谷 孝一, 糸川 秀治1988 年 36 巻 3 号 p. 1180-1184
発行日: 1988/03/25
公開日: 2008/03/31
ジャーナル フリーThe chemical constituents of Hyphear Tanakae HOSOKAWA epiphyting to four different host trees were examined. A new triterpene fatty acid ester (III) and four known flavonoid glycosides, rhamnocitrin-3-O-rhamnoside (V), kaempferol-3-O-rhamnoside (VI), rhamnetin-3-O-rhamnoside (VII), and quercetin-3-O-rhamnoside (VIII) have been isolated from the leaves and twigs of this plant epiphyting to Castanea creanata SIEB., together with fatty acids (I), phytosterol (II), and phytosterol-glucoside (IV). The present investigation has revealed that compounds II-V, VII, and VIII are contained in this plant irrespective of the host, among the four host trees., examined.抄録全体を表示PDF形式でダウンロード (588K) -
福永 武彦, 梶河 郁子, 西谷 公一, 渡辺 好邦, 鈴木 信夫, 竹谷 孝一, 糸川 秀治1988 年 36 巻 3 号 p. 1185-1189
発行日: 1988/03/25
公開日: 2008/03/31
ジャーナル フリーA new flavonol glycoside, isorhamnetin-3-O-[apiosyl(1→6)]glucosyl-7-O-rhamnoside, and a new phenylpropane glycoside, coniferylalcohol-4'-O-[apiosy(1→2)]glucoside, were isolated from the n-BuOH extract of Viscum album L. (Loranthaceae). The structures were established based on the spectral and chemical data. Two known flavonoid glycosides, isorhamnetin-3-O-rutinoside and (2S)-homoeriodictyol-7-O-glucoside, were also isolated.抄録全体を表示PDF形式でダウンロード (519K) -
傳 宏達, 安斉 順一, 長 哲郎, 松尾 正之1988 年 36 巻 3 号 p. 1190-1193
発行日: 1988/03/25
公開日: 2008/03/31
ジャーナル フリーTwo kinds of enzyme sensors were fabricated by chemically immobilizing an enzyme on the gate surface of an ion-sensitive field effect transistor (ISFET). One is a trypsin-membrane/ISFET sensor, which can measure concentrations of N-benzoyl-L-arginine ethyl ester in the range from 5×10-4 to 5×10-2M. The other is an α-chymotrypsin-membrane/ISFET sensor, which can measure concentrations of N-acetyl-L-tyrosine ethyl ester solution in the range of 5×10-4-5×10-3M. The response of the sensors was affected markedly by pH and the concentration of the working buffer.抄録全体を表示PDF形式でダウンロード (410K) -
小嶋 正治, 栗原 悟, 金沢 洋子, 原田平 輝志, 前原 喜彦, 遠藤 英也1988 年 36 巻 3 号 p. 1194-1197
発行日: 1988/03/25
公開日: 2008/03/31
ジャーナル フリーThe metabolic products of 2-deoxy-2-fluoro-D-glucose (FDG) and 2-deoxy-2-fluoro-D-mannose (FDM) in sarcoma 180 cells transplanted in mice were investigated by fluorin-19 nuclear magnetic resonance (19F-NMR) spectroscopy. It became apparent that the administered FDG was converted to FDM (and/or FDM-6-phosphate) in tumor cells, and also the administered FDM was converted to FDG (and/or FDG-6-phosphate). At 9h after administration of FDM, the ratio of FDG (and/or FDG-6-phosphate) and FDM (and/or FDM-6-phosphate) reached equilibrium. On the other hand, it took more than 48h in the case of FDG administration. The equilibrium amount of FDM (and/or FDM-6-phosphate) was approximately four times as much as that of FDG (and/or FDG-6-phosphate) in both cases.抄録全体を表示PDF形式でダウンロード (473K) -
大野 尚仁, 安達 禎之, 宿前 利郎1988 年 36 巻 3 号 p. 1198-1204
発行日: 1988/03/25
公開日: 2008/03/31
ジャーナル フリーFungal (1→3)-β-D-glucans possess two kinds of conformations in the solid state, i.e., helix (curdlan type) and native (laminaran type)(Ohno et al., Chem. Pharm. Bull., 34, 2555 (1986); Saito et al., Bull. Chem. Soc. Jpn., 59, 2903 (1986)). In this paper, the glucan conformations in the fruit bodies of several edible fungi were examined by using carbon-13 cross polarization-magic angle spinning (CP/MAS) nuclear magnetic resonance (NMR) spectroscopy. The fruit bodies were washed extensively with water, defatted by refluxing with ethanol, and/or treated with mataperiodate then borohydride. Most of the fruit bodies showed C-3 signals at about 86ppm, resembling those of the native form. These findings suggested that the (1→3)-β-D-glucan conformation in the fruit body is the "native form."抄録全体を表示PDF形式でダウンロード (741K) -
恒松 英明, 荒谷 秀和, 水崎 幸一, 畑中 美博, 川田 修二, 山本 孫兵, 牧角 啓1988 年 36 巻 3 号 p. 1205-1209
発行日: 1988/03/25
公開日: 2008/03/31
ジャーナル フリーβ-Naphthylamides of p-guanidino-L-phenylalanine (GPA) and p-guanidino-DL-phenylglycine (GPG) were synthesized and tested as substrates of bovine leukocyte aminopeptidase (BL-APase) and porcine liver aminopeptidase B (PL-APaseB) in comparison with L-arginine β-naphthylamide (Arg-βNA). BL-APase-catalyzed bydrolysis of GPA-βNA proceeded as fast as that of Arg-βNA, while the rate of hydrolysis of GPG-βNA was much slower. The specificity constant (Vmax/Km) for the hydrolysis of GPA-βNA by BL-APase was somewhat larger than that for the hydrolysis of Arg-βNA. The benzene ring in the side chain of GPA-βNA is considered to contribute to the binding of this substrate to the specificity side to this enzyme, based on comparison of the Km values for the two β-naphthylamide substrates. Substrate inhibition was observed with BL-APase in the hydrolysis of GPA-βNA in the substrate concentration range higher than about 0.1 mM. Neither GPA-βNA nor GPG-βNA was hydrolyzed by PL-APaseB and they inhibited the hydrolysis of Arg-βNA by this enzyme. GPA-βNA is expected to be a useful substrate in the study of the binding and catalytic specificities of aminopeptidases.抄録全体を表示PDF形式でダウンロード (561K) -
食見 忠弘1988 年 36 巻 3 号 p. 1210-1213
発行日: 1988/03/25
公開日: 2008/03/31
ジャーナル フリーChanges in the activities of lysosomal thiol proteinases and their endogenous inhibitors were examined in the rat pancreatic tissue. Imposed stress such as fasting affected the activities of cathepsins B and H but not those of their endogenous inhibitors. However, changes in the activities of cathepsins B and H are closely related to changes in the activities of their inhibitors. During the phase of hypoglycemia and hyperinsulinemia induced by streptozotocin, there were increments in the activities of cathepsins B and H and their endogenous inhibitors. These changes were not related to increases in the levels of serum insulin but rather to pathological changes in the pancreas.抄録全体を表示PDF形式でダウンロード (469K)