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SHINSAKU NATORI
1983 Volume 103 Issue 11 Pages
1109-1128
Published: November 25, 1983
Released on J-STAGE: May 30, 2008
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This review describes our surveys on mycotoxins using cytotoxicity testing, chemical studies on new mycotoxins such as terphenyllin, xanthoascin, chaetochromin, cochliodinol isomers, and chaetoglobosins A-G and J, and their toxic effects. Since chaetoglobosins belong to the new type of cytochalasans, present status of chemical and cell biological studies on cytochalasans was mentioned. Our recent observations on the effects of cytochalasans at molecular and cellular levels were also described.
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EMIKO TOMITORI, TOSHIHIKO OKAMOTO, TATSUO IDO
1983 Volume 103 Issue 11 Pages
1129-1132
Published: November 25, 1983
Released on J-STAGE: May 30, 2008
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Reaction of 3-nitropyridine (1) with potassium cyanide in methanol gave 4-cyano-3-methoxypyridine (2), 2-cyano-3-methoxypyridine (3) and the corresponding amides. The methylation of acidic by-products with diazomethane gave 3-methyl-4-oxo-3, 4-dihydro [5, 6-c]-1, 2, 3-triazine (8) and 3-methyl-8-and 6-methoxy-4-oxo-3, 4-dihydro [5, 6-c]-1, 2, 3-triazines (9 and 10).
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NORITO KANEDA, HIROYUKI NAKANISHI, TADAYUKI KURAISHI, TATUHIKO KATORI
1983 Volume 103 Issue 11 Pages
1133-1139
Published: November 25, 1983
Released on J-STAGE: May 30, 2008
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The components of Ophiopogon roots (China) was investigated. In addition to the reported components of Ophiopogon japonicus KER-GAWLER, i.e. homoisoflavanoids (methylophiopogonanone A, B, ophiopogonanone A), eight unknown compounds, five homoisoflavanoids (I, II, III, IV, V), amide compound (VI) and two borneol glycosides (VII, VIII) were isolated.
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TAKASHI HARAYAMA, MUNEO TAKATANI, YASUHIRO TEZUKA
1983 Volume 103 Issue 11 Pages
1140-1143
Published: November 25, 1983
Released on J-STAGE: May 30, 2008
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In connection with synthetic study of lycophlegmarine, stereoselective synthesis of the allyl alcohol (D : R=CF
3), which was an intermediate of fawcettimine synthesis, was investigated. In that occasion, acylation of 1 and 2 in pyridine with (CF
3CO)
2O overnight gave mainly the unexpected epoxide (5) and (6), respectively. Acylation with pyridine-(CF
3CO)
2O under oxygen atmosphere gave only the epoxide for 3 h, and acylation with NEt
3-(CF
3CO)
2O or pyridine-Ac
2O afforded the corresponding diacyl olefin even under oxygen atmosphere. Moreover, epoxides (5) and (6) were converted to the allyl alcohol (D : R=CF
3) in a high yield via the same ketone (B=10). This means that stereoselective and formal synthesis of fawcettimine was achieved.
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TETSUJI KAMETANI, KAZUO KIGASAWA, HIROAKI SHIMIZU, SETSU SAITOU, SHIGE ...
1983 Volume 103 Issue 11 Pages
1144-1150
Published: November 25, 1983
Released on J-STAGE: May 30, 2008
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The general acylation of aromatic amides with substituted phenyl acylates was studied. Amides, i.e. benzamide or ethenzamide, were allowed to react with various p-nitrophenyl acylates (acyl moiety ; CH
3CH
2CO, CH
3 (CH
2)
2CO, (CH
3)
2CHCO, CH
3 (CH
2)
3CO, (CH
3)
3CCO, CH
3 (CH
2)
4CO, CH
3 (CH
2)
10CO, CICH
2CO, PhCH
2CO, PhCO, p-NO
2-PhCO, 2-C
4H
3OCO) either in the molten state or in xylene. It was found that benzamide and ethenzamide were acylated with p-nitrophenyl acylates, and that the acidity of the corresponding carboxylic acid with acyl moiety reflects on the yield of imides, although the transacylation of aromatic acylate was generally slower than that of aliphatic acylate.
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TSUNEMATSU TAKEMOTO, SHIGENOBU ARIHARA, TADASHI NAKAJIMA, MEGUMI OKUHI ...
1983 Volume 103 Issue 11 Pages
1151-1154
Published: November 25, 1983
Released on J-STAGE: May 30, 2008
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Fructus Momordicae (fruit of Momordica grosvenori SWINGLE, Cucurbitaceae) is a special crude drug of Kwangsi, China. Isolation and some properties of new sweet triterpene glycosides, named mogrosides IV, V, and VI from Fructus Momordicae, were described.
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TSUNEMATSU TAKEMOTO, SHIGENOBU ARIHARA, TADASHI NAKAJIMA, MEGUMI OKUHI ...
1983 Volume 103 Issue 11 Pages
1155-1166
Published: November 25, 1983
Released on J-STAGE: May 30, 2008
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TSUNEMATSU TAKEMOTO, SHIGENOBU ARIHARA, TADASHI NAKAJIMA, MEGUMI OKUHI ...
1983 Volume 103 Issue 11 Pages
1167-1173
Published: November 25, 1983
Released on J-STAGE: May 30, 2008
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The structure of mogroside V (1), C
60H
102O
29·2H
2O, the sweet principal of Fructus Momordicae, has been established by chemical and spectroscopic evidence as mogrol-3-O-[β-D-glucopyranosyl (1→6)-β-D-glucopyranoside]-24-O-{[β-D-glucopyranosyl (1→2)]-[β-D-glucopyranosyl (1→6)]-β-D-glucopyranoside}.
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TAKEFUMI SHIMIZU, MASANORI KUBO, KAZUYUKI NAKAGAWA
1983 Volume 103 Issue 11 Pages
1174-1179
Published: November 25, 1983
Released on J-STAGE: May 30, 2008
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A simplified coupled column technique for the simultaneous determination of cilostamide and its metabolites in biological fluid by high performance liquid chromatography (HPLC) was developed. In this method, the plasma and urine containing an intact drug and its metabolites are injected into HPLC system directly. The effluent from the primary exclusion column is passed continuously through a four-port valve to waste. When monitoring of the elution of the biopolymers by the refractive index (RI) detector is completed, the valve diverts the metabolites and intact drug concentrated on the hydrophilic gel permeation column to the secondary column for separation. Their separation is achieved by using a gradient elution to elute the sample from the secondary column, and their detection is performed by a ultraviolet (UV) detector and a fluorescence (FL) detector. The detection limit is about 3 ng with the injection volume used in this method, and the coefficient of variation is less than 1% in retention time and less than 3% in the peak height.
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SHIGENORI NISHIDE, TAMIYUKI MIKURA, TERUKATSU YAMADA, YOICHI TOSHIMA, ...
1983 Volume 103 Issue 11 Pages
1180-1184
Published: November 25, 1983
Released on J-STAGE: May 30, 2008
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An improved method for the determination of betahistine mesylate was developed by use of ultraviolet spectrophotometry. It was found that the measurement results of the mesylate in aqueous solution were affected easily by the variation of both concentration of the mesylate and temperature when measured, affording poor reproducibility. The measurement of the mesylate by use of 0.1 N sulfuric acid instead of water as a solvent presented more stable and accurate determination free from influence of these variations.
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NAOHITO OHNO, TOSHIRO YADOMAE, TOSHIO MIYAZAKI
1983 Volume 103 Issue 11 Pages
1185-1189
Published: November 25, 1983
Released on J-STAGE: May 30, 2008
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Streptococcus pneumoniae cell is known to resist to lysozyme digestion. The resistant factor was examined by using cell and solubilized cell wall components (AS') prepared by the autoplast formation. Although the cell bound lysozyme at 4°C, it resists to lysozyme digestion. A certain component contained in AS'formed an insobuble complex with lysozyme and inhibited the activity of lysozyme. The insoluble complex was mainly composed of protein and phosphate ester. The inhibitory activity was destroyed by heat, protease, or nuclease treatment. This suggests that the resistant factor is a non-peptidoglycan component of the cell wall.
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YOSHIYUKI HIRAKAWA, KIYOSHI HARADA
1983 Volume 103 Issue 11 Pages
1190-1194
Published: November 25, 1983
Released on J-STAGE: May 30, 2008
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The physicochemical properties and gastrointestinal absorption of the ultra-fine size reduced oxolinic acid (OA) prepared according to the previous paper were investigated in comparison with original and mechanical pulverized crystals. It was found that there was no change in their crystal forms by powder X-ray diffraction measurement and their dissolution rates increased remarkably. Moreover, by use of this OA, a significant improvement was detected in the level of plasma concentration of OA after oral administration to dogs and the areas under the plasma concentration-time curve of them were 2.5 times the mechanical pulverized crystals.
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MICHIHIRO KOBAYASHI, MAKIO KITAZAWA, TAKENAO SAITO
1983 Volume 103 Issue 11 Pages
1195-1199
Published: November 25, 1983
Released on J-STAGE: May 30, 2008
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Facile synthetic methods of 2, 4-oxazolidinedione (2), a key intermediate of 3-{2-(2-thienyl) ethyl}-2, 4-oxazolidinedione (3) having potent antiulcer activities, were studied. As a result, potassium salt (8a) of 2, 4-oxazolidinedione was conveniently obtained in good yield by the reaction of ethyl glycolate with KOCN. Furthermore, potassium salts (8) of 5-substituted and 5, 5-disubstituted-2, 4-oxazolidinediones were obtained by the reaction of the corresponding 2-hydroxy acid esters (4) with KOCN. The compound (8a) was also prepared by the reaction of ethyl N-chloroacetylcarbamate (14) and NaOAc, followed by treatment of the product (15) with KOH.
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MASAHIKO IKEKITA, YOSHIKO SHINA, YUMI TAKEMOTO, KAZUYUKI KIZUKI, HIROS ...
1983 Volume 103 Issue 11 Pages
1200-1205
Published: November 25, 1983
Released on J-STAGE: May 30, 2008
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An expeditious and sensitive colorimetric method to measure elastase activity using Congo red-elastin as a substrate is described. Highly purified elastase EI as low as 1.65 μg may be assessed accurately within 1 h. This assay is thus 10-100 times more sensitive than previous methods using elastin as a substrate. In this assay method, however, the elastinolytic activity is amplified when a sufficient amount of trypsin and/or chymotrypsin is present in the assay samples. Therefore it is necessary to inhibit the activities of contaminant trypsin and/or chymotrypsin by limabean trypsin inhibitor (LBTI) and chymostatin, by which elastase activity was not influenced. And the coefficients between amidolytic and elastinolytic activities assayed by our methods of both highly purified and crude elastase preparations (AU/CU) were exactly equal to be about 14.
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MIKIO NAKAMURA, MASAHIRO YOSHIKURA, SHIGEO OBATA, TSUNEJI NAGAI
1983 Volume 103 Issue 11 Pages
1206-1209
Published: November 25, 1983
Released on J-STAGE: May 30, 2008
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This paper deals with interfacial viscoelasticities of oil/water-system, which was prepared from a coconut oil as an oil phase and gum arabic solution as a water phase. The measurements were based on the damped oscillation method, using a rheometer aided with computer which was developed in our laboratory. As a result, it was found that the interfacial viscoelasticities increased with an increase in the molecular weight of gum arabic, the concentration of gum arabic or the ionic strength of the solution. The evidence suggested that the interfacial film forms an adsorbed film similar to an elastic solid. This property of film would account for the stability of gum arabic emulsion.
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TOHRU HIROSE, JUNJI NAKANO, HITOSHI UNO
1983 Volume 103 Issue 11 Pages
1210-1214
Published: November 25, 1983
Released on J-STAGE: May 30, 2008
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N-Benzyloxy-2-(N-tert-butoxycarbonyl) amino-2-hydroxymethylpropionamide (8) was synthesized from methyl DL-isocyanopropionate (2). Compound 8 was treated with diethyl azodicarboxylate and triphenylphosphine to give β-lactam derivative (9), which was hydrogenolized with H
2/Pd-C to the N-hydroxy compound (10) followed by treatment with TiCl
3 to give the unsubstituted β-lactam derivative (11). Sulfonation of 11 with a pyridine-sulfur trioxide complex and deprotection with formic acid afforded a key intermediate, DL-3-amino-3-methyl-2-azetidinone-1-sulfonic acid (12). The desired 3-N-acylamino-3-methyl-2-azetidinone-1-sulfonic acid derivatives (13a, 13c and 13e) were obtained by acylation of 12. None of the compounds (13a, 13c and 13e) showed antibacterial activity, although the 4α-methyl counterparts (13f) had some activities against gram-negative bacteria.
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YOSHIYUKI HIRAKAWA, KIYOSHI HARADA
1983 Volume 103 Issue 11 Pages
1215-1218
Published: November 25, 1983
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It was found in the previous papers that oxolinic acid (OA) crystals were reduced to ultra-fine size by the new method of present authors. Therefore, several investigations were carried out to infer the origin for ultra-fine size reduction in this paper. It was inferable from the results that surfactants or polymers which coexisted in the crystal formation-growth process adsorbed on the surface of microparticles, and the size reduction effect had been displayed due to suppressing the aggregation for their dispersing action.
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YOKO MATSUKI, TSUYOSHI GOROMARU, HIROSHI MATSUURA
1983 Volume 103 Issue 11 Pages
1219-1223
Published: November 25, 1983
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After the administration of isoniazid (p.o.) alone or in combination with ascorbic acid (p.o.or i.p.) to rats, the excreted amount of isoniazid and its metabolites, acetylisoniazid, isonicotinuric acid, hydrazine and acetylhydrazine, were determined quantitatively by gas chromatography and liquid chromatography. It was clarified that a marked decrease of free hydrazine and an increase of acetylisoniazid were observed in the case of co-administration of isoniazid and ascorbic acid. Concerning the excretion of isoniazid and isonicotinic acid, no significant difference between co-administration and single administration was observed. The decrease of hydrazine may be due to the reaction of hydrazine with ascorbic acid in vivo.
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