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Volume 104, Issue 11
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ATSUSHI ICHIKAWA1984 Volume 104 Issue 11 Pages 1109-1121
Published: November 25, 1984
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSIn many mammalian cells, cyclic adenosine 3', 5'-monophosphate (cAMP) and calcium (Ca2+) served interrelated second messenger functions in the control of cellular function and growth. We have investigated; (i) the effects of cAMP and Ca2+ on the control of histamine release from mast cells stimulated by active oligomers, of which releases are dependent on extracellular Ca2+ or not. (ii) the fluctuations of cAMP levels, PGE1-binding, and several cellular functions because of the cells respond to Bt2cAMP, and PGE1 with decreased growth rate and increased expression of more mature, differentiated mast cell phenotypes, and also because PGE1 specifically binds to the cells and elevates cAMP levels. (iii) the cell cycle-dependent changes of cAMP and Ca2+ levels, and certain cellular functions in synchronous mastocytoma P-815 cells.View full abstractDownload PDF (1229K) -
EMIKO TOMITORI, TOSHIHIKO OKAMOTO1984 Volume 104 Issue 11 Pages 1122-1132
Published: November 25, 1984
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSReaction of 3-nitro-2, 6-dimethylpyridine (1) with potassium cyanide in methanol gave 3-methoxy-6-methylpyridine-2-carbonitrile 1-oxide (2), 5, 7-dimethyl-3-iminoisoxazolo [3, 4-c]-pyridine dimer (3) and 6, 8-dimethyl-4-oxo-3H-pyrido [3, 4-d] pyrimidine 7-oxide (4). The origin of the carbon atom of the pyrimidine derivative (4) was proved to be the carbon eliminated from 2-methyl group when 2 was produced from 1.View full abstractDownload PDF (984K) -
ISAO TAKEUCHI, YASUHIRO SHIBATA, YOSHIKI HAMADA1984 Volume 104 Issue 11 Pages 1133-1139
Published: November 25, 1984
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSThe reaction of benzo [f] quinoline (1) with various acyl chlorides and trimethyl phosphite in the presence of sodium iodide gave the corresponding N-heterocyclic α-phosphonate (2) and γ-phosphonate (3). In the similar reaction using bulky phosphites, the ratios [2/3] were changed by a steric effect between the benzo [f] quinoline and the trialkyl phosphite.View full abstractDownload PDF (597K) -
KIMIKO NAKANO, MITSUHIKO MIYAMURA, MAYUMI OHE, YASUKO YOSHIOKA, TOSHIH ...1984 Volume 104 Issue 11 Pages 1140-1146
Published: November 25, 1984
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSBy direct measurement of electron impacting mass spectrometry of naturally occurring diosgenin, pennogenin glycosides and their corresponding furostanol glycosides, without leading to the volatile derivatives, the information with regards to the genuine aglycones of the respective glycosides could be obtained. Namely, diosgenin, pennogenin glycosides and their respective furostanol glycosides exhibited characteristic peaks at (m/z 139), (m/z 155, 153, 127, 126), (m/z 576, 139, 126), (m/z 574, 127, 126), respectively, being distinguishable easily from each other.View full abstractDownload PDF (600K) -
KENJI TOKUNO1984 Volume 104 Issue 11 Pages 1147-1154
Published: November 25, 1984
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSSeveral 1-alkyl-4-oxothianium salts were found to form the corresponding orthoketones in aqueous solvents at room temperature. Corresponding acetal and hemiacetal were prepared in absolute alcohol on heating and on standing at room temperature, respectively. The formation and stability of their orthoketones were investigated by in frared, nuclear magnetic resonance and differential thermal analysis. Oxothianium salts were prepared by methylation of 4-oxothiane with CH3I used as a solvent or by thermal dehydration of the corresponding orthoketones. It is shown that the ketone exists as the corresponding dideuteroxy species in D2O, whereas the contribution of the orthoketone decreases in dimethylsulfoxide-d6. The stability of orthoketone depends on the relative magnitude of the positive charge of their onium ion and the difference of their counter anions.View full abstractDownload PDF (745K) -
TSUNEMATSU TAKEMOTO, SHIGENOBU ARIHARA, KAZUKO YOSHIKAWA, KOTOYO HINO, ...1984 Volume 104 Issue 11 Pages 1155-1162
Published: November 25, 1984
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSFive dammarane-oligoglycosides named gypenosides XLVII (1), XLVII (2), XLIX (3), L (4) and LI (5) were isolated from the aerial parts of Gynostemma pentaphyllum MAKINO collected in Tokushima pref. On the basis of chemical and physicochemical evidence, they were characterized as follows : 1, 2α, 3β, 12β, 20 (S), 26-pentahydroxydammar-24-ene-3-O-β-sophoroside-20-O-β-rutinoside : 2, 19-oxo-3β, 20 (S), 21-trihydroxydammar-24-ene-3-O-{[α-rhamnopyranosyl (1→2)] [β-glucopyranosyl (1→3)]-α-L-arabinopyranoside}-21-O-β-glucopyranoside : 3, 19-oxo-3β, 20 (S), 21-trihydroxydammar-24-ene-3-O {[α-rhamnopyranosyl (1→2)] [β-glucopyranosyl (1→3)]-α-L-arabinopyranoside}-21-O-β-glucopyranoside : 4, 2α, 3β, 12β, 20 (S)-tetrahydroxydammar-24-ene-3-O-β-sophoroside : 5, 2α, 3β, 12β, 20 (R)-tetrahydroxydammar-24-ene-3-O-β-sophoroside.View full abstractDownload PDF (773K) -
SHINJI SHIBAMOTO, TAMIO NISHIMURA1984 Volume 104 Issue 11 Pages 1163-1173
Published: November 25, 1984
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSQuantitative relationships between structure and antibacterial activities against Bacillus subtilis, Staphylococcus aureus, Escherichia coli and Trichophyton interdigitale were presented for 52 derivatives of N-alkyl-and N-arylamidinohydrazones of benzaldehydes, alkylphenylketones, benzophenones, biphenylcarboxaldehydes, acetylbiphenyls, acetylnaphtalenes, fluorenecarboxaldehydes, acetylfluorenes, anthracenecarboxaldehydes and acetylphenanthrenes. Satisfactory equations involving benzophenone derivatives were obtained for T. interdigitale but not for the bacteria.View full abstractDownload PDF (785K) -
AKIRA TAKAYAMA, TOMIO KOSHIKAWA, KATSUHIKO OKUMURA, RYOHEI HORI, IKUO ...1984 Volume 104 Issue 11 Pages 1174-1180
Published: November 25, 1984
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSThe effect of heating plate temperature for automatic sealing of wrapping paper on moisture protection of powder preparations was investigated. Powder preparations used were pulverized sodium valproate tablet, lactose monohydrate, potato starch, D-glucose, sodium chloride, fructose and potassium iodide, and these had different critical relative humidities. Five wrapping papers having various moisture permeabilities were also used. It was revealed that (1) heating plate temperature played an important role for moisture protection of pharmaceuticals ; (2) moisture permeation may be derived through sealed area due to incomplete sealing at low temperatures (<100°C) and also through sealed edge due to melting of laminated polyethylene at high temperatures (150°C<); (3) suitable selection of the temperature is necessary to minimize moisture permeation and to protect powder preparation from hygroscopicity.View full abstractDownload PDF (965K) -
TOSHIHISA ASANO, TSUNEAKI INOUE, MASAYASU KURONO1984 Volume 104 Issue 11 Pages 1181-1190
Published: November 25, 1984
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSThe distribution, metabolism and excretion of 14C-azosemide, a new loop diuretic, were studied in rats after bolus intravenous administration and compared with those of other diuretics such as furosemide or bumetanide. The plasma levels of azosemide declined biexponentially, and the half lives estimated were 3.4 min (t1/2α) and 32 min (t1/2β). The whole-body autoradiograms showed that the radioactivity distributed with higher concentrations in the kidney and liver than in the whole blood. In pregnant rats, the distribution profiles were similar to those of male rats. And the radioactivity distributed with lower concentrations in the placenta, uterus and ovarium than in the whole blood, scarcely in the fetus and amniotic fluid. The urinary and fecal excretion of radioactivity were 40 and 58% of the dose, respectively. The biliary excretion was 67% of the dose, and a part of biliary excreta was reabsorbed. The urinary and biliary metabolites were separated on a thin-layer chromatography, and the structures were determined by mass spectra. The total recovery of unchanged drug in 24 h-urine and -bile was only 15% of the dose. And major metabolites were 4-amino-2-chloro-5-(1H-tetrazol-5-yl) benzenesulfonamide and azosemide glucuronide, along with several unidentified minor metabolites. As a result, azosemide was eliminated as rapidly as other diuretics in rats. The metabolic pathway was similar to that of furosemide having a similar chemical structure, but the excretion profile was similar to that of bumetanide with considerably different structure.View full abstractDownload PDF (1877K) -
KAZUO KIGASAWA, HIROAKI SHIMIZU, SHIGERU HAYASHIDA, KAZUMI OHKUBO1984 Volume 104 Issue 11 Pages 1191-1197
Published: November 25, 1984
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSPhotodecomposition of dipyridamol (I) on thin layer chromatography (TLC) and in org. solvents was studied. It was found that photodecomposition product (II) was yielded by oxidation of piperidine ring moiety of I, and the photolysis of I in org. solvents were pseudo first order kinetics. These reactions were shown to be inhibited by the addition of pyrazolone derivatives that gave the charge transfer complex of I, which had a stabilizing effect in org. solvents. It was comfirmed that the charge transfer complex between I and pyrazolone derivatives were composed of 1 : 1 molar ratio. Further, the stability of tablets of I was studied by aging in a room (at room temp., in room light). No significant decrease of I contents after aging for five years in a room was observed, and neither high performance liquid chromatography nor TLC chromatograms showed decomposition products.View full abstractDownload PDF (732K) -
SADAYOSHI MATSUI, HIROSHI YAMAZOE, IKKAN WATANABE, EIICHI HAYASHI, KAZ ...1984 Volume 104 Issue 11 Pages 1198-1206
Published: November 25, 1984
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSAntifungal activity of eighty-two maleimide and forty-two succinimide compounds against Trichophyton asteroides were examined in vitro. Among these compounds, eleven kinds of N-phenylmaleimides exhibited to have more potent antifungal activity than that of pentachlorophenol as a reference compound. In the N-phenylmaleimides, an increase in the activity was obtained by halogen or alkyl substitutions on the phenyl ring. However, the activity was diminished by halogen or other substitutions at α or α, α'positions on the maleimide ring. The results of therapeutic tests by use of guinea-pigs revealed that a tincture containing 1% N-(2, 6-diethylphenyl) maleimide had 57.7% of cure rate on experimental trichophytosis.View full abstractDownload PDF (849K) -
HITOSHI UENO, MASAKATSU TEZUKA, OSAMU TAMEMASA1984 Volume 104 Issue 11 Pages 1207-1210
Published: November 25, 1984
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSThe effect of exogenous adenosine triphosphate (ATP) on the proliferation of cultured tumor cells has been studied. ATP exerted a cell growth-inhibiting effect at concentrations above 2×10-4M and 5×10-6M against Ehrlich tumor cells and L1210 leukemia cells, respectively. At the maximum concentrations of ATP which does not cause the inhibition of the proliferation of both cultured cells, ATP potentiated the growth-inhibiting effect of 5-fluorouracil (FUra), 5-fluoro-2'-deoxyuridine (FdUrd), and 5-fluoro-2'-deoxyuridine 5'-monophosphate (FdUMP). The effect of ATP was much higher with FdUMP than with others in L1210 leukemia cells. These results suggest that ATP may damage tumor cells, at least in part, when FUra and ATP were coadministered intraperitoneally with Ehrlich carcinoma-bearing mice.View full abstractDownload PDF (413K)
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