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Volume 27, Issue 9
Displaying 1-50 of 54 articles from this issue
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POFENG KUO, YUMIKO IWAI, TAKAHARU MIZUTANI, AKIRA MIZUTANI1979 Volume 27 Issue 9 Pages 1957-1964
Published: September 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSIt was found by radioimmunoassay of serum calcitonin in rabbits that a hypocalcemic protein from bovine parotid gland lowers serum calcium without increasing the secretion of calcitonin. Binding of calcitonin and anti-calcitonin was not inhibited by the parotid protein. Furthermore, when calcitonin was administered to rabbits in addition to a maximally hypocalcemic dose of the parotid protein, it caused an additional decrease of blood calcium level. These results suggest that the target organs of the parotid protein and calcitonin are different, or that the parotid protein and calcitonin activate different receptors in the same target organ. Leucocyte-increasing activity was demonstrated in both the parotid protein and calcitonin, but the effect of calcitonin developed more rapidly than that of the parotid protein, as was the case with hypocalcemic activity. It was also found that the parotid protein caused a significant increase of rosette-forming cell activity in the spleen of neonatal mice, whereas calcitonin did not. These observations suggest that the biological effects of the parotid protein are not mediated by calcitonin.View full abstractDownload PDF (857K) -
TAKEHIKO NAKA, YOSHIYASU FURUKAWA1979 Volume 27 Issue 9 Pages 1965-1972
Published: September 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSOxidation of 1, 3-dialkyl-6-(4-substituted-thiosemicarbazido)-uracils (II) with N-chlorosuccinimide in chloroform at room temperature furnished 5, 7-dialkyl-2-substituted-amino-4H-pyrimido [4, 5-e]-1, 3, 4-thiadiazine-6, 8 (5H, 7H)-diones (III) in good yields. Heating of III resulted in ring contraction to afford 3-substituted-aminopyrazolo [3, 4-d]-pyrimidine-4, 6 (5H, 7H)-diones (IV). Treatment of II with bromine gave 4, 6-dialkyl-1, 2, 3-thiadiazolo [4, 5-d] pyrimidine-5, 7 (4H, 6H)-diones (IX) or N, N'-dialkyl-1, 3, 9, 11-tetramethyl-dipyrimido [4, 5-e : 4', 5'-k] [1, 7, 3, 4, 9, 10] dithiatetraazacyclododecine-2, 4, 6, 10, 12, 14 (1H, 3H, 9H, 11H)-hexanone-6, 14-diimines (VIII), depending on the reaction conditions employed. Compounds IX were also obtained either by treatment of 1, 3-dialkyl-6-hydrazinouracils (I) with thionyl chloride or by treatment of III with bromine.View full abstractDownload PDF (837K) -
MIKIO HORI, TADASHI KATAOKA, HIROSHI SHIMIZU, YUTAKA IMAI1979 Volume 27 Issue 9 Pages 1973-1981
Published: September 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA new ring transformation of benzothiazolines to 3-oxo-2, 3-dihydro-4H-1, 4-benzothiazines or benzothiazoles was found in the reactions of 2, 2-disubstituted benzothiazolines (3-5) with haloacyl halides. N, S-Bis (haloacyl) o-aminobenzenethiols were key intermediates of the reactions. In the case of benzothiazoline (1) and 2-methylbenzothiazoline (2), N-acylated products were obtained. Reactions with acid chlorides or acid anhydrides gave the N-acylated compounds in good yields.View full abstractDownload PDF (1027K) -
MIKIO HORI, TADASHI KATAOKA, HIROSHI SHIMIZU, YUTAKA IMAI1979 Volume 27 Issue 9 Pages 1982-1994
Published: September 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe oxidation of 3-acylbenzothiazolines (IV) with m-chloroperbenzoic acid gave 3-acylbenzothiazoline sulfoxides (V) and sulfone (VI) in high yield. The stereochemistry of the compounds V is discussed on the basis of nuclear magnetic resonance spectroscopic studies. Reaction of the compound V with refluxing acetic anhydride resulted in the formation of novel ring expansion products, 4-acylbenzothiazine derivatives. A mechanism involving the sulfenic anhydride as an intermediate is proposed for this ring expansion.View full abstractDownload PDF (1275K) -
TSUGIO SHIMAMOTO, HIROYUKI MIMA, MASAYUKI NAKAGAKI1979 Volume 27 Issue 9 Pages 1995-2002
Published: September 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe interaction of propyl p-hydroxybenzoate (PP) with polyoxyethylene dodecyl ethers (PDE) having various numbers of oxyethylene units in a homogeneous chain was studied by means of ultrafiltration and nuclear magnetic resonance spectrometry. The results indicate that PP molecules are bound to two distinct loci within the surfactant micelles. The primary class of sites had high affinity but a low capacity for PP molecules, whereas the secondary class of sites exhibited low affinity and a large binding capacity. In the primary class of sites, it seems probable that the PP molecules are situated at the interface of the hydrocarbon core and the polyoxyethylene mantle of the micelles. The interaction of the secondary class of sites is probably a simple partitioning of PP molecules into the polyoxyethylene region of the micelles. The interaction of PP with PDE was much greater than that of methyl p-hydroxybenzoate with PDE.View full abstractDownload PDF (890K) -
MAMORU SUGIURA, HIROHIKO YAMAMURA, KAZUYUKI HIRANO, MASANORI SASAKI, M ...1979 Volume 27 Issue 9 Pages 2003-2007
Published: September 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSOxalate oxidase from barley seedlings (Hordeum vulgare L. var. distichon ALEFELD) was purified to homogeneity as determined by disc gel electrophoresis. The enzyme hydrolyzed oxalate, but no other related acids. The optimum pH was around pH 3.5, and this enzyme was stable at acidic pHs. The enzyme appears to consist of two identical subunits. Various other properties were investigated.View full abstractDownload PDF (579K) -
YOSHIYUKI SEYAMA, NOBUO ISHIKAWA, SABURO YAMASHITA1979 Volume 27 Issue 9 Pages 2008-2010
Published: September 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSPlasma of Elaphe quadrivirgata was incubated in vitro under various conditions, and angiotensin I produced was estimated. Renin-like activity deduced from the amount of angiotensin I formation was higher at 37° than at 20° or 4°. The enzyme activity in the snake was higher at pH 4.5 than at 5.0, while that in mammals is highest at pH 5.0. The activity was markedly reduced in winter during hibernation, compared with that in summer. Among the organs renin-like activity was found only in the kidney. Thus, the renin-like active enzyme present in the plasma of Elaphe quadrivirgata may originate mainly from the kidney. The enzyme activity depends on the incubation conditions, and the season of sample collection.View full abstractDownload PDF (433K) -
YOSHIHIRO NISHIKAWA, KIMIHIRO YOSHIMOTO, MASANORI OHKAWA1979 Volume 27 Issue 9 Pages 2011-2015
Published: September 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSAnomeric mixtures of synthetic 1-O-lauroyl-D-glucose showed a marked plant growth-inhibiting effect in the Avena coleoptile straight growth test ; α-anomer-rich mixture and β-anomer-rich mixture were equally effective. The chain length and location of the acylfunction were clearly critical for this biological effect, since the 1-O-glucosyl esters of caprylic, myristic, and stearic acids, and 3-O- and 6-O-lauroyl-D-glucoses were ineffective. The following disaccharide esters were also ineffective in this bioassay : sucrose-monoesters of lauric, palmitic, and stearic acids, trehalose-monoester of lauric acid, and sucrose esters of hydrogenated beef tallow fatty acids. None of the samples tested showed IAA or cytokinin activity.View full abstractDownload PDF (652K) -
TETSURO IKEKAWA, MARI UMEJI, SYUNSUKE YANOMA, KIMIHIRO YOSHIMOTO, YOSH ...1979 Volume 27 Issue 9 Pages 2016-2020
Published: September 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe monoester compositions of nine new sucrose fatty acid ester preparations produced industrially, which contain mono-, di-, and polyesters of stearic and palmitic acids in different ratios, were quantitatively analyzed by gas-liquid chromatography. Monoester-rich preparations had a marked cell growth inhibiting effect upon L-5178Y, as determined by the tissue culture method. It was observed that the ID50 values tend to decrease with increase in HLB (hydrophile-lipophile balance) values. These preparations were effective against Ehrlich ascites carcinoma as determined by the total packed cell volume method. Preparations consisting mainly of monoesters increased the life spans of mice bearing Ehrlich ascites tumor, but were not effective against L-1210.View full abstractDownload PDF (656K) -
YOSHIHARU KANEO, ATSUKO NISHIKAWA, YURIKO KATO1979 Volume 27 Issue 9 Pages 2021-2026
Published: September 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe binding of salicylic acid to rabbit plasma protein in vitro and in vivo was examined using the semi-microultrafiltration method developed by Imamura et al. This method is suitable for the determination of intact binding of drugs in vivo since the plasma sample need not be diluted and the volume of filtrate is so small that the drug-protein equilibrium may not be affected. The binding parameters of salicylic acid to rabbit serum determined in vitro were : n=1.77 and k=2.53×104M-1, where n and k are the maximal number of binding sites and the binding constant, respectively. The percentages of salicylic acid bound in vivo following oral administration of sodium salicylate to rabbits were in fair agreement with the theoretical values estimated using the binding parameters described above. It appears that the plasma protein binding of salicylic acid in vivo is predictable from data obtained in vitro in rabbits.View full abstractDownload PDF (708K) -
AKIHIRO OHTA, YASUO AKITA, MIYOKO HARA1979 Volume 27 Issue 9 Pages 2027-2041
Published: September 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe reactions of 2, 5-dimethylpyrazine 1-oxide (XI), 2, 5-diethylpyrazine 1-oxide (XIII), 2-methyl-5-phenylpyrazine 1-oxide (XV), and 2-methyl-5-phenylpyrazine 4-oxide (XVI) with phosphoryl chloride or acetic anhydride were studied. 2, 5-Dichloro-3, 6-dimethylpyrazine (III) and 2, 5-dichloro-3, 6-diethylpyrazine (VII) were converted to the diketopiperazines, alanine anhydride (I) and α-aminobutyric anhydride (V), respectively, which were shown to exist in a cis configuration by examination of their PMR spectra.View full abstractDownload PDF (1655K) -
KATSUHIRO OTSUKA, TOSHIRO YADOMAE, TOSHIO MIYAZAKI1979 Volume 27 Issue 9 Pages 2042-2047
Published: September 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSAn exo-(1→3)-β-D-glucosidase was isolated from the culture filtrate of the fungus Trichophyton mentagrophytes by ammonium sulfate fractionation, gel chromatography on Sephadex G-200 equilibrated with 0.1M sodium phosphate buffer (pH 7.5), and ion exchange chromatography on DEAE-Sephadex A-50. The enzyme was purified 304 fold, with a recovery of 15%. The Km value of the enzyme with pnitrophenyl-β-D-glucopyranoside was 3.1 mM. The enzyme was strongly inhibited by Ag+, Hg2+, Cu2+ and Co2+ ions and also by N-bromosuccinimide and I2. This enzyme hydrolyzed p-nitrophenyl-β-D-glucopyranoside but did not show any activity towards p-nitrophenyl-α-D-glucopyranoside or other p-nitrophenyl-glycosides. The enzymes also hydrolyzed (1→3)-β-linked glucosides, but not (1→4)-β-and (1→6)-β-linked glucosides. When the enzyme hydrolyzed (1→3)-β-linked oligo and polyglucosides, the only product identified by paper chromatography was glucose monomer. The molecular weight of the enzyme, as determined by sodium dodecyl sulfate disc gel electrophoresis, was 4.9×104 daltons.View full abstractDownload PDF (681K) -
NAOMI I. NAKANO, TAKAYUKI OSHIO, NORIKO SATO, YOSHIMITSU SHIMAMORI, SH ...1979 Volume 27 Issue 9 Pages 2048-2055
Published: September 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe use of albumin immobilized on agarose gel for the characterization of drug-protein binding by means of frontal analysis affinity chromatography is described for the interaction of bovine serum albumin with a variety of ligands including hydroxybenzoic acids, warfarin, phenylbutazone, D- and L-tryptophan, sulfonamides, etc. In all the systems, the binding capacity of the immobilized albumin was increased by the presence of a six-carbon-atom spacer between the agarose gel matrix and albumin, to a level comparable to that of soluble albumin as determined by equilibrium dialysis. The effect of residual fatty acids on the binding properties of albumin was similarly examined by coupling defatted bovine serum albumin with the gel. The results indicated that there is no marked difference in binding properties between the immobilized defatted and undefatted albumin preparations. The advantages and disadvantages of the present affinity chromatographic method are discussed.View full abstractDownload PDF (901K) -
YASUTAKA NAGAI, HITOSHI UNO1979 Volume 27 Issue 9 Pages 2056-2064
Published: September 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSTricyclic compounds (12, 17 and 20) combined with a spiro-system at the 4 position of 1-substituted piperidine were synthesized for pharmacological testing. They could be prepared by a sequence of reactions involving the Pinacol rearrangement of 9-(1-ethoxy-carbonyl-4-piperidinyl) fluorene-9, 4'-diol (9) or the cyclization of 1-benzyl-4-(o-substituted phenyl)-4-carboxy (or cyano) piperidine (15a and 16). 9-(1-Methyl-1, 2, 3, 6-tetrahydro-4-pyridinyl) xanthene (or -anthracene) (21 and 26) and 3-methyl-2, 3, 4, 5-tetrahydro-1H-phenanthro [9, 10-d] azepine (27) were also prepared by the Wagner-Meerwein rearrangement of α hydroxy spiro compounds (19b, 19d, and 11, respectively). Among the compounds synthesized, 1-methyl-1, 2, 3, 5, 6, 7-hexahydrospiro [[4H] azepine-4, 9'-fluorene]-5-ol (8) showed marked anti-convulsant activity.View full abstractDownload PDF (864K) -
YOSHIHIRO NISHIKAWA, KIMIHIRO YOSHIMOTO, REIKO HORIUCHI, KAZUHIKO MICH ...1979 Volume 27 Issue 9 Pages 2065-2072
Published: September 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSTwo lichen polysaccharides with antitumor activity, a partially O-acetylated pustulan (GE-3) and a lichenan-type glucan (UR-1-1), isolated from Gyrophora esculenta MIYOSHI and Usnea rubescens STIRT., respectively, were subjected to various modifications, and the resulting products were tested for noncytotoxic, host-mediated antitumor action against sarcoma 180 solid tumor in mice by intraperitoneal administration. Treatment of GE-3 with urea afforded products with the same antitumor effect as the original glucan. Injection of GE-3 or UR-1-1 together with urea also caused no marked decrease in the antitumor activity. On O-carboxymethylation, both glucans yielded products with greatly reduced antitumor activity. Ten lots of the lauroyl derivative with different degrees of substitution were prepared from GE-3. Among them, three with lauroyl contents less than 3.3% exhibited strong antitumor activity, while the more highly esterified products were all ineffective. Introduction of both carboxymethyl and lauroyl groups into the GE-3 molecule gave a product with moderate antitumor activity. The ten lots of the lauroyl derivative of GE-3 had no direct antitumor action against Ehrlich ascites carcinoma implanted in mice, as determined by the total packed cell volume method.View full abstractDownload PDF (999K) -
ISAO KAWARASAKI, TADAHIRO TAKEDA, YUKIO OGIHARA, HIROYUKI SHIMONAKA, Y ...1979 Volume 27 Issue 9 Pages 2073-2075
Published: September 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSAn alkali-soluble polysaccharide, designated as S-Iaw, has been isolated from the mycelia of Trichophyton mentagrophytes. It gave a single peak on high-speed liquid chromatography. The only component sugar was D-mannose, and its molecular weight was found to be about 24000. Methylation, periodate oxidation, and acetolysis studies suggested that S-Iaw is composed of repeating units of O-(2-O-α-D-mannopyranosyl)-6-O-α-D-mannopyranosyl-α-D-mannopyranose.View full abstractDownload PDF (505K) -
MASAYUKI ONDA, HIROKO YAMAGUCHI1979 Volume 27 Issue 9 Pages 2076-2083
Published: September 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSPhotolysis of the isocarbostyril (5) gives predominantly the regioisomeric dimers (7) and (8). Attempts to trap the initial photo-product (14) with dienophiles are made and the formation mechanisms of the resulting products are discussed. The 4b, 12-epoxyimino compound (18) resulted from trapping with nitrosobenzene is smoothly converted into oxychelerythrines.View full abstractDownload PDF (883K) -
HIDEAKI NATSUGARI, KANJI MEGURO, YUTAKA KUWADA1979 Volume 27 Issue 9 Pages 2084-2092
Published: September 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSRing closure reactions of 2-chloroacetamidobenzophenone (N, N-disubstituted)-hydrazones (5) afforded 1, 4, 5-benzotriazocines (6), 1, 4-benzodiazepines (9) and 1, 4, 5-benzotriazocinium salts (8). On treatment with sodium methoxide, 5 and 8 gave 3-(N, N-disubstituted) amino-1, 4-benzodiazepin-2-ones (11) in good yields through Stevens-type rearrangement.View full abstractDownload PDF (863K) -
HIROTERU SAYO, KOICHI MORI, TAKASHI MICHIDA1979 Volume 27 Issue 9 Pages 2093-2098
Published: September 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSAnodic oxidation of 4'-substituted 2-nitrobenzenesulfenanilides (4'-OMe (3a), 4'-Me (3b), 4'-Cl (3c), 4'-H (3d)) was investigated by cyclic voltammetry and controlled potential electrolysis at a glassy-carbon anode, and the results were compared with those for 4'-substituted benzenesulfenanilides (1a-d). Electrolysis of 3a in acetonitrile containing NaClO4 gave 2, 7-dimethoxyphenazine (2a), 2, 2'-dinitrodiphenyl disulfide (4), p-anisidine (5), 2-nitrobenzenesulfonic acid (6), and N-(2-nitrophenylthio)-p-benzoquinoneimine (7). Electrolysis of 3a in acetonitrile containing ethyltributylammonium trifluoromethane-sulfonate (ETBT) gave 2a, 4, 5, and 7, but did not give 6. These results indicate that the perchlorate anion does act as an oxidizing agent in the anodic oxidation of 3a, even though sodium perchlorate has been used quite extensively as a supporting electrolyte in anodic systems and usually does not participate in anodic oxidation processes. Since benzenesulfonic acid was not obtained on the anodic oxidation of 1a in acetonitrile containing NaClO4, the formation of 6 was interpreted on the basis of one-step two-electron transfer followed by reaction of the dication with perchlorate anion. The introduction of the 2-nitro group may elicit the one-step two-electron transfer. Electrolysis of 3a in the presence of water (1%) gave 7 almost quantitatively. Electrolysis of 3b and 3c in acetonitrile containing NaClO4 gave the corresponding 2, 7-disubstituted phenazines, 4, and 6, whereas that of 3d did not give phenazine.View full abstractDownload PDF (702K) -
CHISAKO YAMAGAMI, MAKIKO SUGIURA, TSUNEKO KITAZAWA, KAZU TAMURA, NARAO ...1979 Volume 27 Issue 9 Pages 2099-2104
Published: September 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESS^<13>C Nuclear magnetic resonance (NMR) spectra of a series of N-ethyl-piperidones were determined in CDCl3 and in CH3OH. The spectra of N-ethyl-3-piperidone and N-ethyl-4-piperidone in CH3OH were complicated compared with those in CDCl3. By examining the 13C chemical shifts, this phenomenon was associated with the equilibrium hemiacetal formation. 13C NMR technique was shown to be a powerful tool for studying such equilibrium systems. Factors controlling the equilibrium are discussed.View full abstractDownload PDF (820K) -
TOSHIO TSUJIMOTO, CHIZUKO KOBAYASHI, TOSHIRO NOMURA, MAKIKO IIFURU, YO ...1979 Volume 27 Issue 9 Pages 2105-2110
Published: September 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSCharge densities of diaza-benzenes-2-substituted pyrazines, 5-substituted pyrimidines and 4-substituted pyridazines-were calculated by the MINDO/2 method. The correlations of the substituent-induced 13C chemical shifts (13C SCS) values of these three diaza-benzenes with total charge densities were determined, and linear relations between the two parameters were found even at the ipso position, whereas the correlations of the ipso SCS with a linear combination of substituent constants were poor.View full abstractDownload PDF (562K) -
AKIHIRO SANDA, REIKO TAKEDA, MASACHIKA IRIE1979 Volume 27 Issue 9 Pages 2111-2115
Published: September 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSIn order to investigate the base specificity of the RNase from Rhizopus sp. (RNase Rh), its kinetic parameters were measured with 16 dinucleoside phosphates (XpY, where X or Y represents one of adenosine, guanosine, uridine and cytidine) as substrates at pH 5.5 and 25°. The average Km values of ApY, GpY, CpY and UpY increased in the order A, G, C and U. The average Km values of ApY, GpY, CpY and UpY increased in the order A, G, U and C. The average Vmax values of ApY, GpY, CpY and UpY were larger for dinucleoside phosphates having A and G at X. However, the average Vmax values of XpA, XpG, XpC and XpU were relatively constant. It was concluded that the X base in XpY contributes mainly to the specificity of the enzyme and the Y base may modify this somewhat. The K1 values of various nucleotides towards RNase Rh were measured at pH 5.5. These compounds inhibited RNase Rh competitively. Although the inhibitory effect depends on the base, sugar and location of the phosphate moiety, for a given location of phosphate on the sugar, the K1 values of ribonucleotides decreased in the order U, C, G and A and those of deoxyribonucleotides decreased in the order T, C, G and A. These data also show that purine bases, especially adenine, have high affinities for RNase Rh.View full abstractDownload PDF (579K) -
MASANORI SAKAMOTO, KYOKO MIYAZAWA, KEIKO KUWABARA, YOSHIO TOMIMATSU1979 Volume 27 Issue 9 Pages 2116-2121
Published: September 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe reactions of diketene with S, S-dimethyl-N-2-pyridinylsulfilimine (IVa) and N-2-benzothiazolyl-S, S-dimethylsulfilimine (IVb) gave 2-(2-dimethylsulfuranylideneaceto-acetamido) pyridine (VIa) and 2-(2-dimethylsulfuranylideneacetoacetamido) benzothiazole (VIb), respectively. However, the reaction of diketene with S, S-dimethyl-N-(4-nitrophenyl) sulfilimine (IVc) and N-2-benzoxazolyl-S, S-dimethylsulfilimine (IVd) gave 3-acetyl-4-hydroxy-6-methyl-1-(4-nitrophenyl)-2-pyridone (VIIc) and 3-acetyl-1-(2-benzoxazolyl)-4-hydroxy-6-methyl-2-pyridone (VIId), respectively. On the other hand, the reaction of diphenylketene with sulfilimines (IVa, IVb, and IVd) gave the corresponding 1, 3-cyclization products (VIII, IX, and X).View full abstractDownload PDF (653K) -
KAZUYA KOHASHI, YASUTO TSURUTA, MASATOSHI YAMAGUCHI, YOSUKE OHKURA1979 Volume 27 Issue 9 Pages 2122-2129
Published: September 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe color observed in the Jaffe reaction is due to the formation of the isomers of the 1 : 1 σ-complex (I) of creatinine and picric acid. The formation of hydroxylated anions of I (I') and the presence of equilibria between the isomers of I and I' were confirmed by nuclear magnetic resonance studies. The phenomenon of the augmentation of the color intensity on neutralizing the alkaline reaction mixture of picric acid and creatinine can be explained in terms of shifts of the equilibria between the isomers of I and I'. Three isomers of the 1 : 2 σ-complex are formed via the isomers of I and I' in an alkaline mixture of picric acid and creatinine, but not in the presence of a large excess of picric acid, as determined by high performance liquid chromatography.View full abstractDownload PDF (784K) -
MICHIKO IIJIMA, TOKUHIKO HIGASHI1979 Volume 27 Issue 9 Pages 2130-2136
Published: September 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe activities of ribonucleic acid (RNA) polymerases I, II and III in a sodium deoxycholate (DOC)-treated enzyme preparation have been differentially determined using three combinations of assay conditions (metal ion ; Mg2+ or Mn2+, (NH4)2SO4 and α-amanitin). Ginsenoside-Rb1 enhanced, while -Rc repressed, the activities of RNA polymerases I and II, whereas both had no effect on that of RNA polymerase III. Rb1-treated rats showed different profiles of stimulation of RNA polymerases I and II ; the maximum increase of RNA polymerase I activity was about +70% at 2 hr, and that of RNA polymerase II activity was +40% at 3 hr after the injection of Rb1. Actinomycin D and cycloheximide both blocked the increase in RNA polymerase I activity on treatment with ginsenoside-Rb1. On the other hand, increased activity of RNA polymerase II was blocked by actinomycin D but not by cycloheximide. These results suggest transcriptional regulation in the enhancement by ginsenoside-Rb1 of RNA polymerase activities I and II, though the mechanisms may differ in detail.View full abstractDownload PDF (789K) -
YASUMITSU TAMURA, SAID M. BAYOMI, MASAYOSHI TSUNEKAWA, MASAZUMI IKEDA1979 Volume 27 Issue 9 Pages 2137-2142
Published: September 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA study of the stereochemical course of the nucleophilic addition of N-unsubstituted sulfoximines 1a-e to dimethyl acetylenedicarboxylate showed that Z-adducts were formed as the major products in methanol whereas E-adducts were predominantly or almost exclusively obtained in DMSO. The reactions of dimethylsulfoximine (1a) with ethyl propiolate and acetylacetylene were complicated by the concomitant isomerization of the adducts under the reaction conditions used. The reaction of 1a with trans-1, 2-dibenzoylethylene gave a normal 1 : 1 adduct, while that with tetracyanoethylene gave an addition-elimination product, N-(1, 2, 2-tricyanovinyl) dimethylsulfoximine. Heating 1a with diphenylcyclopropenone in refluxing toluene gave N-(3-amino-2, 3-diphenylpropenoyl)-dimethylsulfoximine. The mechanisms of these reactions are discussed.View full abstractDownload PDF (716K) -
YOSHIHISA KURASAWA, KATSUHIKO NAGAHARA, ATSUSHI TAKADA1979 Volume 27 Issue 9 Pages 2143-2146
Published: September 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe reaction of 6-hydrazino-1, 3-dimethyluracil (II) with the benzoyloxy radical gave a tricyclic pyridazine derivative, 1, 3, 6, 8-tetramethyl-2, 4, 5, 7-tetraoxo-1, 2, 3, 4, 5, 6, 7, 8-octahydropyridazino [3, 4-d : 6, 5-d'] dipyrimidine (VII), while the reaction of 6-amino-1, 3-dimethyluracil (I) with the benzoyloxy radical afforded 6-amino-5-benzoyloxy-1, 3-dimethyluracil (VI). Treatment of VII with ammonia gave another tricyclic pyridazine derivative, 2, 4, 7, 9-tetramethyl-1, 3, 8-trioxo-1, 2, 3, 4, 7, 8, 9-heptahydropyrimido [4, 5-c] imidazo [4, 5-e] pyridazine (VIII).View full abstractDownload PDF (526K) -
HIROSHI HOSODA, YASUO SAKAI, HIROKO YOSHIDA, TOSHIO NAMBARA1979 Volume 27 Issue 9 Pages 2147-2150
Published: September 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSEnzyme labeling of a steroid by the activated ester method has been investigated. The reaction of the N-hydroxysuccinimide ester of a testosterone derivative with β-D-galactosidase provided a conjugate suitable for enzyme immunoassay. Dose-response curves with satisfactory sensitivity and range of measurement could be obtained by the use of conjugates prepared at a limited molar ratio of steroid to enzyme. The activated ester method proved to be useful for enzyme labeling of antigen because of its simplicity and excellent reproducibility.View full abstractDownload PDF (500K) -
SUSUMU FUNAKOSHI, NOBUTAKA FUJII, KENICHI AKAJI, HIROSHI IRIE, HARUAKI ...1979 Volume 27 Issue 9 Pages 2151-2156
Published: September 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSSulfoxides of Cys (S-p-methoxybenzyl) and Cys (S-benzyl) were prepared by oxidation with sodium perborate. Hydrogen fluoride and methanesulfonic acid converted the former sulfoxide to S-p-methoxyphenylcysteine or S-p-hydroxyphenylcysteine in the presence of anisole or phenol, respectively, while the latter sulfoxide resisted the actions of these deprotecting reagents. Thiophenol appears to be useful as a powerful reducing reagent for protected cysteine sulfoxides.View full abstractDownload PDF (805K) -
NOBUYOSHI KANENIWA, MITSURU HIURA, TOMOO FUNAKI1979 Volume 27 Issue 9 Pages 2157-2162
Published: September 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe effect of fasting on the elimination of barbital and phenobarbital was studied using non-fasted, partly fasted, and fasted rabbits. The renal excretion rate constants of both barbiturates were markedly low during fasting, while the metabolic rate constants were little affected. To clarify the mechanism of reduction of the renal excretion rate of these drugs, creatinine clearance and barbital clearance were simultaneously measured in fasted and non-fasted rabbits. The magnitude of apparent tubular reabsorption rate of barbital increased on fasting without any change of the glomerular filtration rate. The urinary pH, which affects the fraction of undissociated species in the renal tubules, was measured. The urinary pH decreased slowly from 8.4 in freely fed rabbits to 6.0 at 24 hr and 4.7 at 48 hr affter fasting, and it recovered to the original state within 4 hr after refeeding. Therefore, the fraction of undissociated species of both barbiturates in the tubular urine during fasting becomes much larger than that in fed rabbits. Consequently, the relative tubular reabsorption rate should be higher during fasting. Therefore, it can be concluded that the lower renal excretion rate constant during fasting is due to enhanced reabsorption of undissociated species in the acidic tubular urine.View full abstractDownload PDF (752K) -
KOZO OKADA, YOTARO KUROSAWA, SOTOO NAGAI1979 Volume 27 Issue 9 Pages 2163-2170
Published: September 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA series of peptides having a valine or valyvaline moiety at the N-terminus, 1-13, was prepared and their antipepsin activities were tested. All of the peptides possessing an N-acyl-Val-Val moiety, except one, showed some inhibitory activity against pepsin, while compounds lacking N-acyl-Val-Val showed no inhibition even at a concentration of 50 μg/ml. Compound 12, a pepstatin analog, in which a tyrosine residue is present instead of AHMHA of pepstatins, was the most potent inhibitor among the synthetic peptides, but its activity was markedly lower than that of pepstatin A. Compounds 10, 12, and 13 showed neither agonistic nor antagonistic effects on pepstatin A, suggesting major differences in binding abilities of the synthetic peptides and of pepstatin A to the enzyme. The importance of the AHMHA residue of pepstatins in relation to the inhibitory activity is discussed.View full abstractDownload PDF (908K) -
HIROMU SAKURAI, SHUNJIRO OGAWA1979 Volume 27 Issue 9 Pages 2171-2176
Published: September 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSHydroxylation of aniline by several Fe (II)-thiol and hemin-thiol complexes was studied as a model system for cytochrome P-450 in liver microsomes. Cysteine, cysteine methylester, cysteamine, N-acetyl-cysteine, α-mercaptopropionic acid, β-mercapto-propionic acid, thiosalicylic acid and o-aminobenzenethiol were tested as thiolcompounds. In these systems, p-and o-aminophenol were the major products and m-aminophenol was not detected. The hydroxylation was affected by reaction time, pH, the type of thiol compound and the concentrations of thiol compound, aniline, Fe (II) and hemin. The aniline-hydroxylating activity of the hemin-thiol system was 6-20 times that of the Fe (II)-thiol system at pH 4. The Fe (II)-thiol and hemin-thiol systems may be useful chemical models for studies of the structure and function of cytochrome P-450.View full abstractDownload PDF (691K) -
KAZUTOSHI UMENIWA, OSAMU OGINO, KATSUMI MIYAZAKI, TAKAICHI ARITA1979 Volume 27 Issue 9 Pages 2177-2182
Published: September 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSIn order to investigate the absorption characteristics of cephalexin, cephradine, and amoxicillin, which are well absorbed from the gastrointestinal tract, the mechanisms of intestinal absorption of these antibiotics in rats were examined using the recirculating perfusion technique, the loop method, and the everted gut sac technique. Cephradine was shown to be actively transported. Other antibiotics appeared to diffuse across the intestine down a concentration gradient. The accumulations of these drugs, in the intestinal tissue, especially cephalexin and cephradine, were particularly marked, and the accumulation of each of these three drugs was significantly inhibited at low temperature. These observations provide an experimental basis for the known rapid absorption of these antibiotics.View full abstractDownload PDF (682K) -
TAKASHI TSUCHIYA, MICHIKO ENKAKU, JYOJI KURITA, HIROYUKI SAWANISHI1979 Volume 27 Issue 9 Pages 2183-2187
Published: September 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSIrradiation of the fused pyridinium ylides (6) or their dimers (7), prepared from 1, 5-and 1, 8-naphthyridine, thieno [2, 3-b]- and thieno [3, 2-b]-pyridine, and furo [2, 3-b]-pyridine by N-amination with O-mesitylenesulfonylhydroxylamine followed by treatment with base, resulted in the fromation of the corresponding fused 1H-1, 2-diazepines (8), which are previously unknown bicyclic ring systems. However, a similar synthetic route from the pyrrolopyridines (10) failed to yield pyrrolodiazepines.View full abstractDownload PDF (672K) -
TAKASHI TSUCHIYA, MICHIKO ENKAKU, HIROYUKI SAWANISHI1979 Volume 27 Issue 9 Pages 2188-2193
Published: September 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe previously unknown 3H-1, 2-pyrido-(3a, b) and 3H-1, 2-thieno-(3c, d) diazepines were prepared from the corresponding 1H-isomers. Treatment of 3 with bases or acids resulted in tautomerization to give the 1H-diazepines (1), and photolysis of 3 afforded the condensed 3-vinylpyrazoles (4). However, thermolysis of the pyridodiazepines (3a, b) gave 4a, b, whereas the thienodiazepines (3c, d) gave the thienylpyrazoles (5) on irradiation via a [1, 5] hydrogen shift in the diazepine ring ; this mechanism was confirmed by a deuterium-labelling experiment. The 3-acetoxy-(13a) and 3-methoxy-(13b) 3H-1, 2-thienodiazepines were also prepared, and their photolysis afforded 3-vinylpyrazoles (14). However, thermolysis or base treatment of 13 resulted in loss of nitrogen to give compounds (15) and (16).View full abstractDownload PDF (755K) -
NARAO TAKAO, KINUKO IWASA1979 Volume 27 Issue 9 Pages 2194-2197
Published: September 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSDie Struktur des Corynolamins (1), eines neuen Alkaloids des Hydrobenzo [c]-phenan-thridin-Typs aus Corydalis incisa, wurde durch Korrelation zum strukturell bekannten Corynolin (6) als 6-Hydoxymethylcorynolin aufgeklart. Dabei wurde auch die Stereo-chmie am Zentrum 6 erortert.View full abstractDownload PDF (597K) -
KUNIO KOBAYASHI, SHOHEI KAGAWA, YOKO TSUMURA, HISAYO ISE, KEIKO YOSHID ...1979 Volume 27 Issue 9 Pages 2198-2202
Published: September 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe role of extracellular potassium ions in the mechanism of glucose-induced insulin release in the rat was investigated by both dynamic and kinetic analyses of insulin release from islets of Langerhans by slow-rise glucose stimulation in the presence of 6.2 or 12.4 mM K+, or in its absence. The dose-response curves were sigmoidal in profile with a tendency to show a similar maximal rate of insulin release, but the Km values were very different. In particular, removal of potassium ions from the medium reduced the Km value from 8.9 mM (control) to 3.7 mM glucose. Hill's constant (n) was reduced from 5.7 (control) to 4.2 in the absence of K+ and 4.4 in the presence of 12.4 mM K+. The Hill plots were linear with slopes of 4.2 (0 mM K+) and 5.7 (6.2 mM K+), respectively, whereas in the presence of 12.4 mM K+ the Hill plot consisted of two straight lines with a break at 4.7 mM glucose (n=1.4 and 4.4). In conclusion, it is suggested that potassium ions in the medium play important roles not only as an electrolyte in connection with the integrity of the B cell membrane, but also as a heterotropic inhibitory effector in the allosteric interaction between the glucoreceptors, leading to a depression of insulin release at low glucose concentrations.View full abstractDownload PDF (601K) -
MICHIYA KIMURA, TOSHIO YAMAMOTO, KOICHI NAGASAWA, MASAHIKO TOHMA1979 Volume 27 Issue 9 Pages 2203-2206
Published: September 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA new method is presented for the determination of some steroidal epoxides by gas liquid chromatography (GLC). Since such an epoxide undergoes decomposition, giving a complex chromatogram in GLC, the oxirane ring was cleaved stereoselectively to give the corresponding steroidal alcohol by refluxing with LiAlH4 in ether. The alcohol was then derivatized to a trimethylsilyl or tert-butyldimethylsilyl ether and analyzed by quantitative GLC on SE-30 or OV-17, using 5α-cholestane as an internal standard.View full abstractDownload PDF (477K) -
TAKASHI ABIKO, MIHOKO KUMIKAWA, SACHIKO DAZAI, HIROSHI SEKINO, HIROKI ...1979 Volume 27 Issue 9 Pages 2207-2211
Published: September 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESS[Arg3]-STF and [DAla1]-STF were synthesized by the solution method. STF and its analogs caused on increase in E-rosette forming capacity when incubated in vitro with uremic T cells.View full abstractDownload PDF (650K) -
NOBUKO IINO, KAZUO YOSHIDA1979 Volume 27 Issue 9 Pages 2212-2216
Published: September 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSAn affinity adsorbent was prepared by coupling p-aminophenyl 1-thio-β-D-gluco-pyranosiduronic acid with CH-Sepharose 4B. β-Glucuronidase from rabbit liver was adsorbed on p-aminophenyl 1-thio-β-D-glucopyranosiduronic acid-CH-Sepharose then eluted with basic buffer or salt solution. The specific enzyme activity increased 46-fold and essentially all of the activity of the enzyme was recovered in elution buffer containing 0.1M NaCl. N-Acetyl-β-glucosaminidase was adsorbed slightly but β-glucosidase and β-galactosidase were not adsorbed on the affinity adsorbent. The adsorbent retained affinity for the enzyme after being used ten times.View full abstractDownload PDF (674K) -
YOSHIKO ARAKAWA, MITSUE BANDOH, HIDEKI OGASAWARA, HIROFUMI TANAKA, NOB ...1979 Volume 27 Issue 9 Pages 2217-2220
Published: September 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe pharmacokinetics of pentazocine were studied in dogs under halothane anesthesia. Pentazocine was spectrofluorometically measured in plasma and cerebrospinal fluid (CFS) of dogs receiving 2.5, 5.0, 10.0 mg/kg doses intramuscularly. The concentration-time curves of pentazocine were describable in terms of a 2-compartment model, and the pharmacokinetic parameters were calculated accordingly. The half-life of the β-phase (elimination phase) was independent of the dose, while the area under the curves (AUC) were proportional to the dose levels. Pharmacokinetic parameters of pentazocine in unanesthetized dogs were also calculated and compared with those in anesthetized dogs. The half-life was approximately the same in both groups. It is concluded that halothane anesthesia does not significantly modify the half-life of pentazocine.View full abstractDownload PDF (563K) -
SHUNJI SAKAMOTO, KEIJIRO SAMEJIMA1979 Volume 27 Issue 9 Pages 2220-2222
Published: September 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESS2, 3-Trimethylene-1, 2-dihydroquinazolinium hydroxide, a reaction product of Δ1-pyrroline and o-aminobenzaldehyde, was quantitatively converted to 2, 3-trimethylene-4-quinazolone by chromic acid oxidation in dilute sulfuric acid. The reaction was successfully applied for determining as little as 10 nmol of Δ1-pyrroline in deproteinized supernatant of rat liver by gas chromatography using a flame ionization detector.View full abstractDownload PDF (449K) -
MITSURU FURUKAWA, TADASHI OKAWARA, YOSHIHIDE NOGUCHI, YURIKO TERAWAKI1979 Volume 27 Issue 9 Pages 2223-2226
Published: September 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSAsymmetric synthesis of β-amino acids (4) was achieved by the reduction of chiral enamines (3) with 10% palladium hydroxide catalyst on charcoal or with sodium cyanoborohydride in optical purities of 3-28%. The reduction with the former catalyst afforded higher optical purities of 4 than that with the latter reducing agent. These two methods yielded opposite configurations of 4. The steric courses of the reactions are discussed.View full abstractDownload PDF (500K) -
HIDEAKI UMEYAMA, SETSUKO NAKAGAWA1979 Volume 27 Issue 9 Pages 2227-2228
Published: September 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe structure of the side chains of tyrosine and phenylalanine was analyzed by ab initio LCAO-MO calculations. The conformation of the tyrosine side chain of glycyltyrosine, the conformations of the side chains of many tyrosine and phenylalanine residues in proteins, and the conformation of tyrosine could be explained on the basis of calculations for ethylbenzene. It is shown that the dihedral angle (Cα-Cβ-Cγ-Cδ1) of these molecules is determined by the exchange repulsion between the aromatic ring and the Cα-Cβ bond.View full abstractDownload PDF (319K) -
NORIICHI ODA, SHINICHI NAGAI, ISOO ITO1979 Volume 27 Issue 9 Pages 2229-2232
Published: September 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA convenient synthesis is reported of 1-substituted 7, 8, 9, 10-tetrahydro-5, 12-naphthacenediones (3a-d) and 4-substituted 12-hydroxy-5a, 6, 7, 8, 9, 10, 11, 11a-octahydro-5 (12H)-naphthacenones (4a-c) by means of the Diels-Alder reaction of 1, 4-naphthoquinones (1a-d) with 1, 2-dimethylenecyclohexane, followed by aromatization through dehydrogenation (3a-d) or by catalytic hydrogenation (4a-c).View full abstractDownload PDF (531K) -
TAKASHI ABIKO, MIHOKO KUMIKAWA, HIROSHI SEKINO1979 Volume 27 Issue 9 Pages 2233-2237
Published: September 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSTwo peptides, H-Lys-Asp-Val-Tyr-Val-Gln-Leu-Tyr-Leu-OH and H-Arg-Lys-Asp-Val-Tyr-Val-Gln-Leu-Tyr-Leu-OH (fragment of thymopoietin II), were synthesized in a conventional manner utilizing the hydrogen flluoride procedure, and were tested to determine their effects on E-rosette forming cells in the uremic state. The synthetic decapeptide increased E-rosette forming capacity in the presence of uremic serum. The synthetic nonapeptide had no effect on the E-rosette formation inhibiting activity of uremic serum.View full abstractDownload PDF (679K) -
HARUAKI YAJIMA, KENICHI AKAJI, HITOSHI SAITO, HIDEKI ADACHI, MARIKO OI ...1979 Volume 27 Issue 9 Pages 2238-2242
Published: September 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSIn order to examine the side reaction at the tyrosine residue, i.e., O-sulfonation, that occurs during the methanesulfonic acid deprotection of Arg (p-methoxybenzenesulfonyl), [4-Gln]-neurotensin was synthesized as a model peptide. A mixture of cation scavengers, anisole-thioanisole-o-cresol (1 : 1 : 1), suppressed this side reaction sufficiently for practical peptide synthesis.View full abstractDownload PDF (717K) -
EIKO OHTSUKA, TETSUO MIYAKE, MORIO IKEHARA, AKITERU MATSUMOTO, HIDENOB ...1979 Volume 27 Issue 9 Pages 2242-2245
Published: September 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSCyclic volutammetry of phenyl derivatives of various nucleotides was carried out, using the parent nucleosides as a control. The p-N-benzylaminophenyl ester of 3'-O-acetylthymidine 5'-phosphate showed a peak at low anodic potential, and the N-benzyl-aminophenyl group could be removed by controlled potential electrolysis at this potential. p-N-Tritylaminophenyl-, p-N-acetylaminophenyl and p-methoxyphenyl esters of nucleotides were also subjected to controlled potential electrolysis ; the oxidative removal of these phenyl groups was less effective than that of the N-benzylaminophenyl ester.View full abstractDownload PDF (512K) -
HIDEAKI NAGAI, KIYOSHI ZAITSU, CHIZUKO HAMADA, YOSUKE OHKURA1979 Volume 27 Issue 9 Pages 2245-2248
Published: September 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA highly sensitive fluorimetric method is presented for the determination of uric acid in serum, based on the uricase-catalized oxidation of the acid to hydrogen peroxide, which is measured by a fluorimetric technique using the peroxidase-p-hydroxyphenylacetic acid system. The method is rapidly and readily performed with only 2μl of serum without deproteinization.View full abstractDownload PDF (543K) -
JENGSHIOW LAI, KAZUO ITO1979 Volume 27 Issue 9 Pages 2248-2251
Published: September 25, 1979
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSFurther examination of the petroleum ether extracts of Marsdenia formosana MASAMUNE (Asclepiadaceae) led to the isolation and characterization of a new triterpenoid, marsformosanone (III) together with a known steroidal compound, stigmast-5-en-3β, 7α-diol (I).View full abstractDownload PDF (552K)