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Volume 96, Issue 7
Displaying 1-18 of 18 articles from this issue
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YASUYUKI KATO, NORIYUKI ARIMA, HIDEO NISHIMINE1976 Volume 96 Issue 7 Pages 819-826
Published: July 25, 1976
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSAbsorption, excretion, distribution, and metabolism of 2-(5H-[1] benzopyrano [2, 3-b] pyridin-7-yl) propionic acid (Y-8004), a new anti-inflammatory agent, were investigated in rats and mice by the use of 14C-labeled compound (14C-Y-8004). When the radioactive compound was given to rats orally or intraperitoneally, about 50% of the given radio-activity (14C) was excreted in urine and 40% in feces during 72 hr, while about 80% in urine and 20% in feces after oral administration to mice. Approximately 55-60% was recovered in rat bile during 24 hr after oral administration. The highest blood level of 14C was obtained at 0.5-1 hr after oral administration to rats and mice. A good correlation was observed between blood level and dose level. However, apparent species difference in the blood 14C concentration and its disappearance rate were observed between rats and mice. When 14C-Y-8004 was orally administered to bileduct-cannulated rat, the blood 14C concentration and its disappearance rate came close to those of normal mice. The highest concentration of 14C was observed in the serum and relatively high levels in the liver and kidney of rats and mice after oral administration of 14C-Y-8004. In both animals, most of 14C in the serum existed as unchanged material bound to serum protein. Thin-layer chromatography after enzymic, acid, and alkaline hydrolysis experiments showed that the major metabolite in urine and bile of rats was Y-8004 acylglucuronide and in urine of mice Y-8004 acylglucoside. The present investigation provides the first evidence for the formation of an acylglucoside of a drug in mammals.View full abstractDownload PDF (971K) -
TAKEKI OKUMOTO, HIROSHI IMAMURA1976 Volume 96 Issue 7 Pages 827-831
Published: July 25, 1976
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSThe survival rate of cultured HeLa S3, L5, and AH-7974 cells treated with improsulfan decreased exponentially with increasing concentration of the compound. The survival rate of HeLa S3 cells decreased abruptly by their exposure to improsulfan for a short period but remained unchanged by further prolonged exposure. This result may be attributed to the instability of improsulfan in the medium. HeLa S3 cells treated once with improsulfan were more sensitive to it than the untreated cells. Repeated treatment of these cells with 0.2 or 0.5 mM improsulfan, twice for 60 min each, showed the same effect against the survival rate of HaLa S3 cells as the single treatment with 0.4 or 1 mM for 120 min, respectively. This result suggests the usefulness of fractionated doses of improsulfan for a short period in certain tumor systems, if the schedule does not enhance host toxicity. The sedimentation profile of single-stranded DNA derived from HeLa S3 cells treated with 2.5 mM improsulfan showed a fragmentation in the alkaline sucrose gradient.View full abstractDownload PDF (580K) -
TOSHINOBU KAWATA, KAZUNOBU HARANO, TANEZO TAGUCHI1976 Volume 96 Issue 7 Pages 832-840
Published: July 25, 1976
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSIn connection with the preceding study on the catalytic rearrangement of O, S-dialkyl dithiocarbonates to S, S-dialkyl dithiocarbonates with aluminum chloride in carbon disulfide, the effect of structure of O, S-dialkyl dithiocarbonates, catalysts (Lewis acid), and solvents on this rearrangement was examined.View full abstractDownload PDF (932K) -
TAKEYA KOMIYA, MAKOTO TSUKUI, HARUJI OSHIO1976 Volume 96 Issue 7 Pages 841-854
Published: July 25, 1976
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSA new choleretic substance, capillarisin (I), was isolated from the herb of Artemisia capillaris Thunb. (Japanese name, "Inchinko" ?? 〓 ?? ) by tracing the activity in rats. By heating with 1% NaOH or H2SO4 in methanol, I was cleaved to p-hydroquinone and a compound (XI) or p-hydroquinone and the compound (XII). Infrared and ultraviolet spectra suggested that I and XI are chromone derivatives and XII is a coumarin derivative. Positions of the functional groups in XI and XII were determined by direct comparison with the synthetic samples, and the structure of I was established as 2-(p-hydroxy-phenoxy)-6-methoxy-5, 7-dihydroxychromone.View full abstractDownload PDF (1404K) -
TAKETA KOMIYA, YOSHITOMO NARUSE, HARUJI OSHIO1976 Volume 96 Issue 7 Pages 855-862
Published: July 25, 1976
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSFour new 2-phenoxychromone derivatives were isolated from Artemisiae Capillaris Herba (Japanese name, "Inchinko" ?? 〓 ?? ). Their structures were established on the basis of chemical and spectroscopic evidences as 2-(p-methoxyphenoxy)-6-methoxy-5, 7-dihydroxychromone (4'-methylcapillarisin), 6, 7-dimethoxy-2-(p-hydroxyphenoxy)-5-hydroxychromone (7-methylcapillarisin) 2-(p-methoxyphenoxy)-5, 7-dihydroxychromone (6-demethoxy-4'-methylcapillarisin), and 2-(p-hydroxyphenoxy)-5, 7-dihydroxychromone (6-demethoxycapillarisin), respectively. Four flavonoids, cirsilineol, cirsimaritin, genkwanin, and rhamnocitrin, were also isolated from this herb.View full abstractDownload PDF (901K) -
SHIGEKATSU NAKAJIMA, RYUSEI KONAKA, KENICHI TAKEDA1976 Volume 96 Issue 7 Pages 863-879
Published: July 25, 1976
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSIn the oxidation reactions of 3-oxo-steroids with oxygen in a basic solution, the effect of various substituents in B and C rings was examined by product analyses and by ESR measurements. 3-Oxo-5α-steroids themselves produced only 2, 3-diketones although Δ3-semidiones were observed along with Δ2-semidiones in the ESR spectra. Introduction of 11-oxo, 11-methylene, 11β-methyl, Δ7 (8), or Δ9 (11) group into 3-oxo-5α-steroids gave 3, 4-diketones together with 2, 3-diketones, but the substituent effect of 11α-hydroxyl 11α-methyl-11β-hydroxyl, Δ9 (11)-11-methyl, Δ6 (7), Δ11 (12), Δ11 (12)-12-methyl, or 12-meth-ylene group was not observed significantly. 25D.5β-Spirostan-3-one (XLVIII) afforded only the 3, 4-diketone and no substituent effect was observed by introducing an oxo group into the C-11 position of (XLVIII). In the ESR measurements the concentrations of Δ2-semidiones and Δ3-semidiones changed with time and the ratios of the maximum concentration corresponded to the product ratios. The long range effect of these substituents can be interpreted in terms of"conformational transmission"based on the direction of enolation in the A rings.View full abstractDownload PDF (1679K) -
KEISUKE KITAMURA, YOSHIO MORI, MICHIYO HORII, KEIICHIRO HOZUMI1976 Volume 96 Issue 7 Pages 880-885
Published: July 25, 1976
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSSome aromatic hydrocarbons, such as benzene, toluene, ethylbenzene, p-xylene, and styrene, were polymerized by subjecting them to a radio-frequency glow discharge at a reduced pressure (plasma polymerization), resulting in any of three types of products : powder, oil, and solid film, under varied plasma conditions. The oily products soluble in chloroform and carbon tetrachloride exhibited an average molecular weight of 400-600. The infrared spectra of these materials showed similar characteristics and also similar to normal polystyrene having a linear backbone chain, whereas their nuclear magnetic resonance (NMR) spectra did not show resemblance to the latter. NMR spectra of these products showed the presence of aromatic protons, widely shifted aliphatic protons, and olefinic protons, and the comparison of signal intensities of the polymer products with that of monomers suggested the formation of aliphatic chains derived from the cleavage of the aromatic rings. Based on these spectral data, structure of the oily products is postulated to be a polystyrene type but to have longer and branched backbone chains involving some double bonds. By assuming 1.5 hydrogen atoms to be bonded to a chain carbon, as in the normal polystyrene, the number of backbone chain carbons per benzene ring should be about four. Values of H/C ratio calculated from this assumption agreed well with that obtained from elemental analysis.View full abstractDownload PDF (692K) -
TAKUZO HISANO, KIYOKATSU SHOJI, MASATAKA ICHIKAWA1976 Volume 96 Issue 7 Pages 886-890
Published: July 25, 1976
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSNitroanthranilic acids were reacted with picolinic acid, in the presence of phosphoryl chloride, to form 3-, 4-, and 5-nitro-2-picolinamidobenzoic acids which were used as the starting material for the application of anilines, with phosphorus trichloride as the condensation agent, to effect cyclization to 4 (3H)-quinazolinones. The yield of the cyclization product was very poor when the reaction was carried out with ortho-substituted anilines but the yield was raised 3-fold when polyphosphoric acid was used as the condensation agent. Examination of the nitration of 2-(2-pyridyl)-3-phenyl-4 (3H)-quinazolinone showed that the reaction progressed only with nitric acid in sulfuric acid to yield 2-(2-pyridyl)-3-(m-nitrophenyl)-6-nitro-4-(3H)-quinazolinone.View full abstractDownload PDF (568K) -
TEISUKE OKANO, TAKASHI HORIE, NOBORU MOTOHASHI1976 Volume 96 Issue 7 Pages 891-898
Published: July 25, 1976
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSStudies were made on the intermolecular interaction of the oxazine dye Nile Blue A and calf-thymus deoxyribonucleic acid (DNA). It was concluded from these experimental results that two modes of interaction, ionic binding of the basic dye and the phosphate group of DNA, which leads to metachromasis of the dye, and intercalation of the dye between adjacent base-pairs of the macromolecule, are taking part in the binding of Nile Blue A and DNA : (1) When this dye was mixed with DNA at pH 7.0, intensity of its characteristic absorption bands (α and β bands) decreased, and new absorption bands appeared in the vicinity of 550 nm (γ band) and 668 nm (δ band). (2) The γ-band was produced when the molar ratio of [Dye]/[DNA-P] was greater than 1, while the δ-band was produced when this molar ratio was smaller than 1. (3) Flow dichroism spectrum of the δ-band indicated that the Nile Blue A molecule was oriented perpendicularly to the longer axis of the double helix of DNA ; dichroism was not observed with a mixture of this dye and heat-denatured DNA. (4) The γ absorption band was also produced by the mixed system of Nile Blue A and potassium poly (vinylsulfonate) : no spectral change was observed with a monomeric vinyl sulfonate. (5) Mixed systems of Nile Blue A and a high concentration of purine nucleosides or mononucleotides exhibited a larger δ band than the systems in which corresponding pyrimidine derivatives were involved. (6) Larger spectral changes were produced by the interaction systems of Nile Blue A and purine homopolynucleotides than by the systems in which pyrimidine homopolynucleotides were involved. (7) Viscosity and melting temperature of DNA increased with increasing concentration of this dye added.View full abstractDownload PDF (930K) -
HISAKAZU SUNADA, AKINOBU OTSUKA1976 Volume 96 Issue 7 Pages 899-904
Published: July 25, 1976
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSCompaction of a powder has been simulated on two-dimensional model by employing a digital computer. In the process of formation of the initial bed, 400 discs of equal size were dropped one by one into a container, introducing the probability P to make each two discs cohere in contact. Compaction of the beds by tapping was also simulated by shifting each disc into the hole present in the lower layer. In this process the coordination number of a disc and the cohesion probability P'were taken into consideration. Another probability P"was introduced in the step of insertion of a disc into the hole created by the transfer of the former disc. The relation between porosity and tapping number was fitted in Kawakita's equation when P'was relatively large and P"small. On the other hand, Kuno's equation was applicable when P'was small and P"large. It was also indicated that the cohesion probability P'is closely related to the rate constant in these equations.View full abstractDownload PDF (700K) -
MASAHARU KOJIMA, MASAZUMI WATANABE, TANEZO TAGUCHI1976 Volume 96 Issue 7 Pages 905-911
Published: July 25, 1976
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSMethyl 2, 3-dideoxy-2, 3-dithio-α-D-altropyranoside derivatives were synthesized by the thermal rearrangement of xanthate derivative of methyl 4, 6-O-benzylidene-3-S-benzyl-3-deoxy-3-thio-α-D-altropyranoside (III) or methyl 4, 6-O-benzylidene-2-S-benzyl-2-deoxy-2-thio-α-D-altropyranoside (IV).View full abstractDownload PDF (741K) -
TETSUROU HANDA, MASAYUKI NAKAGAKI1976 Volume 96 Issue 7 Pages 912-918
Published: July 25, 1976
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSThe collapse pressure of mixed monolayers of cholesterol and hexadecyl dihydrogen phosphate and the spreading pressure of these mixtures were measured on aqueous solutions of hydrochloric acid and of hydrochloric acid+urea. On the basis of the dependence of the collapse pressure and the spreading pressure on the molar fraction, it was found that, in the mixed monolayer on the aqueous hydrochloric acid, cholesterol and hexadecyl dihydrogen phosphate did not mix with each other and formed a"patched monolayer". On the other hand, the addition of 4M urea made the components miscible. Thus, the important effect of the hydrogen bond between phosphate groups in the monolayer was inferred.View full abstractDownload PDF (716K) -
YUKIMASA TERADA, KOICHI NAKANO, TERUO OKU, AKIRA FUJIMOTO, JUTARO OKAD ...1976 Volume 96 Issue 7 Pages 919-922
Published: July 25, 1976
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSPhotochemical reaction of 2-(1-cyclohexenyl) cyclohexanone (II) with formamide in tert-butanol afforded two cyclization products ; 1, 2, 3, 4, 4a, 7, 8, 9, 10, 10b-decahydro-6 (5H)-phenanthridinone (III) and 1, 2, 3, 4, 7, 8, 9, 10-octahydro-6 (5H)-phenanthridinone (IV). These two products (III and IV) were further dehydrogenated with sulfur to give the known compounds V and VI, respectively. On irradiation of 1, 2-cyclohexanedione (VIII) in acidic solution under various conditions, several dimerization products were obtained ; 4, 4', 5, 5', 6, 6'-hexahydro-2, 2'-dihydroxybiphenyl-3, 3'-dione (IX), perhydro-4a, -9a-epoxydibenzo-p-dioxin-5a, 10a-diol (X), perhydro-2, 3'; 2', 3-diepoxybiphenyl-2, 3, 3'-triol (XI), and an unknown compound (XII).View full abstractDownload PDF (486K) -
MASAMI INOUE, SABURO ENOMOTO1976 Volume 96 Issue 7 Pages 923-926
Published: July 25, 1976
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSMethylation of phenols by methanol was examined with metal salts. At 350°, anisole was formed selectively from phenol and methanol in the presence of chlorides, sulfides, and phosphates of iron and chromium. With 1 g of chromic phosphate (CrPO4·1.8H2O), conversion reached 45% and the selectivity to anisole was 95% at 375°for 12 hr from phenol (10 g) and methanol (15 g). In contrast, aromatic carbon atoms of phenols were methylated by methanol in the presence of metal nitrates. Especially, ferric nitrate and chromium nitrate showed better activity to ortho-methylation. The selectivity of anisole formation and ortho-methylation was discussed in terms of different characters of metal salts.View full abstractDownload PDF (469K) -
TATSUAKI YAMAGUCHI, KIMITOSHI SAITO, KOUICHI KISO, MASARU TAKESHITA, T ...1976 Volume 96 Issue 7 Pages 927-931
Published: July 25, 1976
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSThe base-catalysed reaction of 3-acetyltetramanilide (II) with benzaldehyde in refluxing ethanol gave two isomeric condensation products. This indicates that both the ring methylene group (5-position) and the methyl group in α-phenylaminoethylidene group of II have the possibility of being attacked by the benzaldehyde molecule. Ratio of their yield varied with the nature of the base, the basicity and the steric requirement. Differences in the selective catalytic action between pyridine and piperidine are discussed on the basis of the results on the catalytic H-D exchange rate of the CH bonds of II susceptible to the condensation reaction.View full abstractDownload PDF (594K) -
TATSUO OZAWA, YOSHIYUKI NAKAMURA, NAOHIDE KINAE1976 Volume 96 Issue 7 Pages 932-935
Published: July 25, 1976
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSThe four pigments of isatin derivatives were separated from the browinng reaction of L-ascorbic acid (AAH2) with p-toluidine. These colors were identified as 2, 3-di-(p-tolylimino)-5-methylindoline (I) (reddish brown), 2-deoxy-2-(p-tolylimino)-5, 5'-dimethyl-isoindigo (II) (reddish orange), 5, 5'-dimethylindirubin (III) (violet), and 3-deoxy-3-(p-tolylimino)-5, 5'-dimethylindirubin (IV) (violet), which were found to be formed by the reaction of glucose and p-toluidine. The formation pathway of these pigments is different from those produced by the glucose-p-toluidine reaction, that is, the reaction of 14C1-AAH2, 5, 6-isopropylidene-AAH2, 5-phenyl-2, 3, 4 (5) furantrione, glycolaldehyde, and triose reductone with p-toluidine suggested that they are not formed from C1-C2 fragment of AAH2, but formed from its C5-C6 fragment.View full abstractDownload PDF (546K) -
MINORU MAEDA, HIROSHI KOMATSU, YORIKO YAMAMOTO, HIROSHI SHIMOIRISA, SE ...1976 Volume 96 Issue 7 Pages 935-937
Published: July 25, 1976
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESS5α-Bromo-6, 19-epoxy-cholestan-3β-ol acetate was prepared in a good yield only by heating 5α-Bromo-cholestane-3β, 6β-diol 3-acetate in cyclohexane with I2-Pb (OAc)4 in the presence of calcium carbonate without ultraviolet ray irradiation.View full abstractDownload PDF (414K) -
HISAKAZU SUNADA, AKINOBU OTSUKA1976 Volume 96 Issue 7 Pages 938-939
Published: July 25, 1976
Released on J-STAGE: May 30, 2008
JOURNAL FREE ACCESSComparison between two-dimensional porosity εa and three-dimensional porosity εv was made by a computer simulation study. In the formation of beds based on a random packing model, circles and spheres of equal size were used for the two- and three-dimen-sional systems, respectively. The porosity parameter P was introduced to decide whether the circles or spheres cohere or not when they came into contact with each other. εa and εv for the same P values were then compared. Porosities from the two-and threedimensional regular packing model were also examined. Results obtained by the random packing model were in good agreement with those by the regular packing model, as well as the two-dimensional"open-beam"packing model.View full abstractDownload PDF (341K)
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