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Volume 23, Issue 6
Displaying 1-33 of 33 articles from this issue
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RYOZO HAYASHI, MINORU OKADA, TADAMASA NAKAZAWA, YORIHISA TANAKA, YASUO ...1975 Volume 23 Issue 6 Pages 1173-1183
Published: June 25, 1975
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSOn the basis of the spectral examinations of the isolated materials and direct comparisons with chemically synthesized samples, the main metabolites of 5-methyl-8-(2-hydroxy-3-t-butylaminopropoxy) coumarin (CS-359) in excreta of rats and dogs were established as the 5-hydroxymethyl and 5-carboxyl compounds, resulting from oxidation of the 5-methyl group of the parent compound. 8-Oxyacetic acid was also identified as a minor metabolite. Thin-layer chromatograms of the samples from urine and feces exhibited the similar pattern, irrespective of animal species or routes of administrations. Results from fractionation by AcOEt extraction and paper electrophoresis suggested that both neutral and acidic metabolites may be miner components. Experiments on enzymatic hydrolysis indicated that neither giucerchide (s) nor sulfate (s) occurred in significant amounts in excreta. Possible metabolic pathways of CS-359 are presented.View full abstractDownload PDF (1163K) -
SEIJI KUZUNA, KIYOHISA KAWAI1975 Volume 23 Issue 6 Pages 1184-1191
Published: June 25, 1975
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSRats with adjuvant arthritis were used for an analgesic test in which flection stimuli were applied to the arthritic joints. TAI-284, indomethacin, phenylbutazone, mefenamic acid, ibufenac, aspirin and aminopyrine were effective at the relatively low doses in this method. Oral ED50s of these compounds run parallel to their clinical doses. The method detects not only the analgesic action of morphine, pethidine and codeine, but also that of nalorphine, pentazocine and amphetamine. Prednisolone was mildly effective dose-independently. In spite of the high sensitivities, the method was specific in the sense that CNS-depressant, anti-depressant, anti-epileptic, naloxone, anti-serotonin and anti-histamine drugs were inactive or slightly active at toxic doses. The arthritic flection pain test was concluded to be a sensitive and specific test.View full abstractDownload PDF (803K) -
HIROSHI Y. WATANABE, KAZUO WATANABE1975 Volume 23 Issue 6 Pages 1192-1196
Published: June 25, 1975
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSElectrothermic lesions of the midbrain of rats were made in the region of the median or median plus dorsal raphe nuclei through an unipolar electrode. Concentration of serotonin (5HT) in the telencephalon decreased variously among rats and locomotor activity increased following lesions. No close correlation was obtained between locomotor activity and the 5HT concentration in the telencephalon 7 to 14 days after the lesion. The effect of p-chlorophenylalanine (PCPA, a total dose of 400 mg/kg, i.p.) was also investigated on locomotor activity, and on 5HT and 5-hydroxyindoleacetic acid (5HIAA) levels in the telencephalon of the rat. PCPA lowered the 5HT content to less than 35% of the control in the telencephalon, but did not significantly alter locomotor activity. Only an excess mounting behavior was observed. These results suggest that an increase in locomotor activity due to raphe lesion has no primary connection with lowering the 5HT content of the rat brain.View full abstractDownload PDF (657K) -
SHOZO MIYAZAKI, MASAHIRO NAKANO, TAKAICHI ARITA1975 Volume 23 Issue 6 Pages 1197-1204
Published: June 25, 1975
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe pH-solubility profiles of tetracycline antibiotics in HCl-sodium acetate buffer solution were obtained at 37°. Solubility vs. pH curves of chlortetracycline hydrochloride (CTC-HCl) passes through a maximum at approximately 2.8 whereas solubility of tetracycline hydrochloride (TC-HCl) increases with decrease in pH. The similar solubility vs. pH curve was also obtained for demethylchlortetracycline hydrochloride (DMCT-HCl) and methacycline (MOTC-HCl). From the studies on the salts effect on the solubility of the tetracycline antibiotics, the drop at more acidic pH value in pH-solubility profiles of CTC-HCl, DMCT-HCl, and MOTC-HCl was found to be due to the common ion suppression of the solubility product equilibrium. The dissolution behavior of the free base and the hydrochloride of tetracyclines was examined in dilute hydrochloric acid solutions, whose pH ranges from 1.2 to 2.1. The results indicated that the free base of CTC, DMCT, and MOTC was more soluble than the corresponding hydrochloride at the gastric pH values (pH 1.2-1.4 for CTC and DMCT and pH 1.2-2.1 for MOTC). On the other hand, TC-HCl exhibited a greater solubility than the base in pH 1.2 since the solubility of TC-HCl was little affected by addition of common ion (Cl-).View full abstractDownload PDF (896K) -
YOKO HAMADA, NAOKI NAMBU, TSUNEJI NAGAI1975 Volume 23 Issue 6 Pages 1205-1211
Published: June 25, 1975
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe interactions of α-cyclodextrin (α-CD) and β-cyclodextrin (β-CD) with several non-steroidal antiinflammatory drugs were studied, observing the effects of α- and β-CD on the solubility and the stability of the drugs in aqueous solution in comparison with that of glucose. Moreover, the combined effects of urea and sodium chloride with β-CD on the solubility of drugs were discussed. The solubility of all kinds of drugs was found to increase with the addition of β-CD, while not with glucose. The increase of solubility with β-CD was considered due mainly to the formation of inclusion compounds. From the solubility data, the apparent stability constant K of the formation of inclusion compound were calculated, and moreover the functional groups included by β-CD were estimated for the respective drugs. The dissolution rate of drug increased with β-CD, while not with glucose, as was similar in tendency to the solubility data. β-CD accelerated the degradation of azapropazone in aqueous solution while retarded that of phenylbutazone, and glucose had no effect on the stability of drugs, showing that a formations of inclusion compound with β-CD may make some drugs stable and others labile. The addition of urea was considered to promote the inclusion of drug with β-CD, while sodium chloride gave the opposite effect, and an elevation of temperature gave the promoting effect.View full abstractDownload PDF (767K) -
OSAMU NISHIMURA, CHITOSHI HATANAKA, MASAHIKO FUJINO1975 Volume 23 Issue 6 Pages 1212-1220
Published: June 25, 1975
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSHuman adrenocorticotropic hormone (αh-ACTH), H-Ser-Tyr-Ser-Met-Glu-His-Phe-Arg-Trp-Gly-Lys-Pro-Val-Gly-Lys-Lys-Arg-Arg-Pro-Val-Lys-Val-Tyr-Pro-Asn-Gly-Ala-Glu-Asp-Glu-Ser-Ala-Glu-Ala-Phe-Pro-Leu-Glu-Phe-OH, was synthesized by using N-hydroxy-5-norbornene-2, 3-dicarboximide (HONB) with N, N'-dicyelohexylcarbodiimide (DCC) for the stepwise elongation and fragment condensation. The synthetic αh-ACTH, purified on a column of carboxymethylcellulose, Amberlite XAD-2 resin and Bio-Gel P-6, was found to be homogeneous by various criteria and exhibits full biological activity (ca. 145 units/mg) in in vitro steroidogenic assay.View full abstractDownload PDF (1142K) -
MAMORU SUGIURA, MASAKAZU ISOBE1975 Volume 23 Issue 6 Pages 1221-1225
Published: June 25, 1975
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe hydrolysis of olive oil by the lipase from Chromobacterium was inhibited by the addition emulsion of organic solvents. This inhibition was essentially competitive and was observed with emulsion of any organic solvent used in this study, independently of their chemical structure. The competitive inhibition was also observed on the emulsion prepared with various emulsifiers and on the emulsion in which an organic solvent was dissolved. Lipases from porcine pancreas, Candida sp. and Pseudomonas sp. showed the same behavior. From these results, it was presumed that lipases had a characteristics of adsorption at the interface. This assumption was also supported by the experiment of adsorption to emulsions. On the other hand, the esterase of chiken liver was not inhibited by the emulsion of any organic solvents tested in this study and was not adsorbed to the emulsion. A possible hypothesis on the mechanism of lipase reaction was discussed in relation to these properties.View full abstractDownload PDF (632K) -
MAMORU SUGIURA, MASAKAZU ISOBE1975 Volume 23 Issue 6 Pages 1226-1230
Published: June 25, 1975
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSSubstrate specificity of lipase B (low molecular weight) of Chromobacterium viscosum was studied. It was suggested that the apparent substrate specificity for emulsions of single triglyceride was affected by the physical state of the emulsion. At a lower temperature, triglycerides of medium-chain fatty acids were good substrates, while at higher temperatures, triglycerides of long-chain fatty acids became better substrates. It was concluded from the data on hydrolysis of methyl esters of fatty acid and the mixture of a series of single triglyceride that lipase B had a specificity to long-chain and unsaturated fatty acid esters, but the esters of stearic acid were not good substrates. Further, it was suggested that the mixture of a series of single triglycerides was more appropriate than the single substrates for studies on the substrate specificity of lipase. Lipase B was capable of hydrolyzing the fatty acid ester bonds at the 2-position of triglycerides as well as the 1- and 3-positions at the same rate.View full abstractDownload PDF (669K) -
HIROSHI HIKINO, CHOHACHI KONNO, YAYOI IKEDA, NOBUKO IZUMI, TSUNEMATSU ...1975 Volume 23 Issue 6 Pages 1231-1240
Published: June 25, 1975
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSIncubation of three stereoisomers of α-cyperone (1, 2, and 3) with Colletotrichum phomoides resulted in two types of modification hydroxylation (C-2 and C-6) in one isomer (2) and dehydrogenation (C-6 : C-7) in another isomer (3) at the nuclei and in three types of modification (hydration to an alcohol, allylic hydroxylation to an allyl alcohol, and oxidation to a 1, 2-glycol) at the side chains in all the isomers in different rates. On fermentation with the same microbe of three stereoisomers of dihydro-α-cyperone (16, 17, and 18), prepared for prevention of the side chain modification, hydroxylation at the nucleus (C-1) occurred merely in one isomer (16), and the same types of oxidation at the side chains also took place in all the isomers as in their congeners (1-3). The stereoselectivity and the probable mechanisms of the transformations are discussed.View full abstractDownload PDF (1313K) -
MINORU SEKIYA, TOSHIAKI MORIMOTO1975 Volume 23 Issue 6 Pages 1241-1246
Published: June 25, 1975
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSReaction of 1-pyrrolidino-1-cyclohexene with N-arylbenzimidoyl chlorides has been successfully performed to result in introduction of benzimidoyl groupings at β-carbon of the enamine. Easy hydrolysis of enamine moiety of these products provides an effective means of preparation of mono-anils of 2-benzoylcyclohexanone, from which several phenanthridine derivatives have been newly obtained by action of polyphosphoric acid.View full abstractDownload PDF (790K) -
SHOJI KOJIMA, JUNICHI MIYAKE1975 Volume 23 Issue 6 Pages 1247-1255
Published: June 25, 1975
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe effect of the hypertonic and hypotonic solutions on the absorption of acetanilide, salicylamide, sulfisoxazole, and quinine from rat small intestine was studied using the in situ perfusion technique. Water net flux into the intestinal lumen occurring in the hypertonic solution diminished the absorption of the drugs. Whereas the enhancement of the absorption of the drugs was observed in the hypotonic solution causing water net flux out of the intestinal lumen. The effect of water net flux on the absorption of the drugs was studied by dividing into the four components. It was found that the solvent drag and rate of blood flow, as the two significant components, played a major role in the absorption of the drugs through the intestinal membrane. The rate of intestinal blood flow played an important role in the absorption of acetanilide and salicylamide, which were lipid soluble and very rapidly absorbed. In the case of the more polar and slowly absorbable quinine, the solvent drag played a significant role. Both blood flow and solvent drag were effective for the absorption of sulfisoxazole, which existed mostly in the ionized form at pH 6.0 and was moderately rapidly absorbed. In addition, it was demonstrated that two other components such as the change of drug concentration in the intestinal lumen and intestinal tissue fluid uptake due to water net flux played a minor role in the in situ intestinal absorption of the drugs.View full abstractDownload PDF (1104K) -
YOSHIKO MIYAJI, HIROSHI ICHIKAWA, MICHIHIKO OGATA1975 Volume 23 Issue 6 Pages 1256-1260
Published: June 25, 1975
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSTautomerism of hydroxypyridines is investigated by a version of the modified intermediate neglect of differential overlap method to show that the predominance of tautomerism depends on the total energy of tautomer. The calculations are carried out for 4-hydroxyaminopyridine 1-oxide (I) and 4-hydroxyaminoquinoline 1-oxide (II), leading to a conclusion that the predominant tautomer of I is formulated to be the N-oxide form and that of II is the N-hydroxy form. This structural difference is discussed in relation to difference in the biochemical behaviours of these compounds.View full abstractDownload PDF (605K) -
HIROSHI NAKAMURA, ZENZO TAMURA1975 Volume 23 Issue 6 Pages 1261-1270
Published: June 25, 1975
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSBisulfite reacted with N-(p-dimethylaminophenyl)-1, 4-naphthoquinoneimine (indophenol blue, I) to yield blue fluorescence in alkaline media. The reaction was dependent upon pH and temperature, being optimal at pH 3.5-4.0 and around 37°, and completed within 30 min. Based on these observations, a fluorometric method has been developed for the determination of bisulfite. A linear relationship was obtained in the range of 1.5×10-8-1.5×10-7 mole of bisulfite. By column chromatography, thin-layer chromatography and paper electrophoresis, it was proved that at least two fluorescent compounds were formed in the reaction mixture and they were supposed to be bisulfite adducts of I containing one and two -SO3H groups.View full abstractDownload PDF (897K) -
SHUNSUKE NARUTO, HARUKI NISHIMURA, HIDEHIKO KANEKO1975 Volume 23 Issue 6 Pages 1271-1275
Published: June 25, 1975
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe reaction of acetoneberberine (I) with methyl iodide was found to give 8, 13a-(2'-oxopropano)-13, 13-dimethylberbine derivative (IV) and 8, 13a-(2'-oxopropano)-13-methylberbine derivative (V) as side products together with the expected 13-methyl-berberinium (II) and berberinium iodide (III). Analogous reaction of I with allyl bromide gave rise to 8, 13a-(2'-oxopropano)-13, 13-diallylberbine derivative (XI). The structures of products were deduced from chemical and spectral data.View full abstractDownload PDF (643K) -
SHUNSUKE NARUTO, HARUKI NISHIMURA, HIDEHIKO KANEKO1975 Volume 23 Issue 6 Pages 1276-1282
Published: June 25, 1975
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSOxidation of acetonepalmatine (IV) with potassium permanganate proceeded as well as acetoneberberine (I) to give 8, 13a-propanoberbine derivative (VI). On the other hand, 13-methylacetoneberberine (V) reacted with potassium permanganate to form mainly a lactam (XIV) as a result of the oxidative fission of C13-C13a double bond, together with minor 8, 13a-propanoberbine products, XV and XVI.View full abstractDownload PDF (822K) -
TAKU CHIBA, MASANOBU HAGA, SETSUZO TEJIMA1975 Volume 23 Issue 6 Pages 1283-1289
Published: June 25, 1975
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSBenzylidenation of 1, 6-anhydro-β-lactose afforded 1, 6-anhydro-4', 6'-O-benzylidene-β-lactose (2) in 81% yield. Acylation of 2 yielded tetra-O-acyl-1, 6-anhydro-4', 6'-O-benzylidene-β-lactose [acyl=acetyl (3), benzoyl (4)]. Reflux of 3 with N-bromosuccinimide and BaCO3 in CCl4 and 1, 2-dichloroethane gave crystalline tetra-O-acetyl-1, 6-anhydro-4'-O-benzoyl-6'-bromo-6'-deoxy-β-lactose (5) in 52% yield. Catalytic dehydrobromination of 5 afforded crystalline tetra-O-acetyl-1, 6-anhydro-4'-O-benzoyl-6'-deoxy-β-lactose (6). Deacylation of 5 and successive reacetylation yielded 2, 2', 3, 3', 4'-penta-O-acetyl-1, 6-anhydro-6'-bromo-6'-deoxy-β-lactose (7). Dehydrobromination of 7 gave penta-O-acetyl-1, 6-anhydro-6'-deoxy-β-lactose (8). Heating of 7 and sodium azide in hexamethylphosphoric triamide afforded a mixture of crystalline penta-O-acetyl-1, 6-anhydro-6'-azido-6'-deoxy-β-lactose (9) (36%) and sirupy 2, 3-di-O-acetyl-1, 6-anhydro-4-O-(2, 3, 4-tri-O-acetyl-α-L-arabino-hex-5-eno-pyranosyl)-β-D-glucopyranose (10) (34%). Compound 10 was also prepared by treatment of 7 in dry pyridine with silver fluoride. Acetolysis of 9, reduction of the azido group in the acetolysis product (11), N-acetylation, and finally de-O-acetylation afforded the title compound (13) as hydroscopic crystals, [α]24D+80°→+66.7°. In catalytic hydrogenation of 10 over Pd catalyst, 8 was the sole product in 90% yield. Over Pt oxide or Raney Ni catalyst, a low yield of 8 was effected with fairly amounts of unidentified sirup.View full abstractDownload PDF (1003K) -
YOSHISUKE TSUDA, TAKUNORI FUJIMOTO, KOICHI KIMPARA1975 Volume 23 Issue 6 Pages 1290-1299
Published: June 25, 1975
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSFive new triterpenoids occurring in various Lycopodium plants were shown to be 16-oxoserratenediol (1a), 16-oxo-21-episerratenediol (2a), 16-oxodiepiserratenediol (3a), 16-oxoserratriol (6a), and 16-oxolycoclavanol (7a) respectively, by spectral and chemical means, and the structures assigned were finally confirmed by partial syntheses from the corresponding deoxo-compounds. Potential utility of the solvent shift experiment in NMR and the resulting TH-effect for structural and stereochemical problems was indicated. A conjugated ketone isolated from L. cernuum by Inubushi, et al. was identical with the synthetic 16-oxo-21-episerratriol (19c).View full abstractDownload PDF (1150K) -
TETSUKICHI NIWAGUCHI, TAKAKO INOUE1975 Volume 23 Issue 6 Pages 1300-1303
Published: June 25, 1975
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe nature of LSD-induced difference spectra in rat liver microsomes was investigated. The gradual shift from the type I spectrum to the modified type II spectrum with increasing concentration of LSD in hepatic microsomes suggested a composite change of two spectra. The type I component of LSD was obtained by subtracting the spectra in the presence of both the type I compound and LSD from the spectra of LSD alone. The spectral dissociation constant obtained from the spectra of the type I component of LSD was almost exactly equal to the Km value obtained from the disappearance of LSD in the enzymatic transformation.View full abstractDownload PDF (483K) -
MAMORU SUGIURA, AKIRA ITO1975 Volume 23 Issue 6 Pages 1304-1308
Published: June 25, 1975
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSSome physicochemical properties and amino acid compositions of dextranases from Brevibacterium fuscum and Penicillium funiculosum IAM 7013 were investigated. The values of 4.35S and 4.37S, respectively, were obtained for the sedimentation constant (S20, w) of dextranases from B. fuscum and P. funiculosum, and their isoelectric points (pI) were also determined 4.17 and 4.19, respectively. Gel filtration on Bio Gel P-100 indicated the molecular weight 5.5×104 for B. fuscum and 4.4×104 for P. funiculosum, and their intrinsic viscosities were 0.038 dl/g and 0.027 dl/g, respectively. Amino acid analysis suggested that dextranase of B. fuscum was found to be composed of more than 429 amino acid residues of 17 amino acids and the enzyme of P. funiculosum contained more than 349 of the residues of 18 amino acids. The composition of the enzymes was very similar except for two residues of cystine which were contained in only P. funiculosum dextranase. Dextranase of B. fuscum contained 11 moles of neutral sugars as glucose and 3 moles of amino sugars as glucosamine per one mole of the enzyme, and in P. funiculosum, the former was 10 moles and the later was found to be 1 mole. The results of staining of the enzymes in disc electrophoresis gels by periodic acid and fuchsin-sulfite, and the observations above mentioned indicated that both dextranases were glycoprotein.View full abstractDownload PDF (923K) -
TERUAKI YUZURIHA, KOUICHI KATAYAMA, TAKESHI FUJITA1975 Volume 23 Issue 6 Pages 1309-1314
Published: June 25, 1975
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe preparation and stability of lysozyme labeled with 3H or 131I were studied. 131I-lysozyme was found to be convenient for investigation on biotransformation of the enzyme. The transport of 131I-lysozyme across rat intestine in vitro was studied using rat everted jejunum. The transport of lysozyme from the mucosal to serosal side was confirmed by several methods such as TCA-precipitation, immunoprecipitation and enzymatic activity assay. The intestinal absorption of 131I-lysozyme in vivo was studied in rats paying attention to the lymphatics and the portal vein as the route of absorption. The absorption rate of immunoprecipitable 131I via lymphatics was 0.07% of the dose during the first 6 hr after intraintestinal administration of 2 mg/kg of 131I-lysozyme. The absorption rate of immunoprecipitable 131I via portal vein was calculated as 1.99% of 131I-lysozyme dosed, by pharmacokinetic analyses on the concentration of immunoprecipitable 131I in serum. Absorption via lymphatics was 3.24% of the total immunoprecipitable 131I absorbed via both routes. The main route in intestinal absorption of 131I-lysozyme following intraintestinal administration was suggested to be the portal vein, not lymphatics.View full abstractDownload PDF (792K) -
TERUAKI YUZURIHA, KOUICHI KATAYAMA, TAKESHI FUJITA1975 Volume 23 Issue 6 Pages 1315-1322
Published: June 25, 1975
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe tissue distribution of TCA-precipitable 131I following intravenous injection of 0.4 mg lysozyme labeled with 131I per kg in rats was investigated. The renal concentration of TCA-precipitable 131I was the highest in all the tissues tested, and the level in the kidney reached the maximum of 26.5% of the dose 30 min after injection. Sephadex G-50 gel filtration profiles of radioactivity solubilized by Triton X-100 demonstrated that the radioactivity in kidney was mainly in the form of 131I-lysozyme. The intracellular distribution of TCA-precipitable 131I in the kidney was studied by the differential centrifugation of kidney homogenates during the first 3 hr after intravenous injection of 131I-lysozyme in rats. The specific radioactivity in the 19600×g (20 min) fraction of kidney was found to be the highest among another fractions. The proteinbound radioactivity detected in the 19600×g fraction of kidney 30 min after injection was suggested to be present in phagolysosomes by sucrose density gradient centrifugation and solubilization with Triton X-100. The degradation of injected 131I-lysozyme by the 19600×g fraction or phagolysosomes was examined, in succession. The pH-degradation profile of the 19600×g fraction was a monopeak with the optimum at pH 5.0. Based on the observation of the activation by cysteine and the inhibition by iodoacetamide, it was indicated that the proteolytic enzyme with the optimal pH of 5.0 in phagolysosomes is cathepsin B1. The main degradation product of injected 131I-lysozyme in the phagolysosomes was identified as 131I-diiodotyrosine by paper chromatography. In contrast, the radioactivity excreted in urine was mainly inorganic 131I-.View full abstractDownload PDF (998K) -
MATAO MATSUI, YASUO WATANABE, TOSHIRO IBUKA, KIYOSHI TANAKA1975 Volume 23 Issue 6 Pages 1323-1335
Published: June 25, 1975
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSFour new hasubanan alkaloids, stephamiersine (1), epistephamiersine (2), oxostephamiersine (3) and stephasunoline (4) were isolated together with seven known and three unidentified alkaloids from Stephania japonica MIERS (Menispermaceae). Among these new alkaloids, 1 and 2 were found to be epimeric isomers with respect to the C-7 methoxyl group. Permanganate oxidation of 1 gave 3, and borohydride reduction of 1 and 2 gave the highly stereoselective products, dihydrostephamiersine (6) and dihydroepistephamiersine (5). On mild treatment of 5 with hydrochloric acid gave 4. Acetolyses of 1, 2, 5 and 6 gave the phenanthrene derivatives, 7, 8 and 9, respectively. Further, both 1 and 2 were converted to the conjugated carbonyl compound (14) which was obtained from dihydro-16-oxohasubanonine (17a) (17b). On the other hand, the stereochemistry of 1, 2, 3 and 4 was elucidated by nuclear magnetic resonance (NMR) spectroscopic studies as follows : the C-7 methoxyl group of 1 has the α-axial and that of 2 and 4 has the β-equatorial configuration, and the hydroxyl group of 4 has the β-axial one. On the basis of the above chemical correlation coupled with the spectral arguments, the constitution of the new alkaloids was represented as drawn in the formulas, 1, 2, 3 and 4.View full abstractDownload PDF (1566K) -
YOSHISUKE TSUDA, TAKUNORI FUJIMOTO, AKIRA MORIMOTO, TAKEHIRO SANO1975 Volume 23 Issue 6 Pages 1336-1346
Published: June 25, 1975
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSLycoclavanin, a Lycopodium triterpenoid containing four hydroxy-groups and a conjugated ketone, was established as 16-oxoserrat-14-ene-3α, 20β, 21β, 24-tetraol (7a) by spectral and chemical means. Correlations of lycoclavanin with 16-oxo-lycoclavanol (6a) and with serratenediol (17a) were described. A new tetraol occurring in L. clavatum was also established as serrat-14-ene-3α, 20β, 21β, 24-tetraol (23a).View full abstractDownload PDF (1208K) -
KEIJI SEKIGUCHI, MOTOKO KANKE, NORIKO NAKAMURA, YASUYUKI TSUDA1975 Volume 23 Issue 6 Pages 1347-1352
Published: June 25, 1975
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSTransition temperature and heat of transition between barbital forms I and II were found to be 93° and 210 cal/mole, respectively, measuring their initial dissolution rates by the method reported in the previous paper. The latter value is reasonably close to the value of 330±15 cal/mole obtained by differential scanning calorimetry (DSC). The data obtained in this study indicates that forms I and II are enantiotropic contrary to such a statement appeared in literature as they are monotropic. Furthermore, it was found that there is little difference in solubility values of barbital forms I and II.View full abstractDownload PDF (650K) -
KEIJI SEKIGUCHI, YASUYUKI TSUDA, MOTOKO KANKE1975 Volume 23 Issue 6 Pages 1353-1362
Published: June 25, 1975
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe initial dissolution rate measurement method was applied to physical forms of sulfanilamide, two polymorphs and a hydrate. As the result, the transition temperatures and the heats of transition between the metastable α-and the stable β-forms, and between the β-and the hydrated forms were determined to be -119°, 0.17 kcal/mole, and 38.3°, 1.74 kcal/mole, respectively. At the same time, thermal behaviors and solubilities of all the known forms of sulfanilamide including the above three were investigated by other methods such as differential scanning calorimetry and conventional solubility measurement. Data obtained agree well with those by dissolution study, though direct solubility determination of the metastable α-form was impossible because of rapid conversion to the β-or to the hydrated form. Thus, the total relation among these physical forms could be more clearly understood by combining all these data, and the supposition proposed previously that the α-form was monotropic with respect to the β-polymorph was denied completely.View full abstractDownload PDF (1054K) -
KOUICHI YAMANOUCHI, RYOICHIRO MURASHIMA, KAZUMASA YOKOYAMA1975 Volume 23 Issue 6 Pages 1363-1367
Published: June 25, 1975
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA gas chromatographic method for the quantitative determination of perfluorochemicals (FCs) contained in organs and body fluids was presented. Following destruction of FC emulsion by addition of ethanol, FCs were extracted with 1, 1, 2-trichlorotrifluoroethane and applied to a gas chromatograph equipped with a hydrogen flame ionization detector. A column (2 m×4 mm i.d.) of 20% Silicone OV-17 on Chromosorb W AW (60-80 mesh) was used at 60°. The retention time of each FC peak was found between 0.5 and 1.0 min. Complete separation of FC from the solvent was achieved and any undesirable, interfering peaks were not detected on the gas chromatogram. The determination of their contents was carried out by calculation of peak height ratio of them to benzotrifluoride added as the internal standard. Recovery of four kinds of FCs by this method ranged from 94.7 to 102.6% when known amount of respective FCs in emulsified form was added to the organs or blood with the standard deviation of ±3.3%.View full abstractDownload PDF (588K) -
KAZUMASA YOKOYAMA, KOUICHI YAMANOUCHI, RYOICHIRO MURASHIMA1975 Volume 23 Issue 6 Pages 1368-1373
Published: June 25, 1975
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSAs a part of studies on perfluorochemicals for candidate as an artificial blood, the elimination of six kinds of the substance was studied to find the way and type of excretion in rats given their emulsions intravenously. (1) These compounds are solely excreted through expiration, none through urinary and biliary with an exception of FC-43 (perfluorotrifbutylamine. (2) The elimination curves of these compounds from the body appear to be exponential). (3) The elimination rate of each substance was fairly related to its vapor pressure, the higher, the more rapidly eliminated. (4) Within six compounds examined sofar, FDC (perfluorodecalin) is selected on account of its rapid elimination.View full abstractDownload PDF (668K) -
MITSUO DEKI, MINORU YOSHIMURA1975 Volume 23 Issue 6 Pages 1374-1376
Published: June 25, 1975
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSSome of 2, 4-DNPH of volatile carbonyl compounds were analyzed by mass spectrometry combined with gas chromatography using a column packed with OV-101 (3%). The mixture of 2, 4-DNPH of volatile carbonyl compounds could be resolved on the column under the condition with linear program at a rate 5°/min from 140°-300°. The 2, 4-DNPH of volatile carbonyl compounds could be easily read from the peak with highest mass in the spectrum. The M+-60 and M+-42 were observed in the mass spectra of 2, 4-DNPH of aliphatic aldehydes over carbon number five. The 2, 4-DNPH of furan compounds also do exhibit the parent peak and fragment ions corresponding to the original compounds. M+-NO and M+-NO2 were not significant in the mass spectrum of 2, 4-DNPH of the volatile carbonyl compounds. From the result it was found that 2, 4-DNPH of volatile carbonyl compounds were not decomposed during gas chromatography.View full abstractDownload PDF (447K) -
YORISHIGE IMAMURA, KEIKO SHIGEMORI, HISASHI ICHIBAGASE1975 Volume 23 Issue 6 Pages 1377-1380
Published: June 25, 1975
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe antibacterial activities of sulfadimethoxine in rabbit plasma were significantly increased by concomitant injection of phenylbutazone. On the other hand, the levels of unchanged sulfadimethoxine determined by chemical assay in rabbit plasma were significantly reduced by concomitant injection of phenylbutazone. These results suggest that phenylbutazone increases the transfer of sulfadimethoxine from plasma to tissues in rabbits.View full abstractDownload PDF (512K) -
TORU KOIZUMI, YUICHI YOSHIDA, YUTAKA WATANABE, EIICHI YOSHII1975 Volume 23 Issue 6 Pages 1381-1382
Published: June 25, 1975
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSPresented is a novel phosphorylating reagent of alcohols, 2-phenoxy-benzoxazaphosphole-2-oxide, which reacts quite easily with ordinary alcohols to give, in fair yields, alkyl N-(2-hydroxyphenyl) phosphoroamidates potentially useful for further modification.View full abstractDownload PDF (341K) -
KOUICHIRO UMEMOTO1975 Volume 23 Issue 6 Pages 1383-1384
Published: June 25, 1975
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSIt has already been confirmed that the pattern of crystalline inorganic components in a plant follows a genetic rule, and this fact was elucidated further by observations of such patterns of quartz bodies in wheat leaves and calcium oxalate crystals in willow leaves.View full abstractDownload PDF (688K) -
MINORU MACHIDA, NOBUYUKI USHIJIMA, MIKIKO I. MACHIDA, YUICHI KANAOKA1975 Volume 23 Issue 6 Pages 1385-1386
Published: June 25, 1975
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSDimethylaminocoumarine (1) was proposed as one of candidate fluorogenic groups of choice. Thus N-(7-dimethylamino-4-methyl-coumarinyl) maleimides (4) are shown to be preferable fluorescent thiol reagents.View full abstractDownload PDF (385K) -
TAKEYA KOMIYA, MAKOTO TSUKUI, HARUJI OSHIO1975 Volume 23 Issue 6 Pages 1387-1388
Published: June 25, 1975
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe chemical structure of capillarisin, a new choleretic substance isolated from Artemisiae capillaris Herba, was established to be 2-(p-hydroxyphenoxy)-6-methoxy-5, 7-dihydroxychromone.View full abstractDownload PDF (340K)
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