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Volume 23, Issue 5
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MASATOSHI HARADA, SHINGO YANO1975 Volume 23 Issue 5 Pages 941-947
Published: May 25, 1975
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSEffects of cinnamaldehyde (CA) on the cardiovascular and digestive systems were examined. CA produced a hypotensive effect in anesthetized dogs and guinea pigs, which seemed to be due mainly to its peripheral vasodilatation. The vasodilatation induced by CA in dogs lasted and remained over the recovery period of the fall in blood pressure to its original level. A papaverine-like musculotropic activity of CA, which was shown in the isolated ileum from the guinea pig and the mouse, seemed to participate in the vasodilatation. CA exerted an increase in cardiac contractile force and beating rate in the isolated guinea pig heart preparations, that is, isolated atria and perfusing heart. The actions were distinct from those of adrenaline as a lag time was needed for the appearance of positive inotropic and chronotropic effects. The repeated applications of CA, however, decreased such effects and led to a cardiac inhibition. Coronary flow was increased. CA moderately inhibited both the rat stomach movement and the mouse intestinal propulsion. Gastric erosions produced in stressed mice were protected by oral administration of CA. In rats, CA increased biliary excretion. Some discussions were made upon the relation between pharmacological effects of CA and therapeutic effects of chinese cinnamon.View full abstractDownload PDF (859K) -
AKIRA TAKAMIZAWA, HISAO SATO1975 Volume 23 Issue 5 Pages 948-954
Published: May 25, 1975
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSReaction of 3-ethyl-5-aryl-1, 3, 4-oxadiazolium salts (X) with dialkyl acylphosphonates (V) in the presence of triethylamine afforded 2-aryl-4-ethyl-6-alkyl (or aryl)-5, 6-dihydro-4H-1, 3, 4-oxadiazin-5-one derivatives (XII) via an acyclic intermediate (XI) which is a 1 : 1 adduct of X and V. The mechanism of this novel reaction involving ring expansion is discussed briefly.View full abstractDownload PDF (761K) -
SEIJU KUBOTA, MASAYUKI UDA1975 Volume 23 Issue 5 Pages 955-966
Published: May 25, 1975
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSTautomerism of ten 3, 5-disubstituted 1, 2, 4-triazoles, which can exist in three tautomeric forms, has been studied. The nuclear magnetic resonance (NMR) and ultraviolet (UV) spectra of these 1, 2, 4-triazoles were compared with those of the N-methyl derivatives, which are the model compounds of the three kinds of tautomeric forms. Results indicate that a tautomeric hydrogen atom of the predominant tautomer of 3, 5-disubstituted 1, 2, 4-triazoles is attached to the nitrogen atom at position 1 or 2 which is closer to the more electron-releasing substituents in the 3 or 5 position. For instance, 3-p-nitrophenyl-, 3-p-chlorophenyl-, and 3-γ-pyridyl-5-methylthio-1, 2, 4-triazole exist predominantly in the 1H form, while 3-p-aminophenyl- and 3-p-methoxyphenyl-5-methylthio-1, 2, 4-triazole exist predominantly in the 2H form. These results are explained in terms of the formation of cyclic dimer-type hydrogen bonds involving the N-1 and N-2 atoms of triazole rings with an exchange of a proton between the molecules. However, 5-methylthio-3-α-pyridyl-1, 2, 4-triazole is exceptional in existing in the 2H form, since this compound can form hydrogen bonds of another type involving the nitrogen atom of the α-pyridyl group.View full abstractDownload PDF (1287K) -
AKIRA OHARA, SADAKI FUJIMOTO, HARUO KANAZAWA, TSUTOMU NAKAGAWA1975 Volume 23 Issue 5 Pages 967-970
Published: May 25, 1975
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESS1) The present research has been planed to demonstrate the importance of histidine residues on enzyme activity of papain by means of photooxidation. 2) Papain was rapidly inactivated by methylene blue-sensitized photooxidation. 3) The rate of photo-sensitized inactivation was pH dependent, and about one histidine residue per molecule of papain was lost when complete inactivation took place. 4) Mercuripapain was not inactivated by methylene blue-sensitized photooxidation, and the histidine residue was not affected in the illuminated mercuripapain. 5) These results indicate that the modification of a histidine residue by photooxidation cause loss of the enzyme activity for hydrolysis of benzoyl-L-arginine amide. 6) The state of the histidine residue in the active site of papain is discussed to explain the results of the photooxidation studies described here.View full abstractDownload PDF (482K) -
HIDEAKI NAGASE, YOSHIO HOJIMA, CHIAKI MORIWAKI, HIROSHI MORIYA1975 Volume 23 Issue 5 Pages 971-979
Published: May 25, 1975
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe potent anti-bradykinin activity was found in the beet root ; 4-7 μg of bradykinin was antagonized by the crude beet juice equivalent to 1 g of the root in the assay of contraction of the guinea-pig ileum. This substance was quite stable under heat treatment at 100° for 30 min, and its molecular weight seemed to be around 1000. The bradykinin antagonist was purified as follows : the grated beet roots were lyophilized and then extracted with boiling 99% ethyl alcohol. After removal of the alcohol, the residue was dissolved in water and treated with ether. The aqueous layer was concentrated and applied to a Sephadex G-15 column and a Bio-Gel P-2 column successively. The active fraction obtained by these procedures was developed as a single spot on a silica gel thin-layer chromatogram. The inhibitory effects of this substance were observed on the smooth muscle contraction of guinea-pig, the vasodilatation in dog and the increase in the capillary permeability in rat, all of which were induced by bradykinin. The carrageenin-induced edema in the rat's paw and some of the above biological responses by histamine and 5-hydroxytryptamine were also suppressed distinctly or slightly by the beet antagonist.View full abstractDownload PDF (1000K) -
HIROMU MORI, RIKIO OHUCHI1975 Volume 23 Issue 5 Pages 980-986
Published: May 25, 1975
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe reaction of 1-en-3-oxo A/B trans steroid with vinylmagnesium bromide in the presence of cupric acetate afforded 1α-vinyl-3-oxo steroid. The configuration of the vinyl group introduced by the reaction was found to be α-oriented by the transformation of II into the lactone (VIII). The stereochemistry of the reduction of 1α-alkyl-3-oxo steroids and 5β-alkyl-3-oxo steroids with complex metal hydride was also studied.View full abstractDownload PDF (832K) -
TSUGUTAKA ITO, MASANAO SHIMIZU1975 Volume 23 Issue 5 Pages 987-992
Published: May 25, 1975
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSEffect of antidepressants on the locomotor activity in paired young chicks was examined in comparison with that of other psychotropic drugs. Tricyclic antidepressants, imipramine, chlorimipramine, amitriptyline and nortriptyline caused an increase in locomotor activity together with hyperactivity. PF-82 and cocaine, uptake inhibitors, also caused a similar increase of the locomotor activity and behavioral changes to those of tricyclic antidepressants. On the other hand, behavioral effects of pargyline, iproniazid, methamphetamine, diazepam and chlordiazepoxide were different from those of tricyclic antidepressants. Chlorpromazine increased the locomotor activity in a manner similar to that of imipramine. Phentolamine, α-adrenergic blocking agent, however, caused little or no effects on the locomotor activity and behavioral changes. The locomotor activity increased by imipramine or chlorpromazine was inhibited by phentolamine. These results suggest an involvement of the uptake inhibition of central adrenergic neurones in connection with the increase in chick locomotor activity.View full abstractDownload PDF (762K) -
TOZO FUJII, SHIGEYUKI YOSHIFUJI, KIYOSHI YOSHIDA, MASASHI OHBA, SHIRO ...1975 Volume 23 Issue 5 Pages 993-1002
Published: May 25, 1975
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe alkaline ferricyanide oxidation of the quaternary pyridinium salts (Ia-g) furnished pairs of the isomeric 2-pyridones (IIa-g) and 6-pyridones (IIIa-g) in good total yields. In all cases, the oxidation at the 2-position was much favored over that at the 6-position. The effect of the aryl group in the N-aralkyl chain on the orientation of the oxidation seemed to be negligibly small regardless of the number of the methylene groups separating the aryl group from the nitrogen. The extent of the 6-oxidation was slightly increased as the alkyl group at the 3-position was changed from the methyl to the ethyl group. The nuclear magnetic resonance spectra of these pyridones were measured in deuteriochloroform, carbon tetrachloride, and benzene-d6. On the basis of the results summarized in Tables III-VI, the effects of the aryl group and the number of the methylene groups in the N-substituent on the chemical shifts for the pyridone-ring and neighboring group protons are discussed.View full abstractDownload PDF (1044K) -
YOSHIHARU MACHIDA, TSUNEJI NAGAI1975 Volume 23 Issue 5 Pages 1003-1008
Published: May 25, 1975
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSIntending to explore useful ointment bases containing hydroxypropyl cellulose (HPC), an investigation was made on the spreadability, washing-out time and drug release of combined mixtures of HPC with aqueous glycerine (Aq. G1), propylene glycol (PG) and polyethylene glycol (PEG). The decrease of the spreadability due to the increase of concentration of HPC was remarkable in the low concentration, declining above 10% (w/v) in HPC/PG and above 14% (w/v) in HPC/PEG. HPC/PEG containing above 12% (w/v) lost the fluidity to take a gel-like state and this gel-like mixture indicated a typical thixotropic phenomenon. The washing-out time increased with the concentration of HPC, and it seemed to be related to the increase of viscosity. With the addition of 30% of zinc oxide as an insoluble drug, the decrease of spreadability was 23% at the largest, which was observed for HPC/Aq. G1. The spread radius at 2 min on the measurement for the sample of HPC/PEG (10 : 100, w/v) after heating at 150° for 1 hr was 54% larger than that of the intact one, indicating the structure relating to the thixotropy of the mixture might be crushed by heating. The drug release from each mixture decreased with the increase of concentration of HPC. HPC/PEG showed the fastest drug release at the given spreadability below 4.1 cm. As a result, it was shown that HPC would provide a promising material as bases for ointments and other semisolid preparations combining properly with Aq. G1, PG and PEG.View full abstractDownload PDF (756K) -
KOTAKA SAKAKIBARA, YASUO SHIBATA, TOKUHIKO HIGASHI, SYUICHI SANADA, JU ...1975 Volume 23 Issue 5 Pages 1009-1016
Published: May 25, 1975
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe in vivo effect on cholesterol metabolism of ginsenoside-Rb1, -Rc, -Rd, -Re, and -Rg1 purified from Ginseng (the root of Panax ginseng C.A. MEYER) was investigated. Four hours after the intraperitoneal injection of 5 mg of each pure ginsenoside into rats, the concentrations of serum and liver cholesterol and the incorporation of 14C-acetate into serum and liver cholesterol were determined. The results indicated the enhancement of cholesterol biosynthesis by administered saponins, particularly by ginsenoside-Rb1, a predominant component of Ginseng saponins.View full abstractDownload PDF (718K) -
CHITOSHI HATANAKA, OSAMU NISHIMURA, MASAHIKO FUJINO1975 Volume 23 Issue 5 Pages 1017-1024
Published: May 25, 1975
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA tetracosapeptide (α1-24-ACTH) corresponding to the first 24-amino acid sequence of corticotropin (ACTH) was synthesized by a classical method. The ester exchange method using pentachlorophenyl trichloroacetate (TCAOPCP) was employed successfully for condensation of the main fragments having C-terminal glycine and proline. All protecting groups of the tetracosapeptide were removed using the hydrogen fluoride method. The synthetic peptide thus obtained exhibited an activity of ca. 90 units/mg in in vivo steroidogenic assay.View full abstractDownload PDF (1175K) -
MIKIHIKO KONDA, TAKAYUKI SHIOIRI, SHUNICHI YAMADA1975 Volume 23 Issue 5 Pages 1025-1031
Published: May 25, 1975
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe asymmetric synthesis of a representative benzylisoquinoline alkaloid, (S)-(+)-laudanosine (III) was accomplished by means of the biogenetic-type, asymmetric Pictet-Spengler reaction of L-3-(3, 4-dihydroxyphenyl) alanine methyl ester hydrochloride (IV) with sodium (3, 4-dimethoxyphenyl) glycidate (V) (1, 3-asymmetric induction) and the elimination of the chiral center derived from IV (1, 3-transfer of asymmetry). The latter was conveniently achieved by conversion of the cyclized α-amino acid methyl ester (VIa) to the N-benzyl α-amino nitrile (XIII), followed by reductive decyanization with sodium borohydride.View full abstractDownload PDF (884K) -
SADAO UCHIYAMA, ZENZO TAMURA1975 Volume 23 Issue 5 Pages 1032-1038
Published: May 25, 1975
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe reaction mechanism of the fluorometric determination of dulcin with sodium nitrite was studied and estimated as follows : Dulcin produces 4-ethoxybenzenediazonium (4EBD) ion via. p-phenetidine by the action of nitrous acid. The ion itself decomposes in part to the substances possessing the active methylene neighbouring to a carbony group. Finally, 4EBD ion reacts with the active methylene in the presence of an alkaline solution containing nitrous oxide to form the essential fluorescent compound, 1, 3-bis (4-ethoxyphenyl)-5-tetrazolone.View full abstractDownload PDF (728K) -
YOHMEI OKUNO, OSAMU YONEMITSU1975 Volume 23 Issue 5 Pages 1039-1044
Published: May 25, 1975
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSPhotocyclization of N-chloroacetyl-3-methoxyphenethylamine (I) in water gave 7- and 9-methoxy-1, 2, 4, 5-tetrahydro-3H-3-benzazepin-2-ones (V and VI), whereas in organic solvents the main products changed to N-acetyl-3-methoxyphenethylamine (XVII) and 2-oxa-6-azabicyclo [7, 3, 1] trideca-1 (13), 9, 11-trien-5-one (XIII). Quantum yield for the formation of V and VI is clearly dependent on the polarity of solvent indicating that the formation of V and VI involves an ionic process. In organic solvents, viscous media favor the formation of XIII. Viscosity dependence in some alcohols is probably an indication of a novel cage reaction operative in the formation of the lactam XIII.View full abstractDownload PDF (677K) -
SEIJIRO HONMA, AKIRA KAMBEKAWA1975 Volume 23 Issue 5 Pages 1045-1056
Published: May 25, 1975
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe metabolic fate of D-32, which is a new adrenergic β-blocking agent, has been investigated with rabbit, rat and monkey. Eleven unconjugated metabolites and four conjugated metabolites were separated from urine after oral administration of D-32. The structure of these metabolites were deduced from physico-chemical data and definitely characterized by direct comparison with the authentic samples (see Chart 1). The biochemical significance of the transformation observed and the pharmacological activity of metabolites have been discussed.View full abstractDownload PDF (1398K) -
KIYOSHI ZAITSU, YOSUKE OHKURA1975 Volume 23 Issue 5 Pages 1057-1062
Published: May 25, 1975
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSFluorescent compounds, I and II, were obtained from the ethanolic and sulfuric acid reaction mixtures of benzaldehyde and of cinnamaldehyde with 1, 2-diaminonaphthalene monosulfate, respectively, and proved to be identical fluorescent compounds with those produced under the conditions of the method of aldehyde determination. I and II were characterized as 2-substituted naphth [1, 2-d] imidazole derivatives shown in Chart 1 and 2. From the sulfuric acid reaction mixture of pyruvic acid, fluorescent compounds, III and IV, were separated. III was determined as a benzoquinoxalinone derivative shown in Chart 3 and found not to be fluorescent compound produced under the conditions of the method. IV was main fluorescent compound produced from pyruvic acid under the conditions of the method though its structure could not be elucidated. The thin-layer chromatographic and fluorescence spectral data indicated that IV was identical with a fluorescent compound derived from acetaldehyde under the conditions of the method.View full abstractDownload PDF (880K) -
MIKIHIKO KONDA, TAKAYUKI SHIOIRI, SHUNICHI YAMADA1975 Volume 23 Issue 5 Pages 1063-1076
Published: May 25, 1975
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe asymmetric synthesis of (S)-reticuline (I) was accomplished by means of the biogenetic-type, asymmetric Pictet-Spengler reaction of 3-(3-hydroxy-4-benzyloxyphenyl)-L-alanine methyl ester hydrochloride (XXIII) with sodium 3-benzyloxy-4-methoxy-phenylglycidate (XXIV) (1, 3-asymmetric induction) and the elimination of the chiral center derived from XXIII (1, 3-transfer of asymmetry), the latter of which was achieved by conversion of the cyclized α-amino acid methyl ester (XXVa) to the N-benzyl α-amino nitrile (XXVIII), followed by reductive decyanization with sodium borohydride. The position of the benzyl group of XXIII which was prepared from L-dopa by monobenzylation was proved by the alternate synthesis of XXIII starting from L-tyrosine. By this success, morphinanedienone, aporphine and protoberberine alkaloids, (-)-pallidine (XXXII), (+)-isoboldine (XXXIII), (-)-coreximine (XXXIV), and (-)-scoulerine (XXXV) are formally to have been synthesized from L-dopa.View full abstractDownload PDF (1609K) -
NOBUO MOCHIZUKI, SHOJI OKADA, OSAMU TAMEMASA1975 Volume 23 Issue 5 Pages 1077-1084
Published: May 25, 1975
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSAs a part of the biological investigations on deoxyribonucleic acid (DNA)-interacting aminoquinones, the interaction of 2-hydroxyamino-1, 4-naphthoquinone (HANQ) with nucleic acids and its biological actions were studied. 1. Spectroscopic determinations indicated that HANQ interacted with DNA without effect by Mg2+. The interaction sites in DNA was estimated to be the purine bases from the difference spectra with nucleic acid derivatives. 2. HANQ inhibited thymidine incorporation into DNA in Ehrlich ascites carcinoma, rather than in E. coli cells, to a higher extent than mitomycin C. The precursor incorporation into RNA and proteins in the carcinoma was less inhibited ; the inhibition resulted possibly from a secondary action of HANQ. 3. An antitumor effect of HANQ was observed on Ehrlich ascites carcinoma, ascites sarcoma-180, and L-1210 leukemia at doses less than half of the LD50 (mouse, i.p., 318 mg/kg). 4. The biological actions of HANQ was discussed in analogy to 4-hydroxyamino-quinoline-1-oxide (4HAQO), a proximate carcinogen of 4-nitroquinoline-1-oxide (4NQO).View full abstractDownload PDF (831K) -
YIE W. CHIEN, HOWARD J. LAMBERT1975 Volume 23 Issue 5 Pages 1085-1090
Published: May 25, 1975
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe aqueous solubility of steroids was exponentially increased following the addition of a co-solvent. A theoretical equation was derived to describe the relationship between the amount of drug solubilized and the volume fraction of co-solvent incorporated. Both single and multiple co-solvent systems followed the derived relationship.View full abstractDownload PDF (639K) -
JONG YOON KIM, HARUHIKO YAMAMOTO, TAKAO KWAN1975 Volume 23 Issue 5 Pages 1091-1097
Published: May 25, 1975
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSMethylation of 1, 4-quinones by methylcobalt complexes has been studied in the presence or absence of some metal salts. Methylcobaloximes were found to afford monomethylated quinones though the yield was very small in the absence of metal salts. The transmethylation was, however, remarkably promoted in the presence of transition metal salt such as Pd (II) and reached nearly 70% at the highest. Methylcobalamins were also found to methylate 1, 4-quinones to a slight extent but no promoting effect was recognized with Pd (II) probably due to complexing side reactions. Nevertheless, the observations may indicate that methylcobalt complexes act as methylating reagents not only for mercuric salts but also for organic compound such as 1, 4-quinones. Reaction mechanisms are briefly discussed.View full abstractDownload PDF (775K) -
SHINZO KANO, TSUTOMU YOKOMATSU, SHIROSHI SHIBUYA1975 Volume 23 Issue 5 Pages 1098-1102
Published: May 25, 1975
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe reaction of a series of 1-halogenophenethyl-3, 4-dihydroisoquinolines (6), (10), (14) and (20) with sodium methylsulfinylmethanide was investigated to yield 5, 6, 12, 13, 13a-pentahydro-13a-(methylsulfinyl) methyldibenzo [a, f] quinolizines (7), (12), (18) and (23) which were converted to the corresponding 13a-(methylthio) methyl derivatives (8), (13), (17) and (24), respectively. Desulfurization of 8 and 24 afforded the 13a-methyl derivatives (9) and (25), respectively.View full abstractDownload PDF (702K) -
KUNIO HIROI, SHUNICHI YAMADA1975 Volume 23 Issue 5 Pages 1103-1109
Published: May 25, 1975
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSWe attempted the asymmetric synthesis of key compounds for optically active diterpenes and obtained some optically active key compounds (Ib, c). The effects of solvents and reaction temperatures were examined and the results are discussed.View full abstractDownload PDF (796K) -
KOJIRO MATSUMOTO, TOSHIO IMANARI, ZENZO TAMURA1975 Volume 23 Issue 5 Pages 1110-1113
Published: May 25, 1975
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSArginine-esterase activities of trypsin, plasmin and kallikreins were assayed by high performance liquid chromatography (HPLC) with BAEE (or TAME) and DAME. 1. In the case of conventional method with BAEE (or TAME), only the hydrolyzed product of BA (or TA) was eluted from the column of "Zipax" SCX (20 cm×2.0 mm i.d.) with 0.1M phosphate buffer (pH 7.0), while BAEE (or TAME) was retained on the column. 10-3-10-2 TAME units of these enzymes were easily measurable by determination of eluted product at several minutes intervals. 2. Using DAME as a fluorescent substrate, separation of DA from DAME was performed on the column of Hitachi gel #3010 (15 cm×2.0 mm i.d.) by elution of 20% (v/v) Tris-HCl buffer (0.05M, pH 8.5) in methanol. In this condition, 4 pmole of DA was determined and 10-5-10-4 TAME units of these enzymes were measurable.View full abstractDownload PDF (516K) -
MORIO IKEHARA, YUKO OGISO1975 Volume 23 Issue 5 Pages 1114-1119
Published: May 25, 1975
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESS8.2-Anhydro-9-β-D-arabinofuranosyladenine (I) was converted to 5'-tosyl derivative (II) in a yield of 75%. When Compound (II) was heated with sodium hydrogen sulfide in dimethylformamide (DMF) 8, 5'-S-cyclonucleoside having arabinosyl configuration (IV) was obtained in a yield of 46%. From the ditosyl derivative (III) analogously a cyclonucleoside having 3'-tosyl group (VII) was obtained. 8, 3'-Anhydro-9-β-D-xylofuranosyladenine (VIII) was converted to 5'-tosyl derivative (IX) and heated with sodium hydrogensulfide in DMF. In addition to a 8, 5-S-cyclonucleoside of xylofuranosyl configuration (X), two compounds, 8, 3'-anhydro-8-oxy-9-(5'-deoxy-5'-mercapto-β-D-xylofuranosyl) adenine disulfide (XI) and 5'-deoxy-5'-mercapto-8-oxy-9-β-D-xylofuranosyladenine (XII) was obtained. Compound (XII) was also obtained from X by the treatment with 0.01N sodium hydroxide. Thus, the OH group of xylo configuration in the sugar moiety of 8, 5'-S-cyclonucleoside was found to be able to cleave the S-hydro linkage even in a mild condition.View full abstractDownload PDF (679K) -
YOSHIO HOJIMA, YOSHIFUMI MATSUDA, CHIAKI MORIWAKI, HIROSHI MORIYA1975 Volume 23 Issue 5 Pages 1120-1127
Published: May 25, 1975
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThree preparations of hog pancreatic kallikrein (Hog Panc. K.) were applied to Ampholine isoelectric focusing. Each of them were separated into 5-6 kallikrein components with slightly different pI's in the range of pH 3.7-4.2. The migration distances of these components in disc electrophoresis (pH 8.9, 7% polyacrylamide gel) were not distinguishable. Relating to these results, it was suggested that isoelectric focusing or gel isoelectrofocusing would be preferable to disc electrophoresis for the examination of the real homogeneity of Hog Panc. K. and other glandular kallikreins. It was found by isoelectric focusing that human urinary kallikrein consisted of 3-5 components with pI 3.8-4.3. On the other hand, human salivary kallikrein seemed to be composed of one component with pI 4.2.View full abstractDownload PDF (1062K) -
YOSHIO HOJIMA, CHIAKI MORIWAKI, HIROSHI MORIYA1975 Volume 23 Issue 5 Pages 1128-1136
Published: May 25, 1975
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSDog, rat and hog pancreatic kallikreins were efficiently purified to homogeneous forms by combining preparative disc electrophoresis with acetone fractionation and Sephadex gel filtration. The recoveries of these kallikreins through the whole purification procedures were in the range of 20-45% in vasodilator and Na-benzoyl-L-arginine ethyl ester (BAEE) assays. The purified kallikreins appeared to be homogeneous in analytical disc electrophoresis ; however, isoelectric focusing made it clear that they consisted of several kallikrein multiple forms with slightly different isoelectric points (pI's). The pI's of these kallikreins'multiple forms wer 4.2-4.5 (dog), 4.1 (rat), and 3.6-4.2 (hog). Dog pancreatic kallikrein was not inhibited by Trasylol, but were inhibited considerably by two kallikrein inhibitors from potatoes. Although rat kallikrein has been reported not to be inhibited by Trasylol, our purified one was strongly inhibited. Trypsin inhibitors from soybean etc. hardly inhibited both kallikreins.View full abstractDownload PDF (1082K) -
KUK HYUN SHIN, HIDEO NAKAGAWA, SUSUMU TSURUFUJI1975 Volume 23 Issue 5 Pages 1137-1141
Published: May 25, 1975
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSGlucocorticoid therapy induces rapid involution of chronic granulomatous inflammation which has been provoked by injecting carrageenin solution subcutaneously in rats. Cortisol acetate injected into the granuloma pouch at a dose of 3 mg/kg/day for 3 days caused a marked involution of the granulomatous inflammation. After withdrawal of the steroid treatments, however, rebound of the inflammation took place resulting in a rapid recovery not only in the wet weight and the dry weight of the granuloma but also in vascular permeability response and the volume of the exudate. Determination of vascular permeability of the granulomatous tissue were performed with the aid of radioiodinated human serum albumin which was injected intravenously 30 min before sacrifice. Vascular permeability was expressed in terms of radioactivity exuding into the granuloma pouch fluid for the 30 min. By repeated administrations at 12 hr intervals with hydroxyurea (250 mg/kg×6, injected into the granuloma pouch) after the withdrawal of the steroid treatments, rebound of the inflammation not only in proliferative phases but also in exudative phases was suppressed almost completely.View full abstractDownload PDF (610K) -
YOSHIO ARATA, MIYOJI HANAOKA, SIN KYU KIM1975 Volume 23 Issue 5 Pages 1142-1145
Published: May 25, 1975
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSOn quaternization of 10-ethyl-, 10-vinyl-, and 10-ethynyl-quinolizidine with methyl iodide, the formation of the cis methiodide vs. the corresponding trans methiodide increased according to the order of the bulkiness of the 10-substituent as CH3CH2>CH2=CH>CH=C. The stereochemistry of the above methiodides was established. The N+-methyl signals of the cis 10-substituted quinolizidine methiodides were confirmed to appear at higher field than those of the corresponding trans methiodides except for the 10-ethynyl methiodides in their nuclear magnetic resonance spectra.View full abstractDownload PDF (567K) -
MINEO SANEYOSHI1975 Volume 23 Issue 5 Pages 1146-1151
Published: May 25, 1975
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThiation of the 2', 5'-di-O-trityl-3'-O-acetyluridine or 3', 5'-di-O-trityl-2'-O-acetyluridine with phosphorus pentasulfide in refluxing toluene containing 20-30% pyridine afforded corresponding"4-thio"derivative in good yield. These "4-thio" derivatives were converted to the cytidine counterparts by the reaction with methanolic ammonia. 2', 5'-Di-O-trityl-3'-O-methanesulfonyluridine was also converted to cytidine derivative by similar manner. In addition, phosphorylation and dinucleoside monophosphate synthesis using titled compounds were described.View full abstractDownload PDF (773K) -
TAKAFUMI ITAMI, KENJI FUKUZAWA, MASUMI TAKAHASHI, HIROAKI TSUKATANI1975 Volume 23 Issue 5 Pages 1152-1155
Published: May 25, 1975
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA simple and sensitive method is described for separatory determination of prostaglandin E and prostaglandin F. This method is based on three principles : (1) Prostaglandin E and prostaglandin F are oxidized by prostaglandin dehydrogenase, resulting reduced nicotinamide-adenine dinucleotide (NADH). (2) The sensitive determination of reduced NAD is performed by enzymic cycling with resazurin which serves as the terminal electron acceptor. (3) Alkaline treatment converts only prostaglandin E to insensitive material to prostaglandin dehydrogenase. This method was capable for separatory determination of prostaglandin E and prostaglandin F in the order of 10-11 mole.View full abstractDownload PDF (533K) -
TAKUSHI KURIHARA, HIROYUKI SANO, HIROSHI HIRANO1975 Volume 23 Issue 5 Pages 1155-1157
Published: May 25, 1975
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSReductions of o-nitrobenzylideneacetylacetone analogues (I, II and III) by means of stannous chloride in hydrochloric acid or catalytic hydrogenation of 5% palladium carbon as catalyst gave the mixture of 3-acylquinaldines and these N-oxides, analysed by gas chromatographies.View full abstractDownload PDF (455K) -
TOSHIHIRO NOHARA, FUMIO KUMAMOTO, KAZUMOTO MIYAHARA, TOSHIO KAWASAKI1975 Volume 23 Issue 5 Pages 1158-1160
Published: May 25, 1975
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSIn contrast to the dried rhizomes of Paris polyphylla SM., the dried aerial parts of Paris tetrphylla A. GRAY contained predominantly pennogenin rhamnosyl-chacotrioside (I). From the methanol extracts of fresh underground parts of Trillium tschonoskii MAXIM., dioscin (III) and methyl proto-dioscin (IV) were isolated and any pennogenin glycosides and the related compounds, which were found in Trillium kamtschaticum, could not be obtained. The ratio of yields of III to IV from the dried materials was reverse to that from the fresh ones, and the homogenate of the fresh materials was extracted only to give III. The results may support the claim that III is considered to be a secondary glycoside.View full abstractDownload PDF (445K) -
TSUNEMATSU TAKEMOTO, MASAAKI UCHIDA, KAZUHIRO KOIKE, YUKO HOSHINA, GEN ...1975 Volume 23 Issue 5 Pages 1161-1163
Published: May 25, 1975
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSTwo kinds of new amides were isolated from Chloranthus serratus and characterized as N-β-phenethyl-3-(3, 4-methylenedioxyphenyl) propenamide (I) and N-β-phenethyl-3-(3, 4-dimethoxyphenyl) propenamide (II). Isofraxidin (III) was identified as a constituent of C. japonicus.View full abstractDownload PDF (492K) -
HARUAKI YAJIMA, YOSHIAKI KISO, HIROSHI OGAWA, NOBUTAKA FUJII, HIROSHI ...1975 Volume 23 Issue 5 Pages 1164-1166
Published: May 25, 1975
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSAcidolytic cleavage of various protecting groups currently employed in peptide chemistry by fluorosulphonic and methanesulphonic acids was examined.View full abstractDownload PDF (468K) -
TOSHIO KINOSHITA, FUMIO IINUMA, KAZUYO ATSUMI, YAYOI KANADA, AKIO TSUJ ...1975 Volume 23 Issue 5 Pages 1166-1168
Published: May 25, 1975
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSCycloheptaamylose (C7A) was found to greatly enhance and stabilize the fluorescence intensity of dansyl (DNS) amino acids on silicagel layer and this finding was applied to the detection and determination of these compounds on thin-layer chromatogram. Procedure : After the development of DNS-amino acids, the thin-layer plate is sprayed with 10 ml of 1.8% C7A, dried over phosphorus pentoxide and the spots are detected under a mercury lamp or determined using a scanning fluorometer. Above 10 fold increase in the fluorescence was observed. The fluorescence was stable for 90 min under exposure to air in the diffused light and for 24 hr over phosphorus pentoxide under reduced pressure. Limits of detection for 24 DNS-amino acids were in the range of 0.1 to 0.5 pmole/spot. Standard curves for DNS-amino acids were linear in the ranges of 5 to 30 pmole. Samples from 1 to 5 pmole could also be determined semiquantitatively.View full abstractDownload PDF (472K) -
HIDEO YAMAGUCHI, ATSUSHI NUMATA, EIICHI UEMURA, HIROSHI KANETO, AKIRA ...1975 Volume 23 Issue 5 Pages 1169-1170
Published: May 25, 1975
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe phenolic hydroxyl and ortho proton resonances in 1H NMR spectrum showed the downfield shifts on addition of alkaline earth salts to phenols in (CD3)2SO. Among alkaline earth salts, anhydrous magnesium chloride caused the strongest downfield shifts, both for the hydroxyl and phenolic ortho protons. The selective shifts of phenolic ortho proton resonances due to anhydrous magnesium chloride promise to be generally useful in aiding the structure elucidation of natural phenols.View full abstractDownload PDF (332K) -
SHINZO KANO, TSUTOMU YOKOMATSU, EIJI KOMIYAMA, SATORU TOKITA, YOUKO TA ...1975 Volume 23 Issue 5 Pages 1171-1172
Published: May 25, 1975
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe Stevens rearrangement of the N-methyltetrahydroprotoberberinium iodide (3) in the presence of sodium methylsulfinylmethanide afforded the ochotensine type 1-spiroisoquinoline (4), the structure of which was determined by the chemical and spectroscopic methods.View full abstractDownload PDF (315K)
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