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Volume 25, Issue 8
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SEIJIRO HONMA, YOSHIHIRO KAWABE, AKIRA KAMBEGAWA1977 Volume 25 Issue 8 Pages 1843-1850
Published: August 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe mass spectra of 1-alkylamino-3-aryloxy-2-propanol exhibited prominent losses of the elements of acetaldehyde from the molecular ion. The ion showed an unexpected rearrangement of alkylamino group from 1-alkylaminopropane to aryl group with the formation of six-membered transition state. The new McLafferty-type rearrangement in these compounds was not shown in the replacement of the element of nitrogen by sulfur and oxygen on alkylamino group and also in addition of methylene group to alkylamino group to form alkylaminobutane. The mechanism of the rearrangement was discussed in detail.View full abstractDownload PDF (832K) -
YUKIO ISHIDA, KOUZO WATANABE, SHIGERU KOBAYASHI, MASARU KIHARA1977 Volume 25 Issue 8 Pages 1851-1855
Published: August 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSApogalanthamine analogs were synthesized, and their α-adrenolytic and anti-5-HT activities and those of related compounds on rat aortic strips were compared with those of well known antagonists. It was found that N-alkylated 5, 6, 7, 8-tetrahydrodibenz [c, e]-azocines (I-III) and N-alkylated 10, 11-methylenedioxy-5, 6, 7, 8-tetrahydrodibenz [c, e]-azocines (V-VII) had reversible α-adrenolytic activities ; their activities were as great as those of phentolamine and benzylimidazoline. Of the compounds tested, DA-VIII-Me (II) had the strongest α-adrenolytic activity (pA2=8.76±0.07) / its activity was more than that of phentolamine.View full abstractDownload PDF (586K) -
MITSUJI YANAI, SHIGEKO TAKEDA, MAKOTO NISHIKAWA1977 Volume 25 Issue 8 Pages 1856-1861
Published: August 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSPyridazine derivatives (I, III, V, VII, IX, XI, XIII, XV, XVII, and XIX) were treated with nitromethane and nitroethane in the presence of a basic catalyst to give the corresponding 5-methyl (IIa, IVa, VIa, VIIIa, Xa, XIIa, XIVa, XVIa, XVIIIa, and XXa) and 5-ethyl derivatives (IVb, VIb, VIIIb, Xb, XIIb, XIVb, XVIb, and XVIIIb). Namely, in these reactions nuclear alkylation occurred instead of nitroalkylation.View full abstractDownload PDF (638K) -
TAKUO OKUDA, TAKASHI YOSHIDA, HIDEKAZU NAYESHIRO1977 Volume 25 Issue 8 Pages 1862-1869
Published: August 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe main tannin of Geranium thunbergii has been isolated as yellow crystals, and named geraniin. Geraniin gave upon hydrolysis in boiling water, gallic acid, hexahydroxydiphenic acid, ellagic acid, and corilagin, and is shown by the proton nuclear magnetic resonance spectra to be a corilagin derivative esterified at O-2 and O-4 of D-glucopyranose in the molecule. Upon condensation with o-phenylenediamine, geraniin yielded a phenazine derivative, named phenazine A (X), which was transformed into phenazine B (XI) upon prolonged reaction. These two phenazine derivatives gave phenazine C (XII) by further prolonged reaction, or by hydrolysis of X or XI in boiling water. Corilagin was also isolated from the hydrolysis products mixture. The structure of phenazine C was proved by identification of its hydrolyzed product XV with synthetic specimen which was prepared via hydrogenolysis of dimethyl dimethoxytetrabenzyloxydiphenoate. These data along with the PMR spectra show that the structure of geraniin to be I. The carbon nuclear magnetic resonance spectra of geraniin indicate partial hydration to form geminal diol at the cyclohexenetrione moiety.View full abstractDownload PDF (918K) -
MIYOKO KIUCHI, HISATORA KURODA1977 Volume 25 Issue 8 Pages 1870-1876
Published: August 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe conidia of Cochliobolus miyabeanus were extracted repeatedly with CHCl3-MeOH mixture (2 : 1) and the contents of their lipids, fatty acid composition of these lipids, and the changes of the fatty acid content with advance of germinating processes in conidia were examined. The results of these examinations were as follows. (1) Total lipid compositions : The extractable lipid and bound lipid contents were 6.3-7.5% and 0.3-1.2% of conidial weight, respectively, and the extractable lipid was composed of 1.54-2.85% triglyceride, 0.12-0.36% diglyceride, 0.22-0.66% monoglyceride, 0.72-1.17% free fatty acid, 0.09-0.10% steroid ester, 1.08-2.49% steroid, and 0.99-1.24% phospholipid of conidial weight. (2) Fatty acid composition : The pattern of fatty acid composition in each fraction of the extractable lipids was almost identical and C16 : 0, C18 : 0, C18 : 1, C18 : 2, and C18 : 3 fatty acids were found in each fraction as dominant constituent. These 5 kinds of fatty acids constituted 85% of total conidial lipids. (3) Changes in fatty acid composition during the germination processes : Although a slight change in fatty acid compositions was found in each lipid fraction during all stages of conidial germination, the content of C18 : 2 in the fraction of phospholipid was inclined to increase with the advancement of germinating process.View full abstractDownload PDF (731K) -
AKIRA TAKAMIZAWA, SAICHI MATSUMOTO, TSUYOSHI IWATA, ITSUO MAKINO1977 Volume 25 Issue 8 Pages 1877-1891
Published: August 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESS4-Hydroperoxyisophosphamide and its analogues were simply synthesized by ozonolysis reactions of O-(3-butenyl)-N, N'-bis (2-chloroethyl) phosphorodiamidate and related O-(3-butenyl) phosphoramidates. An acid-catalyzed isomerization of 4-hydroperoxyisophosphamide proceeded with inversion of its phosphorus configuration giving 2-epi-4-hydroperoxyisophosphamide. Both isomers readily afforded C4-substituted isophosphamide derivatives by reactions with nucleophilic agents and acid. L1210 antileukemic activities were tested for the isomers and some analogues revealing that the C4-hydroperoxylation of isophosphamide resulted in a marked enhancement of its activity and that the inverted stereochemistry of an alkylating functionality at the phosphorus atom is also effective in promoting the antitumor action as an alternative activated species of isophosphamide.View full abstractDownload PDF (1787K) -
MASAKATSU KANEKO, MISAKO KIMURA, BUNJI SHIMIZU, JUNICHI YANO, MORIO IK ...1977 Volume 25 Issue 8 Pages 1892-1898
Published: August 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESS9-(β-D-Arabinofuranosyl) adenine 5'-phosphate was obtained from adenosine 5'-phosphate via the novel intermediate 8, 2'-O-cycloadenosine 5'-phosphate. In contrast to the synthesis of 9-(β-D-arabinofuranosyl) adenine, it was difficult to cleave this compound by hydrogen sulfide directly to 8, 2'-O-cycloadenosine 5'-phosphate because of a considerable degree of dephosphorylation. However N-acylated 8, 2'-O-cycloadenosine 5'-phosphate was readily cleaved at the cyclo-bond by hydrogen sulfide. Desulfurization of 8-mercapto-9-(β-D-arabinofuranosyl) adenine 5'-phosphate gave the desired pure crystalline product.'View full abstractDownload PDF (830K) -
ATSUSHI SUGII, NAOTAKE OGAWA, TOSHIHIDE HIDA, HITOSHI IMAMURA1977 Volume 25 Issue 8 Pages 1899-1903
Published: August 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSExtraction and elution behavior of Zn (II), Cd (II) and Hg (II) was investigated by using dithizone-dibutyl phthalate solution retained on macroreticular type polymer beads such as styrene-divinylbenzene and ethylstyrene-divinylbenzene copolymers. The behavior of the metal ions was affected by the degree of cross-linking of polymers used as the support.View full abstractDownload PDF (583K) -
AKIRA MIWA, MASANORI YOSHIOKA, AKIRA SHIRAHATA, ZENZO TAMURA1977 Volume 25 Issue 8 Pages 1904-1910
Published: August 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA method for preparation of antigens of catecholamines and L-3, 4-dihydroxyphenylalanine as haptans was developed. These haptens were conjugated with carrier proteins by the Mannich reaction after N-maleylation of the haptens for protecting the amino groups of the side chain, then the maleyl groups were removed by acid hydrolysis under a mild condition. By immunization of rabbits with these conjugates antibodies were produced. In a cross-reactivity test by Ouchterlony's method the antibodies to each one of the conjugates selectively reacted with the conjugate of that hapten even if the carrier protein was bovine serum albumin or rabbit serum albumin. These results show that the present method for preparation of the conjugates is a desirable one.View full abstractDownload PDF (846K) -
YASUTAKA NAGAI, HITOSHI UNO, SUSUMU UMEMOTO1977 Volume 25 Issue 8 Pages 1911-1922
Published: August 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA series of 1-substituted-3-phenacylpiperidine derivatives (VI) and 1-substituted-3-(p-fluorophenacyl) pyrrolidine derivatives (XI) were synthesized for pharmacological testing. The conversion of 3-phenacyl-4-piperidone derivatives (XXII) into 4, 5, 6, 7-tetrahydrofuro (or-1H-pyrrolo) [3, 2-c] pyridine derivatives (XX, XXV), the rearrangement of the quaternary salts of these products (XXa, XXVb) with phenyllithium and the dimerization of the dehydration product of 1-benzyl-3-hydroxymethyl-4-piperidone (K) were also described. Among the compounds synthesized, 1-(p-fluorobenzoyl) propyl-3-(p-fluorophenacyl)-pyrrolidine (XId) showed remarkable central nervous system depressing activities.View full abstractDownload PDF (1252K) -
TAKAJI KOYAMA, TAKASHI HIROTA, CHIZUKO BASHOU, TETSUTO NANBA, SHINJI O ...1977 Volume 25 Issue 8 Pages 1923-1927
Published: August 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSReactions of pyridines and condensed pyridines having active methyl group with formamide were described. 2- or 4-methylpyridine (I, IV) gave 5-(2- or 4-pyridyl)-pyrimidine (II, V). 2- or 4-methylquinoline (VI, XI) gave 2- or 4-(5-pyrimidinyl)-quinoline (VII, XII) and 1-formyl-2-or 4-methyl-1, 2, 3, 4-tetrahydroquinoline (IX, XIII). 3, 5-Di (2-quinolyl) pyridine (VIII) and 2-(2-pyrazinyl) quinoline (X) were obtained from VI except for VII and IX. 3-Methylisoquinoline (XIV) gave 2-formyl-3-methyl-1, 2, 3, 4-tetrahydroisoquinoline (XV) and quinoline (XVI) gave 1, 2, 3, 4-tetrahydroquinoline (XVIII) and its N-formyl derivative (XVII). Purine (III) was confirmed on thin-layer chromatography in these reactions.View full abstractDownload PDF (600K) -
SEIICHI INAYAMA, TAMIKO OHKURA, YOICHI IITAKA1977 Volume 25 Issue 8 Pages 1928-1933
Published: August 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe molecular structure of spathulin (1a), a highly oxygenated pseudoguaianolide isolated from Gaillardia grandiflora has been established by a three dimensional X-ray crystallographic analysis of diacetylspathulin (1b). The space group of the crystal of 1b is P212121 and the dimensions of the cell with z=4 are a=9.6976 (3), b=26.968 (2), c=8.9288 (3) Å. The structure of the crystal was refined to R=0.05. The conformation of spathulin (1a) was estimated to be similar to that of pulchellin (2a), namely bis-deacetoxyspathulin except some differences particularly at C (6) and C (9), when the conformation of the pseudoguaianolide skeleton in 1b is compared with that in 11, 13-dibromopulchellin (2b).View full abstractDownload PDF (691K) -
KAZUO WATANABE, HIROSHI Y. WATANABE, YOSHIAKI GOTO, YOKO KARIYA1977 Volume 25 Issue 8 Pages 1934-1940
Published: August 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSAn improved method was described for the measurement of gastric acid secretion of isolated rat gastric mucosa. With this method, dose-dependent acid secretory responses were obtained to secretagogues such as histamine, bethanechol, tetragastrin and dibutyryl cyclic adenosine monophophate (AMP). However, the maximum response to tetragastrin was always smaller than that to the other secretagogues in this preparation. Inhibitory effects on acid secretion of some antisecretory agents were also examined. Antagonistic interactions of atropine against bethanechol, and of metiamide against histamine were clearly confirmed. On the other hand, inhibitions of metiamide on bethanechol and of atropine on tetragastrin or histamine were found rather weak in contrast to the results obtained with other methods. Strong stimulatory effect of theophylline and absence of the influence of dibutyryl cyclic GMP were shown in our preparation. The actions of miscellaneous agents including prostaglandin E1, imidazole and metabolic inhibitors were also described.View full abstractDownload PDF (774K) -
HIDEJI ITOKAWA, KOICHI TAKEYA, SUSUMU MIHASHI1977 Volume 25 Issue 8 Pages 1941-1946
Published: August 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSIn the suspension cultures using callus induced from Cannabis sativa L., geraniol, nerol, olivetol and ethyl olivetolate which are cannabinoid precursors were not biotransformed to cannabinoids. We found that primary and secondary allylic alcohols such as geraniol, nerol, trans-cinnamyl alcohol, isophorol and trans-verbenol were biotransformed to the corresponding aldehydes. On the other hand, acyclic secondary allylic alcohols such as α-ionol, β-ionol and 4-phenyl-3-buten-2-ol were not biotransformed. Further, we clarified that the enzyme which catalyzed the oxidation of allylic alcohols was an alcohol oxidase.View full abstractDownload PDF (734K) -
KOICHI TAKEYA, HIDEJI ITOKAWA1977 Volume 25 Issue 8 Pages 1947-1951
Published: August 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSIn the cell-free system of callus induced from Cannabis sativa L. (Moraceae), the pro-R hydrogen from C-1 methylene of primary allylic alcohols such as trans-cinnamyl alcohol and geraniol was abstracted. In an example of secondary allylic alcohols biotransformations, S-(-)-isophorol of the racemate was biotransformed to isophorone, and (+)-trans-verbenol of four isomers, such as (+)-and (-)-trans-verbenol, and (+)-and (-)-cis-verbenol, was preferentially biotransformed to (+)-verbenone. We reported previously that the enzyme which catalyzed the oxidation of these allylic alcohols in the cell-free system of Cannabis callus was an alcohol oxidase.View full abstractDownload PDF (597K) -
SHOJI OZEKI, KIKUO TEJIMA1977 Volume 25 Issue 8 Pages 1952-1958
Published: August 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSBinding to and displacement from bovine serum albumin of five barbiturates, barbital, phenobarbital, pentobarbital, secobarbital, and thiopental, were investigated by the dynamic dialysis method. The analysis of Scatchard plots indicated that there are marked differences in binding affinity and a parallelism in the relationship between chemical structure and their affinity. Furthermore, when these drugs are arranged in the order of their affinity for albumin molecule, there is a close correlation with pharmacological properties. Thus, the more highly protein-binding compounds are short-acting compounds with a rapid onset of action. They tend to be more rapidly degraded metabolically and are more potent hypnotics. For the study of competitive inhibition on the binding between barbiturate and albumin, thiopental was used as the test drug, and chlorpropamide and lauric acid as the competitors. Substantial inhibition of binding of thiopental to albnmin was found in both competitors with molar concentration of 0.7-1.0 times that of thiopental, at a ratio of 7 mol thiopental/mol of albumin. These results indicate that the competitive effect of lauric acid to inhibit the binding of thiopental to serum albumin appears to be greater than that of chlorproamide.View full abstractDownload PDF (809K) -
KIYOMI KIKUGAWA, HIDEO SUEHIRO, RYOBUN YANASE, AKIJI AOKI1977 Volume 25 Issue 8 Pages 1959-1969
Published: August 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA facile synthesis of 2-thioadenosine (IX) and its derivatives from adenosine (I) was described. Treatment of 5-amino-1-β-D-ribofuranosylimidazole-4-carboxamide O-benzyloxime (IV), obtained via 3 steps from I, with CS2-MeOH-pyridine at room temperature gave N1-benzyloxy-2-thioadenosine (VII) which was readily transformed into 2-benzylthioadenosine N-oxide (VIII) by heating. Treatment of IV with CS2-MeOH-NaOH at 180°in an autoclave gave a mixture of 2-thioadenosine (IX), 2-methylthioadenosine (X) and 2-benzylthioadenosine (XI). Reaction of 5-amino-1-β-D-ribofuranosylimidazole-4-carboxamidoxime (XV) obtained from I with CS2-MeOH-H2O at 120°in an autoclave gave IX in an overall yield of 60% (practically 2 steps). Treatment of XV with CS2-MeOH-pyridine at room temperature yielded 2-thioadenosine N-oxide (XVIII) which was subsequently transformed into IX by H2S. Adenines (XX) were also transformed into 2-thioadenine or 9-benzyl-2-thioadenine (XXV) by treatment of the intermediate compounds (XXII) of carboxamidoxime-type with CS2-MeOH-H2O at 120°.View full abstractDownload PDF (1299K) -
ISAMU MURAKOSHI, AKIHIRO SANDA, JOJU HAGINIWA, NOBORU SUZUKI, SHIGERU ...1977 Volume 25 Issue 8 Pages 1970-1973
Published: August 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSCytisine N-methyltransferase, a new enzyme catalyzing the formation of N-methyl-cytisine (II) from cytisine (I) and S-adenosyl-L-methionine, was found in the seedlings of Thermopsis species. 5-Methyltetrahydrofolic acid did not act as a methyl donor for the N-methylation of cytisine. A magnesium cation dependency was not detected. Some other properties of the enzyme are also described.View full abstractDownload PDF (539K) -
RYOHEI HORI, KATSUHIKO OKUMURA, KENICHI INUI, NOBUKUNI NAKAMURA, AKIMA ...1977 Volume 25 Issue 8 Pages 1974-1979
Published: August 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe absorption of Urogastrone, glycoprotein with gastric antisecretory activity, from the rat intestine was studied using the Shild technique, in which the indirect assay of its appearance in the blood stream was facilitated by a concomitant lowering of gastric acid secretion. The intravenous or intraperitoneal administration of Urogastrone produced 40% inhibition of control levels of H+ output. In the intrajejunal administration, it caused only a little inhibitory response. However, when Urogastrone was administered intrajejunally with various bile salts or oil-in-water emulsions, strong inhibitory response of gastric H+ secretion was elicited. Trioctanoin emulsion was most effective on the activity of intrajejunally administered Urogastrone followed by olive oil, diethyl phthalate and liquid paraffin, respectively. The results suggested that orally active dosage forms for poorly absorbable macromolecules such as Urogastrone might be prepared by pharmaceutical modification.View full abstractDownload PDF (719K) -
MASAKAZU ISOBE, MAMORU SUGIURA1977 Volume 25 Issue 8 Pages 1980-1986
Published: August 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSPhysical and chemical properties of the two kinds of lipases (lipase A and lipase B) from Chromobacterium viscosum were investigated. The results were as follows : Sedimentatation constants were 5.35×10-13 cm·g/sec·dyne ; Molecular weights were 1.2×105 and 2.7×104 ; Intrinsic viscosities were 0.060 and 0.051 dl/g ; Partial specific volumes were 0.816 and 0.663 cm3/g ; Isoelectric points were 4.7 and 6.9 for the lipase A and B respectively. From the study of ORD, the α-helix content of the lipase A was calculated to be less than 10% and of the lipase B was to be about 20%. The amino acid compositions of the lipases were different from each other and the lipase B did not contain the half-cystine. Lipid was not detected in the both enzymes and carbohydrate was contained only in the lipase A (14%). By the modification with diazonium-1-H-tetrazole, the enzymic activities were decreased with increase of the modification of histidine residue in the both lipases, and it was assumed that one mole of the histidine residue in the lipase B was related with the catalytic action of the enzyme. Some properties of the lipases which will be concerned with the affinity of the enzymes on their hydrophobic substrates were also discussed.View full abstractDownload PDF (1011K) -
MASAKAZU ISOBE, MAMORU SUGIURA1977 Volume 25 Issue 8 Pages 1987-1991
Published: August 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe lipase of Chromobacterium viscosum in the crude enzyme preparation was specifically adsorbed on glass beads coated with various hydrophobic materials. The enzyme adsorbed on siliconized glass beads was not denatured and eluted with 0.1% Triton X-100 and other detergents. The adsorptive nature of lipase on hydrophobic glass beads was applied to its purification by a one-step process. As the result, lipases of Chromobacterium, Pseudomonas, Candida, and Rhizopus were purified 300-, 670, 160-, and 110-fold, respectively. The lipases purified from Chromobacterium and Candida were examined by disc electrophoresis, and they were judged to be of high purity. Purification of the lipase from Chromobacterium by a column method with siliconized glass beads confirmed that this method allowed about 1000-fold purification.View full abstractDownload PDF (717K) -
TOSHIHIKO MAEDA, HIDEYO SHINDO1977 Volume 25 Issue 8 Pages 1992-2000
Published: August 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESS3, 4-Dihydroxyphenylpyruvic acid-2-14C (DHPP-2-14C) was prepared from glycine-2-14C and the specific formation of L-3, 4-dihydroxyphenylalanine (L-DOPA) from DHPP was shown in vitro. The metabolism of L-DOPA-3-14C was also investigated in vitro for comparison. In rat brain and small intestinal homogenates, L-DOPA was formed gradually as the main metabolite from DHPP-2-14C but dopamine and its metabolites were very slight amount. On the contrary, dopamine was detected dominantly from L-DOPA-3-14C in small intestinal homogenates. In the liver and kidney homogenates, DHPP was metabolized extensively and disappeared immediately with concomitant rapid formation of L-DOPA. Dopamine and 3, 4-dihydroxyphenylacetic acid (DOPAC) were detected subsequently as the main metabolite. The same extensive metabolism of L-DOPA-3-14C was also shown in the liver homogenates. Formation of L-DOPA from DHPP was identified by thin-layer chromatography and reverse isotope dilution method. L-Phenylalanine, L-tyrosine, L-tryptophan and L-glutamate were revealed to be effective amino donors to DHPP. The aromatic L-amino acids were particularly effective but D-phenylalanine showed little activity. The liberation of 14CO2 from DHPP-2-14C was also recognized in vitro. The 14CO2 liberating activity from DHPP-2-14C located in 105000 g supernatant soluble fraction in the liver and kidney wherein the activity in the liver was about 4 fold higher than that in the kidney. The activity was inhibited by sodium azide, sodium diethyldithiocarbamate, p-hydroxyphenylpyruvate and phenylpyruvate but not influenced by SKF 525A, carbon monoxide, EDTA, α, α'-dipyridyl and pyruvate. Methylene blue, dichlorphenolindophenol and ascorbate activated about 2-3 fold.View full abstractDownload PDF (1065K) -
TOSHIHIKO MAEDA, NOBUHIRO MIYAKOSHI, HIDEYO SHINDO1977 Volume 25 Issue 8 Pages 2001-2012
Published: August 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSMetabolic fate of 3, 4-dihydroxyphenylpyruvic acid-2-14C (DHPP-2-14C) in rats was investigated and a rapid conversion of DHPP to L-3, 4-dihydroxyphenylalanine (L-DOPA) was demonstrated in vivo. After intravenous administration, a high uptake of the radioactivity was observed in the adrenal medulla, caudate nucleus, pancreas, hair follicle and renal medulla, in a similar way as L-DOPA-2-14C. DHPP itself appears not to pass through the blood-brain barrier. After oral administration, very little uptake of the radioactivity was observed in the brain even at high doses (10, 50 and 100 mg/kg). Most radioactivity was recovered into the urine (about 44.0% and 85.4% after oral and intravenous administration, respectively) but respiratory excretion of the radioactivity was also observed (28.01 and 6.30% after oral and intravenous administration, respectively). In order to evaluate the efficacy of DHPP as oral precursor of brain dopamine, the brain and other tissue uptake of the radioactivity were compared between DHPP-2-14C and L-DOPA-3-14C after oral administration at various dosages. The results revealed only extremely low uptake of radioactivity in the brain after DHPP administration as compared to L-DOPA. This was found to be mainly due to an extremely slower absorption of DHPP than L-DOPA from intestine.View full abstractDownload PDF (2430K) -
KAZUICHI HAYAKAWA, TOSHIO IMANARI, ZENZO TAMURA, SHIGETOSHI KURODA, HI ...1977 Volume 25 Issue 8 Pages 2013-2018
Published: August 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSBeagle dogs were orally administered with a fixed dose of clioquinol, 300 mg/kg/day, in gelatin capsules every day. Other beagle dogs were orally administered with powder clioquinol, 300 mg/kg/day after increasing dose, in milk twice a day. All beagle dogs administered with clioquinol developed weakness of the hind-limbs and hip swaying in several ten days. Individual differences and daily variations in serum levels of clioquinol, its sulfate and its glucuronide were large. Clioquinol was detected at higher concentrations not only in central nervous system but also in peripheral nervous system, and was retained for a long time.View full abstractDownload PDF (660K) -
SEIJIRO HONMA, SATOSHI IWAMURA, KAZUO IIZUKA, AKIRA KAMBEGAWA, KEIZO S ...1977 Volume 25 Issue 8 Pages 2019-2031
Published: August 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe metabolic fate of chlormadinone acetate (CMA), which is a new anti-androgenic agent, has been investigated with rats, rabbits, dogs and humans. Fourteen unconjugated metabolites and three conjugated metabolites were isolated from urine, feces and bile after oral administration of CMA. The structures of these metabolites were deduced from physico-chemical data and definitely characterized by direct comparison with the authentic samples (see Chart 1). There was a marked species difference in the metabolic pattern. Especially, configuration of 2-hydroxy group in the 2-hydroxylated metabolites was different among species. Further, the occurrence of 1-hydroxylation and 15-hydroxylation, new metabolic pathways in steroidal agents, was found in the rats and humans. The anti-androgenic activities of the metabolites were listed in Table III. 3β-Hydroxy CMA, one of the main metabolites in humans and rats, and its acetate were 0.7 time as active as CMA, whereas other main metabolites, 2α, 3β-dihydroxy CMA and 2α-acetoxy CMA, were not effective.View full abstractDownload PDF (1534K) -
HARUMI NARUSE, NAOKO KATO, EMIKO NASU, SATOSHI KAWAI, KEIJI HASHIMOTO, ...1977 Volume 25 Issue 8 Pages 2032-2034
Published: August 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSGas chromatographic analysis of urinary indole-3-acetic acid as the trifluoroacetyl derivative of its methyl ester was carried out. A 10 ml portion of urine sample, acidified and saturated with sodium chloride, was extracted with benzene. After methylation with diazomethane in ether, indole-3-acetic acid was converted to the trifluoroacetyl derivative. Indole-3-butyric acid was used as an internal standard. This method was applied to human urine samples and the results showed the presence of 1.5-3.5 mg/day or 0.31-2.50 μg/mg creatinine of indole-3-acetic acid in normal urine, while the excretion of indole-3-acetic acid was higher in leukemia, gastric cancer, and phenylketonuria.View full abstractDownload PDF (469K) -
HIDEMI ISHII, TETSUYA SUGA, SHINKICHI NIINOBE, YOSHIHIKO INATSU1977 Volume 25 Issue 8 Pages 2035-2040
Published: August 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSVarious enzyme activities in the rat serum and liver were determined and the effect of 3-amino-1, 2, 4-triazole (AT) on CCl4-induced necrosis was studied. Serum transaminase (GOT and GPT) activities were markedly increased by the injection of CCl4 (0.1 ml/100 g, i.p.). The increase fell about 60 per cent with both the pre- and post-treatment of AT (100 mg/100 g, i.p.). It was demonstrated by biochemical and histological technique that the treatment with AT also repressed the fatty liver which occurrs along with liver necrosis. The effect of CCl4 and AT on subcellular distribution of acid phosphatase was examined. AT repressed the release of enzyme from light mitochondrial fraction to supernatant fraction caused by CCl4. AT significantly depressed the release of enzyme from the liver lysosomes by freezing and thawing in both the control-and CCl4-treated rat. These results indicate that AT shows a depressing effect on fatty liver, a stabilizing effect on lysosomes, and a repression on liver necrosis.View full abstractDownload PDF (863K) -
SHOJI YAHARA, RYOJI KASAI, OSAMU TANAKA1977 Volume 25 Issue 8 Pages 2041-2047
Published: August 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSFrom leaves of Panax japonicus C.A. MEYYR, ginsenoside-F17) and three new dammarane type saponins named chikusetsusaponins-L5 (I), -L10 (II) and -L9a (III) were isolated. The structures of I, II and III were elucidated mainly by mass, 13C-nuclear magnetic resonance and 1H-nuclear magnetic resonance spectroscopy including partially relaxed Fourier transform method.View full abstractDownload PDF (772K) -
HARUAKI YAJIMA, JUN IWAI, HIDEHIKO WATANABE, KANAME KOYAMA, MASUHISA N ...1977 Volume 25 Issue 8 Pages 2048-2054
Published: August 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSH-Asp-Gly-Ile-Asp-Tyr-Lys-Met-Gly-His-Phe-Arg-Trp-Gly-Ala-Pro-Met-Asp-Lys-OH, dogfish β-MSH (Scyliorhinus canicula), was synthesized in a conventional manner by applying the hydrogen fluoride procedure.View full abstractDownload PDF (996K) -
SACHIKO KAWANISHI, RYOJI KASAI, SEIICHI SAKUMA, JUNZO SHOJI1977 Volume 25 Issue 8 Pages 2055-2060
Published: August 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSFour new type oligosaccharides C1, D2, F1 and F2 of Bei-Wujiapi (cortex of Periploca sepium BGE.) were elucidated to be 2-O-acetyl-β-D-digitalopyranosyl (1→4)-β-D-cymaropyranosyl (1→4)-β-D-cymaropyranosyl (1→4)-L-oleandronic acid-δ-lactone (Ia), 2-O-acetyl-β-D-digitalopyranosyl (1→4)-β-D-cymaropyranosyl (1→4)-β-D-canaropyranosyl (1→4)-β-D-digitoxopyranosyl (1→4)-L-oleandronic acid-δ-lactone (IIa), β-D-digitalopyranosyl (1→4)-β-D-cymaropyranosyl (1→4)-β-D-cymaropyranosyl (1→4)-L-oleandronic acid-δ-lactone (IIIa) and β-D-digitalopyranosyl (1→4)-β-D-cymaropyranosyl (1→4)-β-D-canaropyranosyl (1→4)-β-D-digitoxopyranosyl (1→4)-L-oleandronic acid-δ-lactone (IVa). It should be noted that Ia, IIa, IIIa and IVa are the first oligosaccharides composed of 2, 6-dideoxysugars and 2, 6-dideoxyaldonic lactone. Furthermore, it is interesting that the sugar sequences of these oligosaccharides are ruled by the regularity in cardiac and pregnane type glycosides of Asclepiadaceous plants.View full abstractDownload PDF (783K) -
KATSUHIKO MATSUI, YUKIKO TAMEGAI, AKIKO MIYANO, YUKIO KAMEDA1977 Volume 25 Issue 8 Pages 2061-2066
Published: August 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSAlanine dehydrogenase [L-alanine : NAD+ oxidoreductase (deaminating) EC. 1. 4. 1. 1.] from Bacillus natto KMD 1126 was purified 160-fold by ammonium sulfate fractionation, diethylaminoethyl-cellulose chromatography, Sephadex G-200 gel filtration, and adenosine-5'-phosphate Sepharose 4B affinity chromatography. The purified enzyme preparation showed a single band on polyacrylamide gel disc electrophoresis. Specific activity of the purified enzyme was 21 u/mg for oxidative deamination of L-alanine and lower than that of Bacillus subtilis (1350 u/mg). The molecular weight of the enzyme was 280000 daltons as determined by gel filtration on Sephadex G-200. Optimum pH for oxidative deamination of L-alanine was 10.4-10.7, whereas it was 8.2-8.4 for reductive amination of pyruvate. The enzyme was completely inhibited by Hg2+ and p-chloromercuribenzoate at 10-3 M. Nicotinamide adenine dinucleotide and its reduced form were essential as coenzymes and could not be replaced by nicotinamide adenine dinucleotide phosphate and its reduced form. L-Alanine was oxidatively deaminated by the enzyme and L-sereine was also deaminated at the rate of 0.5% of L-alanine, but D-alanine and other amino acids were not deaminated. That is, the enzyme has relatively high substrate specificity.View full abstractDownload PDF (736K) -
NORIO AIMI, ETSUJI YAMANAKA, NOBUO SHINMA, MORIO FUJIU, JUNKO KURITA, ...1977 Volume 25 Issue 8 Pages 2067-2071
Published: August 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSTwo minor alkaloids were newly isolated from Uncaria rhynchophylla MIQ., and their structures elucidated as geissoschizine methyl ether (a new compound) and akuammigine, respectively. The Cotton effect due to the chirality of the E ring of heteroyohimbinoid alkaloids was studied by using some model compounds. The conformation of akuammigine was also studied.View full abstractDownload PDF (634K) -
TOZO FUJII, KIYOSHI YOSHIDA, MASASHI OHBA, MORIHIRO MITSUKUCHI, IZUMI ...1977 Volume 25 Issue 8 Pages 2072-2077
Published: August 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe alkaline ferricyanide oxidation at 32°of 1-(3, 4-dimethoxyphenethyl) pyridinium bromides (3c-f) carrying the n-butyl, isopropyl, benzyl, and phenyl group at the 3-position has been found to produce the corresponding 2-(4c-f) and 6-pyridones (5c-f) in ratios of 74 : 26, 71 : 29, 69 : 31, and 13 : 87. In the case of the 3-benzyl derivative (3e), 1-(3, 4-dimethoxyphenethyl)-5-benzoyl-2 (1H)-pyridone (5g) has also been obtained in 1% yield. On the basis of the present and earlier data, possible factors in determining the orientation in the ferricyanide oxidation of 1, 3-disubstituted pyridinium salts are discussed.View full abstractDownload PDF (717K) -
TOHRU KIKUCHI, TOSHIO YOKOI, MINEO NIWA, TETSURO SHINGU1977 Volume 25 Issue 8 Pages 2078-2081
Published: August 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSHomonuclear internuclear double resonance technique was applied to β-amyrin acetate (Ia) and the related compounds and this technique was proved to be useful for the qualitative measurements of the nuclear Overhauser effects between methyl-methyl protons. Assignments of methyl resonances of β-amyrin (Ib) and β-amyrone (IIa) were also carried out by the use of this technique.View full abstractDownload PDF (556K) -
AKIRA YOSHIDA, SADAO OIDA, EIJI OHKI1977 Volume 25 Issue 8 Pages 2082-2088
Published: August 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESS2-Alkoxy-3-cephem-1-oxides 1b-c were found to be thermally unstable and easily converted into isothiazolones 5a-f, β-lactam 12 and thiazole 14 according to reaction conditions. Further, 2-alkoxy-3-cephem 4a-b was treated with tert-butyl hypochlorite to give azetidinone-oxazoline acetals 18a-b. Formation of these rearrangement products was interpreted via the sulfenic acid intermediate 6 or 17.View full abstractDownload PDF (897K) -
HIROMICHI SAEKI, TERUO HAYASHI, YOSHIKAZU SHIMADA, NORIKO TAKEDA, EIJI ...1977 Volume 25 Issue 8 Pages 2089-2097
Published: August 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSIt was shown that the 3'and 4'hydroxy groups of N-protected butirosin or kanamycin derivatives resist benzoylation in an aqueous medium, furnishing an effective method for chemical modifications of these antibiotics.View full abstractDownload PDF (1123K) -
MASAYOSHI HORIOKA, TOSHINOBU AOYAMA, IKUKO YOKOYAMA, YUMIKO HATTA1977 Volume 25 Issue 8 Pages 2098-2104
Published: August 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSIn order to examine the effect of parenteral solutions on erythrocytes, periodical changes in erythrocyte count were measured by HIAC automatic particle counter and, at the same time, erythrocytes were observed by a scanning electron microscope. It was found that HIAC particle counter is convenient for counting of blood cell number and that changes in the counts of cells in the range of 10-150 μm can be used as an index for the destruction of blood cells. It was also found that removal of ascorbic acid from tetracycline preparations prevented destruction of erythrocytes and that chloramphenicol sodium succinate does not disrupt erythrocytes even in a high concentration. These results indicated that erythrocyte destruction by parenteral solution was possibly due to the pH and osmotic pressure of the drug solution and to additives rather than or in addition to the direct action of drugs. Re-examination of the test methods for hemolysis and establishment of judgement standards are desirable.View full abstractDownload PDF (1424K) -
YUTAKA KASUYA, YENFUN CHIUWEI, KATSUTOSHI GOTO, MINORU WATANABE1977 Volume 25 Issue 8 Pages 2105-2111
Published: August 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSBeta-adrenoceptor blocking activity of a newly synthesized benzothiazole derivative, 6-(2-hydroxy-3-isopropylamino) propoxybenzothiazole succinate (KF-577) was investigated. In in vitro preparation of the guinea pig trachea and the atrium it was approximately 1/100 and 1/10 as potent as propranolol, respectively, in competitively blocking the betareceptors : some cardioselectivity was seen. Like propranolol, it is devoid of intrinsic beta-stimulating activity. In urethane-anesthetized rats KF-577 and propranolol both exhibited a pressor effect at lower doses, while at higher doses both caused a sharp fall in blood pressure. The depressor and positive chronotropic effects of isoproterenol were both blocked by either KF-577 or propranolol. Mechanisms of this pressor effect were explored using vagotomized, adrenalectomized, reserpinized rats, and the results were subjected to discussion. KF-577 had a surface anesthetic potency 1/20 that of propranolol (guinea pig cornea) and a conduction anesthetic potency comparable to propranolol (frog sciatic nerve). KF-577 was thus shown to be a beta-adrenoceptor blocker having some selectivity.View full abstractDownload PDF (816K) -
KUNIO KOBAYASHI, YOKO TSUMURA, HISAYO ISE, SHOHEI KAGAWA, AKIRA MATSUO ...1977 Volume 25 Issue 8 Pages 2112-2116
Published: August 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe dynamics of insulin release from the perifused rat Langerhans islets was investigated under a slow-rise and square-wave stimulation by glucose. Every dose response curve were sigmoidal profile, in which the threshold of glucose was shown to be around 4.2 mM. The Km values of dose response curves were similar each other under a slow-rise and square-wave stimulation by glucose. Since a rise of gradient level from 0.10 to 0.22 mM/min did not alter the dose response curve, it was proved that a profile of insulin release in response to slowly rising glucose was not due to a lag time in insulin release but dependent to an absolute change of glucose level. The stimulation by rapid change of glucose level with 2.80 mM/min of gradient level caused an insulin releasing profile similar to that by the square-wave stimulation. Consequently, it was suggested that the insulin release under a slow-rise stimulation by glucose at gradient levels around 0.10-0.22 mM/min was more physiologic. This stimulation method is an easily available procedure for preparing accurate dose response relationship between the rate of insulin released and the concentration of glucose.View full abstractDownload PDF (672K) -
SHOICHIRO TAGAMI, MANABU ASAKAWA, DENITSU SHIHO1977 Volume 25 Issue 8 Pages 2117-2120
Published: August 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSAluminum can be determined by reaction with ethyl pyridoxyliminopyruvate in methanol. The neutral methanolic solution of pyridoxamine and a methanolic solution of ethyl pyruvate are mixed and heated at 70°for 15 min. This Schiff base solution is added to the methanolic solution of a sample containing aluminum nitrate. The time-absorbance curves have to be recorded for each sample, because the coloration of species absorbing at 488 nm is unstable. Calibration curve is obtained by plotting the maximum values in the time-absorbance curve against aluminum concentration. This spectrophotometric method can be used in the concentration range of 0.89 to 2.11 μg/ml of aluminum.View full abstractDownload PDF (501K) -
HIROSHI TAKAKU1977 Volume 25 Issue 8 Pages 2121-2123
Published: August 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSPhosphorylation of nucleosides by means of 8-quinolyl dihydrogen phosphate has been described. Phosphorylation of nucleosides with 8-quinolyl dihydrogen phosphate could only be carried out in the presence of cupric chloride. By this method, nucleoside 5'-phosphates were obtained in good yields.View full abstractDownload PDF (474K) -
KAZUICHI UEDA, KOUKI KITAGAWA, TADASHI AKITA, SUMIKO HONMA, TOMIO SEGA ...1977 Volume 25 Issue 8 Pages 2123-2126
Published: August 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe hexadecapeptide corresponding to positions 1 to 16 of porcine motilin was synthesized in a conventional manner. The synthetic peptide exhibited the activity of 3% of that of the synthetic motilin, when tested using rabbit duodenal muscle in vitro.View full abstractDownload PDF (640K) -
KAZUYA KOHASHI, YASUTO TSURUTA, YOSUKE OHKURA1977 Volume 25 Issue 8 Pages 2127-2130
Published: August 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESS1 : 2 Complex of picric acid and creatinine was isolated in crystalline forms from the alkaline reaction mixture of creatinine and excess picric acid. Structural characterization of the complex and its absorption spectral behavior were discussed.View full abstractDownload PDF (491K) -
HIDEJI SATO, MASAYOSHI YAMAGUCHI, TAKEO YAMAMOTO1977 Volume 25 Issue 8 Pages 2131-2133
Published: August 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSEffect of theophylline and imidazole on the renal cortex calcium concentration was examined in rats intraperitoneally administered with stannous chloride. The increased calcium concentration in renal cortex caused by the tin administration (Sn 3.0 mg/100 g) was markedly decreased by the treatment of imidazole (20 mg/100 g), while was not altered significantly by the treatment of theophylline (2.0 mg/100 g). Theophylline alone significantly increased the calcium concentration in renal cortex compared with that of control. The present study suggests that the action of tin on renal cortex calcium may be dependent on cyclic AMP.View full abstractDownload PDF (426K) -
TERUO HAYASHI, NORIKO TAKEDA, HIROMICHI SAEKI, EIJI OHKI1977 Volume 25 Issue 8 Pages 2134-2137
Published: August 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSNaphthalene-sodium reaction of 3, 4-dimesylates of N-protected 2, 6-diamino-2, 6-dideoxy-α-D-glycosides (1a, 1b) resulted in a good yield of 3-eno compounds (2a, 2b). Application of this anion-radical reaction to butirosin 3', 4'-dimesylate (3) gave 3', 4'-dideoxy-3'-one butirosin A (4a) which shows a broad inhibitory activity against bacteria which are both sensitive and resistant to butirosin. Kanamycin 3', 4'-dimesylate (5a) also analogously gave a 3'-eno derivative (6).View full abstractDownload PDF (558K) -
ITSUO YOSHIZAWA, RYOKO OHUCHI, AKIKO NAKAGAWA1977 Volume 25 Issue 8 Pages 2137-2139
Published: August 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSRabbit anti-pregnanediol antiserum was obtained using 3α, 20α-dihydroxy-5β-pregnan-7-one O-carboxymethyloxime coupled to bovine serum albumin as the antigen. A radioimmunoassay procedure for pregnanediol utilizing the highly specific antiserum was developed and permitted the measurement of this material in body fluids.View full abstractDownload PDF (480K) -
TOHRU ENDO, HEIHACHIRO TAGUCHI1977 Volume 25 Issue 8 Pages 2140-2142
Published: August 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSFour new iridoid glycosides, kanokoside A, B, C and D have been isolated from valerian root cultivated in Hokkaido area under the name of "Hokkaikisso". From chemical and spectral evidence, their structures have been elucidated to be I, II, III and IV, respectively.View full abstractDownload PDF (477K) -
YOSHIYUKI OHSUGI, TOSHIAKI NAKANO, SHUNICHI HATA, TAKASHI MATSUNO, YAS ...1977 Volume 25 Issue 8 Pages 2143-2145
Published: August 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSEffects of disodium N-(2-carboxyphenyl)-4-chloroanthranilate, which was newly synthesized, on the immune response in mice were investigated. An oral administration of this compound increased the production of splenic plaque forming cells against both a thymus-dependent (sheep red blood cells) and a thymus-independent antigen (bacterial lipopolysaccharide).View full abstractDownload PDF (432K) -
KEI TAKEDA, TOSHIHARU OHTA, KOICHI SHUDO, TOSHIHIKO OKAMOTO, KUNIRO TS ...1977 Volume 25 Issue 8 Pages 2145-2146
Published: August 25, 1977
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA potent mutagen, 3-amino-1-methyl-5H-pyrido [4, 3-b] indole isolated from tryptophan pyrolysate was synthesized.View full abstractDownload PDF (299K)
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