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Volume 21, Issue 1
Displaying 1-38 of 38 articles from this issue
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YOSHITOSHI KASÉ, AKIRA NAKANISHI, AKIYOSHI KAWASAKI, TAKESHI MI ...1973 Volume 21 Issue 1 Pages 1-7
Published: January 25, 1973
Released on J-STAGE: February 08, 2011
JOURNAL FREE ACCESSPiperidine, one of alicyclic amines, shows not only nicotine-like synaptotropic actions but also a marked respiratory stimulant action due to the chemoreflex of carotid body. Accordingly, in expectation of preparing some potent respiratory stimulants, two series of compounds were synthesized by the substitution of the pyridine ring in the nikethamide structure for a piperidine ring and the substitution of morpholino groups in the dimorpholamine (dim.) for two piperidino groups or similar piperidine ones. Among them, N, N'- dibutyl-N, N'-bis (piperidinocarbonyl) ethylenediamine (VII) was the most potent in respiratory stimulant action.
In rabbits, the respiratory stimulant action of VII was 4 to 5 times as potent as that of dim. and the duration of the effect was twice as long as that of dim. Its toxicity in mice was about a half that of dim. Furthermore, the significance of the role of piperidino group in manifestation of pharmacological activities was demonstrated.View full abstractDownload PDF (1198K) -
TETSUYA KAMATAKI, MITSUKAZU KITADA, HARUO KITAGAWA1973 Volume 21 Issue 1 Pages 8-11
Published: January 25, 1973
Released on J-STAGE: February 08, 2011
JOURNAL FREE ACCESS1. Aniline-induced difference spectrum in post-mortem human liver microsomes was recognized as type II similar to that in rat liver. Hexobarbital- and aminopyrineinduced P-450 difference spectra were also of type II in human, but they were different from those in rat liver microsomes.
2. There was no correlation between enzyme activities of the NADPH-linked electron transport system in liver microsomes and aniline hydroxylase activity in human liver, which was similar to that of rat liver. The activity of hydroxylation. of hexobarbital, a type I compound, in human was lower than that in rat liver, and a similar result was observed when aminopyrine was used as substrate.View full abstractDownload PDF (659K) -
HIROSHI TERAYAMA, TAKESHI NARUKE, SAKURO KASAI, MAKOTO NUMATA, HISAO N ...1973 Volume 21 Issue 1 Pages 12-20
Published: January 25, 1973
Released on J-STAGE: February 08, 2011
JOURNAL FREE ACCESSThe metabolic fate of a new analgesic agent, 1-n-butyryl-4-cinnamylpiperazine hydrochloride (BCP-HCl) in the rat was investigated in vivo and in vitro.
The following four urinary metabolites were detected in addition to the unchanged drug by both the thin-layer (TLC) and gas-liquid chromatography (GLC); 1-n-butyrylpiperazine (I), 1-n-butyry1-4-(4'-hydroxycinnamyl) piperazine (III), 1-(4'-hydroxycinnamyl)-piperazine (IV) and 1-cinnamylpiperazine (V). These were isolated and identified physicochemically (ultraviolet, infrared and mass spectrometry and mixed melting point test). In addition to the above metabolites, piperazine hexahydrate (II) and two unidentified products, UK-1 and UK-2 were detected in the urine by the TLC but not by the GLC.
In the bile BCP, I, III, and IV were detected in addition to the glucuronide and sulfate conjugates of III and IV. One unknown metabolite corresponding to the urinary UK-1 was also detected by the TLC of the biliary metabolites hydrolyzed with β-glucuronidase or arylsulfatase.
In vitro incubation of BCP-HCl with the post-mitochondrial fraction of the rat liver resulted in the formation of the four metabolites, I, III, IV and V.View full abstractDownload PDF (1411K) -
TAKESHI ONODERA, TAKESHI HASHIZUME, AKIRA KASAHARA1973 Volume 21 Issue 1 Pages 21-24
Published: January 25, 1973
Released on J-STAGE: February 08, 2011
JOURNAL FREE ACCESSFurazabol showed non-specific inhibitory activities to the responses of guinea pig ileum to various spasmogens, and the activities were considerably higher than those of papaverine. It inhibited also the response of guinea pig υas deferens to adrenaline, depressed spontaneous movements of guinea pig atria and rat uterus and showed a slight and temporal fall in blood pressure which was not affected by the pretreatment of atropine. These data suggest that furazabol has a papaverine-like property. Furazabol showed serum cholesterol-lowering action in normal rats and cholesterol-fed chicks. In addition, it exerted curative action on gastric stress ulcer in rats.View full abstractDownload PDF (445K) -
TAKASHI HARAYAMA, MITSUAKI OHTANI, MASAHARU OKI, YASUO INUBUSHI1973 Volume 21 Issue 1 Pages 25-33
Published: January 25, 1973
Released on J-STAGE: February 08, 2011
JOURNAL FREE ACCESSThe substituent effect on the addition course of the Diels-Alder reaction of butadiene with 2-methyl-1, 4-benzoquinones which carry the cyano (V), dimethylcarbamoyl (VI), β-ethoxycarbonylethyl (VII), β-cyanoethyl (VIII), ethoxycarbonyl-trans-vinyl (IXa) group at the C5 position, respectively, was examined. The addition of V and VI occurred one-sidedly at the ethylene linkage carrying the electronwithdrawing cyano and dimethylcarbamoyl group. In the compound (VII and VIII), butadiene added at both ethylene linkages giving a mixture of adducts in the ratio of XXXIIa/XXXIIb=2/3 and XXXIIIa/XXXIIIb=1/1, respectively. The reaction of 2-methyl-5-(ethoxycarbonyl-trans-vinyl)-1, 4-benzoquinone (IXa) with butadiene furnished the adduct (XXXIVa), indicating that the addition occurred at the ethylene linkage bearing the unsaturated ester group.View full abstractDownload PDF (1526K) -
HITOSHI UNO, AKIRA IRIE, KATSUHIKO HINO1973 Volume 21 Issue 1 Pages 34-39
Published: January 25, 1973
Released on J-STAGE: February 08, 2011
JOURNAL FREE ACCESS8-(Acetylmethyl) thioadenines, which have an amino group on 6-position of purine ring, were cyclized with condensing agents and thiazol [3, 2-e] adenines, in which cyclization took place to 7-nitrogen of purine ring, were obtained. Structures of these thiazoladenines were determined by desulfurization with Raney Ni.View full abstractDownload PDF (737K) -
MITSUO AKIBA, SADAO OHEI1973 Volume 21 Issue 1 Pages 40-46
Published: January 25, 1973
Released on J-STAGE: February 08, 2011
JOURNAL FREE ACCESSAs one of the 10-aza-steroid system, 17-acetoxy-10-aza-androstan-7-one (1) was synthesized. Condensation of hexahydroindanone (16) and ethyl piperidinoacetate (3) gave a mixture of βA-amino-enones with angular (17) and linear (18) structures. The separated 17 was reduced and then oxidized to 1. Reaction between 3 and testosterone (7) mainly gave amino-dienone (8) of linear structure. Such a tendency was also seen in the case of tetrahydroindanone (14) and the amino-dienone (19) of linear structure was obtained solely.View full abstractDownload PDF (1158K) -
KUNIO HIROI, SHUN-ICHI YAMADA1973 Volume 21 Issue 1 Pages 47-53
Published: January 25, 1973
Released on J-STAGE: February 08, 2011
JOURNAL FREE ACCESS2-, or 4-Alkylcyclohexanone enamines of L-proline t-butyl ester were formed. Asymmetric syntheses of 2-alkylcyclohexanone derivatives were carried out by these enamines reacting with alkylating agents, i. e. acrylonitrile, methyl acrylate, and allyl bromide.
The mechanism of this asymmetric induction was deduced from the experimental results.View full abstractDownload PDF (1151K) -
KUNIO HIROI, SHUN-ICHI YAMADA1973 Volume 21 Issue 1 Pages 54-61
Published: January 25, 1973
Released on J-STAGE: February 08, 2011
JOURNAL FREE ACCESSOptically active 2-bromocyclohexanone derivatives were asymmetrically synthesized for the first time. Absolute configurations of products were determined using the axial α-haloketone rule. The solvent effect of (-)-V on optical rotatory dispersion and circular dichroism was studied in various solvents.
Racemization of (-)-V catalyzed with acid or base was examined. Asymmetric synthesis using other ketones was also studied.View full abstractDownload PDF (1079K) -
MITSUO NAGANO, TAKASHI MATSUI, JUNZO TOBITSUKA, KOZO OYAMADA1973 Volume 21 Issue 1 Pages 62-73
Published: January 25, 1973
Released on J-STAGE: February 08, 2011
JOURNAL FREE ACCESSThe reactions of alkoxycarbonyl isothiocyanates and prim-α-acetylenic alcohols afford N-alkoxycarbonyl-O-acetylenyl thiocarbamates, N-alkoxycarbonyl-S-allenyl thiolcarbamates and 4-alkylidene-2-alkoxycarbonylimino-1, 3-oxathiolanes. However, the reaction patterns are dependent on the substituents on the 3-positions of α-acetylenic alcohols: 3-Phenyl-2-propyn-1-ol (40) react smoothly with the isothiocyanates to give 1: 1 adducts which cyclize immediately to 4-benzylidene-1, 3-oxathiolanes (42). 2-Butyn-1-ol (36) reacts slowly with the isothiocyanates to afford N-alkoxycarbonyl-O-2-butyn-1-yl thiocarbamates (37), but these compounds (37) cyclize hardly to 4-ethylidene-1, 3-oxathiolanes (39) even in the presence of a base. In the case of 2-propyn-1-ol (19), N-alkoxycarbonyl-O-2-propyn-1-yl thiocarbamates (24), N-alkoxycarbonyl-S-allenyl thiolcarbamates (25) and 2-alkoxycarbonylimino-4-methylidene-1, 3-oxathiolanes (26) are obtained. Furthermore, the cyclization mechanisms of α-acetylenyl thiocarbamates (45) were confirmed by using N (D)-O-(2-propyn-1-yl)-N-isopropoxycarbonyl thiocarbamate (43).View full abstractDownload PDF (1942K) -
MITSUO NAGANO, TAKASHI MATSUI, JUNZO TOBITSUKA, KOZO OYAMADA1973 Volume 21 Issue 1 Pages 74-86
Published: January 25, 1973
Released on J-STAGE: February 08, 2011
JOURNAL FREE ACCESS1-Alkoxycarbonyl-3-(2-thiazolyl) thioureas (A) were reacted with alkyl halides in presence of potassium carbonate to afford 1 (H)-alkoxycarbony1-2-alkyl-3-(2-thiazolyl)-isothioureas (D), 1-alkoxycarbony1-2-alkyl-3-(3-alkylthiazolin-2-ylidene) isothioureas (E) 2-alkylthio-thiazolo [3, 2-a]-s-triazine-4-ones (C). However, the rate of this reaction the yields of the products were dependent on the kinds of alkyl halide and thiazolyl thioureas (A). The cyclization products (C) were obtained in a good yield by the thermal treatment of the compounds (E).View full abstractDownload PDF (2330K) -
MASAHIKO FUJINO, TSUNEHIKO FUKUDA, SHIGERU KOBAYASHI, MIKIHIKO OBAYASH ...1973 Volume 21 Issue 1 Pages 87-91
Published: January 25, 1973
Released on J-STAGE: February 08, 2011
JOURNAL FREE ACCESSGonadotropin-releasing hormone (Gn-RH or LH-RH/FSH-RH), a decapeptide amide (Pyr) Glu-His-Trp-Ser-Tyr-Gly-Leu-Arg-Pro-Gly-NH2, was synthesized by the use of the d-isobornyloxycarbonyl-protercting group for temporary protection of the all amino groups of the intermediary peptides. The synthetic Gn-RH possessed full biological activity (LH-releasing and FSH-releasing activity) when compared with natural highly purified porcine Gn-RH, and appeared to be pure by various chemical criteria.View full abstractDownload PDF (1005K) -
TAKU NAGAO, MASANORI SATO, HIROMICHI NAKAJIMA, AKIO KIYOMOTO1973 Volume 21 Issue 1 Pages 92-97
Published: January 25, 1973
Released on J-STAGE: February 08, 2011
JOURNAL FREE ACCESSThe coronary vasodilating action of 1, 5-benzothiazepine derivatives and the structureactivity relationship were examined in the anesthetized dog. 2-(4-Methoxyphenyl), 3-acyloxy or alkyloxy, 5-dimethylaminoethyl and 7-hydrogen moieties were important for vasodilation. The action of the derivatives was found to be stereospecific for the d-cis-isomer. Based on these findings, it can be concluded that d-3-acetoxy-cis-2, 3-dihydro-5-[2-(dimethylamino) ethyl]-2-(4-methoxyphenyl)-1, 5-benzothiazepin-4 (5H)-one hydrochloride (CRD-401) was the most potent compound among the derivatives tested. The metabolites of dl-isomer of CRD-401, i.e. deacetyl and deacetyl-O-or N-demethyl compounds, were less active and less toxic than the parent compound.View full abstractDownload PDF (575K) -
TSUTOMU FURUYA, HISASHI KOJIMA, KUNIHIKO SYONO, TAKAFUMI ISHII, KAZUMI ...1973 Volume 21 Issue 1 Pages 98-101
Published: January 25, 1973
Released on J-STAGE: February 08, 2011
JOURNAL FREE ACCESSThe callus derived from the petiole of Panax ginseng has been vigorously grown on Murashige and Skoog's agar medium (minus glycine) supplemented with 2, 4-dichlorophenoxyacetic acid. Saponins such as ginsenosides Rb1 (I) and Rg1 (II) were obtained via the column of Sephadex LH-20 and silica gel, respectively. Sapogenins, such as panaxadiol (III), panaxatriol (IV) and oleanolic acid (V), were also isolated in crystalline form from the hydrolysates of crude saponins. The callus contains a considerable amount of saponins and the thin-layer chromatograms of the saponins are similar to those of ginseng root saponins.View full abstractDownload PDF (529K) -
TETSUYA KAMATAKI, MASAKAZU SHIMOKAWA, HARUO KITAGAWA1973 Volume 21 Issue 1 Pages 102-106
Published: January 25, 1973
Released on J-STAGE: May 27, 2011
JOURNAL FREE ACCESSSubstrate induced difference spectra in microsomes from 3-methylcholanthrene treated rats were investigated using substrates which cause type I difference spectrum in microsomes from control rats. It was found that α, α'-dipyridyl showed only type II spectrum, whereas SKF 525-A and ethylmorphine produced type I spectra. Additionally, hexobarbital, aminopyrine and imipramine produced type I spectra when they were used by rather low concentrations but type II spectra were induced by high concentrations of them.α, α'-Dipyridyl caused type II spectrum when microsomes from control rats were treated with phospholipase C. The type II spectrum of α, α'-dipyridyl in 3-methylcholanthrene-induced microsomes was increased by treatment with phospholipase C.
Moreover, α, α'-dipyridyl showed type II spectrum in microsomes from control rats when SKF 525-A, which has a high affinity to combine with type I binding site of P-450, was added into reference and sample cuvettes.
From above data, the authors concluded that most of type I compounds could combine with both type I and type II binding sites, and discussed on the properties of type I and type II binding sites.View full abstractDownload PDF (718K) -
TSUNEHIKO ASAKO, KENTARO HIRAGA, TAKUICHI MIKI1973 Volume 21 Issue 1 Pages 107-111
Published: January 25, 1973
Released on J-STAGE: February 08, 2011
JOURNAL FREE ACCESS17α-Hydroxy-3-methoxy-8, 14-secoestra-1, 3, 5 (10), 9-tetraen-14-one (IIa) which is an intermediate for the total synthesis of estrogens has been optically resolved. The isomer which has unnatural configuration at C-13 has been converted to estrapentaene 3-methyl ether (IVa) via the 9, 14-epoxy intermediates (XI, XII, XIII, XV).View full abstractDownload PDF (829K) -
YUTAKA ASAHI, MITSUO NUMATA, EIJI MIZUTA1973 Volume 21 Issue 1 Pages 112-117
Published: January 25, 1973
Released on J-STAGE: February 08, 2011
JOURNAL FREE ACCESSThe N-methyls in 2, 3-disubstituted N, N-dimethylpropylamines (I-VIII) have given two peaks with an equal intensity in an acid solution owing to the hindered internal rotation about the C-NMe2H+ bond. The energy barriers between two staggered forms have been estimated to be 0.7 (benzylthio)-7 (thiocyanato) kcal mole-1 from the temperature dependence of the peak separations. The high-field shift and the largest separation of the N-methyls in the benzylthio derivative (I) have been ascribed to an anisotropic effect of the benzene ring. 1, 3-Disubstituted 2-N, N-dimethylaminopropanes (IX) and 2-substituted N, N-dimethylethylamines (XII-XV) have shown a single peak for the N-methyls. A restricted rotation about the CH2-CH bond in 2, N, N-trimethylaminoethyl disulfide (X) has been studied by the temperature dependence of the vicinal coupling constants.View full abstractDownload PDF (838K) -
KAZUYA KOHASHI, YOSUKE OHKURA, TSUTOMU MOMOSE1973 Volume 21 Issue 1 Pages 118-124
Published: January 25, 1973
Released on J-STAGE: February 08, 2011
JOURNAL FREE ACCESSThe color reactions of cyclohexanone, and acetophenone, with 1, 3, 5-trinitrobenzene were investigated. Two main coloring matters, a Meisenheimer type compound, IV Na and a tricyclic type compound, V Na, were isolated from the reaction mixture of cyclohexanone. In the case of the reaction of acetophenone with excessive 1, 3, 5-trinitrobenzene, the Meisenheimer type compound, VII Na, was the sole coloring matter. From a comparison of the absorption spectral behavior of them with the color reaction mixtures, mechanisms of the color reactions of cyclohexanone, and acetophenone, under the spot test procedure were elucidated.View full abstractDownload PDF (900K) -
HIROSHI IGETA, TAKASHI TSUCHIYA, CHISATO KANEKO, SACHIKO SUZUKI1973 Volume 21 Issue 1 Pages 125-129
Published: January 25, 1973
Released on J-STAGE: February 08, 2011
JOURNAL FREE ACCESSThe compounds, in which two pyridazine rings are combined through two carbon atoms, were synthesized. 3-Methylpyridazine 2-oxide (I) was condensed with 3-formylpyridazine 2-oxide (II) to give 1, 2-bis [3'-(2'-oxido)-pyridazinyl]- ethene (III). Reaction of III with PCl3 in CHCl3 afforded the deoxygenated compound, 1, 2-bis (3'-pyridazinyl)-ethene (IV). Oxidation of IV with H2O2 in AcOH gave 1'1'-di-N-oxide (V). Catalytic hydrogenation of III with Pd-C afforded 1, 2-bis (3'-pyridazinyl)-ethane (VI). Oxidation of VI afforded three kinds of di-N-oxides, i.e., 1', 1'-di-N-oxide (VII), 1', 2'-di-N-oxide (VIII), and 2', 2'-di-N-oxide (IX). Wurtz's reaction of chloromethylpyridazines was also carried out, affording the corresponding ethane (XI) and ethene (XII) derivatives.View full abstractDownload PDF (588K) -
SHINICHI NAKAMURA, MASANAO SHIMIZU1973 Volume 21 Issue 1 Pages 130-136
Published: January 25, 1973
Released on J-STAGE: February 08, 2011
JOURNAL FREE ACCESSIt was found that (5-nitro-2-furyl) vinylpyridine derivatives inhibited the synthesis of bacterial macromolecules in intact cell and protoplast lysate systems of Escherichia coli K-12. Among the syntheses tested, DNA, RNA and protein syntheses were inhibited correlating to antibacterial activity but lipid synthesis was independent of it. In the derivatives active against the strain, most inhibited DNA and protein syntheses and some additionary RNA synthesis in intact cell system. In protoplast lysate system, these syntheses were markedly inhibited by all of them. The degree of the inhibition was usually more remarkable in DNA synthesis than in protein synthesis. One derivative, which was inactive against the strain but active against staphylococci, showed only the slight inhibition of DNA synthesis in intact cell system but did the marked inhibition of DNA and RNA syntheses in protoplast lysate system. The derivatives inactive against all bacteria tested showed no inhibition in intact cell system and no or relatively weak inhibition in protoplast lysate system. The results indicate that the inhibition of DNA synthesis is important for antibacterial activity of (5-nitro-2-furyl) vinylpyridine derivatives and the permeability of the derivatives into bacterial cells may have influence on the activity.View full abstractDownload PDF (896K) -
SHINICHI NAKAMURA, MASANAO SHIMIZU1973 Volume 21 Issue 1 Pages 137-143
Published: January 25, 1973
Released on J-STAGE: February 08, 2011
JOURNAL FREE ACCESSUsing 26 nitrofuran derivatives with various chemical structures, the inhibition of deoxyribonucleic acid (DNA), ribonucleic acid (RNA) and protein syntheses was examined in intact cell and protoplast lysate systems of Escherichia coli JG181. All the derivatives active against the strain inhibited DNA synthesis in the both systems. However, RNA and protein syntheses were inhibited by some of them in intact cell system and by all but one in protoplast lysate system. The derivatives inactive against the strain but active against staphylococci showed no inhibition in intact cell system although one of them inhibited DNA and RNA syntheses in protoplast lysate system. The derivatives inactive against all bacteria tested did not show inhibition at all in the both systems. Among the syntheses tested, the most inhibited was DNA synthesis and the degree of inhibition in intact cell system was closely correlated to antibacterial activity. The results indicate that the inhibition of DNA synthesis may be a common mechanism of antibacterial action of nitrofuran derivatives.View full abstractDownload PDF (5233K) -
YOSHIYUKI TAKASE, SHINICHI NAKAMURA, MASAMITSU ISHIYAMA, MASANAO SHIMI ...1973 Volume 21 Issue 1 Pages 144-148
Published: January 25, 1973
Released on J-STAGE: February 08, 2011
JOURNAL FREE ACCESSThe effect of nifurpirinol on deoxyribonucleic acid (DNA), ribonucleic acid (RNA) and protein syntheses was investigated in 2 strains of Escherichia coli. In the both strains these syntheses were all inhibited at the concentrations higher than the minimal inhibitory concentration against the strains. DNA and RNA syntheses were also inhibited at lower concentrations than the minimal inhibitory concentration where bacterial growth was temporarily suppressed. The most sensitive to nifurpirinol was DNA synthesis among the syntheses tested. The concentration and the time inhibiting DNA synthesis almost coincided to those inhibiting bacterial growth. The results indicate that the inhibition of DNA synthesis may be a mechanismof antibacterial action of nifurpirinol.View full abstractDownload PDF (731K) -
KENJI MAKINO, AKIRA YAGI, ITSUO NISHIOKA1973 Volume 21 Issue 1 Pages 149-156
Published: January 25, 1973
Released on J-STAGE: February 08, 2011
JOURNAL FREE ACCESSA new phenolic glucoside named aloearbonaside was isolated from the leaves of Aloe arborescens MILL. var. natalensis BERGER in addition to barbaloin. The structure of aloearbonaside was established as I, methyl 2-(5-methyl-7-hydroxy-4-0-β-D-glucopyranosy1)-chromenylideneacetate, a glucoside of a new type naturally occurring chromene, on the basis of spectral and chemical evidences.View full abstractDownload PDF (1205K) -
YOSHINORI KIDANI, MASAHIDE NOJI, HISASHI KOIKE1973 Volume 21 Issue 1 Pages 157-162
Published: January 25, 1973
Released on J-STAGE: February 08, 2011
JOURNAL FREE ACCESSThe syntheses of the mixed-ligand complexes between alloxan and glycine with bivalent metals (Cu, Ni, Co, Zn, Pb, and Cd) were made by mixing them in the ratios of 1: 1: 1 at pH 3 and by allowing to stand at a room temperature for about a week. The objective products deposited gradually. The separation from their parent complexes, i.e., bisglycinato metal complexes, were made by the differences of solubility in H2O. By decomposing the mixed-ligand complexes in 1N HCl, the constituents were identified by thinlayer chromatography with employing microcrystalline cellulose powder as an adsorbent and BuOH: AcOH: H2O (4: 1: 2) as a solvent mixture. The discussions as to the binding sites with the ligands were made from infrared (IR) spectra and the structures were postulated of the alloxan-metal-glycine and alloxan-Cu-glycylglycine complexes.View full abstractDownload PDF (983K) -
HIROMICHI SAEKI, YOSHIKAZU SHIMADA, NORIO KAWAKITA, BUNJI SHIMIZU, EIJ ...1973 Volume 21 Issue 1 Pages 163-170
Published: January 25, 1973
Released on J-STAGE: February 08, 2011
JOURNAL FREE ACCESSIt was found that lithium aluminum hydride reduction of Na, NG-disubstituted arginine lactam (3a-c) at a low temperature gave a corresponding argininal derivative (4a-c). Analogous reduction of acetyl-L-leucyl-L-leucyl-N-benzyloxycarbonyl-L-arginine lactam (8b) or its dipeptide analog (13) yielded leupeptin Ac-LL (1a) or acetylleucylargininal (11) respectively. Antiplasmin activities of these synthetic leupeptins were also reported.View full abstractDownload PDF (1415K) -
TATSUZO FUJII, TAKASHI SATO, TAKASHI HANZAWA1973 Volume 21 Issue 1 Pages 171-175
Published: January 25, 1973
Released on J-STAGE: February 08, 2011
JOURNAL FREE ACCESSCalcium and magnesium contents of whole erythrocytes and of erythrocyte membranes (stroma) were determined by atomic absorption technique on five mammalian species, man, rabbit, pig, cow and dog.
In every species, the magnesium content of the whole erythrocyte is predominantly higher than the calcium content. Of the total magnesium, about 2-6% are localized in the membrane, whereas 40-86% of the whole cell calcium are found in the membrane. Except that the magnesium content of bovine erythrocyte is remarkably lower (about 1/7) than those of the other species, there seems to be no big species difference in these cation contents in the whole erythrocytes.
The amounts of calcium localized in the membrane were found to be in a range of 1.5-2.6×10-18 mole per cell. The membrane magnesium contents vary considerably among the species examined and fall in a range of 1.6 (cow)-12 (dog)×10-18 mole per cell, with the intermediate values on the other three species of 4.0, 4.1 and 5.6×10-18 mole per cell. The membrane Mg/Ca molar ratios range between 0.65-6.5.
Intracellular concentrations of calcium and magnesium were calculated from the differences between the amounts in the whole cell and those in the membrane, assuming that no release of these cations occurs in the course of preparation of stroma.View full abstractDownload PDF (763K) -
TAKASHI SATO1973 Volume 21 Issue 1 Pages 176-183
Published: January 25, 1973
Released on J-STAGE: February 08, 2011
JOURNAL FREE ACCESSIt was confirmed that the lysolecithin contents of human erythrocyte membranes (stroma) can be varied remarkably depending on the plasma lysolecithin concentration in vitro and that simultaneously certain changes occur in the morphology of the whole cell as revealed by scanning electron microscopy, and also in the osmotic fragility of the membranes.
Incubation of erythrocytes in lysolecithin-rich plasma, prepared by the action of the plasma lecithin-cholesterol acyltransferase or of added phospholipase A of snake venom, resulted in remarkable increase in the lysolecithin content of the erythrocyte membranes and morphological changes in the erythrocytes from normal biconcave discs to crenated or spherical forms. The spherical cells, but not the crenated cells, showed increased osmotic fragility. After washing these lysolecithin-rich erythrocytes with serum albumin solution or with heated normal plasma, the erythrocyte lysolecithin content was restored almost to the normal level whereas the increased osmotic fragility still persisted.
Similar washes of the normal erythrocytes with albumin solution gave rise to about 43% decrease in the lysolecithin content, slight morphological change and also slight increase in the osmotic fragility. When these cells were incubated in heated normal plasma, the lysolecithin content was restored to the normal level, and at the same time both the slightly-altered shape and osmotic fragility were restored back to normal.
From these experimental findings, probable existence of two kinds of lysolecithin pools in human erythrocyte membranes and their roles in the maintenance of the membrane structure and functions were discussed.View full abstractDownload PDF (5088K) -
NAOKI SHIMIDZU, TOYOZO UNO1973 Volume 21 Issue 1 Pages 184-190
Published: January 25, 1973
Released on J-STAGE: February 08, 2011
JOURNAL FREE ACCESSA number of 2-, 4-and 7-substituted benzothiazole derivatives were synthesized to inquire into the relationship between the fluorescence of metal chelates and their structures, and to investigate their applications as analytical reagents. The color and fluorescence reactions of metal ions with these benzothiazole derivatives were investigated by spot tests. On the formation of metal complexes in solution, the color change of 2-substituted derivatives was more remarkable than that of 4-and 7-substituted. As fluorometric reagents for metal ions, however, 4-aminobenzothiazole derivatives were superior to 2-amino and 7-aminobenzothiazole derivatives. 7-Substituted derivatives were inferior in the reactivity with metal ions to 2-and 4-substituted.View full abstractDownload PDF (740K) -
KIYOSHI TATSUMI, TOSHIO OU, TOSHIRO YAMAGUCHI, HIDETOSHI YOSHIMURA1973 Volume 21 Issue 1 Pages 191-201
Published: January 25, 1973
Released on J-STAGE: February 08, 2011
JOURNAL FREE ACCESSThe factors influencing the absorption of nitrofuran derivatives from the rat gastrointestinal tract were examined using 14C-labeled AF-2, NF-161 and Nitrofurazone, and the following results were obtained.
1) The in vivo and in vitro studies revealed that the above compounds were degraded mainly in the mucosa of rat small intestine.
2) The in vivo absorption rate from the gastrointestinal tract and the in vitro permeability in everted sacs were lower in the degraded products than in the parent compounds.
3) In the case of 14C-NF-161, its solubility in the gastrointestinal tract affected partly the absorption rate of radioactivity.
From these results, it may be concluded that when 14C-nitrofuran derivatives are given to rat orally, the absorption rate of the radioactivity from the gastrointestinal tract has close relationship with the degradation of these compounds in the small intestinal mucosa, and in some cases with the solubility in the gastrointestinal tract.View full abstractDownload PDF (1609K) -
TORU KOIZUMI, YOSHIYUKI ARAI, EIICHI YOSHII1973 Volume 21 Issue 1 Pages 202-206
Published: January 25, 1973
Released on J-STAGE: February 08, 2011
JOURNAL FREE ACCESSThe reaction of o-phenylenediamine with phenylphosphorodichloridate was reexamined. Unlike Autenrieth and Bolli's report, 2-phenoxy-1, 3-dihydro-2H-1, 3, 2-benzodiazaphosphole 2-oxide (I) has not been obtained by their procedure. Instead, phenyl hydrogen N-(2-aminophenyl) phosphoroamidate (V) was obtained by the reaction in refluxing benzene. When the reaction was carried out by the fusion method, a roughly equal amount of V and o-phenylenediamine salt of diphenyl phosphate (VI) were isolated. The solubility and reactivity of both compounds V and VI were compared with those of the Autenrieth and Bolli's compound and it was concluded that their synthesis should be refuted. Finally the diazaphosphole I was synthesized by the reaction in bromobenzene and the properties of I was quite different from those of the Auterieth and Bolli's compound.View full abstractDownload PDF (819K) -
TSUNEO BABA, HIROSHI SUGIYAMA, SHUICHI SETO1973 Volume 21 Issue 1 Pages 207-209
Published: January 25, 1973
Released on J-STAGE: February 08, 2011
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Tozo FUJII, TOHRU SAITO, TAISUKE ITAYA, KENICHI YOKOYAMA1973 Volume 21 Issue 1 Pages 209-211
Published: January 25, 1973
Released on J-STAGE: February 08, 2011
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MAMORU KAMIYA, TAKEHIRO MITSUI, YUKIO AKAHORI1973 Volume 21 Issue 1 Pages 211-214
Published: January 25, 1973
Released on J-STAGE: February 08, 2011
JOURNAL FREE ACCESSDuring the course of numerous studies on phenothiazine radicals, it has been indicated by electron spin resonance (ESR) method that neutral phenothiazinyl radical which is rather unstable can be produced from phenothiazine by several methods. However, any work has not been published regarding the electronic absorption spectrum of these radicals. This may be chiefly because, as seen in general, measuring and assigning the spectrum of such unstable radical are seriously prevented from coexistence of various radical decay products. In this note we shall report the electronic absorption spectra of non-substituted and 1-methylsubstituted phenothiazinyl radicals which are generated in degassed dimethylsulfoxide-acetic anhydride mixture. By referring to the ESR spectra in the same systems and by performing theoretical calculations on the electronic transition of the radicals, a brief comment will be given to the assignment of the new absorption maxima in the electronic absorption spectra.View full abstractDownload PDF (559K) -
AKIÉ IJIMA, KIYOSHI TAKAHASHI1973 Volume 21 Issue 1 Pages 215-219
Published: January 25, 1973
Released on J-STAGE: February 08, 2011
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TETSUYA KONISHI, SIGEO BABA, HISAO SONE1973 Volume 21 Issue 1 Pages 220-224
Published: January 25, 1973
Released on J-STAGE: February 08, 2011
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YUJIRO MORI, TOSHIO KAWASAKI1973 Volume 21 Issue 1 Pages 224-227
Published: January 25, 1973
Released on J-STAGE: February 08, 2011
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AKIRA MORIMOTO, TETSUYA OKUTANI, KATSUTADA MASUDA1973 Volume 21 Issue 1 Pages 228-231
Published: January 25, 1973
Released on J-STAGE: February 08, 2011
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KOHEI FURUYA, Ko AIDA, YUKIKO Koiso, SHIGENOBU OKUDA1973 Volume 21 Issue 1 Pages 231-234
Published: January 25, 1973
Released on J-STAGE: February 08, 2011
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