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Volume 22, Issue 5
Displaying 1-39 of 39 articles from this issue
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CHIAKI MORIWAKI, YOSHIO HOJIMA, HIROSHI MORIYA1974 Volume 22 Issue 5 Pages 975-983
Published: May 25, 1974
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThough there are several assay methods for the kallikreins, there are neither standard units nor standard methods. The representative activities of kallikreins, such as the vasodilator, kinin forming and esterolytic activities, were determined by various methods on hog pancreatic, human salivary, urinary and plasma and guinea pig coagulating gland kallikreins and also on trypsin. Some enzymatic properties of these kallikreins were discussed from comparison of their activities, and the procedures of these assay methods were also examined in detail.View full abstractDownload PDF (1129K) -
1974 Volume 22 Issue 5 Pages 984-987
Published: May 25, 1974
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSDownload PDF (547K) -
TAMOTSU KOIZUMI, MICHIHIRO UEDA, MASAWO KAKEMI, JUICHIRO SHIBASAKI, SH ...1974 Volume 22 Issue 5 Pages 988-1002
Published: May 25, 1974
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSBlood concentration of unchanged N-phenylurea and the urinary excreted amount of its metabolites were determined periodically, after intravenous administration of N-phenylurea. Blood concentration time course of N-pheylurea observed was well explained by a pharmacokinetic model that assumes Michaelis Menten equation for hydroxylation step and a first order process for the metabolism of N-phenylurea other than hydroxylation. This result is analogous to that of acetanilide reported previously. In addition, elimination rate of acetanilide from the blood was affected and reduced by the simultaneous administration of N-phenylurea. It was proved that the hydroxylation process of these drugs was mutually inhibited. Computation of the theoretical values were carried out by means of an analog computer.View full abstractDownload PDF (1306K) -
YOSHIO ARATA, TETUO KIKUTI, MINEO TAKAHASHI, TADASHI AOKI1974 Volume 22 Issue 5 Pages 1003-1007
Published: May 25, 1974
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSReaction of Δ1, 10-hexahydroquinolizine (VI) with a combination of nitromethane and methyl iodide gave 5-methyl-10-nitromethyloctahydroquinolizinium iodide (VII), which, on treatment with lithium-liquid ammonia, gave the ten-membered ring amines, XIV and XV. Similar reduction of the N-acetyl methiodide (X) and the betaine (XI) derived from VII gave XVIII and XIX, respectively.View full abstractDownload PDF (621K) -
NOBUO AOYAGI, RYOHEI KIMURA, TOSHIRO MURATA1974 Volume 22 Issue 5 Pages 1008-1013
Published: May 25, 1974
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe compositions of the fractionized samples of Passiflora incarnata dry extract were investigated. Harmine was found in the ether soluble fraction by paper and thinlayer chromatographies. Maltol was isolated from the 2 N HCl soluble fraction. The pharmacological properties of Passiflora incarnata dry extract, the 2 N HCl soluble fraction, maltol and ethyl maltol were investigated. The 2 N HCl soluble fraction decreased the oxygene uptake by rat brain cortex slices at a high concentration. Maltol caused a depression in mice and showed potentiation on hexobarbital induced sleep, anticonvulsant action with such high doses as toxic, and inhibition on the spontaneous motor activity in mice with low doses. Ethyl maltol showed similar actions but more potent anticonvulsant avtivity and less potent inhibitory effects on the spontaneous motor activity.View full abstractDownload PDF (683K) -
EIJI OHKI, SADAO OIDA, YOSHIHIKO OHASHI, AKIRA YOSHIDA, KATSUO KAMOSHI ...1974 Volume 22 Issue 5 Pages 1014-1021
Published: May 25, 1974
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESS4β-Methoxy-4α-phenyl-3α, 5α-propanopiperidine derivatives were prepared and tested biologically. Introduction of a m-hydroxy substituent into the phenyl group of these derivatives results in radical potentiation of analgesic and antitussive activities. Also, some N-carbamates of these derivatives exhibit appreciable anti-inflammatory effects with analgesic activity.View full abstractDownload PDF (1088K) -
EIKO OHTSUKA, HISAYO TSUJI, MORIO IKEHARA1974 Volume 22 Issue 5 Pages 1022-1028
Published: May 25, 1974
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSN, 2'-O-Dibenzoyladenosine 3'-phosphate was polymerized using dicyclohexylcarbodiimide as the activating reagent to give linear and cyclic oligoadenylic acids. When 5'-O-monomethoxytrityl-N, 2'-O-dibenzoyladenosine 3'-phosphate was added as the chain terminator linear oligoadenylic acids were obtained as major products. Cyclic di- and triadenylic acids were also synthesized by cyclization of the corresponding linear oligonucleotides and were found to be sensitive to RNase M. Their CD spectra were measured in aqueous and methanolic solution.View full abstractDownload PDF (736K) -
CHIAKI MORIWAKI, KEIKO YAMAGUCHI, HIROSHI MORIYA1974 Volume 22 Issue 5 Pages 1029-1034
Published: May 25, 1974
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSA perfusion with Krebs-Ringer solution containing dextran through the mesenteric vascular system was performed on rat to which 131I-labelled α-chymotrypsin was administered in the jejunum. This method sufficed for the purpose of eliminating various blood components, such as the inhibitors for the enzyme, which interfer with quantitative assay of a small amount of the enzyme absorbed. Using the method, the non-diffusible 131I-bound substance (s) and N-acetyl-L-tyrosine ethyl ester (ATEE)-hydrolyzing activity were found in the mesenteric perfusates of the rats, and the amount of the enzyme absorbed during 90 min was estimated to be about 0.6% of the infused dose. Furthermore, when the immunoreactivity with the antiserum against α-chymotrypsin was examined on the mesenteric perfusate, a precipitin band sharply indicating the enzyme was formed with the perfusate collected during the first 30 min after the administration. These results strongly suggest that small but significant amount of α-chymotrypsin is transmitted across the intestinal wall into the mesenteric vascular system as retaining its enzymic and immunochemical properties.View full abstractDownload PDF (804K) -
MASAMICHI FUKUOKA, SHINSAKU NATORI1974 Volume 22 Issue 5 Pages 1035-1040
Published: May 25, 1974
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe "anthrasteroid"-type rearrangement of bauera-7, 9 (11)-dienyl acetate (1) was reexamined and the product was proved not to be 2 but to be expressed by 6. The aromatisation reaction was applied for 7, 9 (11)-dienes (13, 14, 15, 16) of tirucallane, lanostane, fernane, and arborane series and the same type of hydrocarbons (17, 18, 19, 20) were obtained in good yields.View full abstractDownload PDF (719K) -
TETSUYA KAMATAKI, HARUO KITAGAWA1974 Volume 22 Issue 5 Pages 1041-1045
Published: May 25, 1974
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSEffects of ethylenediamine tetraacetic acid (EDTA) on aging-induced changes in activities of drug metabolizing enzymes were investigated. Aging of microsomes at 45° produced a reduction of lipid peroxidation while aging of 9000×g supernatant fraction at 45° resulted in a marked increase in the formation of lipid peroxides. From this finding, it was assumed that there might be heat stable stimulator of lipid peroxidation in addition to the heat labile inhibitor of lipid peroxidation which was found recently by us. EDTA completely prevented the inactivation of aniline hydroxylase and aminopyrine N-demethylase when rat liver 9000×g supernatant fraction was aged at 45°. When rat liver 9000×g supernatant fraction and microsomes were aged at 5° aerobically, activity of ethylmorphine N-demethylase was decreased and, inversely, amount of lipid peroxides formed during aging was increased. EDTA effectively inhibited the lipid peroxidation and decrease in ethylmorphine N-demethylase activity. The close relationship between lipid peroxidation and activity of ethylmorphine N-demethylase was confirmed using NADPH-generating system and ferrous ion as stimulators of lipid peroxidation.View full abstractDownload PDF (623K) -
HIROSHI MITSUHASHI, YUZURU SHIMIZU, TOMOTAKA MORIYAMA, MITSURU MASUDA, ...1974 Volume 22 Issue 5 Pages 1046-1052
Published: May 25, 1974
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe rearrangement of 3β, 20β-dihydroxy-5α-pregnan-12-one derivatives to C-nor-D-homosteroid was studied by several methods, and a few new methods were devised.View full abstractDownload PDF (712K) -
TOHRU HINO, TOSHIKAZU SUZUKI, MASAKO NAKAGAWA1974 Volume 22 Issue 5 Pages 1053-1060
Published: May 25, 1974
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe thione-thiol tautomerism and the oxidation of the 2-indolinethione have been studied. The ultraviolet (UV) and nuclear magnetic resonance spectra of 3-aryl-2-indoline-thiones disclosed the predominance of their thiol form in various solvents, while the oxo form was the sole species in the 3-phenyloxindole. However, the spectral data of 1-methyl-3-aryl-2-indolinethiones showed the predominance of the thione form in solution. The oxidation of the 2-indolinethiones with oxygen to the corresponding disulfide in EtOH has been followed by the oxygen uptake and the UV spectral change. The oxidation of 3-(p-nitrophenyl)-2-indolinethiones (5 and 9) was very rapid, while 3-tert-butyl-(14), 1-methyl-(11), and 2-indolinethione (10) resisted the oxidation. Other 2-indolinethiones were oxidized to the disulfide at moderate speed. The prolonged oxidation of 11 gave a small amount of 3-oxo-2-indolinethione (18) instead of the disulfide.View full abstractDownload PDF (843K) -
HARUAKI YAJIMA, YOSHIAKI KISO1974 Volume 22 Issue 5 Pages 1061-1066
Published: May 25, 1974
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe protected dodecapeptide, Z-Arg (NO2)-Pro-Asp (OBzl)-Phe-Cys (Bzl)-Leu-Glu-(OBzl)-Pro-Pro-Tyr-Thr-Gly-OH, corresponding to positions 1 to 12 of the basic trypsin inhibitor from bovine pancreas (Kunitz and Northrop) was synthesized. The synthesis was achieved by condensation of three peptide subunits, Z-Arg (NO2)-Pro-OH, Z (OMe)-Asp (OBzl)-Phe-Cys (Bzl)-Leu-Glu (OBzl)-Pro-OH and H-Pro-Tyr-Thr-Gly-OH with pentachlorophenyl trichloroacetate.View full abstractDownload PDF (818K) -
HARUAKI YAJIMA, YOSHIO OKADA, HIDEHIKO WATANABE, YOSHIAKI KISO1974 Volume 22 Issue 5 Pages 1067-1074
Published: May 25, 1974
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe protected hexadecapeptide, Z (OMe)-Pro-Cys (Bzl)-Lys (Z)-Ala-Arg (Tos)-Ile-Ile-Arg (Tos)-Tyr-Phe-Tyr-Asn-Ala-Lys (Z)-Ala-Gly-OH, corresponding to positions 13 through 28 of the basic trypsin inhibitor (Kunitz and Northrop) was synthesized by the successive azide coupling of four peptide subunits, H-Asn-Ala-Lys (Z)-Ala-Gly-OH, Z (OMe)-Tyr-Phe-Tyr-NHNH2, Z (OMe)-Ala-Arg (Tos)-Ile-Ile-Arg (Tos)-NHNH2 and Z (OMe)-Pro-Cys (Bzl)-Lys (Z)-NHNH2.View full abstractDownload PDF (1059K) -
HARUAKI YAJIMA, NARIAKIRA MIZOKAMI, MICHIKO KISO, TOORU JINNOUCHI, YOS ...1974 Volume 22 Issue 5 Pages 1075-1078
Published: May 25, 1974
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe protected nonapeptide, Z (OMe)-Leu-Cys (Bzl)-Gln-Thr-Phe-Val-Tyr-Gly-Gly-OH, corresponding to positions 29 to 37 of the basic trypsin inhibitor (Kunitz and Northrop), was synthesized by the azide coupling of Z (OMe)-Leu-Cys (Bzl)-Gln-Thr-NHNH2 and H-Phe-Val-Tyr-Gly-Gly-OH.View full abstractDownload PDF (642K) -
HARUAKI YAJIMA, YOSHIAKI KISO, KOUKI KITAGAWA1974 Volume 22 Issue 5 Pages 1079-1086
Published: May 25, 1974
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe protected nonadecapeptide and the C-terminal dipeptide corresponding to positions 38 through 56 and 57-58 of the basic trypsin inhibitor from bovine pancreas were prepared. Synthesis of the protected nonadecapeptide, Z (OMe)-Cys (Bzl)-Arg (Tos)-Ala-Lys (Z)-Arg (Tos)-Asn-Asn-Phe-Lys (Z)-Ser-Ala-Glu (OBzl)-Asp (OBzl)-Cys (Bzl)-Met-Arg (Tos)-Thr-Cys (Bzl)-Gly-OH, was achieved by condensation of three subunits : Z (OMe)-Cys (Bzl)-Arg (Tos)-Ala-Lys (Z)-Arg (Tos)-NHNH2 (positions 38-42), Z (OMe)-Asn-Asn-Phe-Lys (Z)-Ser-Ala-NHNH2 (positions 43-48) and Z (OMe)-Glu (OBzl)-Asp (OBzl)-Cys (Bzl)-Met-Arg (Tos)-Thr-Cys (Bzl)-Gly-OH (positions 49-56). The C-terminal dipeptide was prepared in a form of Z (OMe)-Gly-Ala-OH.View full abstractDownload PDF (1128K) -
HARUAKI YAJIMA, YOSHIAKI KISO1974 Volume 22 Issue 5 Pages 1087-1094
Published: May 25, 1974
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSFive protected peptide subunits which cover the entire 58 amino acid residues of the bovine pancreatic basic trypsin inhibitor, i.e., Z-Arg (NO2)-Pro-Asp (OBzl)-Phe-Cys (Bzl)-Leu-Glu (OBzl)-Pro-Pro-Tyr-Thr-Gly-OH (I, positions 1-12), Z (OMe)-Pro-Cys (Bzl)-Lys (Z)-Ala-Arg (Tos)-Ile-Ile-Arg (Tos)-Tyr-Phe-Tyr-Asn-Ala-Lys (Z)-Ala-Gly-OH (II, positions 13-28), Z (OMe)-Leu-Cys (Bzl)-Gln-Thr-Phe-Val-Tyr-Gly-Gly-OH (III, positions 29-37), Z (OMe)-Cys (Bzl)-Arg (Tos)-Ala-Lys (Z)-Arg (Tos)-Asn-Asn-Phe-Lys (Z)-Ser-Ala-Glu (OBzl)-Cys (Bzl)-Met-Arg (Tos)-Thr-Cys (Bzl)-Gly-OH (IV, positions 38-56), Z (OMe)-Gly-Ala-OH (V, positions 57-58), were successively assembled on the polymer support by means of dicyclohexylcarbodiimide plus N-hydroxysuccinimide. In each step, the Z (OMe) group was deprotected by trifluoroacetic acid and the unreacted amino component on the resin was masked by acetylation. After deblocking of all protecting groups by HF and subsequent oxidation followed by affinity chromatographic purification, a highly active peptide, specific activity 82%, indistinguishable from the natural bovine pancreatic basic trypsin inhibitor, was isolated.View full abstractDownload PDF (1133K) -
SHIGERU AONUMA, TADANORI MAYUMI, TAMIO NOGUCHI, KOJI SUZUKI, MASARU OK ...1974 Volume 22 Issue 5 Pages 1095-1101
Published: May 25, 1974
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSIt was demonstrated that rabbit spermatozoa was acquired the fertilizing capacity in estrous uterus. And this capacitated spermatozoa was inhibited to penetrate into the ova treating with seminal plasma. In the present report, to clear these phenomena from the biochemical aspect, it was studied that how respiration and anaerobic fructolysis of guinea pig spermatozoa were influenced by the uterine environment and uterine extract. 1) Guinea pig spermatozoa incubated in estrogen dominated uterus shows much greater respiration and anaerobic fructolysis activity than that of incubated in progesterone dominated uterus. 2) Treatment with seminal plasma caused great inhibition of respiratory activity of spermatozoa that was incubated in estrogen dominated uterus. 3) Respiration and anaerobic fructolysis stimulating factor of guinea pig spermatozoa was extracted from the estrogen treated guinea pig uterus. And from bovine uterus the same stimulating factor (a protein of approximately 50000 molecular weight estimated from the behavior on Sephadex G-75 gel filtration). 4) This bovine uterine extract recovered or accelerate the low respiratory activity of the spermatozoa for the existence of seminal plasma. From these results, it is suggested that the extract from the guinea pig and bovine uterus might play a major role in sperm respiration and anaerobic fructolysis, and further be related to capacitation process in estrous uterus.View full abstractDownload PDF (769K) -
SHIGEO UKAI, KAZUO HIROSE, TADASHI KIHO, CHIHIRO HARA1974 Volume 22 Issue 5 Pages 1102-1107
Published: May 25, 1974
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSPolysaccharides have been isolated from the fruit bodies of Tremella fuciformis BERK, which grows in Japan and China. Some chemical and physical properties of these polysaccharides (AC and BC : from Chinese fungus ; AJI and BJ : from Japanese fungus) were examined. The polysaccharides were homogeneous as judged by gelfiltration (Sepharose 4B), electrophoresis (Zone and Tiselius), and ultracentrifugal analysis. These polysaccharides are acidic heteroglycans composed mainly of xylose, glucuronic acid and mannose, and contain acetyl groups in their molecules (the molar ratios of them are given in Table II). The chemical properties of BC were closely similar to those of BJ in the numerical values of elemental analyses, component sugar content and acetyl content. However, significant differences were observed between BC and BJ in the physical properties, such as intrinsic viscosity, sedimentation coefficient and molecular weight.View full abstractDownload PDF (912K) -
HIROSHI KISHIMOTO, KUNIHARU SUMIDA1974 Volume 22 Issue 5 Pages 1108-1118
Published: May 25, 1974
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSFor the elucidation of molecular behaviors of surfactant solutions from the view-point of thermodynamic parameters, the standard heats of solution and micelle formation per mole of sodium dodecyl sulfate (NaDS), typical anionic surfactant, or ΔH°sol and ΔH°m were determined by calorimetry in the wide range of temperature from 20° to 45°, with parallel experiments determining critical micelle concentration by conductivity measurement and degree of Na+ ion dissociation on micelle by electromotive force measurement using Na+ ion responsive electrode. From the values of both the standard heats, the standard enthalpies of NaDS in monomeric and micellar states, H°mono and H°mie, were calculated on the relative base of standard enthalpy of solid state. The change of these values with temperature gave ca. 120 and 16 cal deg-1 mole-1 to the increases of the standard partial molar heat capacity of NaDS on transferring from solid state to monomeric and micellar states, i.e. ΔC°p (solid→mono, NaDS) and ΔC°p (solid→mic, NaDS), respectively. By applying a simple additivity rule, it was concluded that the change of heat capacity of the paraffin portion of NaDS plays an important role in the above-mentioned ΔC°ps, implying the formation of hydrophobic interaction between the paraffin portion and water. With other experimental data, also the systematic description of surfactant solution was done in thermodymanic terms.View full abstractDownload PDF (1243K) -
OSAMU MATSUDA, KEIICHI ITO, MINORU SEKIYA1974 Volume 22 Issue 5 Pages 1119-1125
Published: May 25, 1974
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSOn the reaction of N-(dialkylaminomethyl) imides and -amides with nucleophiles the previous papers have exhibited the substitution of the imide or the amide residue and that of the dialkylamine residue. Although the actual substitution has been shown to depend on the substrate and the reaction condition, preferential substitution site of the substrate and how this is influenced by the reaction condition have been still in the dark. In pursuit of the substitution reaction of N-(piperidinomethyl) phthalimide, -succinimide and -benzamide it has been presumed that the substitution of the imide or amide residue is processed directly and the substitution of the piperidine residue is processed by succeeding secondary substitution or through elimination of piperidine, if possible, followed by addition of nucleophiles.View full abstractDownload PDF (709K) -
YASUHIRO YAMANE, KAZUO SAKAI1974 Volume 22 Issue 5 Pages 1126-1132
Published: May 25, 1974
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe effect of copper on the metabolism of 4-dimethylaminoazobenzene (DAB) in rat liver was examined, comparing with those of manganese, nickel, and zinc. Copper had the highest effect, followed by manganese, and the effect of nickel was slightly higher than or almost comparable to that of the control group. The effect of zinc gave almost the same or slightly lower activity as the control group. The effect of copper on the activity of DAB metabolism was observed in the microsomal fraction of the rat liver, and the elevation of activity was found with the increase of copper content in the microsomes. The fact seems to indicate that copper plays some role in elevating the metabolic activity. It was also found that the effect of copper on DAB metabolism concerned the elevations of azo reductase activity and ring hydroxylase activity.View full abstractDownload PDF (737K) -
ATSUSHI MURAKAMI, YUKIO AKAHORI1974 Volume 22 Issue 5 Pages 1133-1139
Published: May 25, 1974
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe computer experiment was applied on the calculation of sterically allowed conformations of tri-(p-bromobenzoate) of methyl ester of prostaglandin F1β in order to accumulate conformational informations of prostaglandins and develop a useful calculation method which could be applied on compounds containing saturated chains. Eightyfour forms of sterically allowed conformations were found. Calculations on the conformational energies of each of these conformations were carried out in order to find the conformation with the lowest energy and to research the relationships between sterically allowed conformations and their conformational energies. The calculation on the energies were restricted to the nonbonded and electrostatic energies, and the sum of them was approximated as the conformational energy. In this calculation, the values of van der Waals radii were parametrized and the effects on the conformations were discussed in detail. Different conformations of the lowest energy were given by the different values of van der Waals radii. The geometrical properties of the most stable conformation that were calculated using larger values of van der Waals radii than the usual values were identical with the information from X-ray diffraction study on prostaglandin F1β derivative.View full abstractDownload PDF (795K) -
JUNICHI GOTO, KENICHI SUDO, TOSHIO NAMBARA1974 Volume 22 Issue 5 Pages 1140-1144
Published: May 25, 1974
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSIn order to examine the physiological activity the preparation of 3, 17-dihydroxy-19-nor-13α-pregna-1, 3, 5 (10)-trien-20-one 17-acetates (IIId, IXc) has been undertaken. The Grignard reaction of 13α-estrone (I) with ethynylmagnesium bromide provided two epimeric 17-ethynyl-17-ols (II, VIIIa), which on hydration were led to 3, 17-dihydroxy-19-nor-13α-pregnatrien-20-ones (IIIa, IXa). Elucidation of the stereochemistry at C-17 was attained by the degradative means. First, IIIa was submitted to metal hydride reduction, usual acetylation followed by Serini reaction to afford 19-nor-13α-pregnatrien-20-one (V). Upon treatment with base V was readily transformed into the thermody-namically much more stable 17α-epimer (VIb), whose structure was confirmed by leading to the known 13α-estratriene-3, 17α-diol (VIIa) employing Baeyer-Villiger reaction. The desired compounds were unequivocally obtained from the 3, 17-diacetates (IIIc, IXb) by partial hydrolysis, respectively.View full abstractDownload PDF (698K) -
HIROMICHI SAEKI, YOSHIKAZU SHIMADA, YOSHIHIKO OHASHI, MASAZO TAJIMA, S ...1974 Volume 22 Issue 5 Pages 1145-1150
Published: May 25, 1974
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSIn order to overcome butirosin-resistant microorganisms of 3'-O-phosphorylation type, 3', 4'-dideoxybutirosin A (2) was synthesized according to the method of Umezawa, et al. The synthesized 3', 4'-dideoxy derivative (2) exhibited significant activities agaisnt both butirosin-sensitive and resistant strains in vitro and in vivo and its acute toxicity was found to be at a similar level to that of butirosin.View full abstractDownload PDF (699K) -
HIROMICHI SAEKI, YOSHIKAZU SHIMADA, YOSHIHIKO OHASHI, SHINICHI SUGAWAR ...1974 Volume 22 Issue 5 Pages 1151-1158
Published: May 25, 1974
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESS1-N-[(S)-4-Amino-2-hydroxybutyryl]-neamine (3) derived from butirosin, an aminoglycoside antibiotic, has been chemically modified in its amide side chain. The N-benzenesulfonyl derivative (5) was hydrazinolysed and the resulting amine (6) was reacylated with another amino and/or hydroxy carboxylic acid. Removal of benzenesulfonyl groups were carried out with sodium in liquid ammonia, giving several kinds of analogues. In addition, an hydroxy epimer (31) and amino varients (25 and 30) in the α-position of the amide side chain of 3 were prepared starting from tetra-N-mono-O-benzenesulfonyl derivative (23). Antibacterial activity of these analogues were tested and discussed.View full abstractDownload PDF (976K) -
AKIRA YAGI, KENJI MAKINO, ITSUO NISHIOKA1974 Volume 22 Issue 5 Pages 1159-1166
Published: May 25, 1974
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe constituents of fresh young subterranean stem of Aloe saponaria HAW. were examined to give six pigments ; aloesaponols I, -II, aloesaponarins I, -II, laccaic acid D methyl ester and desoxyerythrolaccin. On the basis of the spectral and chemical evidences the structures of aloesaponols I, -II and aloesaponarins I, -II were established to be I, II, IV and VI, respectively, in relation with laccaic acid D methyl ester (III) and desoxyerythrolaccin (V). Aloesaponols I, and -II were the first tetrahydroanthracene homologue obtained from the higher plant.View full abstractDownload PDF (1028K) -
TOSHIO NAMBARA, MASAKI TAKAHASHI, MITSUTERU NUMAZAWA1974 Volume 22 Issue 5 Pages 1167-1173
Published: May 25, 1974
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSIn order to obtain much more specific antiserum required for radioimmunoassay of estradiol, the preparation of new promising haptens has been undertaken. First, the C-6 epimeric 6-hydroxyestradiol 3, 17-bis (tetrahydropyranyl) ethers (VIII, XI) were treated with succinic anhydride and pyridine in the usual manner, respectively. Subsequent removal of the protecting groups provided the desired 6-hydroxyestradiol 6-hemisuccinates (X, XIII). Secondly, 7α-hydroxyestradiol 7-hemisuccinate (XXIII) has been also synthesized from 6-dehydroestradiol (XIV) by way of the 6α, 7α-epoxide (XVIII) as a key intermediate. Reductive cleavage of the 6, 7-oxido ring with metal hydride yielded solely the 7α-hydroxyl compound (XIX). Transformation into the 7-hemisuccinate (XXI) followed by elimination of the protecting group afforded XXIII in a satisfactory yield.View full abstractDownload PDF (939K) -
EIICHI FUJIHIRA, TAKASHI OHSHIMA, ISAMU USHIODA, NORIMITSU TAKAHASHI1974 Volume 22 Issue 5 Pages 1174-1178
Published: May 25, 1974
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSFeeding of a synthetic, vitamin B6-deficient diet for 7 weeks caused a marked increase in the ratio of glycine- to taurine-conjugated bile acids in the bile of rats. The highly elevated ratio, however, was reduced spontaneously by the elapsing time of biliary drainage, and the decrease in the ratio was accelerated by a subcutaneous administration of 2 g/kg of taurine. An intravenous injection of 5 mg/kg of sodium deoxycholate caused a temporary increase in the biliary secretion of taurodeoxycholic acid in both groups of normal and vitamin B6-deficient animals, and taurine loading prior to the deoxycholate-injection further augmented the increased secretion of this taurine-conjugated bile acid fraction. The glycodeoxycholic acid secretion in vitamin B6-deficient rats was not increased significantly after the deoxycholate-injection.View full abstractDownload PDF (607K) -
SHIGEO SENDA, KOSAKU HIROTA, JIYOJI NOTANI1974 Volume 22 Issue 5 Pages 1179-1185
Published: May 25, 1974
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSAs a part of our studies on the structure-activity relationship of 1, 3-disubstituted 5-dialkylamino-6-methyluracil derivatives, we have synthesized 1, 3-disubstituted 5-dialkylaminomethyl-6-methyluracils (B). In the synthesis, 1, 3-disubstituted 5-cyano-uracils (1-6) were hydrogenated with Raney-cobalt followed by methylation to give the 5-dimethylaminomethyluracil compounds (16-20). The Mannich reaction of 1, 3-disubstituted uracils (23-26, 33) did not proceed, but halogenomethylation of them and subsequent amination gave the 5-dialkylaminomethyl compounds (20, 34-41). As to their pharmacological activities, analgetic, antipyretic and antiinflammatory activities and acute toxicity were tested. The compounds (B) showed only antiinflammatory activity.View full abstractDownload PDF (764K) -
TSUKINAKA YAMANA, AKIRA TSUJI, YUZO MIZUKAMI1974 Volume 22 Issue 5 Pages 1186-1197
Published: May 25, 1974
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSThe kinetics of the hydrolyses of carbenicillin, sulbenicillin, propicillin, cyclacillin, 6-(α-toluenesulfonamido)-penicillanic acid (TSPA), the substituted phenylpenicillins and 6-aminopenicillanic acid (6-APA) were studied over wide pH ranges at 35° and μ=0.5. For the hydrolysis of penicillins, the psuedo first-order rate constants, kpH at zero buffer concentration were formulated as the equation : kpH=(kH [H3O+]+k0)ƒHP+(k'0+k'OH [OH-])ƒp-, where ƒHP and ƒp- are the fractions of free-acid penicillin (HP) and ionized penicillin (P-), respectively. These catalytic rate constants were compared with those reported previously for other penicillins. The activation parameters were also determined for some penicillins. In acidic solution, penicillins except TSPA were confirmed to be hydrolyzed to the penicillenic acids via hydronium ion-catalyzed rearrangement of HP the (kH) and spontaneous rearrangement of HP (k0). The Hammett plots for kH and k0 of the substituted phenylpenicillin series gave excellent linear correlations with both ρ=-1.60. The magnitude and sign of the ρ values were consistent with the intramolecular catalyzed mechanism by the neighboring side-chain amido groups. The hydrolysis of 6-APA was found to follow first-order kinetics at low initial concentration in the range of 0.005-0.01M. From the log kpH-pH profile and the pertinent primary salt effects, the possible mechanisms for the acidic hydrolysis of 6-APA were discussed. The activation parameters were evaluated at each reaction region. At pH 5, 6-APA was found to be hydrolyzed 3-6 times faster than relatively acid-stable penicillins, which may be attributed to the inductive effect by the protonated 6-amino group. The k'0 and k'OH values were nearly the same in the hydrolyses of all penicillins and 6-APA. It can be concluded that the basic and neutral hydrolyses of these compounds are, respectively, simple hydroxide catalyzed and water catalyzed reactions.View full abstractDownload PDF (1183K) -
YOSHIHISA MIZUNO, YOSHIBUMI WATANABE, KAZUYOSHI IKEDA1974 Volume 22 Issue 5 Pages 1198-1200
Published: May 25, 1974
Released on J-STAGE: March 31, 2008
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SHUICHI TAKAYAMA, FUJIO ASHIZAWA, JIRO SUZUKI, MINORU SEKIYA1974 Volume 22 Issue 5 Pages 1200-1202
Published: May 25, 1974
Released on J-STAGE: March 31, 2008
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YASUMITSU TAMURA, JUNICHI MINAMIKAWA, OSAMU NISHIKAWA, MASAZUMI IKEDA1974 Volume 22 Issue 5 Pages 1202-1203
Published: May 25, 1974
Released on J-STAGE: March 31, 2008
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KOICHI SHUDO, TOSHIHIKO OKAMOTO1974 Volume 22 Issue 5 Pages 1204-1205
Published: May 25, 1974
Released on J-STAGE: March 31, 2008
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TETSUZO KATO, HIROSHI YAMANAKA, TAKAO SAKAMOTO, TAKAYUKI SHIRAISHI1974 Volume 22 Issue 5 Pages 1206-1208
Published: May 25, 1974
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSDownload PDF (428K) -
HIDEO BANDO, KOJI HAYASHI, YOSHIKO KITAICHI, HIROSHI MITSUHASHI1974 Volume 22 Issue 5 Pages 1209-1211
Published: May 25, 1974
Released on J-STAGE: March 31, 2008
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RYOJI KASAI, KEIKO SHINZO, OSAMU TANAKA, KENICHI KAWAI1974 Volume 22 Issue 5 Pages 1213-1216
Published: May 25, 1974
Released on J-STAGE: March 31, 2008
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MIYOJI HANAOKA, HIRONORI SASSA, CHIEKO SHIMEZAWA, YOSHIO ARATA1974 Volume 22 Issue 5 Pages 1216-1217
Published: May 25, 1974
Released on J-STAGE: March 31, 2008
JOURNAL FREE ACCESSDownload PDF (323K)
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