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AKIRA OKURA, TADATOSHI KINOSHITA, NOBUO TANAKA
1971 Volume 24 Issue 10 Pages
655-661
Published: October 25, 1971
Released on J-STAGE: April 12, 2006
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Fusidic acid increases the binding of GTP with ribosomes and G factor. GTPis hydrolyzed to GDPin the complex with or without the antibiotic. Fusidic acid binds with G factor in a molar ratio of 1: 1 with an association constant 1.2×10
5M
-1. The binding is strongly stimulated by ribosomes and GTP. Formation of fusidic acid-G factor-GDP-ribosome complex is demonstrated by equilibrium dialysis and ultracentrifugal separation methods. Measurements of binding at equilibrium indicate a stoichiometric combination of thefoursubstances in a molarratio of 1: 1: 1: 1, provided that half of the ribosomes employed are active in this function. The association constant of fusidic acid is 2.2×10
6 M
-1. Less binding of the antibiotic is observed when fusidic acid-resistant G factor is used. A significant binding of fusidic acid is demonstrated when 70S ribosomes are replaced by 50S ribosomes or when GDP is used instead of GTP. Ki value for fusidic acid is 10
6M in the GTPase reaction. It is in accordance with the association constant in the complex formation.
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HYOZO TANIYAMA, YOSUKE SAWADA, TSUNEHIRO KITAGAWA
1971 Volume 24 Issue 10 Pages
662-666
Published: October 25, 1971
Released on J-STAGE: April 12, 2006
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Partial hydrolysis of streptothricin was most readily carried out in dilute acid solution. The hydrolysate had no antimicrobial activity, and its toxicity was six times that of streptothricin. From this inactive substance the original active antibiotic was regenerated with dicyclohexylcarbodiimide.
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BILIARY EXCRETION AND METABOLISM OF 14C-CEPHACHLOMEZINEAND ITS PARENT COMPOUND
MASAO OKUI, KIYOSHI HATTORI, MINORU NISHIDA
1971 Volume 24 Issue 10 Pages
667-674
Published: October 25, 1971
Released on J-STAGE: April 12, 2006
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The excretion and metabolic fate of two cephalosporin antibiotics, cephachlomezine (CEC), and its parent compound,
m-chlorophenyl-acetamidocephalosporanic acid (
m-Cl-PACA), was studied in rats, with emphasis being placed on biliary excretion and serum protein binding. When
14C-
m-Cl-PACAwas given intramuscularly, about 40 percent of the administered radioactivity was found in the bile, which contained only 1.6 %of the administered antibiotic activity.
Lactone of
m-Cl-PACA, one of the metabolites of
m-Cl-PACA, has beei isolated in a crystalline form as a result of hydrolysis by citrus acetylase. After a single intramuscular administration of
14C-CEC, more than 60 % of the administered dose was excreted in urine in the unchanged form and 15 % was recovered either in the bile as shown by radioassay or in microbioassay. Orally administered
14C-CEC underwent suspected degradation in the gut. Binding of CECand
m-Cl-PACAto serum protein was examined by means of an ultra filtration technique chiefly in relation to the biliary excretion.
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V. QUANTITATIVE DETERMINATION OF MAGROTETROLIDEANTIBIOTICS
KOJI SUZUKI, YOSHIHARU NAWATA, KUNIO ANDO
1971 Volume 24 Issue 10 Pages
675-679
Published: October 25, 1971
Released on J-STAGE: April 12, 2006
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Amethod for quantitative determination of tetranactin and other macrotetrolide antibiotics is presented. The assay is based on the complex formation of the antibiotics with sodium picrate followed by extraction of the complexes into an organic solvent. The macrotetrolide antibiotics can be determined by the present method with accuracy and simplicity in the assay range of l-40 μg/ml.
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ISOLATION AND PROPERTIES OF TUBERACTINOMYCIN-N, A NEW TUBERACTINOMYCIN GROUP ANTIBIOTIC
TAKUJI ANDO, KAZUO MATSUURA, ROKURO IZUMI, TOSHIHARU NODA, TERUO TAKE, ...
1971 Volume 24 Issue 10 Pages
680-686
Published: October 25, 1971
Released on J-STAGE: April 12, 2006
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A new basic peptide antibiotic of the tuberactinomycin group has been isolated from the culture broth of an artificial mutant derived from the streptomyces producing tuberactinomycin
1). The antibiotic, named tuberactinomycin-N, showed somewhat stronger antituberculous activity and lower ototoxicity than the tuberactinomycin obtained from the parent strain. The isolation, characterization and properties of tuberactinomycin-N are described in this paper.
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TAKAAKI AOYAGI, SETSUKO KUNIMOTO, HAJIME MORISHJMA, TOMIO TAKEUCHI, HA ...
1971 Volume 24 Issue 10 Pages
687-694
Published: October 25, 1971
Released on J-STAGE: April 12, 2006
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Pepstatin is shown to be a specific inhibitor of acid proteases. It also inhibits humangastricsin, but the effect is weaker than against humanpepsin. The content of pepsin and gastricsin in gastric juice of stomach ulcer patients is described and the pepstatin which remains in gastric juice collected at 60 minutes after its administration is also determined. These results and those obtained by the direct measurements of the peptic activity of the gastric juice indicate that a sufficient amount of pepstatin to inhibit pepsin remains in the gastric juice 60 minutes after oral administration. The peptic activity of gastric juice is 0-9.8% of the activity of the gastric juice collected before the administration of pepstatin. A method of testing for peptic activity of gastric juice containing pepstatin is described. Free and bound sialic acid in gastric juice of pylorus-ligated rats treated with pepstatin is determined, and pepstatin was shown to inhibit release of bound sialic acid from the mucous membrane. The activity of pepstatin derivatives are described.
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R. RAAP
1971 Volume 24 Issue 10 Pages
695-703
Published: October 25, 1971
Released on J-STAGE: April 12, 2006
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α-Amino-4-isothiazolylacetic acid has been prepared by reaction of α-bromo-4-isothiazalylacetic acid with ammonium hydroxide and by catalytic hydrogenation of α-azido-4-isothiazolylacetic acid. The α-azido acid has been resolved into its two optical isomers from which the optically active amino acids were prepared. The absolute configurations of these amino acids are tentatively assigned. The dextrorotatory isomer can also be prepared directly by resolution of the racemic amino acid with
d-camphor-10-sulfonic acid. From the optically active amino acids the penicillins were synthesized by the activated ester method using the
p-nitrocarbobenzoxy protecting group. Some MIC and CD
50 values against Gram-positive and Gram-negative bacteria are given. The introduction of an α-amino group into 4-isothiazolylmethylpenicillin produces only a minimal effect in the Gram-negative activity.
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1. MICROBIAL TRANSFORMATION OF ANTIMYCIN A
Kartar Singh, Sumanas Rakhit
1971 Volume 24 Issue 10 Pages
704-705
Published: October 25, 1971
Released on J-STAGE: April 12, 2006
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Nobuyoshi Machiyama
1971 Volume 24 Issue 10 Pages
706-707
Published: October 25, 1971
Released on J-STAGE: April 12, 2006
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HYOZO TANIYAMA, YOSUKE SAWADA
1971 Volume 24 Issue 10 Pages
708-709
Published: October 25, 1971
Released on J-STAGE: April 12, 2006
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SUMIO UMEZAWA, TSUTOMU TSUCHIYA, TETSUO JIKIHARA, HAMAO UMEZAWA
1971 Volume 24 Issue 10 Pages
711-712
Published: October 25, 1971
Released on J-STAGE: April 12, 2006
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EUGENE L. DULANEY, LESLEE M. MARX
1971 Volume 24 Issue 10 Pages
713-714
Published: October 25, 1971
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R. W. RICKARDS
1971 Volume 24 Issue 10 Pages
715-716
Published: October 25, 1971
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SADAFUMI OMURA, SHINJURO NAMIKI, MICHINORI SHIBATA, TOSHIO MURO, SADAO ...
1971 Volume 24 Issue 10 Pages
717-718
Published: October 25, 1971
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FUJIO KOBAYASHI, MASAHITO YAMAGUCHI, JUNJI EDA, FUMIKO HIGASHI, SUSUMU ...
1971 Volume 24 Issue 10 Pages
719-721
Published: October 25, 1971
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KEN KATAGIRI, SHINZO MATSUURA
1971 Volume 24 Issue 10 Pages
722-723
Published: October 25, 1971
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MITSUHIRO KINOSHITA, MASAO WADA, SHIMPEI ABURAGI, SUMIO UMEZAWA
1971 Volume 24 Issue 10 Pages
724-726
Published: October 25, 1971
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YUKIO ITO, YOSHITAMI OHASHI, YOSHIYUKI EGAWA, TOTARO YAMAGUCHI, TAMOTS ...
1971 Volume 24 Issue 10 Pages
727-731
Published: October 25, 1971
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SHINICHI KONDO, HARUO YAMAMOTO, KENJI MAEDA, HAMAO UMEZAWA
1971 Volume 24 Issue 10 Pages
732-734
Published: October 25, 1971
Released on J-STAGE: April 12, 2006
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