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THEODOR FEHR, HAMILTON D. KING, MAX KUHN
1977 Volume 30 Issue 11 Pages
903-907
Published: 1977
Released on J-STAGE: April 12, 2006
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Mutalomycin is a new metal-complexing polyether antibiotic produced by a strain of
Streptomyces mutabilis NRRL 8088. The metabolite, a monocarboxylic acid, was isolated as the sodium salt C
41H
69NaO
12. The structure of this polyether was established by X-ray analysis of its potassium salt C
41H
69KO
12. Mutalomycin contains six heterocyclic rings and is structurally related to nigericin. The metabolite is active against gram-positive bacteria and
Eimeria tenella (chicken coccidiosis).
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SATOSHI OMURA, HARUO TANAKA, RUIKO OIWA, JUICHI AWAYA, ROKUROU MASUMA, ...
1977 Volume 30 Issue 11 Pages
908-916
Published: 1977
Released on J-STAGE: April 12, 2006
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New antibiotics, OS-4742 A
1, A
2, B
1 and B
2, were isolated from the culture broth of the strain OS-4742, which was designated as
Streptomyces matensis subsp.
vineus. These compounds have anthracycline chromophores and sugar moieties, but do not contain nitrogen. They possess antimicrobial activities against Gram-positive bacteria and antitumor activities against S-180 solid tumor on mice.
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IN VITRO EVALUATION
MINORU NISHIDA, YASUHIRO MINE, SHIGEO NONOYAMA, HITOSHI KOJO, SACHIKO ...
1977 Volume 30 Issue 11 Pages
917-931
Published: 1977
Released on J-STAGE: April 12, 2006
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Nocardicin A, a new monocyclic β-lactam antibiotic, exerts a comparatively potent antimicrobial activity against gram-negative organisms, especially
Pseudomonas aeruginosa, the indole-positive and indole-negative
Proteusgroups (except
Pr. morganii),
Serratia marcescens and the
Neisseria groups. The
in vitroantimicrobial activity of nocardicin A against clinical isolates of
Ps. aeruginosa was about twice that of carbenicillin. The mean MICs of nocardicin A for
Pr. mirabilis, Pr. rettgeri and
Pr. inconstans ranged from 3.13 to 12.5 μg/ml and were 25-50 μg/ml for
Pr. vulgaris. Nocardicin A in concentrations of 12.5-50 μg/ml inhibited 30 strains (48%) of
S. inarcescens usually resistant to β-lactam antibiotics. However, nocardicin A had no significant
in vitro activity against
Staphylococci and
Escherichia coli. No cross-resistance was seen between nocardicin A and other β-lactam antibiotics. This antibiotic was stable to β-lactamase. The
in vitroactivity of nocardicin A against
Ps. aeruginosa and
Pr. mirabilis was greatly influenced by the assay media used. Nocardicin A was bactericidal and appeared to act synergistically with serum bactericidal factors against
Ps. aeruginosa and with polymorphonuclear leukocytes against
Ps. aeruginosa, E. coli and
Pr. vulgaris. The bactericidal activity of nocardicin A against the above 3 organisms, therefore, increased markedly in the presence of fresh serum and polymorphonuclear leukocytes.
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FACTORS INFLUENCING THE IN VITRO ACTIVITY OF NOCARDICIN A
HITOSHI KOJO, YASUHIRO MINE, MINORU NISHIDA, TAKESHI YOKOTA
1977 Volume 30 Issue 11 Pages
926-931
Published: 1977
Released on J-STAGE: April 12, 2006
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Factors influencing the
in vitro antimicrobial activity of nocardicin A against
Pseudomonas aeruginosa and
Proteus mirabilis were investigated. Sodium chloride was identified as a major inhibitor. Some of the amino acids, sugars and divalent cations were found to be
minor inhibitors. The presence of potassium phosphates enhanced nocardicin A activity against
P. aeruginosa, but antagonized the activity against
P. mirabilis.
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IN VIVO EVALUATION
YASUHIRO MINE, SHIGEO NONOYAMA, HITOSHI KOJO, SHIGEMI FUKADA, MINORU N ...
1977 Volume 30 Issue 11 Pages
932-937
Published: 1977
Released on J-STAGE: April 12, 2006
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Nocardicin A is a new monocyclic β-lactam antibiotic which provides a potent therapeutic effect in mice experimentally infected with gram-negative bacilli. When given subcutaneously to mice, the therapeutic effect of the drug was stronger than had been anticipated from
in vitro studies. Nocardicin A was more potent in therapeutic effect than carbenicillin against infections due to
Pseudonionas aeruginosa, Proteus mirabilis, Pr. vulgaris, Pr. rettgeri and
Pr. inconstans, and was similar in effect to carbenicillin against infections due to
Escherichia coli in mice. In addition, nocardicin A proved to be active against infections due to
Serratia marcescens and other organisms resistant to β-lactam antibiotics. When nocardicin A was given subcutaneously to mice, blood and hepatic levels of the drug were higher than those of
carbenicillin.
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ABSORPTION, EXCRETION AND TISSUE DISTRIBUTION IN ANIMALS
YASUHIRO MINE, SHIGEO NONOYAMA, HITOSHI KOJO, SHIGEMI FUKADA, MINORU N ...
1977 Volume 30 Issue 11 Pages
938-944
Published: 1977
Released on J-STAGE: April 12, 2006
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The absorption, excretion and tissue distribution of nocardicin A, a new monocyclic β-lactam antibiotic, were studied in various animals. When nocardicin A was given intramuscularly in single doses of 20 mg/kg to rats, rabbits, and dogs, the peak serum levels of nocardicin A were about 1.6-2.8 times higher than those of carbenicillin in all animals though the levels varied among the species tested. The serum half-life of nocardicin A in
these animals was about twice that of carbenicillin. The 24-hour urinary recovery rate of nocardicin A after intramuscular injection was 68.5% in rabbits and 77.0% in dogs, but was low in rats;
i.e., 0.7%. When nocardicin A was given intravenously in single doses of 20 mg/kg to these animals, the peak serum levels varied widely among the test species;
i.e. about 3 times higher than those of carbenicillin in rabbits and dogs, similar to those in rats. The peak serum and tissue levels of nocardicin A after intramuscular to intravenous injection were the highest in the kidneys, followed by the liver, serum, lungs, heart and spleen. The levels in the liver were prolonged. Nocardicin A, and traces of unknown substances less active
than nocardicin A were observed as active substances in the urine recovered after injection of nocardicin A.
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I. ISOLATION AND IDENTIFICATION OF METABOLITES
J. BÉRDY, J. KÁDÁR PAUNCZ, ZS. MÉHESFALVI ...
1977 Volume 30 Issue 11 Pages
945-954
Published: 1977
Released on J-STAGE: April 12, 2006
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From the cultural broth of a
Micronionospora species 25 aminocyclitol antibiotics were isolated by repeated ion-exchange chromatographic processes. The main components of the metabolites were identified as gentamicin C
1, C
2, and C
1a. The other previously reported gentamicin type antibiotics and some other degradation products including gentamicin A, B, B
1, X
2, sisomicin, garamine, gentamines
etc. , were identified by chemical, PMR, and mass spectroscopic studies. Besides these, seven new gentamicin type antibiotics were isolated and characterized.
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SHINYA NOMOTO, TADASHI TESHIMA, TATEAKI WAKAMIYA, TETSUO SHIBA
1977 Volume 30 Issue 11 Pages
955-959
Published: 1977
Released on J-STAGE: April 12, 2006
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The total structures of capreomycins IA and IB were determined mainly from the results of the comparative study on the NMR spectra of capreomycins and tuberactinomycins, resulting in a revision of the formerly proposed structure. The &-lysine residue as a branched part was revealed to be linked with the &-amino group of an α, &-diaminopropionic acid residue in the cyclic pentapeptide moiety in a different manner than in tuberactinomycins.
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CHLORO-DEOXY ANALOGS
RONALD E. CARNEY, WILLIAM ROSENBROOK Jr.
1977 Volume 30 Issue 11 Pages
960-964
Published: 1977
Released on J-STAGE: April 12, 2006
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9-
Epichloro-9-deoxy-4(R)-dihydrospectinomycin (
3), 9-chloro-9-deoxy-4(R)-dihydrospectinomycin (
7), 9-deoxy-8, 9-epimino-4(R)-dihydrospectinomycin (
6), and 9-
epichloro-9-deoxyspectinomycin (
10) have been prepared and their structures established by proton magnetic resonance. These analogs are devoid of antibiotic activity.
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P. LECOINTE, M. WRIGHT, A. DEDIEU
1977 Volume 30 Issue 11 Pages
965-968
Published: 1977
Released on J-STAGE: April 12, 2006
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A derivative of griseofulvin has been synthesised, in which the 2'-O-methyl group is replaced by a 2'-(2-iodoethoxy),
125I-labelled group. This derivative is at least as potent as griseofulvin itself, when assayed for inhibition of growth on the Myxomycete
Physarum polycephalum.
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TOSHIRO MOROHOSHI, TETSU SAITO
1977 Volume 30 Issue 11 Pages
969-973
Published: 1977
Released on J-STAGE: April 12, 2006
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The cephalosporin β-lactamase (cephalosporinase) produced by
Acinetobacter was studied. The enzyme was partially purified by means of column chromatography and its properties were investigated. The enzyme was induced by benzylpenicillin, 6-aminopenicillanic acid and cephaloridine. Its molecular weight is 30, 000, its optimal temperature 40°C, and its optimal pH 7.25-7.50. Substrate specificity studies using various cephalosporins and penicillins, showed that the enzyme functioned as a cephalosporinase rather than penicillinase.
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G. N. VERNON, A. D. RUSSELL
1977 Volume 30 Issue 11 Pages
974-979
Published: 1977
Released on J-STAGE: April 12, 2006
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Methicillin-sensitive (MS) cells of
Staphylococcus aureus had a minimum electrophoretic mobility at pH 4.5, whereas methicillin-resistant (MR) strains showed only a slight plateau effect. Trypsin removed the trough effect of the MS Oxford strain. There was no correlation between surface lipid and resistance in MR strains. Cell walls of MS strains contained much more teichoic acid than walls of MR strains. Lysostaphin lysed all MR and MS strains, and
mucopeptide does not appear to be involved in resistance to methicillin.
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JOHN FREDERICK GROVE, MICHAEL POPLE
1977 Volume 30 Issue 11 Pages
980-982
Published: 1977
Released on J-STAGE: April 12, 2006
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Flavensomycinoic acid, the N-containing moiety common to the
Streptomyces sp. antibiotics flavensomycin and prasinons A and B, shows only weak insecticidal activity compared with the parent substances.
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A. KATHRINE MILLER, EVEMARIE CELOZZI, BARBARA ANN PELAK
1977 Volume 30 Issue 11 Pages
983-986
Published: 1977
Released on J-STAGE: April 12, 2006
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Novobiocin demonstrates an effect similar to that of probenecid (the "probenecid effect") in enhancing the therapeutic efficacy of antibiotics excreted mainly by the renal tubules. The ability of cefoxitin, cephalexin, cephalothin and penicillin G to protect mice against infection with
Salmonella schottmuelleri was enhanced 2- to 3-fold when the animals were given oral doses of either probenecid or of novobiocin. The efficacy of cephaloridine, excreted mainly by glomerular filtration, was not enhanced by either probenecid or by novobiocin.
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IV. O-METHYLATION OF THE ANTIBIOTIC AND IDENTIFICATION OF THE ACTIVE TYROSINE RESIDUE
P. C. BANERJEE
1977 Volume 30 Issue 11 Pages
987-992
Published: 1977
Released on J-STAGE: April 12, 2006
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Methylation of mycobacillin with dimethyl sulfate and methyl iodide produced respectively mono- and di-methyl derivatives. The products were inactive against fungal spores and erythrocytes. Tyrosine hydroxyl groups only were methylated; in the monomethyl derivative, the hydroxyl of the tyrosine residue in position 6 is methylated, whereas the hydroxyl of the tyrosine in position 4 remains free; both hydroxyl groups are methylated in the dimethyl
derivative. The results indicate that the hydroxyl group of the tyrosine residue in position 6 is essential for the biological activity of mycobacillin.
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TAKASHI DEGUCHI, SHUZO OKUMURA, AKIO ISHII, MASAO TANAKA
1977 Volume 30 Issue 11 Pages
993-998
Published: 1977
Released on J-STAGE: April 12, 2006
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Sagamicin, an aminoglycoside antibiotic, was labeled with tritium by means of a platinum catalyzed hydrogen exchange reaction and by carbon-14 in two biosynthetic procedures.
14C-Methyl-L-methionine was used as the radioactive precursor in these biological processes involving
Micromonospora sagamiensis. The distribution of radioactivity in
14C-sagamicin and gentamicin C
1 was studied by mild acid hydrolysis and HOFMANN degradation. The results showed that both C- and N-methyl groups were derived from methionine. One of
the biosynthetic processes involved the conversion of gentamicin into sagamicin with resting cells and labeled methionine.
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VINCENT GROUPÉ, RICHARD DONOVICK
1977 Volume 30 Issue 11 Pages
999-1001
Published: 1977
Released on J-STAGE: April 12, 2006
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SOICHIRO TODA, SUSUMU NAKAGAWA, TAKAYUKI NAITO
1977 Volume 30 Issue 11 Pages
1002-1003
Published: 1977
Released on J-STAGE: April 12, 2006
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SYNTHESIS AND ACTIVITY OF 4'-DEOXYKANAMYCIN B
YOSHIO ABE, SUSUMU NAKAGAWA, KEI-ICHI FUJISAWA, TAKAYUKI NAITO, HIROSH ...
1977 Volume 30 Issue 11 Pages
1004-1007
Published: 1977
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MODIFICATION OF β-UREIDODEHYDROALANINE RESIDUE IN TUBERACTINOMYCIN N
S. NOMOTO, T. SHIBA
1977 Volume 30 Issue 11 Pages
1008-1011
Published: 1977
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J. W. CORCORAN, M. L. B. HUBER, F. M. HUBER
1977 Volume 30 Issue 11 Pages
1012-1014
Published: 1977
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KATSUHIRO TAKAHASHI, AKINORI KUBO
1977 Volume 30 Issue 11 Pages
1015-1018
Published: 1977
Released on J-STAGE: April 12, 2006
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THE ISOLATION AND STRUCTURE OF BLASTICIDIN H
HARUO SETO, HIROSHI YONEHARA
1977 Volume 30 Issue 11 Pages
1019-1021
Published: 1977
Released on J-STAGE: April 12, 2006
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ISOLATION OF DEMETHYLBLASTICIDIN S
HARUO SETO, HIROSHI YONEHARA
1977 Volume 30 Issue 11 Pages
1022-1024
Published: 1977
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SEIJI SATO, TAKAO IIDA, RYO OKACHI, KUNIKATSU SHIRAHATA, TAKASHI NARA
1977 Volume 30 Issue 11 Pages
1025-1027
Published: 1977
Released on J-STAGE: April 12, 2006
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