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HAROLD C. NEU, KWUNG P. FU
1978 Volume 31 Issue 5 Pages
385-393
Published: 1978
Released on J-STAGE: April 12, 2006
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1-N HAPA gentamicin B is a new aminoglycoside active against most Enterobacteriaceae,
Pseudomonas aeruginosa and
Staphylococcus aureus. Among 504 clinical isolates at a concentration of 12.5 μg/ml all
Staph. aureus, Escherichia coil, Klebsiella, Enterobacter, Proteus
rettgeri, Providencia and 78% of
Pseudomonas, 86% of
Proteus morganii were inhibited. Like other aminoglycosides, the activity was greatest at an alkaline pH and reduced by high cations concentrations. 1-N HAPA gentamicin B was equal in activity to amikacin against
both gentamicin-sensitive and resistant isolates. It inhibited bacteria containing many of the aminoglycoside inactivating enzymes. When combined with carbenicillin it inhibited in a synergistic manner many Gram-negative bacteria, particularly
Pseudomonas and
Serratia.
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I. DESCRIPTION AND FERMENTATION OF THE ORGANISM PRODUCING THE LL-BM123 ANTIBIOTICS
H. D. TRESNER, J. H. KORSHALLA, A. A. FANTINI, J. D. KORSHALLA, J. P. ...
1978 Volume 31 Issue 5 Pages
394-397
Published: 1978
Released on J-STAGE: April 12, 2006
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The producing organism for the new broad spectrum glycocinnamoylspermidine antibiotics designated LL-BM123β, γ
1 and γ
2 was characterized as a
Nocardia sp. by chemical analysis of the cell wall, growth requirements, morphology and physiological reactions.
Fermentation conditions to elaborate and analytical methods to characterize these antibiotics in fermentation filtrates are described.
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II. ISOLATION, PHYSICOCHEMICAL AND BIOLOGICAL PROPERTIES OF LL-BM123β, γ1, AND γ2
J. H. MARTIN, M. P. KUNSTMANN, F. BARBATSCHI, M. HERTZ, G. A. ELLESTAD ...
1978 Volume 31 Issue 5 Pages
398-404
Published: 1978
Released on J-STAGE: April 12, 2006
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LL-BM123β, γ
1, andγ
2 are three new antibiotics produced by fermentation of an
unidentified species of
Nocardia. These strongly basic, water-soluble compounds were isolated
from the culture filtrate by CM-Sephadex ion-exchange and carbon chromatography.
All three antibiotics are active against both gram-positive and gram-negative bacteria. A
mixture of LL-BM123γ
1 andγ
1 is more active than the β component but generally less
active than gentamicin.
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V. ANTIBACTERIAL EVALUATION OF THE ISOPROPYL DERIVATIVE OF LL-BM123γ
N. A. KUCK, G. S. REDIN
1978 Volume 31 Issue 5 Pages
405-409
Published: 1978
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Isopropyl LL-BM123γ, a novel semisynthetic glycocinnamoylspermidine antibiotic, was active
in vitro against both Gram-negative and Gram-positive bacteria with broad spectrum bactericidal activity against clinically important Gram-negative strains. In parallel tests, it was equal to or more potent than reference aminoglycoside antibiotics against
Escherichia coli, Proteus, Enterobacter-Klebsiella, Serratia, Salmonella, and
Acinetobacter strains. Against clinical isolates of
Pseudomonas aeruginosa, isopropyl LL-BM123γ compared favorably with gentamicin, verdamicin and amikacin but was less potent than tobramycin. Isopropyl LL-BM123γ was active against many Gram-negative bacteria that were relatively resistant to aminoglycosides. It was rapidly absorbed following subcutaneous administration in mice and showed greater potency than gentamicin on both dosage and plasma concentration bases against several experimental infections.
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I. TAXONOMY OF PRODUCING ORGANISMS AND FERMENTATION
MASATOSHI INUKAI, RYUZO ENOKITA, AKIO TORIKATA, MASAKI NAKAHARA, SEIGO ...
1978 Volume 31 Issue 5 Pages
410-420
Published: 1978
Released on J-STAGE: April 12, 2006
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A new peptide antibiotic, globomycin, was found to be produced by four different strains of the actinomycetes. They were identified as
Streptomyces halstedii No. 13912,
Streptoverticillium cinnamoneum No. 15037,
Streptomyces neohygroscopicus subsp.
globomyceticus No. 15631 and
Streptomyces hagronensis No. 17834, respectively. Fermentation of globomycin was conducted by conventional submerged culture for antibiotic production, in which 10 μg/ml of globomycin was produced by cultivation of
S. halstedii No. 13912 for 96 hours at 27°C.
Globomycin was named after its activity to form global-shape spheroplasts when
Escherichia coli was incubated in the presence of this antibiotic.
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II. ISOLATION AND PHYSICO-CHEMICAL AND BIOLOGICAL CHARACTERIZATION
MASATOSHI INUKAI, MUTSUO NAKAJIMA, MASAAKI OSAWA, TATSUO HANEISHI, MAM ...
1978 Volume 31 Issue 5 Pages
421-425
Published: 1978
Released on J-STAGE: April 12, 2006
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The peptide antibiotic globomycin was extracted from the culture filtrate of
Streptomyces halstedii No. 13912, purified on silica-gel columns and crystallized from acetonitrile to give colorless needles. It is a neutral substance with m.p. of 115°C and a molecular formula of C
32H
57N
5O
9. On amino-acid analysis, it gave serine, threonine, glycine and an unidentified amino acid. It is soluble in methanol, ethyl acetate and chloroform but sparingly soluble in water. The antimicrobial spectrum of globomycin revealed its specific activity against Gram-negative bacteria. Formation of spheroplasts was observed when
Escherichia coli was grown in the presence of globomycin, indicating inhibition of the bacterial cell wall synthesis as its mode of action.
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III. STRUCTURAL DETERMINATION OF GLOBOMYCIN
MUTSUO NAKAJIMA, MASATOSHI INUKAI, TATSUO HANEISHI, AKIRA TERAHARA, MA ...
1978 Volume 31 Issue 5 Pages
426-432
Published: 1978
Released on J-STAGE: April 12, 2006
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The structure of globomycin has been determined by mass, PMR and CMR spectra and by chemical degradation. Globomycin is a new cyclic peptide antibiotic composed of L-serine, L-
allo-threonine, glycine, N-methylleucine, L-
allo-isoleucine and 3-hydroxy-2-methyl-nonaic acid. Among these components, L-
allo-threonine, L-
allo-isoleucine and 3-hydroxy-2-methylnonaic acid are novel components from natural products. A newly developed mass analysis has been introduced for determining the diastereoisomers of
allo-threonine.
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III. IN VITRO ANTIMICROBIAL ACTIVITY OF ANTIBIOTIC M-4365G2 (DE-EPOXY ROSAMICIN)
TOUTARO YAMAGUCHI, HARUO HAYASAKA, HIROTSUGU YOSHIDA, TADAHIRO MATSUSH ...
1978 Volume 31 Issue 5 Pages
433-440
Published: 1978
Released on J-STAGE: March 27, 2006
JOURNAL
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Antibiotic M-4365G
2 (de-epoxy rosamicin) produced by
Micromonospora capillata MCRL 0940 is a new basic 16-membered macrolide antibiotic with activity equal to or superior to erythromycin and josamycin against Gram-positive bacteria. Of interest are the high degree of activity against Gram-negative bacilli and mycoplasmas, and striking inhibitory effects against indole-producing
Proteus spp. Bactericidal activity of M-4365G
2 is also to be noticed.
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RONALD E. CARNEY, JAMES B. MCALPINE, MARIANNA JACKSON, RUTH S. STANASZ ...
1978 Volume 31 Issue 5 Pages
441-450
Published: 1978
Released on J-STAGE: April 12, 2006
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Attempted removal of the 3'-hydroxyl group of seldomycin factor 5
via displacement of a sulfonate ester has led to 3'-
epi-seldomycin factor 5. Removal of the hydroxyl group has been effected by the BARTON procedure. The antibacterial activity of 3'-
epi- and 3'-deoxyseldomycin factor 5 against various aminoglycoside-resistant strains is discussed.
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7-DEOXY-4(R)-DIHYDROSPECTINOMYCIN
WILLIAM ROSENBROOK, Jr., RONALD E. CARNEY, RICHARD S. EGAN, RUTH S. ST ...
1978 Volume 31 Issue 5 Pages
451-455
Published: 1978
Released on J-STAGE: April 12, 2006
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7-Deoxy-4(R)-dihydrospectinomycin (
7) has been prepared and its structure firmly established by proton magnetic resonance and high resolution mass spectrometry. This spectinomycin analog is devoid of antibiotic activity.
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OSAMU MAKABE, AKIHIKO MIYADERA, MITSUHIRO KINOSHITA, SUMIO UMEZAWA, TO ...
1978 Volume 31 Issue 5 Pages
456-467
Published: 1978
Released on J-STAGE: April 12, 2006
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The syntheses of N
1- and N
2-isopropylformycin (
10, 11), formycin 3', 5'-cyclic and 2', 3'-cyclic phosphate (
3, 7) and their
N-methyl and
N-isopropyl derivatives (
13, 15, 19, 23) are described. It was observed that substitution at
N1 or
N2 with a bulky alkyl group or cyclic phosphorylation of the ribose moiety made formycin resistant to adenosine deaminase.
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HIROSHI MAEDA, HIROKO ICHIMURA, HIROSHI SATOH, KENZO OHTSUKI
1978 Volume 31 Issue 5 Pages
468-472
Published: 1978
Released on J-STAGE: April 12, 2006
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The toxicity of the bis-succinyl derivative of the protein antibiotic, neocarzinostatin, was compared with the parent compound, neocarzinostatin (NCS), in rats. The derivative was found to be about two to five fold more active than NCS
in vivo. The antitumor activity in rats bearing eleven distinct YOSHIDA hepatoma ascitic cell lines was tested under four possible combinations with regard to sites of drug and tumor cell administration. The results indicate that the antitumor spectrum of the derivative had changed slightly. Antitumor activity in mice was also tested with L1210 and P388 lymphatic leukemia, and with B16 melanocarcinoma. When the effect of the derivative was compared with parental NCS at the molecular level with respect to the inhibition of DNA synthesis
in vitro, the specific activities of the two were found to be almost identical. These results were interpreted to indicate that the succinyl derivative of NCS was more stable to inactivation and proteolytic break-down
in vivo than NCS as observed previously in
in vitro studies.
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KANKI KOMIYAMA, IWAO UMEZAWA
1978 Volume 31 Issue 5 Pages
473-476
Published: 1978
Released on J-STAGE: April 12, 2006
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Examination of blood and organ concentrations of sporamycin in normal mice showed a rapid decrease of sporamycin from peripheral blood and a high level of sporamycin in urine 10 minutes after intravenous injection of the antibiotic. At the same time, the highest level was found in the kidneys and low levels were found in the lungs and spleen. When sporamycin was added to mouse organ homogenate at 37°C, remarkable inactivation of sporamycin by the homogenate of the liver, kidney, testis,
etc., was noted but this inactivation was slight by tumor homogenate. Sporamycin inhibited the tritiated thymidine incorporation into DNA of normal tissues, but a different pattern of inhibition and recovery on the incorporation of
3H-TdR into DNA was observed among mouse organs. It was noted that the antibiotic may damage normal tissues in spite of a rapid excretion and inactivation of sporamycin in mice, but this damage was recovered rapidly within 1-2 days after the treatment.
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IV. CHEMICAL MODIFICATION OF LL-BM123γ
JOSEPH J. HLAVKA, PANAYOTA BITHA, JAMES BOOTHE, THOMAS FIELDS
1978 Volume 31 Issue 5 Pages
477-479
Published: 1978
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KAZUHIKO OKAMURA, SHOJI HIRATA, YASUSHI OKUMURA, YASUO FUKAGAWA, YASUT ...
1978 Volume 31 Issue 5 Pages
480-482
Published: 1978
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TAKUZO YAMAMOTO, KATSUHISA KOJIRI, HAJIME MORISHIMA, HIROSHI NAGANAWA, ...
1978 Volume 31 Issue 5 Pages
483-484
Published: 1978
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C. A. CLARIDGE, W. T. BRADNER, HENRY SCHMITZ
1978 Volume 31 Issue 5 Pages
485-486
Published: 1978
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A. NESZMÉLYI, H. BOJARSKA-DAHLIG
1978 Volume 31 Issue 5 Pages
487-489
Published: 1978
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PIJUSH K. DAS, MITALI BASU, GORA C. CHATTERJEE
1978 Volume 31 Issue 5 Pages
490-492
Published: 1978
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TOSHIO NISHIMURA, KEIKO MUTO, NOBUO TANAKA
1978 Volume 31 Issue 5 Pages
493-495
Published: 1978
Released on J-STAGE: April 12, 2006
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