The Journal of Antibiotics
Online ISSN : 1881-1469
Print ISSN : 0021-8820
ISSN-L : 0021-8820
Volume 31 , Issue 9
Showing 1-25 articles out of 25 articles from the selected issue
  • WEN-CHIN LIU, DOROTHY SMITH SLUSARCHYK, GAIL ASTLE, WILLIAM H. TREJO, ...
    1978 Volume 31 Issue 9 Pages 815-819
    Published: 1978
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    Ionomycin, a new polyether antibiotic with a high affinity for calcium ions, is obtained in pure form from fermentation broths of Streptomyces conglobatus sp. nov. TREJO by solvent extraction. It is unique amongst known polyether antibiotics in that it has a UV absorption maximum at 300 nm, thereby distinguishing it from other antibiotics of its class. The Ca salt has the molecular formula C41H70O9Ca. Ionomycin is a narrow spectrum antibiotic being active against Gram-positive bacteria.
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  • CAMILLA KELLER-JUSLÉN, HAMILTON D. KING, MAX KUHN, HANS-RUDOLF ...
    1978 Volume 31 Issue 9 Pages 820-828
    Published: 1978
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    Noboritomycins A and B, two new polycyclic ionophoric polyethers were isolated from a strain of Streptomyces noboritoensis. The crystal structure and absolute configuration of noboritomycin A were established by X-ray analysis of its silver salt C43H63O14Ag. Noboritomycin A is the first metabolic polyether possessing two carboxylic acid functions on the carbon backbone (C-31), namely a free acid and an additional carboxylic acid ethylester group. An unusual spiroketal system as well as a salicylic acid chromophore represent further remarkable elements. Noboritomycin A shows in this respect a structural relationship to salinomycin and lasalocid respectively. Comparison of physico-chemical data, in particular the interpretation of the 1H- and 13C-NMR spectra, revealed that noboritomycins A and B are structurally closely related, noboritomycin B carrying an ethyl substituent on the aromatic ring in the place of a methyl group present in noboritomycin A. Both metabolites exhibit activity against Gram-positive bacteria and against Eimeria tenella (chicken coccidiosis).
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  • MAMORU ARAI, YASUHIRO ITOH, RYUZO ENOKITA, YASUYUKI TAKAMATSU, TAICHI ...
    1978 Volume 31 Issue 9 Pages 829-833
    Published: 1978
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    New antibiotics, enaminomycins A, B and C, were found in the culture broth of streptomycete strain No. 13120, which was identified as Streptomyces baarnensis and designated as S. baarnensis No. 13120. Fermentation of enaminomycins were performed by conventional submerged culture in a 30-liter jar fermentor. Isolation of the antibiotics was performed by centrifugation of the culture broth and adsorption of the antibiotics from the supernatant on a column of activated carbon, followed by elution with aqueous acetone. Enaminomycins A, B and C were separated from each other on a column of Sephadex LH-20.
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  • YASUHIRO ITOH, TOMOKO MIURA, TOSHIAKI KATAYAMA, TATSUO HANEISHI, MAMOR ...
    1978 Volume 31 Issue 9 Pages 834-837
    Published: 1978
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    Physico-chemical characterization of enaminomycins revealed that these antibiotics are new members of the epoxy quinone family. From elementary analysis and mass spectroscopic measurements the molecular formulae of enaminomycins A, B and C appear to be C7H5NO5, C10H11NO6 and C7H7NO5, respectively. They are very unique in their chemical properties, possessing various functions, such as epoxy, primary amine and carboxylic acid, in their small structural units.
    Enaminomycin A, the most potent component, has activity against Gram-positive and Gram-negative bacteria and shows cytostatic effect on L1210 mouse leukemia cells in vitro, but enaminomycins B and C are only weakly active against Gram-positive and Gram-negative bacteria.
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  • YASUHIRO ITOH, TATSUO HANEISHI, MAMORU ARAI, TADASHI HATA, KIMIE AIBA, ...
    1978 Volume 31 Issue 9 Pages 838-846
    Published: 1978
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    The structures of enaminomycins A and B were determined by their physico-chemical properties and X-ray crystallographic analyses to be 4-amino-2, 5-dioxo-7-oxa-bicyclo[4, 1, 0]-hept-3-ene-3-carboxylic acid and 2-oxo-4-amino-5-hydroxy-5-acetonyl-7-oxa-bicyclo[4, 1, 0]-hept-3-ene-3-carboxylic acid, respectively. The structure of enaminomycin C was also determined by the analysis of NMR spectrum and other physico-chemical properties to be 2-oxo-4-amino-5-hydroxy-7-oxa-bicyclo[4, 1, 0]hept-3-ene-3-carboxylic acid.
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  • HIROSHI FUKUMI, FUMIO MARUYAMA, KAYOKO YOSHIDA, MAMORU ARAI, AKINORI K ...
    1978 Volume 31 Issue 9 Pages 847-849
    Published: 1978
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    A procedure is described for the large-scale production of mimosamycin, a satellite antibiotic found in the culture filtrate of Streptomyces lavendulae No. 314. The 1H and 13C NMR, and mass spectroscopic data, are explained in terms of the structure of mimosamycin.
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  • M. PODOJIL, Z. VANEK, V. PRIKRYLOVÁ, M. BLUMAUEROVÁ
    1978 Volume 31 Issue 9 Pages 850-854
    Published: 1978
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    From a mixture of substances formed by producing strains of Streptomyces aureofaciens under conditions of submerged fermentation a new metabolite, ekatetrone, was isolated. Its isolation and basic physical and chemical data are described. Ekatetrone is a quinone derivative with a carboxamide group. In tests in vitro with cells of EHRLICH's ascites tumour evidence was provided that ekatetrone inhibits proteo- and nucleosynthesis.
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  • VERA PRIKRYLOVÁ, MILOSLAV PODOJIL, PETR SEDMERA, JINDRICH VOKOU ...
    1978 Volume 31 Issue 9 Pages 855-862
    Published: 1978
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    The structure of ekatetrone has been determined from physico-chemical data obtained using the natural compound, its derivatives and products of degradation reactions. Ekatetrone was found to be the lactone of 1, 8-dihydroxy-2-(1'-hydroxy-2'-carbamoyl)ethyl-9, 10-anthraquinone-3-acetic acid (I). It is proposed that ekatetrone is related, biogenetically, to protetrone.
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  • ISAMU WATANABE, TSUTOMU TSUCHIYA, FUJIO NAKAMURA, MASA HAMADA, SUMIO U ...
    1978 Volume 31 Issue 9 Pages 863-867
    Published: 1978
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    The titled compound was prepared by condensation of 3'-deoxyparomamine derivative (5) with 2, 3-O-bis(p-nitrobenzoyl)-5-O-tosyl-D-xylofuranosyl bromide followed by 1-N-acylation with the active ester of (S)-4-benzyloxycarbonylamino-2-hydroxybutyric acid.
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  • D. J. FLOURNOY
    1978 Volume 31 Issue 9 Pages 868-871
    Published: 1978
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    Ten clinical isolates of Serratia marcescens were tested on MUELLER-HINTON agar containing gentamicin or netilmicin with carbenicillin. The isolates grew on plates where inactivation occurred, at higher antibiotic concentrations, but failed at lower concentrations. This growth response was individualistic and not closely related to the minimum inhibitory concentrations.
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  • SUMIO UMEZAWA, SHIGEAKI SATO, TAKASHI SUGIMURA
    1978 Volume 31 Issue 9 Pages 872-874
    Published: 1978
    Released: April 12, 2006
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    Pepstatin, an acid protease inhibitor purified from the culture medium of Actinomycetes, had a strong diuretic effect in C3H/He mice. A single subcutaneous injection of pepstatin at 80 mg/kg body weight caused 3- to 4-fold increase in the urine volume over that of control mice during the first 24 hours after the injection and 6- to 7-fold increase during the second and third 24-hour periods. The effect was maximal after 72-96 hours, and gradually disappeared within 168 hours after the injection. The serum potassium concentration increased to 7.6 mEq/liter at 24 hours after the injection but the serum sodium concentration did not change significantly. This change in electrolytes disappeared within 168 hours after the injection. The soluble derivative of pepstatin, lactyl-pepstatin, which has a higher ID50 than pepstatin for renin, had no significant diuretic effect at the same molar dose. From these findings the strong diuretic effect of pepstatin is concluded to be due to inhibition of rennin-mediated conversion of angiotensinogen to angiotensin I, which in turn is normally converted to angiotensin II, resulting in release of aldosterone.
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  • HIDEO SUZUKI, TOSHIO NISHIMURA, KEIKO MUTO, NOBUO TANAKA
    1978 Volume 31 Issue 9 Pages 875-883
    Published: 1978
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    The effects of macromomycin (MCR), a high molecular weight peptide antibiotic, on cell division, DNA synthesis and DNA fragmentation were examined in cultured mammalian tumor cells. When MCR was added to HeLa cell culture simultaneoussly with [3H]thymidine, inhibition of DNA synthesis was observed depending on the amount of the drug present, although the inhibition was partial even at a high concentration of the drug. Preincubationof cells with MCR for 2 hours before assay was required for the complete inhibition of DNA synthesis. Cell division of synchronized L5178Y cells, arrested at metaphase, was strongly inhibited by MCR, indicating that the inhibition of cell mitosis by the drug was not dependent on the inhibition of DNA synthesis.
    Strand scission of DNA in MCR-treated cells was observed by alkaline sucrose gradient centrifugation. The fragmentation of cellular DNA occurred at low concentration of the drug and within a very short incubation time (37°C, 5 minutes). At high concentrations of the drug, however, the size of the fragmented DNA remained constant. DNA polymerase activity in isolated nuclei from HeLa and L5178Y cells was stimulated by MCR. These data suggest that MCR works directly on cell nuclei and strand scission of DNA is one of the more important actions of the drug.
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  • KEN TAKEDA, SETSUKO KAWAI, FUMIO KATO, TSUNAO TETSUKA, KUNIO KONNO
    1978 Volume 31 Issue 9 Pages 884-887
    Published: 1978
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    The activity of purified prolyl hydroxylase (proline, 2-oxoglutarate dioxygenase, EC 1. 14. 11. 2) was enhanced 3-8-fold at a low concentration of ferrous ion (1×10-5 M) by addition of bleomycin, a glycopeptide antibiotic with antineoplastic activity and a side effect of producing pulmonary fibrosis. The maximum stimulation was attained at a concentration of 15 μg/ml bleomycin (about 1×10-5 M), which was approximately equimolar with the ferrous ion, one of the cofactors of this enzyme. Addition of bleomycin to the assay mixture resulted in a change of the optimal concentration of ferrous ion from 2 ×10-3 M to 1×10-5 M. Changing the order of addition of ferrous ion, enzyme and bleomycin in assay medium before
    incubation at 37°C, the stimulatory activity was varied. Bleomycin A2-Cu++(Cu++-chelated bleomycin), which scarcely complexed with Fe++, had no enhancing effects on the enzymatic activity. We discuss the possible reasons as to why the activity of prolyl hydroxylase was enhanced by addition of bleomycin in the assay mixture.
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  • MITSUAKI MITANI, NOBORU OTAKE
    1978 Volume 31 Issue 9 Pages 888-893
    Published: 1978
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    The effects of various carboxylic ionophores on divalent metal cation translocation in mitochondria have been investigated. High levels of divalent cation ionophores lysocellin and lasalocid A (10-50 μM) produced mitochondrial osmotic swelling in Ca2+ or Mg2+ medium, which was associated with an increase of cation influx. The extent of swelling was a function of both the ionophore and cation concentrations in the medium. This effect was larger in mitochondria de-energized by treatment with antimycin A and oligomycin than in respiring mitochondria. On the other hand, the monovalent cation ionophores carriomycin and etheromycin at concentrations of 50- 100 μM also induced mitochondrial swelling in Ca2+ medium but were ineffective in Mg2+ medium. Addition of ruthenium red reversed divalent cation ionophore-induced swelling and released Ca2+ from preloaded mitochondria. In contrast, ruthenium red increased monovalent cation ionophore-induced swelling. In a divalent cation-free medium, lysocellin and lasalocid A caused depletion of membrane-bound Ca2+ and released endogenous Ca2+ and Mg2+ from mitochondria, while carriomycin and etheromycin exerted only a limited effect. These results indicate that the divalent cation ionophores affect divalent cation distribution in mitochondria by increasing both influx and efflux of the cations through the inner membrane.
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  • ALESSANDRO ASSANDRI, TITO CRISTINA, LUIGI MORO
    1978 Volume 31 Issue 9 Pages 894-901
    Published: 1978
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    The disposition of four C3-substituted piperazinyl rifamycins was studied in the rat following the intravenous administration of 5 mg/kg of the 14C-labelled antibiotics. Considerable quantitative differences in the pharmacokinetics of these antibiotics were shown in blood levels, tissue distributions and body clearances. Feces were largely the major route of elimination for the parent drug and metabolites. The results suggest that the liver compartimentalization, regulating the biliary excretion, is to be the kinetic parameter affecting the pharmacokinetic behaviour of this class of antibiotics.
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  • A. CIHÁK, L. KORBOVÁ, J. KOHOUT
    1978 Volume 31 Issue 9 Pages 902-905
    Published: 1978
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    Cycloheximide and streptovitacin A administered in vivo to rats display a similar dual effect on the labelling of soluble liver proteins by valine-14C, and result in a similar enhancement of liver uridine kinase activity. On the other hand, in pylorus-ligated rats, both antibiotics markedly depress gastric secretion, acid output, and the level of mucoproteins and proteolytic activity in secreted juice. Streptovitacin A on a molar basis was in all cases 5-8 times more effective than cycloheximide.
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  • NILS MILMAN, JORGEN DAHLAGER
    1978 Volume 31 Issue 9 Pages 906-910
    Published: 1978
    Released: April 12, 2006
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    The in vitro effects of polymyxin antibiotics on o-125I-hippurate (OIH) accumulation in rabbit renal cortical slices were studied using incubation media with pH ranging from 6.9 to 7.9 and containing polymyxin B sulfate, colistin sulfate, sodium colistimethate and antibacterially inactive N-succinyl colistin in concentrations ranging from 1 to 2, 000μg base/ml. Polymyxin B, colistin and colistimethate depressed OIH accumulation significantly in Concentrations≥300μg/ml. The effects on accumulation were clearly pH-dependent and most pronounced at alkaline pH. N-Succinyl colistin had only a marginal influence on accumulation, even in high concentrations. Colistimethate produced a significantly smaller decrease in accumulation at all pH values than both polymyxin B and colistin. The results suggest that the presence of free amino groups is necessary to obtain a decrease in accumulation and correlate with the known in vivo nephrotoxicity of these antibiotics.
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  • M. A. HANNAN, LAURENCE H. HURLEY
    1978 Volume 31 Issue 9 Pages 911-913
    Published: 1978
    Released: April 12, 2006
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  • VWILLIAM V. CURRAN, JAMES H. BOOTHE
    1978 Volume 31 Issue 9 Pages 914-918
    Published: 1978
    Released: April 12, 2006
    JOURNALS FREE ACCESS
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  • IWAO KITAMURA, TOSHIKAZU OKI, TAIJI INUI
    1978 Volume 31 Issue 9 Pages 919-922
    Published: 1978
    Released: April 12, 2006
    JOURNALS FREE ACCESS
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  • HIROSHI OGAWARA, TAKEHITO MINAGAWA, HIROKO NISHIZAKI
    1978 Volume 31 Issue 9 Pages 923-925
    Published: 1978
    Released: April 12, 2006
    JOURNALS FREE ACCESS
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  • HARUO SETO, MARIKO SHIBAMIYA, HIROSHI YONEHARA
    1978 Volume 31 Issue 9 Pages 926-928
    Published: 1978
    Released: April 12, 2006
    JOURNALS FREE ACCESS
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  • HARUO SETO, KAZUTOSHI MIZOUE, NOBORU OTAKE, MICHIO YAMAGISHI, TAKU MIZ ...
    1978 Volume 31 Issue 9 Pages 929-932
    Published: 1978
    Released: April 12, 2006
    JOURNALS FREE ACCESS
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  • TSUTOMU TSUCHIYA, ISAMU WATANABE, FUJIO NAKAMURA, MASA HAMADA, SUMIO U ...
    1978 Volume 31 Issue 9 Pages 933-935
    Published: 1978
    Released: April 12, 2006
    JOURNALS FREE ACCESS
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  • YUKIHIKO KAMEDA, NAOKI ASANO, TADASHI HASHIMOTO
    1978 Volume 31 Issue 9 Pages 936-938
    Published: 1978
    Released: April 12, 2006
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