The Journal of Antibiotics
Online ISSN : 1881-1469
Print ISSN : 0021-8820
ISSN-L : 0021-8820
Volume 39, Issue 7
Displaying 1-25 of 25 articles from this issue
  • JAMES L. MERTZ, JAMES S. PELOSO, BILL J. BARKER, GEORGE E. BABBITT, JO ...
    1986 Volume 39 Issue 7 Pages 877-887
    Published: 1986
    Released on J-STAGE: April 19, 2006
    JOURNAL FREE ACCESS
    Avilamycin is an antibiotic complex produced by cultures of the organism Streptomyces viridochromogenes, strain NRRL 2860. These compounds belong to the orthosomycin family of antibiotics. Structural composition of the major avilamycins and several minor avilamycins are known. Nine additional minor avilamycins, designated F through N, have been isolated via semi-preparative silica gel or reverse-phase high performance liquid chromatography with final purification using a reverse-phase column loading solvent switching technique. 1H NMR and mass spectroscopy, negative ion fast atom bombardment (neg FAB) and electron impact, were used to structurally identify the avilamycins. All of the compounds were microbiologically
    active and similar in structure to other known avilamycins.
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  • NONGNUCH VANITTANAKOM, WOLFGANG LOEFFLER, ULRIKE KOCH, GÜNTHER JU ...
    1986 Volume 39 Issue 7 Pages 888-901
    Published: 1986
    Released on J-STAGE: April 19, 2006
    JOURNAL FREE ACCESS
    Fengycin is an antifungal lipopeptide complex produced by Bacillus subtilis strain F-29-3. It inhibits filamentous fungi but is ineffective against yeast and bacteria. The inhibition is antagonized by sterols, phospholipids and oleic acid, whereas two other unsaturated fatty acids increase the antifungal effect. Fengycin consists of two main components differing by one amino acid exchange. Fengycin A is composed of 1 D-Ala, 1 L-Ile, 1 L-Pro, 1 D-allo-Thr, 3 L-Glx, 1 D-Tyr, 1 L-Tyr, 1 D-Orn, whereas in fengycin B the D-Ala is replaced by D-Val. The lipid moiety of both analogs is more variable, as fatty acids have been identified as anteiso-pentadecanoic acid (ai-C15), iso-hexadecanoic acid (i-C16 ), n-hexadecanoic acid (n-C16), and there is evidence for further saturated and unsaturated residues up to C18.
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  • AKIHIRO YOSHIMOTO, SHIZUKA FUJII, OSAMU JOHDO, KATSURO KUBO, TOMOYUKI ...
    1986 Volume 39 Issue 7 Pages 902-909
    Published: 1986
    Released on J-STAGE: April 19, 2006
    JOURNAL FREE ACCESS
    A new potent anthracycline antibiotic oxaunomycin was isolated from the culture broth of a blocked mutant derived from a baumycin producer and was identified as 7-O-(α-L-daunosaminyl)-β-rhodomycinone. It exhibited about 100 times more strongly cytotoxic activity against leukemic L1210 cell culture than doxorubicin.
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  • GYULA BATTA, FERENC SZTARICSKAI, JÁNOS CSANÁADI, ISTV&Aa ...
    1986 Volume 39 Issue 7 Pages 910-913
    Published: 1986
    Released on J-STAGE: April 19, 2006
    JOURNAL FREE ACCESS
    The configuration of the glycosidic linkages and the conformation of the carbohydrate moieties in the molecules of the glycopeptide-type antibiotics actinoidins A and B (1a, 1b) have been determined by means of two-dimensional 13C/1H correlation NMR technique and with the application of model compounds 2-4.
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  • A. G. PISABARRO, F. J. CAÑADA, D. VÁZQUEZ, P. ARRIAGA, A ...
    1986 Volume 39 Issue 7 Pages 914-921
    Published: 1986
    Released on J-STAGE: April 19, 2006
    JOURNAL FREE ACCESS
    We have studied the modification of Escherichia coli peptidoglycan induced by bicyclomycin. For this purpose liquid chromatography for peptidoglycan analysis has been used. The main alteration found was an increase of diaminopimelyl-diaminopimelyl bridge containing subunits. Our results show that bicyclomycin impairs the normal breakage of that interpeptidic bond, whose cleavage is needed for the normal remodeling of peptidoglycan
    and cell growth. Based on the analysis of the possible structure of diaminopimelyl-diaminopimelyl bond and bicyclomycin, we propose a hypothesis on the mechanism of action of bicyclomycin.
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  • III. MODIFICATION OF BENZOXAZOLE RING SUBSTITUENTS, IONOPHOROUS PROPERTIES IN AN ORGANIC PHASE
    M. PRUDHOMME, G. DAUPHIN, G. IEMINET
    1986 Volume 39 Issue 7 Pages 922-933
    Published: 1986
    Released on J-STAGE: April 19, 2006
    JOURNAL FREE ACCESS
    Ten semi-synthetic analogs of A23187 (calcimycin), with only the benzoxazole ring substituents modified together with the ionophore X14885A were studied with regard to their calcium and magnesium carrier properties through an organic phase (toluene-butanol, 70:30). The results indicate that the carboxylic group and the oxazolic nitrogen, maintained in the ortho position are essential for the ionophorous properties. Further, the introduction
    of a substituent in place of the NHCH3 group, producing steric hindrance of the carboxylic group leads to a destabilization of the 2:1 associations with cations.
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  • IV. CATION CARRIER PROPERTIES IN MITOCHONDRIA OF ANALOGS WITH MODIFIED BENZOXAZOLE RINGS. ANTIMICROBIAL ACTIVITY
    M. PRUDHOMME, J. GUYOT, G. JEMINET
    1986 Volume 39 Issue 7 Pages 934-937
    Published: 1986
    Released on J-STAGE: April 19, 2006
    JOURNAL FREE ACCESS
    The transporting abilities in the mitochondrial membrane for Ca++ and Mg++ of ten semi-synthetic analogs A23187 (calcimycin) and X14885A are compared. Analogs classified as efficient divalent cation carrier retained the calcimycin antimicrobial activity against three Gram-positive strains tested.
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  • M. E. GRACE, F. J. GREGORY, P. P. HUNG, K. P. Fu
    1986 Volume 39 Issue 7 Pages 938-942
    Published: 1986
    Released on J-STAGE: April 19, 2006
    JOURNAL FREE ACCESS
    A cephalosporin-hydrolyzing enzyme from strains of Proteus penneri resistant to β-lactam antibiotics was purified and characterized. The enzyme gave a single protein band on SDS-polyacrylamide gel electrophoresis with a molecular weight of 30, 000. This cephalosporinase has an isoelectric point of 6.8, a pH optimum of 6.5 and a temperature optimum of 45°C. The enzyme hydrolyzed cephaloridine, cephalothin, cefuroxime, and cefotaxime more
    rapidly than penicillins. The relative rate, with cephaloridine as 100, were: cephalothin, 50; cefuroxime, 93; cefotaxime, 48; ceftriaxone, 23; cefoperazone, 11; benzylpenicillin, 3; ampicillin, 9; and carbenicillin, <1. Cephamycins had low affinities for the enzyme. However, clavulanic acid and sulbactam, with high affinites for the enzyme, were inhibitors of this enzyme.
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  • TOMIZO NIWA, TAKASHI YOSHIDA, ATSUSHI TAMURA, YUZO KAZUNO, SHIGEHARU I ...
    1986 Volume 39 Issue 7 Pages 943-955
    Published: 1986
    Released on J-STAGE: April 19, 2006
    JOURNAL FREE ACCESS
    SF-2103A, a new carbapenem antibiotic, exhibited a broad antibacterial spectrum and a potent inhibitory activity against a wide range of β-lactamases, in particular, against cephalosporinases, with lower I50 values than those displayed by sulbactam and clavulanic acid. Using a fixed combination and checkerboard titration, in vitro synergy against the majority of the β-lactamase-producing strains tested was demonstrated between SF-2103A and various β-lactam antibiotics, especially cefotaxime, ceftizoxime, and cefoperazone. The synergistic effect of SF-2103A was more pronounced than that of sulbactam. The in vitro synergy was also confirmed by bactericidal and bacteriolytic activities and morphological effects.
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  • TAKASHI YOSHIDA, YUZO KAZUNO, TOMOKO SHOMURA, SHINJIRO MURATA, SHIGEHA ...
    1986 Volume 39 Issue 7 Pages 956-965
    Published: 1986
    Released on J-STAGE: April 19, 2006
    JOURNAL FREE ACCESS
    Combinations of SF-2103A with cefotaxime, cefoperazone or cefazolin showed synergistic efficacy at a wide range of combination ratios against experimental infection in mice due to Proteus vulgaris GN76/C-1, producing type Ic cephalosporinase, Escherichia coli No. 29/36 RGN823, producing type IIIa (TEM-2) penicillinase and E. coli GN206, producing type Ib cephalosporinase. These effects by SF-2103A were greater than those seen with sulbactam. The in vitro and in vivo synergistic activities were roughly correlated. Potent in vivo activity of SF-2103A was related to good pharmacokinetic properties, with blood half-life of 30 minutes and urinary recovery of 55.2% after parenteral administration to rats. Furthermore, SF-2103A was stable to rat kidney homogenate. The high stability of SF-2103A in aqueous and biological media was correlated with the sulfonate group at C-3.
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  • KAZUO EBIHARA, FUMINORI ABE, TAKUMI YAMASHITA, KYOICHI SHIBUYA, EMIKO ...
    1986 Volume 39 Issue 7 Pages 966-970
    Published: 1986
    Released on J-STAGE: April 19, 2006
    JOURNAL FREE ACCESS
    The effect of ubenimex on the progression of N-methyl-N'-nitro-N-nitrosoguanidine (MNNG)-induced stomach tumor in rats was studied. Tumor induction was performed by giving MNNG via drinking water for 34 weeks. Ubenimex was ip administered twice a week at 0.5mg/kg for 84 weeks in one group and 49 weeks in another starting from the first and 36th weeks after initiation of MNNG administration, respectively. The stomachs were endoscopically examined 2 times. At the 64th week after initiation of MNNG administration tumorous lesions were observed with about 70% of the rats in both ubenimex administration groups. In the ubenimex non-administration group nearly 90% of the rats had the lesions. After completion of ubenimex administration almost all the rats had the lesions in the three groups but the sizes were much smaller with the two ubenimex administration groups. Almost all of these lesions were histopathologically identified as tumorous. The tumor volume per rat in the two ubenimex administration groups from the 1 and 36th weeks was 21.0 and 19.2% of the volume in the control group, respectively. Tumor number per rat was similar among the three groups.
    The natural killer activity of rats was also examined after completion of the above experiment. The activity markedly increased when ubenimex was administered from the 36th week after initiation of MNNG administration. When ubenimex was administered from the first week, the activity did not increase demonstratively. From all the results described above we conclude that ubenimex exerts an inhibitory action against the progression of MNNG-induced stomach tumor in rats. Contribution of the increase of natural killer activity to ubenimex antitumor action may be dependent on schedule of ubenimex administration.
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  • N. KLESEL, D. ISERT, M. LIMBERT, G. SEIBERT, I. WINKLER, E. SCHRINNER
    1986 Volume 39 Issue 7 Pages 971-977
    Published: 1986
    Released on J-STAGE: April 19, 2006
    JOURNAL FREE ACCESS
    The chemotherapeutic efficacy of cefpirome (HR 810), a new polar aminothiazolylcephalosporin and that of ceftazidime, cefotaxime, cefoperazone, latamoxef and cefodizime were examined against experimental pneumonia caused by Klebsiella pneumoniae DT-S in mice. When compared in terms of MIC values against the infecting organism and the pharmacokinetic pattern, cefpirome showed equal activity and a similar pharmacokinetic behavior to ceftazidime and cefotaxime in mice. Trials to assess the bactericidial activity in vivo, however, showed that cefpirome displayed a more marked bactericidal effect in pneumonic mice than the other cephalosporins tested. Only cefodizime, a cephalosporin with extremely high and prolonged blood and tissue levels in experimental animals exerted chemotherapeutic effects similar to cefpirome. After cefpirome or cefodizime medication (50mg/kg), the viable counts in the lungs of experimental animals fell steadily to 1/10, 000 of the pretreatment level and, in contrast to the reference compounds, no regrowth of the challenge organisms could be observed with both drugs. Moreover, with ED50s ranging from 1.1 to 59.1mg/kg in treatment studies, cefpirome as well as cefodizime were two to ten times more effective than ceftazidime and cefotaxime, whereas cefoperazone and latamoxef were considerably less effective.
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  • JOYCE I. CIALDELLA, JAMES J. VAVRA, VINCENT P. MARSHALL
    1986 Volume 39 Issue 7 Pages 978-984
    Published: 1986
    Released on J-STAGE: April 19, 2006
    JOURNAL FREE ACCESS
    The effects of subinhibitory concentrations of antibiotics on polymorphonuclear leukocyte (PML) and serum killing of Staphylococcus aureus 502A (UC 9116) and Escherichia coli UC 9451 were studied. Exposure of these bacteria to subinhibitory levels of certain lincosaminides, spectinomycin, or 6'-n-propylspectinomycin altered their susceptibility to these host defense mechanisms, while exposure to gentamicin had no effect. However, each organism responded differently to treatment with the antibiotics. S. aureus pretreated during log phase growth with subinhibitory concentrations of clindamycin, lincomycin, or pirlimycin was more susceptible to killing by PMLs than untreated bacteria. No effect on phagocytic killing was found when S. aureus was pretreated with spectinomycin, 6'-n-propylspectinomycin, or gentamicin. The S. aureus remained resistant to serum lysis despite antibiotic treatment. In contrast, spectinomycin and 6'-n-propylspectinomycin as well as clindamycin dramatically increased the susceptibility of E. coli to serum lysis (>99% destroyed). Moderate killing of E. coli by PMLs was also found.
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  • AKIO IWASAKI, HIROSHI KISHIDA, MASANORI OKANISHI
    1986 Volume 39 Issue 7 Pages 985-993
    Published: 1986
    Released on J-STAGE: April 19, 2006
    JOURNAL FREE ACCESS
    The gene for an extracellular xylanase from Streptomyces sp. No. 36a was cloned into Streptomyces lividans TK21 using pIJ702 as a vector plasmid. The smallest DNA fragment encoding the xylanase gene and its possible promotor was determined to be a 1.04kb Sph I-Sac I fragment by sub-cloning studies. This xylanase gene fragment was transferred into the pSK2 series of plasmids and introduced into Streptomyces kasugaensis G3 protoplasts. The cloned xylanase gene was expressed in both S. lividans TK21 and S. kasugaensis G3, and these clones produced and secreted high yields of xylanase into the culture medium. The xylanase production was not detected when a foreign DNA fragment was inserted into the BclI site locating in the xylanase gene fragment.
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  • KEI-ICHI NUMATA, HARUAKI YAMAMOTO, MASAMI HATORI, TAKEO MIYAKI, HIROSH ...
    1986 Volume 39 Issue 7 Pages 994-1000
    Published: 1986
    Released on J-STAGE: April 19, 2006
    JOURNAL FREE ACCESS
    An aminoglycoside hypersensitive mutant, Kp-126, was isolated from the aminoglycoside-resistant strain, Kp-8, of Klebsiella pneumoniae through selection using sorbistin, a nonaminocyclitol-aminoglycoside antibiotic. The mutant Kp-126 was approximately 100-fold more sensitive to sorbistin than the parent strain Kp-8. The mutant also showed hypersensitivityto various aminocyclitol-aminoglycoside antibiotics. K. pneumoniae Kp-126 was used in screening and a new aminoglycoside antibiotic, 3, 3'-neotrehalosadiamine (BMY-28251), was discovered in the fermentation broths of soil isolate strain of Bacillus pumilus.
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  • TAKASHI TSUNO, CHIHARU IKEDA, KEI-ICHI NUMATA, KOJI TOMITA, MASATAKA K ...
    1986 Volume 39 Issue 7 Pages 1001-1003
    Published: 1986
    Released on J-STAGE: April 19, 2006
    JOURNAL FREE ACCESS
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  • LEONE DALL'ASTA, ANDREA COMINI, EUGENIO GAREGNANI, DARIO ALBERTI, GERM ...
    1986 Volume 39 Issue 7 Pages 1004-1006
    Published: 1986
    Released on J-STAGE: April 19, 2006
    JOURNAL FREE ACCESS
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  • A. L. DEMAIN, Y.-Q. SHEN, S. E. JENSEN, D. W. S. WESTLAKE, S. WOLFE
    1986 Volume 39 Issue 7 Pages 1007-1010
    Published: 1986
    Released on J-STAGE: April 19, 2006
    JOURNAL FREE ACCESS
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  • JUN'ICHI SHOJI, TOSHIYUKI KATO, HIROSHI HINOO, TERUO HATTORI, KEIICHIR ...
    1986 Volume 39 Issue 7 Pages 1011-1012
    Published: 1986
    Released on J-STAGE: April 19, 2006
    JOURNAL FREE ACCESS
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  • KUNIO ISSHIKI, TSUTOMU SAWA, KEIKO MIURA, BINGSHENG LI, HIROSHI NAGANA ...
    1986 Volume 39 Issue 7 Pages 1013-1015
    Published: 1986
    Released on J-STAGE: April 19, 2006
    JOURNAL FREE ACCESS
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  • HIROSHI NAKAYAMA, TOSHIAKI HANAMURA, YUICHI ABE, AKIRA SHIMAZU, KEIKO ...
    1986 Volume 39 Issue 7 Pages 1016-1020
    Published: 1986
    Released on J-STAGE: April 19, 2006
    JOURNAL FREE ACCESS
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  • TSUTOMU TSUCHIYA, SHUICHI SAKAMOTO, NORIO KAJIKAWA, SUMIO UMEZAWA, MAS ...
    1986 Volume 39 Issue 7 Pages 1021-1024
    Published: 1986
    Released on J-STAGE: April 19, 2006
    JOURNAL FREE ACCESS
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  • ANDRZEJ CZERWINSKI, JOLANTA GRZYBOWSKA, EDWARD BOROWSKI
    1986 Volume 39 Issue 7 Pages 1025-1027
    Published: 1986
    Released on J-STAGE: April 19, 2006
    JOURNAL FREE ACCESS
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  • F. SÁNCHEZ, G. JIMÉNEZ, A. AGUILAR, F. BAQUERO, V. RUBIO
    1986 Volume 39 Issue 7 Pages 1028-1030
    Published: 1986
    Released on J-STAGE: April 19, 2006
    JOURNAL FREE ACCESS
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  • J. DAVIES
    1986 Volume 39 Issue 7 Pages 1031-1032
    Published: 1986
    Released on J-STAGE: April 19, 2006
    JOURNAL FREE ACCESS
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