The Journal of Antibiotics
Online ISSN : 1881-1469
Print ISSN : 0021-8820
ISSN-L : 0021-8820
Volume 30 , Issue 7
Showing 1-20 articles out of 20 articles from the selected issue
  • I. PRODUCING ORGANISM, FERMENTATION AND BIOLOGICAL PROPERTIES OF FORTIMICINS
    TAKASHI NARA, MITSUYOSHI YAMAMOTO, ISAO KAWAMOTO, KENICHIRO TAKAYAMA, ...
    1977 Volume 30 Issue 7 Pages 533-540
    Published: 1977
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    A culture of Micromonospora species MK-70 was found to produce two new antibiotics, fortimicins A and B. Antibacterial and paper chromatographic data on an eluate from IRC-50 treatment of fermentation beers indicated that fortimicins A and B are new antibiotics with broad-spectrum, basic and water-soluble properties. Fortimicin A exhibited potent, unique, broad-spectrum antibacterial activity against Gram-positive and negative bacteria both in vitro and in vivo, while fortimicin B was only weakly active.
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  • II. ISOLATION, PHYSICO-CHEMICAL AND CHROMATOGRAPHIC PROPERTIES
    RYO OKACHI, SEIGO TAKASAWA, TOMOYASU SATO, SEIJI SATO, MITSUYOSHI YAMA ...
    1977 Volume 30 Issue 7 Pages 541-551
    Published: 1977
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    The aminoglycoside antibiotics fortimicins A and B produced by a naturally occurring strain Micromonospora sp. MK-70 were isolated from its fermentation beer. Fortimicins A and B were isolated as water-soluble, basic, white amorphous powders having molecular formula C17H35N5O6 and C15H32N4O5, respectively. Acid hydrolysis of fortimicin A indicated
    that it has one mole of glycine in its molecule while fortimicin B has not. Paper chromatography, silica-gel and carbon thin-layer chromatography revealed that fortimicins A and B are novel aminoglycoside antibiotics.
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  • III. STRUCTURAL IDENTIFICATION
    RICHARD S. EGAN, RUTH S. STANASZEK, MOMIR CIROVIC, SANDRA L. MUELLER, ...
    1977 Volume 30 Issue 7 Pages 552-563
    Published: 1977
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    The structures of fortimicins A and B have been determined by PMR, CMR, mass spectra and CD combined with chemical degradations. Both antibiotics are pseudodisaccha-rides and incorporate a novel aminocyclitol, fortamine. Incontrast to the diaminocyclitol moieties of known aminoglycosides, fortamine is a 1, 4-diamine, contains both N- and O-methyl groups and possesses chiro stereochemistry. Both antibiotics are glycosides of 6-epi-pur-purosamine B, but fort imicin A differs from fortimicin B by being a glycyl amide.
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  • IV. IN VITRO STUDY OF FORTIMICIN A COMPARED WITH OTHER AMINOGLYCOSIDES
    ROLAND L. GIROLAMI, JOHN M. STAMM
    1977 Volume 30 Issue 7 Pages 564-570
    Published: 1977
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    The in vitro antimicrobial activity of fortimicin A, the most active member of the fortimicin complex, was compared with that of amikacin, gentamicin, sagamicin and tobramycin against 352 strains of Enterobacteriaceae and other medically significant organisms. Against most
    of these organisms fortimicin and amikacin had comparable levels of antimicrobial activity, generally slightly less than that of gentamicin, sagamicin or tobramycin. Fortimicin had relatively weak activity against Pseudomonas aeruginosa strains. Fortimicin shows many of the characteristics of other aminoglycoside antibiotics: (i) improved activity at alkaline pH, (ii) rapid, bactericidal action, (iii) reduced activity with increasing inoculum levels, and (iv) synergistic activity with penicillin against enterococci. The activity of fortimicin was compared to that of gentamicin, tobramycin and amikacin against a group of 95 naturally occurring, antibiotic-resistant Gram-negative bacilli other than Pseudomonas. The organisms were isolated from clinical sources and selected primarily for gentamicin resistance by the sensitivity disc test. Fortimicin showed excellent activity against this group of organisms. At a concentration of 6.2 mcg/ml, fortimicin inhibited the most strains (92.6%) followed by amikacin (90.5%), gentamicin (23.2%) and tobramycin (8.4%).
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  • K. H. MICHEL, P. V. DEMARCO, R. NAGARAJAN
    1977 Volume 30 Issue 7 Pages 571-575
    Published: 1977
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    The isolation, biological properties and structure elucidation of a sixteen-membered macrocyclic lactone antibiotic, designated A26771B (1), obtained from Penicillium turbatum are discussed.
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  • A COLLABORATIVE IN VITRO SUSCEPTIBILITY COMPARISON TO CEPHALOTHIN AGAINST 5, 762 CLINICAL BACTERIAL ISOLATES
    RONALD N. JONES, PETER C. FUCHS, THOMAS L. GAVAN, E. HUGH GERLACH, ART ...
    1977 Volume 30 Issue 7 Pages 576-582
    Published: 1977
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    The in vitro activity of Compound BL-S786 was compared with that of cephalothin against 5, 762 clinical isolates by the microdilution broth method. BL-S786 demonstrated a broader spectrum and a significantly lower MIC against the Enterobacteriaceae. Although greater susceptibility to BL-S786 than to cephalothin was exhibited by Serratia marcescens, Proteus morganii and Proteus vulgaris, these three species were generally resistant to both drugs. By contrast, the staphylococci were significantly more susceptible to cephalothin than to BL-S786. Resistance to both drugs was demonstrated by Pseudomonas aeruginosa and other pseudomonads, enterococci and Bacteroides fragilis.
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  • IN VITRO ANTIMICROBIAL ACTIVITY COMPARISON WITH SIX RELATED CEPHALOSPORINS
    R. N. JONES, C. THORNSBERRY, A. L. BARRY, P. C. FUCHS, T. L. GAVAN, E. ...
    1977 Volume 30 Issue 7 Pages 583-592
    Published: 1977
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    BL-S786 was compared by in vitro studies with 6 other parenteral cephalosporins (cefamandole, cefazolin, cefoxitin, cephaloridine, cephalothin and cephradine). The following parameters were assessed: Comparative MICs against a wide variety of bacterial isolates, MIC/MBC comparisons and the effect of inoculum size on the MIC. BL-S786 showed the greatest antimicrobial activity against K. pneumoniae, C. diversus and Salmonella species; was equal to cefamandole against E. coli, E. agglomerans and P. mirabilis; and was second to cefamandole against Shigella, E. tarda, C. freundii, E. cloacae, E. aerogenes and the pathogenic Neisseriae. Essentially no activity against Serratia and Pseudomonas species was observed. Compared to the other cephalosporins tested, BL-S786 showed poor activity against staphylococci and streptococci. For most species tested, the MBC of the various cephalosporins was the same or within one dilution of their respective MICs. However, for Enterobacter and indole-positive Proteus species, the MBC of BL-S786 and cefamandole was usually ≥8-fold higher than the MICs. Cefoxitin, on the other hand, showed little MIC/MBC variations against indole-positive Proteus species. Inoculum size had only a small effect on the MICs against most gram-negative species-in some instances 64-fold increases in MIC resulted by increasing inoculum size from 105 to 107 organisms per ml.
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  • MARTIN J. RAFF, JAMES T. SUMMERSGILL, FRANK J. FONTANA, PATRICIA A. BA ...
    1977 Volume 30 Issue 7 Pages 593-596
    Published: 1977
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    Minocycline was added to normal and hyperlipemic serum samples in concentrations of 1-10 mcg/ml. These specimens had similar protein contents. Chemically extractable minocycline was quantitated fluorometrically. Hyperlipemic serum (cholesterol 480 mg/ 100 ml; triglycerides 321 mg/100 ml) yielded an average of 50% less minocycline than did normal serum (cholesterol 170 mg/100 ml; triglycerides 114 mg/100 ml). When ultrafiltrates of serum containing 6, 12 and 20 mcg/ml minocycline were assayed microbiologically, it was evident that variations in serum triglyceride and cholesterol levels did not alter the ratio
    of bound to free drug. Minocycline appears to be reversibly associated with, and/or soluble in, triglyceride-cholesterol components of serum.
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  • EFFECTS OF AMINOGLYCOSIDE ANTIBIOTICS ON IODOHIPPURATE ACCUMULATION IN RABBIT RENAL CORTICAL SLICES
    JÖRGEN DAHLAGER, NILS MILMAN
    1977 Volume 30 Issue 7 Pages 597-603
    Published: 1977
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    The effects of aminoglycoside antibiotics on the accumulation of O-125I-hippurate (OIH) in rabbit renal cortical slices were assessed in an attempt to establish an in vitro model for aminoglycoside nephrotoxicity. Accumulation of OIH was measured after incubation of cortex slices in media containing aminoglycosides in different concentrations. All aminoglycosides depressed OIH accumulation in the following minimum concentrations: Dihydrostreptomycin and kanamycin, 2, 000 μg/ml (P<0.01); streptomycin and neomycin, 1, 000 μg/ml (P<0.05 and P<0.01); amikacin and tobramycin, 300μg/ml (P<0.05); gentamicin, 100 μg/ml (P<0.05). A concentration of 2, 000 μg/ml caused the following reduction in 0IH accumulation: Dihydrostreptomycin, 19.3%; streptomycin, 28.9%; kanamycin, 23.8%; neomycin, 62.5%; gentamicin, 68.0%; amikacin and tobramycin, 100%. Changes in pH of the incubation media after addition of aminoglycosides were only partially responsible for the observed depression of OIH accumulation and there was no evidence of substrate competition between aminoglycosides and OIH. The in vitro model described here appears to be inadequate as a sole predictor of aminoglycoside nephrotoxicity, but may provide a supplementary tool in the investigation of aminoglycoside proximal tubular cell toxicity.
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  • J. R. EVANS, GLENIS WEARE
    1977 Volume 30 Issue 7 Pages 604-606
    Published: 1977
    Released: April 12, 2006
    JOURNALS FREE ACCESS
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  • HISASHI SAKURAI, MASATAKA IWANO, NAOTOSHI GOH, TSUNEO YAOITA, KAZUO AO ...
    1977 Volume 30 Issue 7 Pages 607-609
    Published: 1977
    Released: April 12, 2006
    JOURNALS FREE ACCESS
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  • JOHN W. WESTLEY, JOHN F. BLOUNT, RALPH H. EVANS, Jr., CHAO-MIN LIU
    1977 Volume 30 Issue 7 Pages 610-612
    Published: 1977
    Released: April 12, 2006
    JOURNALS FREE ACCESS
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  • TOSHIKAZU OKI, TADAZUMI KOMIYAMA, HIROSHI TONE, TAIJI INUI, TOMIO TAKE ...
    1977 Volume 30 Issue 7 Pages 613-615
    Published: 1977
    Released: April 12, 2006
    JOURNALS FREE ACCESS
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  • IWAO KITAMURA, NORIO SHIBAMOTO, TOSHIKAZU OKI, TAIJI INUI, HIROSHI NAG ...
    1977 Volume 30 Issue 7 Pages 616-618
    Published: 1977
    Released: April 12, 2006
    JOURNALS FREE ACCESS
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  • TADAZUMI KOMIYAMA, YASUE MATSUZAWA, TOSHIKAZU OKI, TAIJI INUI, YOSHIKA ...
    1977 Volume 30 Issue 7 Pages 619-621
    Published: 1977
    Released: April 12, 2006
    JOURNALS FREE ACCESS
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  • YOSHIKAZU TAKAHASHI, HIROSHI NAGANAWA, TOMIO TAKEUCHI, HAMAO UMEZAWA, ...
    1977 Volume 30 Issue 7 Pages 622-624
    Published: 1977
    Released: April 12, 2006
    JOURNALS FREE ACCESS
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  • A. K. GANGULY, Y. T. LIU, O. Z. SARRE, S. SZMULEWICZ
    1977 Volume 30 Issue 7 Pages 625-627
    Published: 1977
    Released: April 12, 2006
    JOURNALS FREE ACCESS
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  • P. F. WILEY, J. L. JOHNSON, D. J. HOUSER
    1977 Volume 30 Issue 7 Pages 628-629
    Published: 1977
    Released: April 12, 2006
    JOURNALS FREE ACCESS
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  • YOSUKE SAWADA, SADAKO KAWAKAMI, HYOZO TANIYAMA, YOSHIHIKO INAMORI
    1977 Volume 30 Issue 7 Pages 630-632
    Published: 1977
    Released: April 12, 2006
    JOURNALS FREE ACCESS
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  • M. BOSTIAN, K. MCNITT, A. ASZALOS, J. BERDY
    1977 Volume 30 Issue 7 Pages 633-634
    Published: 1977
    Released: April 12, 2006
    JOURNALS FREE ACCESS
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