The Journal of Antibiotics
Online ISSN : 1881-1469
Print ISSN : 0021-8820
ISSN-L : 0021-8820
Volume 32 , Issue 5
Showing 1-22 articles out of 22 articles from the selected issue
  • I. SCREENING, TAXONOMY AND MORPHOLOGY-PRODUCTIVITY RELATIONSHIP OF STREPTOMYCES HALSTEDII, STRAIN SF-1993
    TAKASHI SHOMURA, JUNKO YOSHIDA, SHOICHI AMANO, MICHIO KOJIMA, SHIGEHAR ...
    1979 Volume 32 Issue 5 Pages 427-435
    Published: 1979
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    Soil Actinomycetales that produce antibiotics during growth on agar but not in submerged culture were searched for and about 25 strains were obtained. One of these, Streptomyces halstedii, strain SF-1993, which produces an antibiotic designated SF-1993 was studied taxonomically and morphologically. The antibiotic-productivity of strain SF-1993 was correlated with mycelial morphology. The vegetative mycelium was filamentous in antibiotic-producing agar cultures, but fragmented in non-producing submerged cultures. By maintaining submerged cells filamentous, production of antibiotic in the submerged fermentations was accomplished. Filamentation was maintained by the use of diluted media or non-fragmented mutant substrains.
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  • II. ISOLATION, STRUCTURE AND BIOLOGICAL PROPERTIES OF N-CARBAMOYL-D-GLUCOSAMINE (SUBSTANCE SF-1993)
    SHOJI OMOTO, TAKASHI SHOMURA, HIROKO SUZUKI, SHIGEHARU INOUYE
    1979 Volume 32 Issue 5 Pages 436-441
    Published: 1979
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    N-Carbamoyl-D-glucosamine was isolated from the culture of Streptomyces halstedii SF-1993. It showed weak antimicrobial activity against some Gram-negative bacteria and some fungi.
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  • MASAJI KASAI, KUNIKATSU SHIRAHATA, SHINZO ISHII, KAZUYUKI MINEURA, HIR ...
    1979 Volume 32 Issue 5 Pages 442-445
    Published: 1979
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    A new component, nanaomycin E, has been isolated from the culture broth of Streptomyces rosa var. notoensis, which had been found to produce nanaomycins A, B, C and D. Nanaomycin E was an epoxy derivative of nanaomycin A and was converted into nanaomycin A and 4a-epi-nanaomycin B by treatment with sodium hydrosulfite in an acidic aqueous solution. 4a-epi-Nanaomycin B was quantitatively converted into nanaomycin A under alkaline conditions.
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  • FERENC SZTARICSKAI, CONSTANCE M. HARRIS, THOMAS M. HARRIS
    1979 Volume 32 Issue 5 Pages 446-452
    Published: 1979
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    Hydrolysis of the O-methylated aglycone of ristomycin A by a mixture of KOH and NaBH4 yielded a mixture of aromatic amino acids which, after N-acetylation and O-methylation, were separated by chromatography on silica gel. Compounds III-VII were isolated and identified by pmr and mass spectroscopy. Compounds V-VII were also oxiiatively degraded to the corresponding benzoate esters. Compounds III and IV are derived from ristomycinic acid (I) and V from actinoidinic acid (II), both of which had been
    obtained in earlier acid hydrolyses of the antibiotic. Compounds VI and VII had not been detected previously nor glycine which was also found to be a product of base hydrolysis. It is postulated that the new products arise from bisdechlorovancomycinic
    acid (X). It is concluded that aglycoristomycin A comprises I, II and X which also constitute the aglycone of ristocetin A.
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  • YUKIO SUGIURA, KAZUHIKO ISHIZU, KIYONORI MIYOSHI
    1979 Volume 32 Issue 5 Pages 453-461
    Published: 1979
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    The 1:1 bleomycin-A2-Cu(II) complex shows an absorption maximum at 595 nm (ε 120), circular dichroism extrema at 555 nm (Δε+1.21) and 665 nm (-0.61), and electron spin resonance (ESR) signal with g11=2.211, g=2.055, and A11=178×10-4 cm-1. The formation constant (log K=12.630) and deprotonation constant (pKc=3.585) of the 1:1 bleomycin-Cu(II) complex were determined by computer analysis of potentiometric data. The results of potentiometric titration also indicate that the stability of bleomycin-metal complexes is in the order Fe(II)Zn(II) and that these divalent metal complexes have a similar coordination environment. The bleomycin-Cu(II) complex
    has substantially a square-pyramidal configuration in which the secondary amine nitrogen, pyrimidine(N-1) ring nitrogen, deprotonated peptide nitrogen of histidine residue, and histidine imidazole(N-1) nitrogen coordinate to Cu(II) as planar ligand donors, and the α-amino nitrogen as axial donor. The specific Cu(II)-binding site of bleomycin has been compared with that of human serum albumin.
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  • JUN HAGINAKA, TERUMICHI NAKAGAWA, TOYOZO UNO
    1979 Volume 32 Issue 5 Pages 462-467
    Published: 1979
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    In order to provide fundamental knowledge about the determination of deacetylcephaloglycin excreted in human urine as an active metabolite of cephaloglycin, the degradation of cephaloglycin in acidic media has been investigated with varying reaction temperature between 30°and 50°C and pH between 1.2 and 2.8. The degradation pathway observed under these conditions was the elimination of the 3-acetyl group yielding deacetylcephaloglycin followed by formation of deacetylcephaloglycin lactone. Estimation of first order rate constants revealed that deacetylation is the rate-determining step for the degradation of cephaloglycin to the lactone. It is found from the kinetic results that reproducible assays of deacetylcephaloglycin excreted in urine can be achieved by a quantitative conversion to deacetylcephaloglycin lactone in a medium of pH 1.4 at 37°C for 2 hours, followed by a reversed-phase ion-pair high-performance liquid chromatography. The utility of the present method is demonstrated by determining the time course of urinary excretion of deacetylcephaloglycin after oral administration of cephaloglycin capsule.
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  • STEPHEN R. BAKER, CHARLES T. HOLDREGE, DONALD N. MCGREGOR
    1979 Volume 32 Issue 5 Pages 468-471
    Published: 1979
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    The synthesis of a new penicillin, disodium D-6-[α-(1, 2, 4-triazine-3, 5-dione-6-carboxamido)-4-hydroxyphenylacetamido]penicillanate (BL-P1908), is described. The compound shows superior in vitro activity against Pseudomonas aeruginosa compared to carbenicillin and ticarcillin and produces higher intramuscular serum levels in mice than does carbenicillin.
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  • AKIHIRO YOSHIMOTO, TATSUO OGASAWARA, IWAO KITAMURA, TOSHIKAZU OKI, TAM ...
    1979 Volume 32 Issue 5 Pages 472-481
    Published: 1979
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    A specific oxidoreductase converting aclacinomycin A to a new analog, aclacinomycin Y, was purified to apparent homogeneity from the culture filtrate of aclacinomycin-producing microorganisms. The isolated enzyme was a weakly acidic protein (isoelectric point, 5.9) with a molecular weight of about 72, 000. The enzymatic reaction requires molecular oxygen and has a pH optimum at 5.5. The enzyme catalyzed an oxidation of the terminal sugar, L-cinerulose, of the trisaccharide
    moiety of aclacinomycin A to L-aculose (2, 3, 6-trideoxyhex-2-enopyranos-4-ulose)
    with removal of two electrons. Studies of substrate specificity revealed that the enzyme is
    an oxidoreductase capable of modifying anthracyclic triglycosides by oxidizing their terminal
    sugars.
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  • A. A. DOMINGUEZ-GIL, M. CEPEDA, J. L. VILA, J. J. GARCIA
    1979 Volume 32 Issue 5 Pages 482-487
    Published: 1979
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    The pharmacokinetics of AL-226, a new semi-synthetic cephalosporin, were studied
    after i.v. and i.m. administrations to rabbits at doses of 10, 20, 30 and 40 mg/kg. The
    average values of the pharmacokinetic parameters after bolus i.v. administration of the
    ant biotic expressed by an open two-compartment kinetic model were: α=0.131 min.-1,
    β=0.0341 min-1, K12=0.0287 min.-1, K21=0.0552 min.-1, K13=0.081 min.-1
    A linear relationship between C0 and dose was found. The urinary excretion constants
    after i.v. administration were: 0.0266 min.-1, 0.0294 min-1, 0.0289 min.-1, 0.0306 min.-1,
    for doses of 10, 20, 30 and 40 mg/kg, respectively. The pharmacokinetic parameters after
    i.v. administration were used to determine the absorption constant: 0.0525 min.-1, 0.057 min.-1,
    0.0596 min.-1, 0.0511 min.-1, after i.m. administration for doses of 10, 20, 30 and 40 mg/kg,
    respectively.
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  • KANJI TSUCHIYA, OSAMU SHIHO, MASAHIRO KONDO
    1979 Volume 32 Issue 5 Pages 488-495
    Published: 1979
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    The immunological cross-reaction among sulfocephalosporins (cefsulodin, SFC-I, SFC-II), cephaloridine, sulbenicillin, penicillin G and 7-aminocephalosporanic acid has been investigated. A specific antibody was produced in rabbits against several structurally related haptens. The sensitization was conducted with a hapten-human serum albumin conjugate, which was prepared in an alkaline solution, with FREUND'S complete adjuvant. A crossreaction was clearly demonstrated between sulfocephalosporins and sulbenicillin, but not between sulfocephalosporins and cephaloridine, penicillin G or 7-aminocephalosporanic acid.
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  • J. DREYFUSS, S. M. SINGHVI, J. M. SHAW, P. EGLI, J. J. Ross, Jr., R. C ...
    1979 Volume 32 Issue 5 Pages 496-503
    Published: 1979
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    The metabolism of tiamulin hydrogen fumarate, labeled with 3H, 14C, or both, was studied in dogs, rats, and weanling pigs. After a dose of radiolabeled tiamulin, all three species excreted more radioactivity in feces (via bile) than in urine. Dogs absorbed 86% of a single oral dose of tiamulin-3H, and the disposition of the compound was similar after a single or multiple dosage regimen. The ratio of antimicrobial activity to total radioactivity in dog plasma was only about 0.25, and was still less in dog urine. After dosing with tiamulin-14C, rats and pigs excreted at least 1% of the dose as 14CO2 in expired air. In dual-labeled studies, pigs excreted less total 14C than 3H and had greater residues of 14C than 3H in edible tissues, blood, and plasma. After the administration of tiamulin-14C to pigs, radioactivity was incorporated into liver glycogen, indicating metabolic cleavage of the side chain of tiamulin. Tiamulin-3H is the isotopically-labeled compound of choice for studying metabolism and tissue residues in animals.
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  • ANGELA M. ALEXANDER, IGOR GONDA, ERNEST S. HARPUR, JOHN B. KAYES
    1979 Volume 32 Issue 5 Pages 504-510
    Published: 1979
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    Microelectrophoresis was found to be a rapid method for studying the interaction between aminoglycoside antibiotics and liposomes prepared from acid phospholipids. The ability to cause charge reversal of liposomes prepared from phosphatidyl inositol was rarked in the order neomycin > gentamicin > tobramycin > amikacin > kanamycin > ribnstamycin > streptomycin > dihydrostreptomycin > Ca2+. Similar results were obtained with liposomes prepared from a mixture (8: 2) of phosphatidyl choline and phosphatidic acid, but no effect was detectable with neutral liposomes made from phosphatidyl
    choline only. The results support the view that the attraction between positively charged nitrogen groups on the antibiotics and the negatively charged groups of acidic phospholipids are predominantly responsible for the interaction. Extension of the studies to ionic strengths and calcium concentrations similar to those found in vivo showed a reduction, but not elimination, of the observed effects.
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  • PAUL E. SWANSON, DANIEL R. STORM
    1979 Volume 32 Issue 5 Pages 511-517
    Published: 1979
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    Octapeptin is a peptide antibiotic which affects bacterial membrane structure and selective membrane permeability for protons and potassium. The influence of octapeptin on the formation of a membrane potential generated across bacterial vesicles was monitored using the Rb+-valinomycin transport system. Octapeptin inhibited the respiratory-linked generation of membrane potentials formed in the presence of succinate or Asc/PMS. In addition, the antibiotic inhibited [3H]-leucine transport driven either by succinate or Asc/PMS. These studies support the proposal that the antimicrobial activity of octapeptin is due to inhibition of the formation of a membrane potential generated in the presence of appropriate respiratory substrates.
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  • TOSHIO NISHIMURA, HIDEO SUZUKI, KEIKO MUTO, NOBUO TANAKA
    1979 Volume 32 Issue 5 Pages 518-522
    Published: 1979
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    The biochemical mechanism of anthracycline resistance was studied with an adriamycinresistant subline of mouse lymphoblastoma L5178Y cells. Both uridine and thymidine uptakes in the resistant cells were observed more resistant to adriamycin and daunorubicin than those in the parental cells. Aclacinomycin A exhibited the same degree of inhibition of nucleic acid syntheses in the sensitive cells and in the resistant cells. The resistance pattern observed by the inhibition of RNA and DNA syntheses seemed to parallel that by growth inhibition. No significant difference was demonstrated between the parental and
    resistant cells in the inhibition of RNA and DNA polymerase reactions with isolated nuclei. The uptake and retention of [3H]adriamycin was observed significantly less in the resistant cells than in the sensitive cells. The results suggested that the adriamycin resistance may be due to alteration of the cytoplasmic mambrane and/or cytoplasm, resulting in decreased uptake and retention of the antibiotic in the resistant cells.
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  • KAYOKO SUZUKAKE, TAKAO FUJIYAMA, HIDEMI HAYASHI, MAKOTO HORI, HAMAO UM ...
    1979 Volume 32 Issue 5 Pages 523-530
    Published: 1979
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    An enzyme which condenses acetyl-L-leucyl-L-leucine and L-arginine into acetyl-L-leucyl-L-leucyl-L-arginine (leupeptin acid) was partially purified from a cell extract of Streptomyces roseus MA839-A1. With respect to this catalytic activity, the enzyme showed the following characteristics: ATP is essential; optimum pH is 9.5; the activity is inhibited either by EDTA or pyrophosphate or N-ethylmaleimide. The molecular weight of the enzyme is about
    260, 000 daltons. It also catalyzes some other extension reactions, such as, acetyl-L-leucine+L-leucine+L-arginine→leupeptin acid, and acetyl-L-leucine+L-leucine→ acetyl-L-leucyl-L-leucine, but neither L-leucine+L-arginine→(L-leucyl) 1-2-L-arginine, nor acetyl-L-leucine+L-arginine→ acetyl-L-leucyl-L-arginine. ATP-PPi exchange, catalyzed by this enzyme, proceeds with either acetyl-L-leucine, or acetyl-L-leucyl-L-leucine or L-leucine, but not with acetate or arginine.
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  • HUBERT MAEHR, JOANNE SMALLHEER, MARCIA CHIN, NORBERTO PALLERONI, FLORE ...
    1979 Volume 32 Issue 5 Pages 531-532
    Published: 1979
    Released: April 12, 2006
    JOURNALS FREE ACCESS
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  • FRANCOIS LE GOFFIC, MARIE-LOUISE CAPMAU, TAM HYNH DHIN, MICHËLE B ...
    1979 Volume 32 Issue 5 Pages 533-534
    Published: 1979
    Released: April 12, 2006
    JOURNALS FREE ACCESS
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  • THEODOR FEHR, CAMILLA KELLER-JUSLËN, HAMILTON D. KING, HANS-RUDOL ...
    1979 Volume 32 Issue 5 Pages 535-536
    Published: 1979
    Released: April 12, 2006
    JOURNALS FREE ACCESS
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  • MASAMI SHIMAZAKI, SHINICHI KONDO, KENJI MAEDA, MASAJI OHNO, HAMAO UMEZ ...
    1979 Volume 32 Issue 5 Pages 537-538
    Published: 1979
    Released: April 12, 2006
    JOURNALS FREE ACCESS
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  • HIROSHI NAGANAWA, TOMOHISA TAKITA, HAMAO UMEZAWA, WILLIAM E. HULL
    1979 Volume 32 Issue 5 Pages 539-541
    Published: 1979
    Released: April 12, 2006
    JOURNALS FREE ACCESS
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  • ROKURO OKAMOTO, HIDEO NOMURA, MASAMI TSUCHIYA, HIROSHI TSUNEKAWA, TSUM ...
    1979 Volume 32 Issue 5 Pages 542-544
    Published: 1979
    Released: April 12, 2006
    JOURNALS FREE ACCESS
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  • KAZUKIYO ONODERA, AKIYOSHI HIRAGUN, MAYUMI SATO, HIROMI MITSUI, KAZUYA ...
    1979 Volume 32 Issue 5 Pages 545-547
    Published: 1979
    Released: April 12, 2006
    JOURNALS FREE ACCESS
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