The Journal of Antibiotics
Online ISSN : 1881-1469
Print ISSN : 0021-8820
ISSN-L : 0021-8820
Volume 33 , Issue 6
Showing 1-23 articles out of 23 articles from the selected issue
  • SHIGEJI KONDO, NORIO MEGURIYA, HISAKO MOGI, TOSHINAO AOTA, KENJI MIURA ...
    1980 Volume 33 Issue 6 Pages 533-542
    Published: 1980
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    A new basic peptide antibiotic designated as K-582 was isolated, purified and characterized. When K-582 was applied to a column of Al2O3 or Bio-Gel P-2 or CM Sephadex, two major peaks which were named Fraction I (K-582 A) and Fraction II (K-582 B) were obtained. The nitrogen content, the behavior in color reaction, the absorption bands of amide linkages in the infrared absorption spectrum, 1H NMR spectrum and C-13 NMR
    spectrum indicated the peptide nature of K-582 A and K-582 B. K-582 was effective against yeasts, but inactive against other Gram-positive bacteria, Gram-negative bacteria and Mycobacterium. The toxicity was low in mice.
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  • I. MICROBIAL DEACETYLATION OF PS-5
    YASUO FUKAGAWA, KATSURO KUBO, TOMOYUKI ISHIKURA, KAGEAKI KOUNO
    1980 Volume 33 Issue 6 Pages 543-549
    Published: 1980
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    PS-5 was deacetylated to NS-5(deacetylated PS-5) by L-aminoa cid acylase from porcine kidney and D-amino acid acylase from Streptomyce oslivaceus but not by L-aminoa cid acylase from Aspergillus sp. Using PS-5, N-chloroacetyl-L-phenylalanine and N-chloroacetyl-D-valine as substrates, acylase producers were screened among facultative methanol-assimilating bacteria. Most of the microbes tested were active and could be classified into two groups of L-acylase producers and L-& D-acylase producers. Pseudomonas sp. 1158 which deacetylated the three substrates was chosen for further study. Cells of the bacterium entrapped in polyacrylamide gel and its acylase activities immobilized on DEAE-Sephadex were found to be useful for conversion of PS-5 to NS-5.
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  • II. SEPARATION AND PURIFICATION OF L- AND D-AMINO ACID ACYLASES FROM PSEUDOMONAS SP. 1158
    KATSURO KUBO, TOMOYUKI ISHIKURA, YASUO FUKAGAWA
    1980 Volume 33 Issue 6 Pages 550-555
    Published: 1980
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    L-Amino acid acylase and D-amino acid acylase of Pseudomonas sp . 1158 which converted PS-5 to NS-5 (deacetylated PS-5) were separated and purified by sonication, streptomycin and Ammonium sulfate fractionations, DEAE-Sephacel column chromatography and gel filtration. Molecular weight and the isoelectric point were estimated to be 75, 000 and pI 5.45 for L-amino acid acylase and 100, 000 and pI 4.95 for D-amino acid acylase.
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  • III. ENZYMOLOGICAL CHARACTERIZATION OF L-AMINO ACID ACYLASE AND D-AMINO ACID ACYLASE FROM PSEUDOMONAS SP. 1158
    KATSURO KUBO, TOMOYUKI ISHIKURA, YASUO FUKAGAWA
    1980 Volume 33 Issue 6 Pages 556-565
    Published: 1980
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    L-Amino acid acylase and D-amino acid acylase were stable below 50°C, although the D-enzyme was more thermostable than the L-enzyme at higher temperatures. At 30°C they Showed the highest reaction velocity in phosphate buffer of pH 7.4. Hg++ and Cu++ severely inactivated their activity. Activation by Co++ was observed on L-amino acid acylase, but not on D-amino acid acylase. p-Chloromercuribenzoate inhibited both enzymes, whereas ethylenediamine tetraacetate was very inhibitory on L-amino acid acylase only. With N-acetyl- and
    N-chloroacetyl-aminao aids as substrates, they were relatively stereo-specific. They acted as a Peptidase on dipeptides and tripeptides. Although N-acetylglycine wes attacked by the two enzymes, N-acetylglucosamine and N-acetylethanolamine were insusceptible. PS-5 was converted to NS-5 (deacetyl PS-5) by L-amino acid acylase as well as by D-amino acid acylase.
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  • I. THE 5-O-(DEOXY-3'-C-ACETYL-β-D-HEXOPYRANOSYL)- PLATENOLIDES I AND II
    U. GRÄFE, W. SCHADE, W. IHN, G. REINHARDT, K. DORNBERGER, H. THRU ...
    1980 Volume 33 Issue 6 Pages 566-573
    Published: 1980
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    Four novel nitrogen-free glycosides of platenolides I and II were isolated as secondary shunt metabolites of the turimycin biosynthesis from the culture broth of an industrial strain of Streptomyces hygroscopicus IMET JA 6599. By spectral (MS, 1H and 13C NMR) studies the structures of the glycosides have been settled as 5-O-(4', 6'-dideoxy-3'-C-acetyl-β-D-hexopyranosyl)-platenolide I (DDAH-Pl-I), 5-O-(4', 6'-dideoxy-3'-C-acetyl-β-D-hexopyranosyl)-platenolide II (DDAH-Pl-II), 5-O-(4', 6'-dideoxy-3'-C-acetyl-β-D-hexopyranosyl)-14-hydroxylplatenolide
    II (DDAH-OH-Pl-II) and 5-O-(6'-deoxy-3'-C-acetyl-β-D-hexopyranosyl)-platenolide II (DAH-Pl-II). A fifth glycoside, 5-O-(6'-deoxy-3'-C-acetyl-β-D-hexopyranosyl)-platenolide I (DAH-Pl-I) was identified through its MS data.
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  • II. THE 5-O-(α-MYCAROSYL)- AND 5-O-(3'-DEMETHYL-β-MYCAROSYL)- PLATENOLIDES I AND II
    U. GRÄFE, W. SCHADE, W. IHN, G. REINHARDT, K. DORNBERGER, H. THRU ...
    1980 Volume 33 Issue 6 Pages 574-578
    Published: 1980
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    Three novel glycosides of platenolides I and II containing either mycarose (2, 6-dideoxy-3-C-methyl-L-ribohexopyranose) or 3-demethyl-mycarose (2, 6-dideoxy-L-ribohexopyranose) were isolated as the shunt products of turimycin biosynthesis by an industrial strain of Streptomyces hygroscopicus IMET JA 6599. By means of MS, 13C and 1H NMR spectroscopic studies, their structures were assigned as 5-O-(α -mycarosyl)-platenolide I (MYC-Pl-I), 5-O-(α-mycarosyl)- platenolide II (MYC-Pl-II) and 5-O-(3'-demethyl-β-mycarosyl)-platenolide II (DM-MYC-Pl-II). The occurrence of 3-demethyl-mycaroside amongst the shunt metabolites is discussed in terms of its biosynthesis.
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  • MARILYN K. SPEEDIE, MYUNG OCK PARK
    1980 Volume 33 Issue 6 Pages 579-584
    Published: 1980
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    The regulation of tyrosine production in the anthramycin-producing organism Streptomyces refuineus var. thermotolerans has been studied with wild-type and tyrosine auxotrophic organisms. Growth of the auxotroph on minimal medium plus phenylalanine suggested that phenylalanine may increase the supply of tyrosine. In incubation with whole cells, tyrosine levels increased in response to added phenylalanine. However, no radiolabeled tyrosine was detected after incubation with 14C-phenylalanine. Thus, no phenylalanine hydroxylase is present. Phenylalanine was found to feedback inhibit prephenate dehydratase, resulting in an increase in NAD-dependent prephenate dehydrogenase activity, thus channeling prephenic
    acid toward tyrosine.
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  • NOBUFUSA SERIZAWA, KEIKO NAKAGAWA, TATSUO HANEISHI, SHOJI KAMIMURA, AT ...
    1980 Volume 33 Issue 6 Pages 585-590
    Published: 1980
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    D-Amino acid oxidase (EC 1.4.3.3) systems from Trigonopsis variabilis SANK 59963 were found to catalyze cephamycin C. The reaction products were assigned to 7β-(5-carboxy-5-oxovalerylamido)-7α-methoxy-3-carbamoyl-3-cephem-4-carboxylica cid, and 7β-(4-carboxy-butyrylamido)-7α-methoxy-3-carbamoyl-3-cephem-4-carboxylic acid, respectively. D-Amino acid oxidase from hog kidney was not able to catalyze cephamycin C.
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  • W. MECHLINSKI, C. P. SCHAFFNER
    1980 Volume 33 Issue 6 Pages 591-599
    Published: 1980
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    High performance liquid chromatographic (HPLC) procedures were utilized for the rapid and efficient separation and characterization of the aromatic heptaene macrolide group of antifungal antibiotics. The instrument utilized a 350nm phosphor converted ultraviolet detector and a μ Bondapak C18 column packing. Optimum resolution of eleven commercial aromatic heptaene macrolide preparations was obtained with solvent systems consisting of mixtures of acetonitrile and 0.05 M aqueous sodium citrate buffer, pH 5.3. The presence of two distinct types of aromatic heptaene macrolides with numerous well-defined individual components has been established.
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  • ARIE ROSNER, HAIM AVIV
    1980 Volume 33 Issue 6 Pages 600-603
    Published: 1980
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    The use of bioautography for quantitative measurement of gentamicin concentrations wzs compared with the disk test. Following chromatographic separation and bioautography, gentamicin produced inhibition zones, 2-7 times larger than the inhibition zones formed by the same amounts of gentamicin in the disk test. Bioautography, therefore, is a more sensitive assay method.
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  • ALLEN H. HELLER, REYNOLD SPECTOR, MOLLY AALYSON
    1980 Volume 33 Issue 6 Pages 604-613
    Published: 1980
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    The kinetics of gentamicin accumulation by a sensitive strain of Escherichia coli were investigated at gentamicin concentrations from 0.02 to 200μg/ml. Accumulation with time shows two energy-dependent phases and is saturable. Sodium chloride delays the onset of the second more rapid energy-dependent phase and decreases the magnitude of gentamicin accumulation for incubations up to 60 minutes at all gentamicin concentrations tested. Simultaneous determinations of accumulation, cell viability, and growth inhibition indicate that antimicrobial activity is correlated with the magnitude of gentamicin accumulation. These observations suggest that altered bacterial accumulation of gentamicin explains the effect of sodium chloride on the antimicrobial activity of gentamicin.
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  • SUSUMUH ORIKAWA, HIROSHI OGAWARA
    1980 Volume 33 Issue 6 Pages 614-619
    Published: 1980
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    Several, β-lactams were investigated on the affinity for the penicillin-binding proteins (PBPs) and the antibacterial activity in Bacillus subtilis. The β-lactams such as ampicillin, PS-5, methicillin and SCE-963, which had high affinities for PBP-2 showed strong antibacterial activities and the 3-lactams such as cephamycin C, Y-G19Z-GG and Y-G19Z-G, which had high affinities for PBP-1 but low affinities for PBP-2, showed weak antibacterial activities. Clavulanic acid and nocardicin A, which had almost no affinities for all the PBPs detected, showed very low antibacterial activities. These results suggest that PBP-2 in Bacillus subtilis is the lethal target of these, β-lactam antibiotics.
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  • HIROSHIO GAWARA, SUSUMUH ORIKAWA
    1980 Volume 33 Issue 6 Pages 620-624
    Published: 1980
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    Penicillin-binding proteins (PBPs) in membrane of Streptomyces cacaoi were investigated by sodium dodecylsulfate-polyacrylamide gel electrophoresis-fluorography. At the same time, eleven β-lactamsw ere examined on the affinities for these PBPs and the antibacterial activities against S. cacaoi, comparing with those in Bacillus subtilis reported in the preceding paper. The affinity patterns of β-lactams for PBPs both in S. cacaoi and B. subtilis were similar in many points. Here again, the grouping of β-lactams based on the affinity for PBP-2 (M. W., 91, 000) was in accord with that based on the antibacterial activity. These results suggest that among PBPs detected in S. cacaoi, PBP-2 is the most likely target of killing by these β-lactam antibiotics.
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  • I. EFFECT OF CEFAZOLIN ON PROTEIN BINDING AND PHARMACOKINETICS OF CEFOPERAZONE
    YASUO WATANABE, TOSHIO HAYASHI, RIEKO TAKADA, TAKASHI YASUDA, ISAMU SA ...
    1980 Volume 33 Issue 6 Pages 625-635
    Published: 1980
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    The effect of cefazolin (CEZ) on the protein binding and the pharmacokinetics of cefoperazone (T-1551) was investigated. For the simultaneous determination of T-1551 and CEZ, high pressure liquid chromatography (HPLC) was used. The extent of protein binding, the number of binding sites and the association constant to human serum albumin were 90.4%, 0.87 and 2.16×104 in T-1551, and 89.2%, 0.78 and 2.46×104 in CEZ, respectively. T-1551 and CEZ appeared to bind to the same site on the protein, since each drug competitively inhibited the binding of the other to serum protein. The mode of the binding of T-1551 to serum protein was similar to that of CEZ. When T-1551 and CEZ were co-administered, the serum level of T-1551 was lower than that with the single administration, while, urinary excretion was higher. These results suggested that the concomitantly administered drugs influenced one another's binding to serum protein in vivo and subsequently an increase in the concentration of the unbound drug in the serum made the drug available for glomerular filtration. It seemed that the high protein binding of T-1551 to serum was an important factor affecting its pharmacokinetics.
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  • INA HAUPT, JIRI JONÁK, IVAN RYCHLÍK, HEINZ THRUM
    1980 Volume 33 Issue 6 Pages 636-641
    Published: 1980
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    The effect of streptothricin F on elongation factor-dependent and on elongation factor-free translation systems was studied. Streptothricin F inhibits factor-dependent as well as factor-free polypeptide synthesis. The results suggest that streptothricin F inhibits polypeptide synthesis via interaction with the ribosome. In partial reactions streptothricin F impairs EF-G-dependent translocation and to a lesser extent EF-Tu-dependent binding of as-RNA to the ribosome, while it does not affect peptide bond formation significantly.
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  • MASAAKI ISHIZUKA, TORU MASUDA, NOBUO KANBAYASHI, SHIGEKI FUKASAWA, TOM ...
    1980 Volume 33 Issue 6 Pages 642-652
    Published: 1980
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    Effect of bestatin on the establishment of delayed-type hypersensitivity (DTH) to sheep red blood cells (SRBC) and oxazolone was examined in normal and immunity-impaired mice. Administration of a low dose of bestatin (0.1-100μg/mouse)augmented DTH to SRBC and restored their impaired DTH to oxazolone. The effect of bestatin in the mouse was age-dependent. Bestatin retarded the growth of slow growing solid tumors of GARDNER lympho-sarcoma and IMC carcinoma and the effect was influenced by the time of the administration and the number of cells inoculated. Bestatin enhanced the antitumor action of the antitumor antibiotics, bleomycin and adriamycin. Bestatin also retarded the induction of skin cancer by 20-methylcholanthrene.
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  • MASAAKI ISHIZUKA, JUNICHI SATO, YUKO SUGIYAMA, TOMIO TAKEUCHI, HAMAO U ...
    1980 Volume 33 Issue 6 Pages 653-662
    Published: 1980
    Released: April 12, 2006
    JOURNALS FREE ACCESS
    The incorporation of 3H-thymidine into the acid insoluble fraction of spleen cells was increased by intraperitoneal injection of 10μg bestatin/mouse. Bestatin (0.01, 0.1, 1.0μg/ml) which was added to mouse spleen cell culture increased 3H-thymidine incorporation into lymphocytes, but 10μg/ml did not. This mitogenic action of bestatin was not observed when adherent cells were removed or T cells were destroyed, suggesting that bestatin causes the proliferate T cells probably through the activation of macrophages. Bestatin given to mice did not modulate mitogenicity of lectins. Bestatin treatment of human peripheral huffy coat cells increased 3H-thymidine incorporation into lymphocytes. The addition of bestatin at a high concentration such as 100μg/ml to mouse spleen cell cultures exhibited a high mitogenic effect on B cells in preference to T cells but this effect was not seen with bestatin at 50μg/ml. In this case, the mitogenicity of Con A or LPS was expanded and antibody formation to SRBC in spleen cell cultures were also stimulated.
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  • U. GRÄFE, W. F. FLECK, W. SCHADE, G. REINHARDT, D. TRESSELT, H. T ...
    1980 Volume 33 Issue 6 Pages 663-664
    Published: 1980
    Released: April 12, 2006
    JOURNALS FREE ACCESS
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  • SETSUKO KUNIMOTO, TORU MASUDA, NOBUO KANBAYASHI, MASA HAMADA, HIROSHI ...
    1980 Volume 33 Issue 6 Pages 665-667
    Published: 1980
    Released: April 12, 2006
    JOURNALS FREE ACCESS
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  • F. TOMITA, T. TAMAOKI, K. SHIRAHATA, M. KASAI, M. MORIMOTO, S. OHKUBO, ...
    1980 Volume 33 Issue 6 Pages 668-670
    Published: 1980
    Released: April 12, 2006
    JOURNALS FREE ACCESS
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  • SUSUMU TOHMA, TOSHIO YONETA, SHUNZO FUKATSU
    1980 Volume 33 Issue 6 Pages 671-674
    Published: 1980
    Released: April 12, 2006
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  • STEPHEN HANESSIAN, JEAN-MICHEL VATELE
    1980 Volume 33 Issue 6 Pages 675-678
    Published: 1980
    Released: April 12, 2006
    JOURNALS FREE ACCESS
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  • MOTOO SHIBATA, MASARU UYEDA, KAZUO MORI
    1980 Volume 33 Issue 6 Pages 679-681
    Published: 1980
    Released: April 12, 2006
    JOURNALS FREE ACCESS
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