The Journal of Antibiotics
Online ISSN : 1881-1469
Print ISSN : 0021-8820
ISSN-L : 0021-8820
Volume 54 , Issue 1
Showing 1-16 articles out of 16 articles from the selected issue
  • KIN SING LAM, DANIEL R. SCHROEDER, JACQUELINE M. VEITCH, KIMBERLY L. C ...
    2001 Volume 54 Issue 1 Pages 1-9
    Published: January 25, 2001
    Released: September 19, 2008
    JOURNALS FREE ACCESS
    Saccharothrix aerocolonigenes ATCC 39243 produces an indolocarbazole antitumor agent rebeccamycin under submerged fermentation conditions. Adding DL-6-fluorotryptophan to culture of S. aerocolonigenes ATCC 39243 induces the formation of two novel indolocarbazoles, fluoroindolocarbazoles A and B. Feeding DL-5-fluorotryptophan to culture of S. aerocolonigenes ATCC 39243 induces the production of a novel indolocarbazole, fluoroindolocarbazole C. These fluoroindolocarbazoles have been isolated from culture broth and purified to homogeneity by vacuum liquid chromatography and column chromatography. All three fluoroindolocarbazoles are more potent than rebeccamycin against P388 leukemia by ip route in murine model.
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  • YOKO HONDA, MASASHI UEKI, GEN OKADA, RIE ONOSE, RON USAMI, KOKI HORIKO ...
    2001 Volume 54 Issue 1 Pages 10-16
    Published: January 25, 2001
    Released: September 19, 2008
    JOURNALS FREE ACCESS
    A new cell growth inhibitor, curvularol, was isolated from the fermentation broth of Curvularia sp. RK97-F166. Curvularol showed no antibacterial activity, and very weak antifungal activity. However, curvularol inhibited the cell cycle progression of normal rat kidney (NRK) cells in G1 phase at 150ng/ml. Curvularol induced the morphological reversion of srcts-transformed NRK cells at 100ng/ml, and inhibited protein synthesis same as cycloheximide.
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  • I. Taxonomy, Fermentation, Isolation, and Biological Properties
    KENICHI KAIDA, RYOSUKE FUDOU, TOSHIYUKI KAMEYAMA, KEISUKE TUBAKI, YOSH ...
    2001 Volume 54 Issue 1 Pages 17-21
    Published: January 25, 2001
    Released: September 19, 2008
    JOURNALS FREE ACCESS
    Clavariopsins were isolated from the fermentation broth of Clavariopsis aquatica AJ117363. Clavariopsins are cyclic depsipeptide antibiotics with the molecular weight of 1, 153 and 1, 139. Clavariopsins showed in vitro antifungal activity against not only Aspergillus fumigatus but also, although to a lesser extent, A. niger and Candida albicans.
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  • YOSHIHIRO SUZUKI, MAKOTO OJIKA, YOUJI SAKAGAMI, KENICHI KAIDA, RYOSUKE ...
    2001 Volume 54 Issue 1 Pages 22-28
    Published: January 25, 2001
    Released: September 19, 2008
    JOURNALS FREE ACCESS
    The structures of new cyclic decadepsipeptides, clavariopsins A and B, were determined to be cyclo[-(R)-2-hydroxyisovaleryl-L-pipecolyl-L-MeVal-L-Val-L-MeAsp-L-Mene-L-Melle-Gly-L-MeVal-L-Tyr(OMe)-] and cyclo[-(R)-2-hydroxyisovaleryl-L-pipecolyl-L-Val-L-Val-L-MeAsp-L-Melle-L-Melle-Gly-L-MeVal-L-Tyr(OMe)-], respectively, by spectroscopic analyses, especially using 2D NMR techniques. The absolute stereochemistry was elucidated by the advanced MARFEY'S method and chiral HPLC analysis.
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  • I. Taxonomy, Fermentation, Isolation and Antimalarial Activity
    AMONLAYA JATURAPAT, MASAHIKO ISAKA, NIGEL L. HYWEL-JONES, YUWAPIN LERT ...
    2001 Volume 54 Issue 1 Pages 29-35
    Published: January 25, 2001
    Released: September 19, 2008
    JOURNALS FREE ACCESS
    Eleven bioxanthracenes and two monomers, six novel in nature, were isolated from the insect pathogenic fungus Cordyceps pseudomilitaris BCC 1620. Growth optimization of the strain led to the improvement of bioxanthracenes production. The bioxanthracenes were evaluated for their antimalarial activity and cytotoxicity.
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  • II. Structure Elucidation
    MASAHIKO ISAKA, PALANGPON KONGSAEREE, YODHATHAI THEBTARANONTH
    2001 Volume 54 Issue 1 Pages 36-43
    Published: January 25, 2001
    Released: September 19, 2008
    JOURNALS FREE ACCESS
    Structures of eleven bioxanthracenes (1-11) and two monomers (12 and 13), isolated from the insect pathogenic fungus Cordyceps pseudomilitaris BCC 1620, were elucidated. The structure, including the axial stereochemistry, of one of the major symmetrical dimers (1) was determined by X-ray crystallographic analysis, while the stereochemistries of the other isomers were deduced by chemical conversions and spectroscopic means.
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  • DOMINIQUE AUBEL, ROWAN MORRIS, BARBARA LENNON, MARKUS RIMANN, HITTO KA ...
    2001 Volume 54 Issue 1 Pages 44-55
    Published: January 25, 2001
    Released: September 19, 2008
    JOURNALS FREE ACCESS
    Screening and development of new antibiotic activities to counteract the increasing prevalence of multidrug-resistant (MDR) human pathogenic bacteria has once again become a priority in human chemotherapy. Here we describe a novel mammalian cell culture-based screening platform for the detection of Streptogramin antibiotics. Quinupristin-dalfopristin (Synercid®), a synthetically modified Streptogramin, is presently the sole effective agent in the treatment of some MDR nosocomial infections. A Streptomyces coelicolor transcriptional regulator (Pip) has been adapted to modulate reporter gene expression (SEAP, secreted alkaline phosphatase) in Chinese hamster ovary cells (CHO) in response to Streptogramin antibiotics. This CHO cell-based technology was more sensitive in detecting the production of the model Streptogramin pristinamycin, from Streptomyces pristinaespiralis, than antibiogram tests using a variety of human pathogenic bacteria as indicator strains. The reporter system was able to detect pristinamycin compound produced by a single S. pristinaespiralis colony. The assay was rapid (17 hours) and could be carried out in a high-throughput 96-well plate assay format or a 24-well transwell set-up. This novel mammalian cell-based antibiotic screening concept enables detection of bioavailable and non-cytotoxic representatives of a particular class of antibiotics in a single assay and represents a promising alternative to traditional antibiogram-based screening programs.
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  • JOAN COMBIE, JOAN COMBIE, FRED G. ALBERT, KIM VAN TRAN, JESSICA CABRER ...
    2001 Volume 54 Issue 1 Pages 56-65
    Published: January 25, 2001
    Released: September 19, 2008
    JOURNALS FREE ACCESS
    Extracts of the biomasses and fermentation broths of 217 extremophilic microorganisms isolated from a number of locales were screened for antifungal activity using whole-cell and mechanism-based in vitro assays. Importantly, eleven broth extracts had activity against several Candida species and Aspergillus fumigatus in whole-cell in vitro assays. One broth specifically inhibited (1, 3)β-glucan synthase activity and four specifically inhibited ketol-isomefase activity, suggesting a mode of action of the antifungal compound(s) present in these extracts. The extract from one thermophile, a novel species of Pseudomonas, was fractionated, an active compound purified and its structure determined. The compound was identified as pyochelin, a previously identified iron-binding compound with heretofore undescribed antifungal activity. To our knowledge, this is the first report demonstrating that extremophiles synthesize compounds that have antifungal activity.
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  • SHANG GUANGDONG, DAI JIANLU, WANG YIGUANG
    2001 Volume 54 Issue 1 Pages 66-73
    Published: January 25, 2001
    Released: September 19, 2008
    JOURNALS FREE ACCESS
    Shengjimycin is a group of 4′′-acylated spiramycins with 4′′-isovalerylspiramycin as the major component, produced by recombinant S. spiramyceticus F21 harboring a 4′′-O-acyltransferase gene from S. mycarofaciens 1748. A stable bioengineered strain of Streptomyces spiramyceticus WSJ-1 was constructed by integrating the 4′′-O-acyltransferase gene (ist) by homologous recombination into the chromosome of the spiramycin-producing strain S. spiramyceticus F21. In this construction, a Streptomyces/E. coli shuttle plasmid pKCl39 (AmR) was used as the vector with the tsr gene used as selection marker for homologous recombination. The constructed strain, S. spiramyceticus WSJ-1, was genetically stable in production titer and proportion of components of Shengjimycin as well as in maintaining the tsr selective marker when grown without selection. Southern hybridization confirmed the integrated status of the ist gene in the host genome. The production and the proportion of major component of 4′′-isovalerylspiramycin of S. spiramyceticus WSJ-1 was also improved comparing with the strain harboring an autonomous plasmid -S. spiramyceticus F21/pIJ680(311) as shown by HPLC analysis. Physiological studies indicated that increase of the VDH (valine dehydrogenase) and LDH (leucine dehydrogenase) activities of WSJ-1 may be involved in this improvement.
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  • VINOD R. HEGDE, JACK SILVER, MAHESH PATEL, VINCENT P. GULLO, RAYMOND Y ...
    2001 Volume 54 Issue 1 Pages 74-83
    Published: January 25, 2001
    Released: September 19, 2008
    JOURNALS FREE ACCESS
    Two novel antifungal compounds, 1 (SCH 466457), and 2 (SCH 466456), active in a "cell wall" assay, were isolated from the fermentation broth of an unidentified fungus. The active compounds were separated from the broth filtrate by adsorption on a macroreticular resin and were purified on reverse phase HPLC. Detailed mass spectrometric and NMR experiments and degradative studies helped in elucidating the structures of these compounds. The compounds were identified to be peptides containing amino acids such as alanine, aminoisobutyric acid, proline, leucine, valine, glycine and a previously identified β-keto acid, 2-methyl 3-oxotetradecanoic acid.5) Both compounds were active against Candida, dermatophytes and Aspergillus (Geometric Mean MIC's, 8.9, 20 and 16 μg/ml, and 64, 128 and 23 μg/ml, respectively for 1 and 2).
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  • EIKO TSUCHIYA, MASASHI YUKAWA, TOKICHI MIYAKAWA, KEN-ICHI KIMURA, HIDE ...
    2001 Volume 54 Issue 1 Pages 84-90
    Published: January 25, 2001
    Released: September 19, 2008
    JOURNALS FREE ACCESS
    We identified borrrelidin, a member of macrolide antibiotic, as an inhibitor of a cyclindependent kinase of the budding yeast, Cdc28/Cln2. A 50% inhibition concentration (IC50) of borrelidin for Cdc28/Cln2 was 24 μM. In addition, borrelidin arrests both haploid and diploid cells in Gl phase at the point indistinguishable from that of α-mating pheromone, at concentrations not affecting the gross protein synthesis. Although the inhibition of CDK activity may not be a solo cause of the Gl arrest, our results indicate that borrelidin is a potential lead compound for developing novel CDK inhibitors of higher eukaryotes.
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  • DIETHILD TORNUS, HEINZ G. FLOSS
    2001 Volume 54 Issue 1 Pages 91-101
    Published: January 25, 2001
    Released: September 19, 2008
    JOURNALS FREE ACCESS
    Four genes, ORF 22-25, from the granaticin biosynthetic gene cluster of Streptomyces violaceoruber Tü22 were analyzed for their involvement in the biosynthesis of the two deoxysugar moieties of the granaticins. Each gene was individually inactivated on a cosmid carrying the entire gra gene cluster and the mutant cosmids were transformed into S. coelicolor CH999. Analysis of the pattern of pigment production by the transformants revealed that each of the four ORFs is required for the formation/attachment of the L-rhodinose moiety of granaticin B, but not that of the D-olivose moiety of granaticin. Based on these results and sequence homologies a pathway of dTDP-L-rhodinose formation is proposed which implicates ORF23, and possibly also ORF 24, in the 3-deoxygenation reaction, ORF 25 in the epimerization and ORF 22 in the final 4-ketoreduction.
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  • SEIICHI SATO, TAKAYUKI KAJIURA, MISATO NOGUCHI, KENJI TAKEHANA, TSUYOS ...
    2001 Volume 54 Issue 1 Pages 102-104
    Published: January 25, 2001
    Released: September 19, 2008
    JOURNALS FREE ACCESS
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  • KUNIAKI TATSUTA, HIROSHI MUKAI, KAZUKI MITSUMOTO
    2001 Volume 54 Issue 1 Pages 105-108
    Published: January 25, 2001
    Released: September 19, 2008
    JOURNALS FREE ACCESS
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  • KUNIAKI TATSUTA, HANA MISAWA, KEN CHIKAUCHI
    2001 Volume 54 Issue 1 Pages 109-112
    Published: January 25, 2001
    Released: September 19, 2008
    JOURNALS FREE ACCESS
    Download PDF (191K)
  • 2001 Volume 54 Issue 1 Pages C1
    Published: 2001
    Released: September 19, 2008
    JOURNALS FREE ACCESS
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