The Journal of Antibiotics
Online ISSN : 1881-1469
Print ISSN : 0021-8820
ISSN-L : 0021-8820
Volume 56 , Issue 12
Showing 1-12 articles out of 12 articles from the selected issue
  • I. Taxonomy of Producing strain, Fermentation, Isolation, Physico-chemical Properties, and Biological Properties
    FUMITO KOIZUMI, ATSUHIRO HASEGAWA, KEIKO OCHIAI, KATSUHIKO ANDO, HIDEM ...
    2003 Volume 56 Issue 12 Pages 985-992
    Published: December 25, 2003
    Released: January 27, 2009
    JOURNALS FREE ACCESS
    EI-2346, a novel interleukin-1β converting enzyme (ICE) inhibitor, was isolated from the culture broths of Streptomyces sp. E-2346. EI-2346 selectively inhibited the human recombinant ICE activity with an IC50 value of 3.9μM, without inhibiting elastase and cathepsin B. EI-2346 also inhibited mature interleukin-1β secretion from THP-1 cells induced by LPS with an IC50 value of 5.2μM.
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  • I. Taxonomy, Fermentation, Isolation and Biological Properties
    JONG-PYUNG KIM, BYOUNG-KWON KIM, BONG-SIK YUN, IN-JA RYOO, CHOONG HWAN ...
    2003 Volume 56 Issue 12 Pages 993-999
    Published: December 25, 2003
    Released: January 27, 2009
    JOURNALS FREE ACCESS
    New melanin synthesis inhibitors, melanocins A, B and C, were isolated from the fermentation broth and mycelium extract of Eupenicillium shearii F80695. Melanocin A, an isocyanide compound, inhibited mushroom tyrosinase and melanin biosynthesis of B16 melanoma cells with IC50 value of 9.0nM and MIC value of 0.9μM, respectively. Melanocin A also inhibited growth of Streptomyces bikiniensis. While, the structurally very related but non-isocyanide compounds melanocins B and C did not show inhibitory activity in these assays. Melanocins A, B and C showed potent antioxidant activity with scavenging activity of DPPH radical and superoxide anion radical.
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  • II. Physico-chemical Properties and Structure Elucidation
    JONG-PYUNG KIM, BYOUNG-KWON KIM, BONG-SIK YUN, IN-JA RYOO, IN-KYOUNG L ...
    2003 Volume 56 Issue 12 Pages 1000-1003
    Published: December 25, 2003
    Released: January 27, 2009
    JOURNALS FREE ACCESS
    New melanin synthesis inhibitors, melanocins A, B and C, were isolated from the fermentation broth and extract of mycelium of Eupenicillium shearii F80695. The structures of melanocins were established by spectroscopic methods. They are formamide compounds. In particular, melanocin A has an isocyanide group.
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  • I. Taxonomy, Isolation, Physico-chemical Properties and Biological Activities
    SETSUKO KUNIMOTO, JIE LU, HIROYASU ESUMI, YOHKO YAMAZAKI, NAOKO KINOSH ...
    2003 Volume 56 Issue 12 Pages 1004-1011
    Published: December 25, 2003
    Released: January 27, 2009
    JOURNALS FREE ACCESS
    Novel antibiotics named kigamicin A, B, C, D, and E were discovered from the culture broth of Amycolatopsis sp. ML630-mF1 by their selective killing activity against PANC-1 cells only under a nutrient starved condition. Under a condition of nutrient starvation, kigamicins A, B, C, and D inhibited PANC-1 cell survival at 100 times lower concentration than in normal culture. Kigamicins showed antimicrobial activity against Gram-positive bacteria including methicillin resistant Staphylococcus aureus (MRSA). Kigamicin D inhibited the growth of various mouse tumor cell lines at IC50 of about 1μg/ml.
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  • II. Structure Determination
    SETSUKO KUNIMOTO, TETSUYA SOMENO, YOHKO YAMAZAKI, JIE LU, HIROYASU ESU ...
    2003 Volume 56 Issue 12 Pages 1012-1017
    Published: December 25, 2003
    Released: January 27, 2009
    JOURNALS FREE ACCESS
    Kigamicin A (1), B (2), C (3), D (4) and E (5) are novel antitumor antibiotics. Their structures were determined by spectroscopic analyses including various NMR measurements. Kigamicins have a unique aglycone of fused octacyclic ring system containing seven of sixmembered rings and one oxazolidine. The aglycone links a sugar chain composed of one to four deoxysugars. These sugars were found to be amicetose and oleandrose.
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  • JOHN G. ONDEYKA, DEBORAH L. ZINK, ANNE W. DOMBROWSKI, JON D. POLISHOOK ...
    2003 Volume 56 Issue 12 Pages 1018-1023
    Published: December 25, 2003
    Released: January 27, 2009
    JOURNALS FREE ACCESS
    HIV-1 integrase is one of the three enzymes that are critical for replication and spread of HIV and its inhibition is one of the most promising new drug targets for anti-retroviral therapy with potential advantage over existing therapies. This paper describes the isolation and structure elucidation of exophillic acid, a novel dimeric 2, 4-dihydroxy alkyl benzoic acid, derived from Exophiala pisciphila, a fungus isolated from a soil sample collected in Georgia, USA. Exophillic acid (1) and aquastatin A (2), a related compound, inhibited the strand transfer reaction of HIV-1 integrase with IC50 values of 68 and 50μM, respectively.
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  • Physico-chemical Properties and Structure Elucidation
    TAKAO OHYAMA, YUKO IWADATE-KURIHARA, TOMIO ISHIKAWA, SHUNICHI MIYAKOSH ...
    2003 Volume 56 Issue 12 Pages 1024-1032
    Published: December 25, 2003
    Released: January 27, 2009
    JOURNALS FREE ACCESS
    Arborcandins A, B, C, D, E and F, which possess potent 1, 3-β-glucan synthase inhibitory activity, were isolated from the cultured broth of a filamentous fungus, strain SANK 17397. The structures of arborcandins A, B, C, D, E and F were elucidated by a combination of NMR and mass spectrometry, and established to be novel cyclic peptides containing uncommon amino acid residues.
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  • Taxonomy and Biological Activities
    MAYA P. SINGH, FANGMING KONG, JEFFREY E. JANSO, DANIEL A. ARIAS, PAOLA ...
    2003 Volume 56 Issue 12 Pages 1033-1044
    Published: December 25, 2003
    Released: January 27, 2009
    JOURNALS FREE ACCESS
    Inhibitors of the enzymes involved in fatty acid biosynthesis (FAB) have been reported as antibacterial agents. These include thiolactomycin, cerulenin, triclosan, diazoborine, naphthyridinones, aminopyridines and pyridoindoles. Our search for new FAB inhibitors, using a lacZ reporter cell-based screen, led to several confirmed hits. Culture F92S91, later identified as a Pseudomonas sp. based on 16S profiling, was found to produce two α-pyrones (I and II) and three high molecular weight peptides. The pyrones were unstable under acidic conditions, and they were rearranged into a furanone derivative (III). Of these compounds, pyrone I was the most active with MICs (μg/ml) against B. subtilis (1-2), MRSA (2-4), M. catarrhalis (4) and VRE (2-64). Effects on macromolecular synthesis and membrane functions were tested in B. subtilis. Pyrone I nonspecifically inhibited incorporation of radiolabeled precursors into DNA, RNA and protein within 5 minutes of drug exposure, similar to that of triclosan. Both compounds also inhibited the cellular uptake of these precursors. Cerulenin did not have an effect until 30 minutes of drug treatment. Pyrone I and triclosan were membrane-active (BacLight test); however, pyrone I (at≤128μg/ml concentration) was not hemolytic to human RBCs in contrast to triclosan, which was hemolytic at 16μg/ml. These data suggest that pyrone-I, unlike triclosan, selectively affects bacterial membrane function.
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  • TAKAFUMI WATANABE, YOSHIKI HASHIMOTO, KANEYOSHI YAMAMOTO, KIYO HIRAO, ...
    2003 Volume 56 Issue 12 Pages 1045-1052
    Published: December 25, 2003
    Released: January 27, 2009
    JOURNALS FREE ACCESS
    The set of sensor kinase YycG and response regulator YycF is the only essential two-component system (TCS) in Bacillus subtilis and Staphylococcus aureus. We have developed a screening method for antibacterial agents that inhibit YycG, the essential histidine kinase (HK). To increase screening sensitivity, a temperature-sensitive yycF mutant (CNM2000) of B. subtilis with super-sensitivity to HK inhibitors was constructed, which was used for the screening of acetone extracts from 4000 microbes. A total of 11 samples showed higher sensitivity to CNM2000 than to wild-type parent 168, and seven of those were characterized to be potent inhibitors against autophosphorylation of YycG. One sample compound was purified and identified as aranorosinol B, a known antibacterial agent against Gram-positive bacteria including B. subtilis and S. aureus. Aranorosinol B inhibited YycG from both B. subtilis and S. aureus with a half-maximum inhibitory concentration (IC50) of 223 and 211μM, respectively.
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  • FUMITAKA HIRAMOTO, NOBUHIKO NOMURA, TAMOTSU FURUMAI, YASUHIRO IGARASHI ...
    2003 Volume 56 Issue 12 Pages 1053-1057
    Published: December 25, 2003
    Released: January 27, 2009
    JOURNALS FREE ACCESS
    Pradimicin is an antifungal antibiotic which induces apoptosis like cell death in the yeast Saccharomyces cerevisiae. Pradimicin-resistant mutants were isolated from the S. cerevisiae and the mutation points were analyzed. A point mutation of YPD1 that led to a substitution of the 74th glycine (Gly74) to cysteine (Cys) was identified in a mutant strain NH1. In S. cerevisiae, Ypd1 transfers a phosphoryl group from the sensor kinase Sln1 to the response regulator Ssk1 which regulates a downstream MAP kinase in response to hyperosmotic stress. Gly74 is located in a three-residue reverse turn domain that connects two α-helices, one of which contains a histidine residue which is phosphorylated. In the reverse turn, glycine (relative position +10 to the active-site histidine) is highly conserved in Ypd1 and other histidine-containing phosphotransfer proteins. It was therefore suggested that the substitution of Gly74 to Cys altered the Ypd1 structure, which resulted in the resistance to pradimicin.
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  • ALEXANDRA HÖLTZEL, ANKE DIETER, DIETMAR G. SCHMID, ROSE BROWN, MI ...
    2003 Volume 56 Issue 12 Pages 1058-1061
    Published: December 25, 2003
    Released: January 27, 2009
    JOURNALS FREE ACCESS
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  • MASATO KASHIMURA, TOSHIFUMI ASAKA, KEIKO SUZUKI, SHIGEO MORIMOTO
    2003 Volume 56 Issue 12 Pages 1062-1065
    Published: December 25, 2003
    Released: January 27, 2009
    JOURNALS FREE ACCESS
    Download PDF (632K)
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