FR901469, a Novel Antifungal Antibiotic from an Unidentified Fungus No. 11243. II. In Vitro and In Vivo Activities.

DOI PubMed 4 Citations
  • FUJIE AKIHIKO
    Exploratory Research Laboratories, Fujisawa Pharmaceutical Co., Ltd.
  • IWAMOTO TOSHIRO
    Exploratory Research Laboratories, Fujisawa Pharmaceutical Co., Ltd.
  • MURAMATSU HIDEYUKI
    Exploratory Research Laboratories, Fujisawa Pharmaceutical Co., Ltd.
  • OKUDAIRA TERUMI
    Exploratory Research Laboratories, Fujisawa Pharmaceutical Co., Ltd.
  • SATO IKUKO
    Exploratory Research Laboratories, Fujisawa Pharmaceutical Co., Ltd.
  • FURUTA TAKAHISA
    Department of Parasitology, The Institute of Medical Science, The University of Tokyo
  • TSURUMI YASUHISA
    Exploratory Research Laboratories, Fujisawa Pharmaceutical Co., Ltd.
  • HORI YASUHIRO
    Exploratory Research Laboratories, Fujisawa Pharmaceutical Co., Ltd.
  • HINO MOTOHIRO
    Exploratory Research Laboratories, Fujisawa Pharmaceutical Co., Ltd.
  • HASHIMOTO SEIJI
    Exploratory Research Laboratories, Fujisawa Pharmaceutical Co., Ltd.
  • OKUHARA MASAKUNI
    Exploratory Research Laboratories, Fujisawa Pharmaceutical Co., Ltd.

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Other Title
  • II. <i>In Vitro</i> and <i>In Vivo</i> Activities

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Description

FR901469 is a water-soluble macrocyclic lipopeptidolactone (C71H116N14O23) that has inhibitory activity against 1, 3-β-glucan synthase and exhibits in vitro and in vivo antifungal activity against both Candida albicans and Aspergillus fumigatus. The MICs of FR901469 against Candida albicans FP633 and Aspergillus fumigatus FP1305 in a micro-broth dilution test were 0.63 and 0.16μg/ml, respectively. FR901469 showed excellent efficacy by subcutaneous injection against both Candida albicans and Aspergillus fumigatus in a murine systemic infection mode, with ED50s of 0.32 and 0.2mg/kg, respectively. This compound also showed potent anti-Pneumocystis activity in the nude mice model with experimental Pneumocystis pneumonia. The hemolytic activity of FR901469 towards mouse red blood cells is about 30-fold weaker than that of amphotericin B.

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Details 詳細情報について

  • CRID
    1390282679128233856
  • NII Article ID
    130003503793
  • DOI
    10.7164/antibiotics.53.920
  • COI
    1:CAS:528:DC%2BD3cXntVanu7o%3D
  • ISSN
    18811469
    00218820
    http://id.crossref.org/issn/00218820
  • PubMed
    11099225
  • Text Lang
    en
  • Article Type
    journal article
  • Data Source
    • JaLC
    • Crossref
    • PubMed
    • CiNii Articles
  • Abstract License Flag
    Disallowed

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