FR901469, a Novel Antifungal Antibiotic from an Unidentified Fungus No. 11243. II. In Vitro and In Vivo Activities.
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- FUJIE AKIHIKO
- Exploratory Research Laboratories, Fujisawa Pharmaceutical Co., Ltd.
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- IWAMOTO TOSHIRO
- Exploratory Research Laboratories, Fujisawa Pharmaceutical Co., Ltd.
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- MURAMATSU HIDEYUKI
- Exploratory Research Laboratories, Fujisawa Pharmaceutical Co., Ltd.
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- OKUDAIRA TERUMI
- Exploratory Research Laboratories, Fujisawa Pharmaceutical Co., Ltd.
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- SATO IKUKO
- Exploratory Research Laboratories, Fujisawa Pharmaceutical Co., Ltd.
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- FURUTA TAKAHISA
- Department of Parasitology, The Institute of Medical Science, The University of Tokyo
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- TSURUMI YASUHISA
- Exploratory Research Laboratories, Fujisawa Pharmaceutical Co., Ltd.
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- HORI YASUHIRO
- Exploratory Research Laboratories, Fujisawa Pharmaceutical Co., Ltd.
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- HINO MOTOHIRO
- Exploratory Research Laboratories, Fujisawa Pharmaceutical Co., Ltd.
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- HASHIMOTO SEIJI
- Exploratory Research Laboratories, Fujisawa Pharmaceutical Co., Ltd.
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- OKUHARA MASAKUNI
- Exploratory Research Laboratories, Fujisawa Pharmaceutical Co., Ltd.
書誌事項
- タイトル別名
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- II. <i>In Vitro</i> and <i>In Vivo</i> Activities
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説明
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.
収録刊行物
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- The Journal of Antibiotics
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The Journal of Antibiotics 53 (9), 920-927, 2000
公益財団法人 日本感染症医薬品協会