Fr901469, a novel antifungal antibiotic from an unidentified Fungus No.11243. II. In vitro and in vivo activities

FR901469 is a water-soluble macrocyclic lipopeptidolactone (C71H116N14O23) that has inhibitory activity against 1,3-beta-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...

Full description

Saved in:
Bibliographic Details
Published in:Journal of antibiotics 2000-09, Vol.53 (9), p.920-927
Main Authors: FUJIE, Akihiko, IWAMOTO, Toshiro, OKUHARA, Masakuni, MURAMATSU, Hideyuki, OKUDAIRA, Terumi, SATO, Ikuko, FURUTA, Takahisa, TSURUMI, Yasuhisa, HORI, Yasuhiro, HINO, Motohiro, HASHIMOTO, Seiji
Format: Article
Language:English
Subjects:
Animals
Antibiotics. Antiinfectious agents. Antiparasitic agents
Antifungal agents
Antifungal Agents - pharmacology
Antifungal Agents - therapeutic use
Aspergillosis - drug therapy
Aspergillosis - mortality
Aspergillus fumigatus
Aspergillus fumigatus - drug effects
Biological and medical sciences
Candida albicans
Candida albicans - drug effects
Candidiasis - drug therapy
Candidiasis - mortality
Depsipeptides
Disease Models, Animal
Female
FR901469
Hemolysis - drug effects
lipopeptidolactones
Medical sciences
Mice
Mice, Inbred ICR
Mice, Nude
Microbial Sensitivity Tests
Peptides, Cyclic - pharmacology
Peptides, Cyclic - therapeutic use
Pharmacology. Drug treatments
Pneumocystis
Pneumocystis - drug effects
Pneumonia, Pneumocystis - drug therapy
Pneumonia, Pneumocystis - mortality
Treatment Outcome
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary:FR901469 is a water-soluble macrocyclic lipopeptidolactone (C71H116N14O23) that has inhibitory activity against 1,3-beta-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 0.16 microg/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 0.2 mg/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.
ISSN:0021-8820
1881-1469
DOI:10.7164/antibiotics.53.920