WF11899A, B AND C, NOVEL ANTIFUNGAL LIPOPEPTIDES: II. BIOLOGICAL PROPERTIES

• Published in: Journal of antibiotics 1994/10/25, Vol.47(10), pp.1092-1097
• Main Authors: IWAMOTO, TOSHIRO, FUJIE, AKIHIKO, NITTA, KUMIKO, HASHIMOTO, SEIJI, OKUHARA, MASAKUNI, KOHSAKA, MASANOBU
• Format: Article
• Language: English
• Subjects: Animals; Antibiotics. Antiinfectious agents. Antiparasitic agents; Antifungal agents; Antifungal Agents - pharmacology; Aspergillus fumigatus; Aspergillus fumigatus - drug effects; Aspergillus niger; Aspergillus niger - drug effects; Biological and medical sciences; Candida - drug effects; Candida albicans; Candida albicans - drug effects; Candidiasis - drug therapy; Glucosyltransferases - antagonists & inhibitors; Hemolysis; Lipopeptides; Medical sciences; Membrane Proteins; Mice; Mice, Inbred ICR; Peptides, Cyclic - pharmacology; Peptides, Cyclic - toxicity; Pharmacology. Drug treatments; Schizosaccharomyces pombe Proteins
• ISSN: 0021-8820; 1881-1469
• DOI: 10.7164/antibiotics.47.1092

WF11899A, B and C, novel water-soluble lipopeptides related to the echinocandins, possess potent anti-Candida activities. The IC50s of the compounds against four clinical isolates of Candida albicans ranged from 0.004 to 0.03 μg/ml by microbroth dilution assay. These compounds mildly suppressed the growth of Aspergillus fumigatus and A. niger. WF11899A, B and C showed a potent in vivo anti-Candida activity. Particularly, WF11899A was superior to cilofungin, and equal to fluconazole. 1, 3-β-glucan synthase was inhibited by these compounds at the IC50s of 0.7, 0.7 and 1.8μg/ml for WF 11899A, B and C, respectively. However, they hemolysed mouse red blood cells in vitro at the concentration of 62 μg/ml.