WF11899A, B and C, novel antifungal lipopeptides. II. Biological properties.

T Iwamoto, A Fujie, K Nitta, S Hashimoto, M Okuhara, M Kohsaka

Exploratory Research Laboratories, Fujisawa Pharmaceutical Co., Ltd., Ibaraki, Japan.

The Journal of antibiotics 1994 Oct

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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 microgram/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-beta-glucan synthase was inhibited by these compounds at the IC50s of 0.7, 0.7 and 1.8 micrograms/ml for WF11899A, B and C, respectively. However, they hemolysed mouse red blood cells in vitro at the concentration of 62 micrograms/ml.

Citation

T Iwamoto, A Fujie, K Nitta, S Hashimoto, M Okuhara, M Kohsaka. WF11899A, B and C, novel antifungal lipopeptides. II. Biological properties. The Journal of antibiotics. 1994 Oct;47(10):1092-7