Abstract
The in vitro antifungal activity of amphotericin B methyl ester (AME), a water-soluble derivative of amphotericin B, was compared to that of the parent compound against a variety of pathogenic and potentially pathogenic fungi. AME has a significant antifungal activity, but the activity of AME was slightly lower than that of amphotericin B. Among the yeast-like organisms, only the yeast cells of Sporothrix schenckii were more resistant than others to both antibiotics, with a minimal fungicidal concentration of 5 to 10 μg/ml. The yeast cells of other fungi were killed at concentrations of 1 μg or less of either antibiotic per ml. The filamentous forms of S. schenckii and Oidiodendron kalrai were more resistant than the filamentous forms of other dimorphic fungi to both drugs. The minimal fungicidal concentration for S. schenckii was 10 μg/ml and for O. kalrai, 50 μg/ml. The dermatophytes, phycomycetes, and dematacious and other potentially pathogenic fungi were inhibited fairly well by both drugs, but up to 50 μg/ml was required for fungicidal action. The water solubility and wide spectrum of antifungal activity of AME warrant evaluation of its chemotherapeutic activity against experimental fungal infections.
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- Bonner D. P., Mechlinski W., Schaffner C. P. Polyene macrolide derivatives. 3. Biological properties of polyene macrolide ester salts. J Antibiot (Tokyo) 1972 Apr;25(4):261–262. [PubMed] [Google Scholar]
- Hamilton-Miller J. M. Chemistry and biology of the polyene macrolide antibiotics. Bacteriol Rev. 1973 Sep;37(3):166–196. [PMC free article] [PubMed] [Google Scholar]
- Keim G. R., Jr, Poutsiaka J. W., Kirpan J., Keysser C. H. Amphotericin B methyl ester hydrochloride and amphotericin B: comparative acute toxicity. Science. 1973 Feb 9;179(4073):584–585. doi: 10.1126/science.179.4073.584. [DOI] [PubMed] [Google Scholar]
- LECHEVALIER H., BOROWSKI E., LAMPEN J. O., SCHAFFNER C. P. Water-soluble N-acetyl derivatives of heptaene macrolide antifungal antibiotics: microbiological studies. Antibiot Chemother (Northfield) 1961 Oct;11:640–647. [PubMed] [Google Scholar]
- Lampen J. O. Amphotericin B and other polyenic antifungal antibiotics. Am J Clin Pathol. 1969 Aug;52(2):138–146. doi: 10.1093/ajcp/52.2.138. [DOI] [PubMed] [Google Scholar]
- Mechlinski W., Schaffner C. P. Polyene macrolide derivatives. I. N-acylation and esterification reactions with amphotericin B. J Antibiot (Tokyo) 1972 Apr;25(4):256–258. [PubMed] [Google Scholar]
- Schaffner C. P., Mechlinski W. Polyene macrolide derivatives. II. Physical-chemical properties of polyene macrolide esters and their water soluble salts. J Antibiot (Tokyo) 1972 Apr;25(4):259–260. [PubMed] [Google Scholar]
- Shadomy S. In vitro antifungal activity of clotrimazole (Bay b 5097). Infect Immun. 1971 Aug;4(2):143–148. doi: 10.1128/iai.4.2.143-148.1971. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Tewari R. P., Kugel H. L. Suppressive effect of streptomycin on the phagocytic activity of mouse peritoneal macrophages for Histoplasma capsulatum. Mycopathol Mycol Appl. 1971 May 28;44(3):231–240. doi: 10.1007/BF02128636. [DOI] [PubMed] [Google Scholar]
- Waksman S. A., Lechevalier H. A., Schaffner C. P. Candicidin and other polyenic antifungal antibiotics. Bull World Health Organ. 1965;33(2):219–226. [PMC free article] [PubMed] [Google Scholar]