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N-Methyl-N-D-fructosyl-amphotericin B methyl ester (MFAME) is a new derivative of amphotericin B, which is characterised by low toxicity to mammalian cells and good solubility in water of its salts. The antifungal activity and effects of MFAME towards Candida albicans and Saccharomyces cerevisiae multidrug resistant MDR(+) and sensitive MDR(-) strains was compared with those of parent compound. The results obtained indicate that MDR(+) S. cerevisiae was sensitive to MFAME as well as to AMB. MFAME exhibited the same effects on fungal cells studied as parent antibiotic. The two antibiotics, depending on the dose applied induced cell stimulation, K+ efflux, and/or had a toxic effect.
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p.133-140,fig.
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- Technical University of Gdansk, 80-952 Gdansk, Poland
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Bibliografia
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- 4. Mazerski, J., Grzybowska, J. & Borowski, E. (1990) Influence of net charge on the aggregation and solubility behaviour of Amphotericin B and its derivatives in aqueous media. Eur. Biophys. J. 18, 159.
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- 7. Bontemps-Gracz, M.M., Grzybowska, J., Supino, R. & Borowski, E. (1999) In vitro evaluation of toxicity of amphotericin B derivatives towards mammalian cells. 7th International Symposium on Molecular Aspect ofChemotherapy, September, 1999, Gdansk, Poland. Abstracts book; p. 159.
- 8. Bolard, J. (1986) How do the polyene macrolide antibiotics affect the cellular membrane properties? Biochim.. Biophys. Acta. 864, 257- 304.
- 9. Borowski, E. & Cybulska, B. (1967) Potassiumless death of Saccharomyces cerevisiae cells treated with N-succinyl perimicin and the reversal fungicidal action of the antibiotic by potassium ions. Nature 213, 1034.
- 10. Malewicz, B. & Borowski, E. (1979) Energy dependence and reversibility of membrane alterations induced by polyene macrolide antibiotics in Chlorella vulgaris. Nature 281, 80-82.
- 11. Malewicz, B., Jenkin, J.H. & Borowski, E. (1981) Repair membrane alternation induced in baby hamster kidney cells by polyene antibiotics. Antimicrob. Agents Chemother. 19, 238-247.
- 12. Brajtburg, J., Elberg, S., Medoff, J. & Kobayashi, G. (1981) Increase in colony forming units of C. albicans after treatment with polyene antibiotics. Antimicrob. Agents Chemother. 19, 199-200.
- 13. Brajtburg, J., Elberg, S., Medoff, J., Kobayashi, G., Schlessinger, D. & Medoff, G. (1984) Stimulatory, permeabilizing, and toxic effect of amphotericin B on L cells. Antimicrob. Agents Chemother. 26, 892-897.
- 14. Mignini, F., Cybulska, B., Santoni, G., Giogi, M. & Borowski, E. (1995) Polyene macrolides stimulate growth of E. coli and influence siderophores production. 5th International Symposium on Molecular Aspects ofChemotherapy August 1995, Gdansk, Poland. Abstracts book; p. 99.
- 15. Malewicz, B., Howard, M., Jenkin, J.H. & Borowski, E. (1980) Dissociation between the induction of potassium efflux and cytostatic activity of polyene macrolides in mammalian cells. Antimicrob. Agents Chemother. 17, 699-706.
- 16. Brajtburg, J., Powderly, W.G., Kobayashi, G.S. & Medoff, G. (1990) Amphotericin B: current understanding of mechanism of action. Antimicrob. Agents Chemother. 34, 183-188.
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Bibliografia
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