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N-methyl-N-D-fructosyl amphotericin B methyl ester [MF-AME], a novel antifungal agent of low toxicity: monomer-micelle control over selective toxicity

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Cybulska B., Gadomska I., Mazerski J., Grzybowska J., Borowski E., Cheron M., Bolard J.

Acta Biochimica Polonica

2000

tom 47

nr 1

Rational chemical modification of amphotericin B (AMB) led to the synthesis of sterically hindered AMB derivatives. The selected optimal compound, N-methyl- N-D-fructosyl amphotericin B methyl ester (MF-AME) retains the broad spectrum of antifungal activity of the parent antibiotic, and exhibits a two orders of magnitude lower toxicity in vivo and in vitro against mammalian cells. Comparative studies of MF-AME and AMB comprising the determination of the spectroscopic properties of monomeric and self-associated forms of the antibiotics, the investigation of the influence of self-association on toxicity to human red blood cells, and of the antibiotic-sterol interaction were performed. On the basis of the results obtained it can be assumed that the improvement of the selective toxicity of MF-AME could in part be a consequence of the diminished concentration of water soluble oligomers in aqueous medium, and the better ability to differentiate between cholesterol and ergosterol.

Ograniczanie wyników

1 Acta Biochimica Polonica

1 Bolard J.

1 Borowski E.

1 Cheron M.

1 Cybulska B.

1 Gadomska I.

1 Grzybowska J.

1 Mazerski J.

1 2000

Wyniki wyszukiwania

N-methyl-N-D-fructosyl amphotericin B methyl ester [MF-AME], a novel antifungal agent of low toxicity: monomer-micelle control over selective toxicity