Molecular Umbrellas Modulate the Selective Toxicity of Polyene Macrolide Antifungals - Publikacja - MOST Wiedzy

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Molecular Umbrellas Modulate the Selective Toxicity of Polyene Macrolide Antifungals

Abstrakt

Antifungal polyene macrolide antibiotics Amphotericin B (AmB) and Nystatin (NYS) were conjugated through the ω-amino acid linkers with diwalled “molecular umbrellas” composed of spermidine-linked deoxycholic or cholic acids. The presence of “umbrella” substituents modulated biological properties of the antibiotics, especially their selective toxicity. Some of the AmB-umbrella conjugates demonstrated antifungal in vitro activity comparable to that of the mother antibiotic but diminished mammalian toxicity, especially the hemolytic activity. In contrast, antifungal in vitro activity of NYS-umbrella conjugates was strongly reduced and all these conjugates demonstrated poorer than NYS selective toxicity. No correlation between the aggregation state and hemolytic activity of the novel conjugates was found.

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Andrzej Stanisław Skwarecki, Kornelia Skarbek, Dorota Martynow, Marcin Serocki, Irena Bylińska, Maria Jolanta Milewska, Sławomir Milewski. (2018). Molecular Umbrellas Modulate the Selective Toxicity of Polyene Macrolide Antifungals, 29(4), 1454-1465. https://doi.org/10.1021/acs.bioconjchem.8b00136

Informacje szczegółowe

Kategoria:
Publikacja w czasopiśmie
Typ:
artykuł w czasopiśmie wyróżnionym w JCR
Opublikowano w:
BIOCONJUGATE CHEMISTRY nr 29, strony 1454 - 1465,
ISSN: 1043-1802
Język:
angielski
Rok wydania:
2018
Opis bibliograficzny:
Skwarecki A., Skarbek K., Martynow D., Serocki M., Bylińska I., Milewska M., Milewski S.: Molecular Umbrellas Modulate the Selective Toxicity of Polyene Macrolide Antifungals// BIOCONJUGATE CHEMISTRY. -Vol. 29, nr. 4 (2018), s.1454-1465

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