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Abstract
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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Authors (7)
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Irena Bylińska
- Uniwersytet Gdański Katedra Chemii Biomedycznej
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Details
- Category:
- Articles
- Type:
- artykuł w czasopiśmie wyróżnionym w JCR
- Published in:
-
BIOCONJUGATE CHEMISTRY
no. 29,
pages 1454 - 1465,
ISSN: 1043-1802 - Language:
- English
- Publication year:
- 2018
- Bibliographic description:
- 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
- DOI:
- Digital Object Identifier (open in new tab) 10.1021/acs.bioconjchem.8b00136
- Verified by:
- Gdańsk University of Technology
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