Molecular umbrella-amphotericin B conjugates.
Publication
, Journal Article
Janout, V; Bienvenu, C; Schell, W; Perfect, JR; Regen, SL
Published in: Bioconjug Chem
August 20, 2014
A tetrawalled and an octawalled molecular umbrella conjugate of amphotericin B (AmB) have been synthesized. Both conjugates exhibit high water solubility, a low tendency to aggregate, negligible hemolytic activity at 100 μM, and an ability to release a derivative of AmB under reducing conditions that exhibits high antifungal activity. Whereas the larger, octawalled conjugate shows slight adsorption to liposomal membranes and an ability to cross them by passive transport, the tetrawalled analogue shows significant adsorption and much lower bilayer transport activity. The potential of molecular umbrella-AmB conjugates as therapeutic agents is briefly discussed.
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Published In
Bioconjug Chem
DOI
EISSN
1520-4812
Publication Date
August 20, 2014
Volume
25
Issue
8
Start / End Page
1408 / 1411
Location
United States
Related Subject Headings
- Water
- Structure-Activity Relationship
- Solubility
- Organic Chemistry
- Micelles
- Hydrophobic and Hydrophilic Interactions
- Antifungal Agents
- Amphotericin B
- 3404 Medicinal and biomolecular chemistry
- 3101 Biochemistry and cell biology
Citation
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Janout, V., Bienvenu, C., Schell, W., Perfect, J. R., & Regen, S. L. (2014). Molecular umbrella-amphotericin B conjugates. Bioconjug Chem, 25(8), 1408–1411. https://doi.org/10.1021/bc500277v
Janout, Vaclav, Celine Bienvenu, Wiley Schell, John R. Perfect, and Steven L. Regen. “Molecular umbrella-amphotericin B conjugates.” Bioconjug Chem 25, no. 8 (August 20, 2014): 1408–11. https://doi.org/10.1021/bc500277v.
Janout V, Bienvenu C, Schell W, Perfect JR, Regen SL. Molecular umbrella-amphotericin B conjugates. Bioconjug Chem. 2014 Aug 20;25(8):1408–11.
Janout, Vaclav, et al. “Molecular umbrella-amphotericin B conjugates.” Bioconjug Chem, vol. 25, no. 8, Aug. 2014, pp. 1408–11. Pubmed, doi:10.1021/bc500277v.
Janout V, Bienvenu C, Schell W, Perfect JR, Regen SL. Molecular umbrella-amphotericin B conjugates. Bioconjug Chem. 2014 Aug 20;25(8):1408–1411.
Published In
Bioconjug Chem
DOI
EISSN
1520-4812
Publication Date
August 20, 2014
Volume
25
Issue
8
Start / End Page
1408 / 1411
Location
United States
Related Subject Headings
- Water
- Structure-Activity Relationship
- Solubility
- Organic Chemistry
- Micelles
- Hydrophobic and Hydrophilic Interactions
- Antifungal Agents
- Amphotericin B
- 3404 Medicinal and biomolecular chemistry
- 3101 Biochemistry and cell biology