Molecular Umbrella as a Nanocarrier for Antifungals.
Andrzej S SkwareckiDorota MartynowMaria J MilewskaSławomir MilewskiPublished in: Molecules (Basel, Switzerland) (2021)
A molecular umbrella composed of two O-sulfated cholic acid residues was applied for the construction of conjugates with cispentacin, containing a "trimethyl lock" (TML) or o-dithiobenzylcarbamoyl moiety as a cleavable linker. Three out of five conjugates demonstrated antifungal in vitro activity against C. albicans and C. glabrata but not against C. krusei, with MIC90 values in the 0.22-0.99 mM range and were not hemolytic. Antifungal activity of the most active conjugate 24c, containing the TML-pimelate linker, was comparable to that of intact cispentacin. A structural analogue of 24c, containing the Nap-NH2 fluorescent probe, was accumulated in Candida cells, and TML-containing conjugates were cleaved in cell-free extract of C. albicans cells. These results suggest that a molecular umbrella can be successfully applied as a nanocarrier for the construction of cleavable antifungal conjugates.
Keyphrases
- candida albicans
- induced apoptosis
- cancer therapy
- fluorescent probe
- cell free
- drug delivery
- biofilm formation
- cell cycle arrest
- living cells
- meta analyses
- single molecule
- randomized controlled trial
- cell death
- systematic review
- signaling pathway
- room temperature
- anti inflammatory
- cell proliferation
- pi k akt
- circulating tumor cells