The synthesis and antifungal activity of (20S)-3β-acetoxy-5α-pregnane-20,16β-carbolactone against fluconazole - Resistant Candida cells

- Efficient and short procedure for the synthesis of the bioactive compound.
- Biocompatibility against host cells.
- Selective activity and restriction of fungal cells growth.
- Eradication of fungal cells embedded in biofilm.
- Approaches for treatment infections caused by antibiotic-resistant fungal strains.

An efficient procedure for the synthesis of (20S)-3β-acetoxy-5α-pregnane-20,16β-carbolactone is described. Bactericidal and fungicidal activity of the lactone against different bacteria such as MSSA, MRSA, E. coli ESBL, P. aeruginosa and clinical isolates of Candida spp., in planktonic and biofilm growth stage were assessed. Additionally, the affinity of this new compound to microbial plasma membrane and hemoglobin release from human red blood cells were determined using fluorometric and colorimetric assay, respectively. Our studies revealed that the lactone exhibits strong antifungal activity, and the ability to prevent pathogens' biofilm formation. Additionally, upon lactone treatment a significant affinity to fungal, but not to human cell membranes, indicating suitable biocompatibility was observed.

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