Discovery of deguelin derivatives in combination with fluconazole against drug-resistant Candida albicans

In this study, a series of deguelin (Deg) derivative were prepared and identified with in vitro antifungal activity against drug-resistantC. albicans combined with fluconazole (FLC). The combination of Deg derivative17c and FLC exhibited the best activity, with a fractional inhibitory combination index (FICI) of 0.02. The sensitization effect of17c + FLC was further validated by the temporal fungicidal curve analysis. In addition,17c + FLC also demonstrated inhibitory effects on the mycelial transformation and biofilm formation of resistantC. albicans, and significantly reduced the expression of key genes related to the RAS1/cAMP/PKA cell-transduction pathway.
Source: Medicinal Chemistry Research - Category: Chemistry Source Type: research