Possible Interaction: Berberine and Fluconazole

“Our previous study demonstrated that concomitant use of berberine (BBR) and fluconazole (FLC) showed a synergistic action against FLC-resistant C. albicans in vitro and BBR had a major antifungal effect in the synergism, while FLC played a role of increasing the intracellular BBR concentration.”

“However, berberine at concentrations of >1.9 μg/ml combined with a fluconazole supra-MIC (i.e., >1.9 μg/ml) eliminated the residual turbidity in the incubation wells.”

“The MIC of fluconazole was 1.9 μg/ml when the drug was tested alone and decreased to 0.48 μg/ml in the presence of berberine concentrations of 1.9 μg/ml.”

“Functional analyses revealed that FLC + BBR treatment increased mitochondrial membrane potential, decreased intracellular ATP level, inhibited ATP-synthase activity, and increased generation of endogenous reactive oxygen species (ROS) in FLC-resistant strains.”

“Our previous study showed that concomitant use of berberine (BBR) and fluconazole (FLC) provided a synergistic action against FLC-resistant Candida albicans (C. albicans) clinical strains in vitro.”

“We demonstrate the synergistic effect of combination of berberine with fluconazole (52.38%), itraconazole (66.67%), voriconazole (71.43%), amphotericin B (71.43%) or caspofungin (52.38%) of T. marneffei strains, respectively.”

“Biochemical analysis indicated that FLC significantly inhibited cellular ergosterol synthesis, leading to a decrease in cell membrane stability, which increased the rate of BBR uptake and utilisation and reduced the inhibitory concentrations of BBR in wild-type yeast cells.”

“OBJECTIVES Although berberine (BBR) is reported to exhibit weak activity against Candida albicans, combined use of BBR and fluconazole (FLC) showed synergism against FLC-resistant C. albicans in vitro.”

“After the treatments of BBR … species (ROS), (ii) FLC … BBR , (iii) BBR decreased the extracellular rhodamine 123 (Rh123) via inhibiting efflux transporters, (iv) FLC assisted BBR to reduce ergosterol content, … 1 (CDR1) and CDR2 but impact slightly multidrug resistance 1 (MDR1), and upregulate the expression of ergosterol 11 (ERG11).”

“The synergism of BBR and FLC was also confirmed microscopically.”

“We also suggested BBR played a major antifungal role in the synergism of FLC and BBR, while FLC increased intracellular BBR concentrations.”

“Abstract: Our previous work revealed berberine can significantly enhance the susceptibility of fluconazole against fluconazole-resistant Candida albicans, which suggested that berberine has synergistic antifungal activity with fluconazole.”

“These results contribute to our understanding of the mechanism of synergistic effect of BBR and FLC.”

“ABSTRACT It was found in our previous study that berberine (BBR) and fluconazole (FLC) used concomitantly exhibited a synergism against FLC-resistant Candida albicans in vitro.”

“Detection of intracellular BBR accumulation by fluorescence measurement showed that FLC played a role in increasing intracellular BBR concentration, probably due to its effect in disrupting the fungal cell membrane.”

“These results suggest that BBR plays a major antifungal role in the synergism of FLC and BBR, while FLC plays a role in increasing the intracellular BBR concentration.”