Insights into the antimicrobial effects of tafenoquine against enterococcus and its biofilms

Aim: The purpose of this study is to assess the in vitro antimicrobial and anti-biofilm effects of the anti-protozoal agent tafenoquine (TAF) on Enterococcus and elucidate its underlying mode of action.

Methods and results: The present work investigated the susceptibility of TAF on 3 type strains and 11 clinical isolates of enterococci. The results indicated that TAF exhibited powerful anti-microbial activity against both of E. faecalis and E. faecium with minimum inhibitory and bactericidal concentrations ranging from 8 to 16 μg.mL-1. Meanwhile, biofilm inhibition and eradication assays showed that TAF exhibited potent anti-biofilm activity against E. faecalis ATCC 29212 and E. faecium ATCC 19434. Ultra-microscopic observations revealed significant changes in Bacterial morphology and structure caused by TAF, particularly for the disruption of plasma membrane. Mechanistic investigations also revealed that TAF altered both membrane permeability and potential, while also impacting adenosine triphosphate production as well as Reactive Oxygen Species generation. In addition, no detectable cytotoxicity of TAF on human cells was observed at concentrations near the minimal inhibitory concentration.

Conclusions: In summary, this study confirmed that TAF could effectively inhibit Enterococcus as well as its biofilm formation.

Enterococcus; Tafenoquine; antimicrobial; biofilm; membrane disruption; membrane potential.