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Background Previous reports have demonstrated two thiazolidione derivatives (H2-60 and H2-81) can robustly inhibit the planktonic growth and biofilm formation of  S. epidermidis  and  S. aureus  by targeting the histidine kinase YycG .  Whereas the antibacterial and anti-biofilm activity of these two thiazolidione derivatives (H2-60 and H2-81) against  Enterococcus faecium  remains elusive. Here, the pET28a-YycG recombinant plasmid were in vitro expressed in  E. coli  competent cell BL21 (DE3) and induced to express YycG’ protein (conding HisKA and HATPase_c domain) by 0.5 mM IPTG and was purified by Ni – NTA agarose and then for the autophosphorylation test. Antimicrobial testing and time-killing assay were also be determined. Anti-biofilm activity of two derivatives with sub-MIC concentration towards positive biofilm producers of clinical  E. faecium  were detected using polystyrene microtiter plate and CLSM. Results The MICs of H2-60 and H2-81 in the clinical isolates of  E. faecium  were in the range from 3.125 mg/L to 25 mg/L. Moreover, either H2-60 or H2-81 showed the excellent bactericidal activity against  E. faecium  with monotherapy or its combination with daptomycin by time-killing assay.  E. faecium  planktonic cells can be decreased by H2-60 or H2-81 for more than 3 × log10 CFU/mL after 24 h treatment when combined with daptomycin. Furthermore, over 90% of  E. faecium  biofilm formation could markedly be inhibited by H2-60 and H2-81 at 1/4 × MIC value. In addition, the frequency of the eradicated viable cells embedded in mature biofilm were evaluated by the confocal laser microscopy, suggesting that of H2-60 combined with ampicillin or daptomycin was significantly high when compared with single treatment (78.17 and 74.48% vs. 41.59%, respectively,  P  &lt; 0.01). Conclusion These two thiazolidione derivatives (H2-60 and H2-81) could directly impact the kinase phosphoration activity of YycG of  E. faecium . H2-60 combined with daptomycin exhibit the excellent antibacterial and anti-biofilm activity against  E. faecium  by targeting YycG.

In vitro activities of thiazolidione derivatives combined with daptomycin against clinical Enterococcus faecium strains