Article Figures & Data
Figures
- FIG. 1.
Structures of oxazolidinones linezolid and eperezolid.
- FIG. 2.
Linezolid and eperezolid inhibit rat heart mitochondrial protein synthesis. Mitochondrial protein synthesis was carried out in isolated rat heart mitochondria as described in Materials and Methods in the presence or absence of varying concentrations of linezolid ▪ or eperezolid ▾. Results shown are the average of duplicate determinations in one experiment; error bars show the range.
- FIG. 3.
Eperezolid inhibits the growth of human K562 cells. K562 cells were incubated in the presence or absence of varying concentrations of eperezolid, and cell counts were monitored as described in Materials and Methods. A. Cells were treated with the following: ▪, vehicle (0.5% DMSO); ▴, 1.7 μM; ▾, 5 μM; ⧫, 15 μM; •, 45 μM; □, 135 μM; or Δ, 400 μM eperezolid. B. K562 cells were incubated with varying concentrations of eperezolid, and cell proliferation was monitored by cell counts after 120 h.
- FIG. 4.
Growth inhibition by eperezolid is reversible. K562 cells were grown in the presence of ▪, vehicle (0.5% DMSO); ▾, 15 μM eperezolid; or •, 30 μM eperezolid for 72 h. Cells were then washed in RPMI media and replated in media containing ▪, vehicle (0.5% DMSO); ▾, 15 μM eperezolid; ▴, vehicle (15 μM eperezolid recovery); •, 30 μM eperezolid; or ⧫, vehicle (30 μM eperezolid recovery) and cultured for an additional 5 days. Results shown are the average of triplicate determinations, and error bars show the standard errors of the means.
- FIG. 5.
Eperezolid decreases mitochondrial Cox-1 protein levels. K562 cells were treated with vehicle (0.5% DMSO), 100 μM chloramphenicol, or varying concentrations of eperezolid for 5 days, and mitochondria were isolated. Aliquots of mitochondrial protein (10 μg) were electrophoresed on sodium dodecyl sulfate-polyacrylamide gel electrophoresis, transferred to polyvinylidene difluoride membranes, and probed with an antibody to Cox-1 (top gel). The blot was stripped and reprobed with an antibody to Tom-20 (bottom gel). Lane 1, vehicle; 2, 3.1 μM eperezolid; 3, 6.2 μM eperezolid; 4, 12 μM eperezolid; 5, 25 μM eperezolid; 6, 50 μM eperezolid; 7, 100 μM eperezolid; 8, 100 μM chloramphenicol. The 30-kDa and 40-kDa molecular mass markers are designated on the left.
- FIG. 6.
Eperezolid inhibits cell proliferation in 143B cells but not in rho zero cells. Parent 143B (A) or rho zero (B) cells were incubated with □, vehicle (0.5% DMSO); ▪, 3 μM eperezolid; ▴, 10 μM eperezolid; ▾, 100 μM eperezolid; •, 1.7 μM etoposide; ⋄, 1.75 μM cycloheximide; or ○, 30 μM chloramphenicol, and cells were counted at 48, 72, 96, and 120 h.
