Antitrypanosomal Activities of Proteasome Inhibitors

DOI: 10.1128/AAC.46.6.2038-2040.2002

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FIG. 1.
Effects of Z-Leu-Leu-Leu-B(OH)₂ and Z-Ile-Glu(OtBu)-Ala-Leu-CHO in inducing apoptosis in T. brucei and human cells. TC221 bloodstream forms (•) and HL-60 cells (□) were incubated with various concentrations of the proteasome inhibitors. After 24 h of culture, cells were stained with propidium iodide and analyzed with a fluorescence-activated cell sorter. Cells from the sub-G₀/G₁ peak were counted as apoptotic cells. The percentages of apoptotic cells were calculated in relation to the respective controls in the absence of proteasome inhibitor. Data points represent mean values from three independent experiments. The standard errors were typically less than 10%. 1.E-11 to 1.E-04, 10⁻¹¹ to 10⁻⁴.

TABLE 1.

ED₅₀s and MICs of proteasome inhibitors for bloodstream form T. brucei and human HL-60 cells^a

↵ a Values are the means of three independent experiments. The standard error never exceeded 30%.

TABLE 2.

ED₅₀ and MIC ratios of cytotoxic to trypanocidal activities of proteasome inhibitors^a