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Susceptibility

Antitrypanosomal Activities of Proteasome Inhibitors

Joseph Nkemgu-Njinkeng, Vera Rosenkranz, Michael Wink, Dietmar Steverding
Joseph Nkemgu-Njinkeng
1Abteilung Parasitologie, Hygiene-Institut
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Vera Rosenkranz
2Institut für Pharmazeutische Biologie, Ruprecht-Karls-Universität, Heidelberg, Germany
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Michael Wink
2Institut für Pharmazeutische Biologie, Ruprecht-Karls-Universität, Heidelberg, Germany
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Dietmar Steverding
1Abteilung Parasitologie, Hygiene-Institut
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  • For correspondence: dsteverding@hotmail.com
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.

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  • TABLE 1.

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

    CompoundT. bruceiHL-60
    ED50 (nM)MIC (nM)ED50 (nM)MIC (nM)
    Ac-Leu-Leu-Nle-CHO45100,0004,600>100,000
    Ac-Leu-Leu-Met-CHO1,600100,00020,000>100,000
    Z-Ile-Glu(OtBu)-Ala- Leu-CHO0.0864036100,000
    Z-Leu-Leu-Leu-CHO5.54,00073>100,000
    Z-Leu-Leu-Phe-CHO1507,000120100,000
    Z-Leu-Leu-Tyr-COCHO720100,0003,000>100,000
    Z-Leu-Leu-Leu-B(OH)20.32101.11,000
    • ↵ 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 inhibitorsa

    CompoundED50 (HL-60)/ED50 (T. brucei)MIC (HL-60)/MIC (T. brucei)
    AC-Leu-Leu-Nle-CHO102>1
    AC-Leu-Leu-Met-CHO13>1
    Z-Ile-Glu(OtBu)-Ala-Leu-CHO4192,500
    Z-Leu-Leu-Leu-CHO13>25
    Z-Leu-Leu-Phe-CHO0.814
    Z-Leu-Leu-Tyr-COCHO4>1
    Z-Leu-Leu-Leu-B(OH)23100
    • ↵ a ED50 and MIC ratios were calculated from ED50s and MICs shown in Table 1.

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Antitrypanosomal Activities of Proteasome Inhibitors
Joseph Nkemgu-Njinkeng, Vera Rosenkranz, Michael Wink, Dietmar Steverding
Antimicrobial Agents and Chemotherapy Jun 2002, 46 (6) 2038-2040; DOI: 10.1128/AAC.46.6.2038-2040.2002

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Antitrypanosomal Activities of Proteasome Inhibitors
Joseph Nkemgu-Njinkeng, Vera Rosenkranz, Michael Wink, Dietmar Steverding
Antimicrobial Agents and Chemotherapy Jun 2002, 46 (6) 2038-2040; DOI: 10.1128/AAC.46.6.2038-2040.2002
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  • Top
  • Article
    • ABSTRACT
    • Proteasome inhibitors.
    • Assays.
    • Antitrypanosomal activities of proteasome inhibitors.
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KEYWORDS

Multienzyme Complexes
Trypanocidal Agents
Trypanosoma brucei brucei

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