TABLE 2.
In vitro trypanocidal activities of FTY720, sphingolipids, and SPHKI against T. brucei subspecies
Compound | IC50 (mean ± SD) (μM) fora: |
SI HEK293b | |||
---|---|---|---|---|---|
T. brucei brucei | T. brucei rhodesiense | T. brucei gambiense STIB930 | T. brucei gambiense K048 | ||
FTY720 | 0.59 ± 0.01 | 0.20 ± 0.01 | 0.01 ± 0.01 | 0.072 ± 0.08 | 16.8 |
FTY720P(S) | 1.21 ± 0.07 | 0.71 ± 0.09 | 0.03 ± 0.01 | 0.40 ± 0.13 | 14.8 |
FTY720P(R) | 1.98 ± 0.26 | 1.06 ± 0.21 | 0.11 ± 0.05 | 0.67 ± 0.05 | 9 |
Sphingosine | 1.26 ± 0.35 | 0.63 ± 0.09 | 0.54 ± 0.02 | 0.53 ± 0.08 | 31.4 |
d-Erythro-sphinganine | 1.71 ± 0.05 | 0.99 ± 0.04 | 0.86 ± 0.04 | 0.72 ± 0.08 | 6 |
d-Methyl-sphingosine | 1.63 ± 0.12 | 0.58 ± 0.11 | 0.02 ± 0.02 | 0.18 ± 0.01 | 12.2 |
N-hexanoyl-d-sphingosine | 2.89 ± 0.83 | 3.03 ± 0.17 | 6.17 ± 0.91 | 4.25 ± 0.43 | 1.4 |
CAY10621 | 0.48 ± 0.36 | 0.19 ± 0.03 | 0.06 ± 0.06 | 0.09 ± 0.14 | 20.8 |
PF543 | 10.79 ± 3.07 | 3.10 ± 1.25 | 0.51 ± 0.14 | 2.13 ± 0.16 | 1.8 |
SKI2 | 1.95 ± 0.92 | 3.73 ± 0.09 | 0.20 ± 0.03 | 0.34 ± 0.27 | 20.3 |
Pentamidine | 0.0027 ± 0.0007 | 0.0007 ± 0.0002 | 0.051 ± 0.016 | 260.8 | |
Diminazene aceturate | 0.027 ± 0.001 | 957 | |||
Puromycin | 0.038 ± 0.002 | 12 | |||
Melarsoprol | 0.007 ± 0.003 | 0.0006 ± 0.002 | 0.014 ± 0.002 |
Results from three independent experiments.
Selectivity index (SI) compared to HEK293 cells.