Table 1.
Anti-kinetoplastid effects of the tested chalcones and flavanones.
|
T. b. brucei EC50 (µM) |
T. congolense EC50 (µM) |
L. mexicana EC50 (µM) | HFF | |||||
|---|---|---|---|---|---|---|---|---|
| Compound | MW | 427-WT | B48 | IL3000-WT | DA-Res | WT | EC50 (µM) | SI (Tbb) |
| 1 | 284.3 | 2.04 ± 0.07 | 1.80 ± 011 | 8.8 ± 0.39 | 8.8 ± 0.28 | 18.2 ± 1.0 | >350 | >172 |
| 2 | 300.3 | 14.6 ± 0.80 | 13.9 ± 0.60 | 34.0 ± 1.2 | 28.6 ± 1.4 * | 83.6 ± 0.7 | >330 | >22.8 |
| 3 | 284.3 | 30.1 ± 0.95 | 30.3 ± 1.1 | 137 ± 10 | 106 ± 15 | 271 ± 31 | >350 | >11.7 |
| 4 | 300.3 | 55.3 ± 1.6 | 51.9 ± 1.6 | 63.3 ± 7.9 | 48.0 ± 6.2 | 338 ± 9 | >330 | >6.0 |
| Diminazene | 0.15 ± 0.01 | 2.4 ± 0.36 ** | 0.15 ± 0.01 | 1.43 ± 0.03 *** | ND | ND | -- | |
| Pentamidine | 0.0034 ± 0.0004 | 0.72 ± 0.03 *** | 0.72 ± 0.07 | ND | 0.56 ± 0.07 | ND | -- | |
| PAO | ND | ND | ND | ND | ND | 1.31 ± 0.08 | -- | |
All of the data listed are the average and standard error of the mean (SEM) of at least three independent determinations. PAO—phenylarsine oxide; ND—not done. Statistical significance was determined using an unpaired Student’s t-test; * p < 0.05; ** p < 0.01; ***, p < 0.001. Selectivity index (SI) = EC50(HFF)/EC50(Tbb).