Table 2.
Activity (EC50 and EC90, µM, n = 3) and selectivity of lipid biosynthesis inhibitors on Trypanosoma cruzi epimastigotes (STIB 980 strain) and intracellular amastigotes (Tulahuen strain in rat L6 myoblasts).
| Epimastigotes (mean ± SD) (µM) | Amastigotes (mean ± SD) (µM) | L6 cells (mean ± SD) (µM) | ||||
|---|---|---|---|---|---|---|
| Compound | EC50 | EC90 | EC50 | EC90 | EC50 | SIa |
| Benznidazole | 13.9 ± 2.2 | 101 ± 18 | 2.22 ± 0.98 | 6.61 ± 2.5 | >384 | >172 |
| Bezafibrate | >276 | >276 | 132.3 ± 38.6 | 226 ± 65 | >276 | >2.1 |
| D609 (potassium salt) |
154 ± 32 | >375 | 99.4 ± 17.6 | 198 ± 32 | 247 ± 20 | 2.5 |
| FTY720 | 7.55 ± 0.4 | 11.6 ± 0.3 | 0.81 ± 0.5 | 1.84 ± 1.3 | 0.39 ± 0.1 | 0.5 |
| FTY720 Phosphate | >258 | >258 | 93.8 ± 3.3 | 168 ± 25 | 127 ± 22 | 1.4 |
| Quinuclidine hydrochloride | >677 | > 677 | 478 ± 174 | > 677 | >677 | >1.4 |
| 3-Amino quinuclidine dihydrochloride |
>502 | >502 | 268 ± 10 | 485 ± 28 | >502 | >1.8 |
| Ro48-8071 | 11.6 ± 6.1 | 29.4 ± 16.2 | 0.47 ± 0.09 | 2.5 ± 1.9 | 5.7 ± 2.4 | 12 |
| Posaconazole | >14.2 | >14.2 | 0.002 ± 0.001 | 0.016 ± 0.005 | >1.42 | >700 |
| Tomatidine (hydrochloride) | 192 ± 8.1 | >221 | 0.78 ± 0.2 | 1.8 ± 0.2 | 89.5 ± 26.7 | 115 |
| TMP-153 | 106 ± 27 | >228 | 0.09± 0.04 | 3.9 ± 2.1 | 0.12 ± 0.03 | 1.4 |
| Myriocin | >249 | >249 | 130 ± 34 | 231 ± 25 | >249 | >1.9 |
| Fumonisin B1 | >92 | >92 | 50.8 ± 5.7 | 84 ± 9.1 | >92 | >1.8 |
| PDMP (hydrochloride) | 47.9 ± 9.4 | 88.7 ± 18 | 12.5 ± 2.9 | 24.6 ± 9 | 33.5 ± 3.1 | 2.7 |
| AMP-Deoxy nojirimycin |
158 ± 5.9 | 237 ± 2 | 34.8 ± 15.1 | 66.6 ± 15.4 | 40.4 ± 10.9 | 1.2 |
| Amitriptyline (hydrochloride) | 59.9 ± 5.4 | 96.8 ± 3.3 | 12.2 ± 3.6 | 20.9 ± 3 | 17.2 ± 1.2 | 1.4 |
| GW4869 (hydrochloride hydrate) | >173 | >173 | 106 ± 44 | >173 | >173 | >1.7 |
aSelectivity Index based on the EC50 and EC50 on intracellular amastigotes and the mammalian cells, respectively.