Table 1. Trypanocidal and leishmanicidal activities of cytochalasins A–D against intracellular T. cruzi Tulahuen LacZ and L. infantum amastigotes and cytotoxicity for fibroblasts (HFF-1), human macrophages (THP-1) and hepatocytes (HepG2).
| T. cruzi IC50 (μM ± SD) | HFF-1 CC50 (μM ± SD) | SI1 | L. infantum IC50 (μM ± SD) | THP-1 CC50 (μM ± SD) | SI2 | HepG2 CC50 (μM ± SD) | SI3 | SI4 | |
|---|---|---|---|---|---|---|---|---|---|
| Cytochalasin A | 3.02 ± 2.16 | 27.07 ± 0.17 | 8.96 | 2.76 ± 1.17 | 17.03 ± 1.34 | 6.17 | 21.12 ± 4.51 | 6.99 | 7.65 |
| Cytochalasin B | 16.87 ± 1.47 | 21.81 ± 3.57 | 1.29 | 23.87 ± 3.02 | 109.20 ± 2.4 | 4.57 | 46.27 ± 19.33 | 2.74 | 1.93 |
| Cytochalasin C | 10.24 ± 1.13 | 76.3 ± 3.12 | 7.45 | 23.22 ± 4.90 | 84.84 ± 6.84 | 3.65 | 22.46 ± 6.47 | 2.19 | 0.96 |
| Cytochalasin D | 20.15 ± 3.27 | 96.47 ± 10 | 4.78 | 22.54 ± 0.97 | 122.20 ± 11.31 | 5.42 | 123.20 ± 20 | 6.11 | 5.46 |
| BZ | 5.20 ± 1.87 | > 64 | >12.3 | - | - | - | - | - | - |
| MIL | - | - | - | 1.10 ± 0.16 | 58.46 ± 5.37 | 53.14 | - | - | - |
| DOX | - | 0.69± 0.08 | - | - | 0.97± 0.31 | - | 0.24 ± 0.06 | - | - |
SI, selectivity index; BZ, reference drug for Chagas disease; MIL, reference drug for leishmaniasis; DOX, positive control for cytotoxicity evaluation; SI1 CC50 HFF-1/IC50 T. cruzi; SI2 CC50 THP-1/IC50 L. infantum; SI3 CC50 HepG2/IC50 T. cruzi; and SI4 CC50 HepG2/IC50 L. infantum.