Table 1. Potency of GNF7686 and prototypic cytochrome b Inhibitors on wild-type (WT) and GNF7686-resistant (DR) T. cruzi morphological forms.
Amastigote EC50 [μM] | Epimastigote EC50 [μM] | Trypomastigote EC50 [μM] | ||||
---|---|---|---|---|---|---|
Compound | WT | DR | WT | DR | WT | DR |
GNF7686 | 0.15 ± .03* | 0.66 ± 0.12* | 0.16 ± 0.02* | 0.73 ± 0.04* | 0.71 ± 0.16* | 4.5 ± 0.84* |
Antimycin A | N.A. | N.A. | 0.046 ± 0.01* | 1.8 ± 0.21* | 0.20 ± 0.04* | 4.3 ± 1.3* |
Myxothiazol | N.A. | N.A. | 0.49 ± 0.05 | 0.43 ± 0.08 | 2.9 ± 0.48 | 2.9 ± 0.43 |
Strobilurin | N.A, | N.A. | 0.59 ± 0.13 | 0.34 ± 0.01 | 1.7± 0.41 | 1.4 ± 0.36 |
Benznidazole | 1.4 ± 0.17 | 0.82 ± 0.13 | 5.5 ± 0.15 | 6.7 ± 0.6 | 13± 1.8 | 11 ± 0.58 |
EC50 values were calculated from three independent repeats (n = 3), each performed in duplicate. Standard error values are also shown. N.A. in the table stands for ‘not applicable’.
*P-value for wild-type versus drug-resistant T. cruzi EC50 values is < 0.05.