Table 3.
Efficacy of tested compounds in cells infected with intracellular L. donovani, and cytotoxicity against THP-1 and HEK293T cells.
| Compounds | Intracellular L. donovani IC50 ± SDa (μM) |
Extracellular L. donovani Promastigotes IC50 ± SDa (μM) |
THP-1 cell CC50± SDa (μM) |
HEK293T CC50 ± SDa (μM) |
Selectivity indexb | Safety indexc |
|---|---|---|---|---|---|---|
| 1a | 11.32 ± 1.81 | 52.59 ± 1.44 | 25.28 ± 3.56 | 30.64 ± 2.31 | 2.2 | 2.7 |
| 1e | 14.31 ± 2.03 | 28.32 ± 1.38 | 15.78 ± 3.23 | 45.10 ± 5.01 | 1.1 | 3.2 |
| Erufosine | 3.61 ± 1.05 | 9.75 ± 2.41 | 3.94 ± 1.02 | 40.80 ± 3.36 | 1.1 | 11.3 |
| Miltefosine | 2.55 ± 0.63 | 4.94 ± 0.47 | 40.84 ± 3.32 | >200 | 16.0 | >78.4 |
aShown are mean EC50 ± SD (standard deviations) of data from duplicate measurements.
bSelectivity index was calculated by dividing determined CC50 against human monocytic cell line derived from an acute monocytic leukaemia; THP-1 by determined IC50 for inhibition of Intracellular L. donovani.
cSafety index was calculated by dividing determined CC50 against normal human embryonic kidney cells; HEK293T by determined IC50 of Intracellular L. donovani.