Table 1.
Blood-stage and liver-stage (EEF) IC50 values (with standard deviations) of select characterized compounds. Blood stage IC50 values were measured against P. falciparum W2 parasites using a SYBR green assay (30). The median EEF P. yoelii parasite area (in μm2±SD) was calculated from two or more independent experiments with ~50 schizonts each. All drugs were dissolved in DMSO. Median parasite size of control P. yoelii DMSO-treated EEFs ranged from 160 to 180 μm2.
| Compound | P. yoelii EEF IC50 (nM) | HepG21 inhibition IC50 (μM) | Median parasite area (μm2)
|
Blood IC50 (nM) | |
|---|---|---|---|---|---|
| 1 μM | 10 μM | ||||
| Cyclosporin | 71±3 | 2.3±0.7 | < 9 | < 9 | 345±116 |
| Lasalocid | 37±20 | 3.9±1.4 | < 9 | < 9 | 50±8 |
| Pyrimethamine | 2.4±1.6 | 6.3±3.3 | 31.1±0.7 | 29.6±2.0 | 15±2 |
| Berberine | 224±152 | 2.6±0.5 | 46.4±7.0 | 22.4±2.3 | 117±9 |
| Atovaquone | 9.4±15 | 9.5±2.5 | 18.2±1.0 | 18.6±1.0 | 2.2±0.4 |
| Primaquine | 1,162±85 | 6.1±1.9 | 56.8±15.6 | < 9 | 317±60 |
| Chloroquine2 | 1,650±132 | 1.6±0.3 | 65.4±9.5 | < 9 | 84±3 |
| Ovalicin | 0.7±0.3 | >10 | 35.1±3.1 | 19.1±0.9 | >10,000 |
| Artemisinin | >10,000 | >10 | na | na | 3.3±0.4 |
| Mefloquine | 3,270±840 | 3.1±0.6 | 65.4±4.7 | < 9 | 9.5±10 |
| Strobilurin3 | 8.8±0.6 | >1 | 22.3±3 | na | 7±0.1 |
| Cycloheximide | 78±28 | 0.22±0.10 | <9 | <9 | 366±69 |
| Decoquinate | 0.16±0.02 | >10 | 17.7±0.3 | 18.8±4.7 | 0.25±0.06 |
1
HepG2-A16-CD81EGFP inhibition was calculated by determining the dose response for host nuclei number.
2
Chloroquine was dissolved in water, not DMSO.
3
Maximum concentration tested was 1μM.
na, not applicable