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 by 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. HepG2-A16-CD81EGFP inhibition in the third column was calculated by determining the dose response for host nuclei number. Chloroquine was the only compound dissolved in water instead of DMSO. Maximum concentration of strobilurin tested was 1 μM. na, not applicable.

    Compound    P. yoelii EEF IC50 (nM)    HepG2 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    1162 ± 85    6.1 ± 1.9    56.8 ± 15.6    <9    317 ± 60
    Chloroquine    1650 ± 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    3270 ± 840    3.1 ± 0.6    65.4 ± 4.7    <9    9.5 ± 10
    Strobilurin    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