TABLE 2.
In vitro activities of E10, G5, and G25 against various P. falciparum clones and strainsa
| Strain and/or place of origin | Laboratory | IC50 (nM)
|
||||||
|---|---|---|---|---|---|---|---|---|
| CQ | Qui | MFQ | Pyr or Cyc | E10 | G5 | G25 | ||
| Nigerian strain | CNRS 5539 | 20 | S | S | 64 | 4 | 0.64 | |
| 3D7 | CNRS 5539 | 6 | 0.2 | |||||
| L-16, Sierra Leone | CNRCP | S | S | 103 (R) | 12.3* | 9.5* | ||
| FCR3, The Gambia | IMTSSA | 820 (R) | 1,680 (R) | 65 (R) | Cyc, 3,500 (R) | 129 | 12.7 | 3.5 |
| L1, Liberia | IMTSSA | 906 (R) | 2,300 (R) | 68 (R) | Cyc, 3,015 (R) | 77 | 5 | 1.4 |
| FCB-1, Colombia | MNHN | 420 (R) | 240 | 240* | 22* | 9.4* | ||
| Palo Alto, Calif. | Pasteur Institute | 50 | 4.9 | |||||
| F147, Nigeria | LSHTM | 19 | 2.3 | |||||
| H1, Honduras | LSHTM | 24 | Pyr (R) | 3.6 | ||||
| K1, Thailand | LSHTM | 288 (R) | (R) | M (R) | Pyr (R) | 15.3 | ||
| T996, Thailand | LSHTM | 27 | M (R) | Pyr (R) | 1.1 | |||
| 7G8, Brazil | LSHTM | 228 (R) | M (S) | 3.4 | ||||
| W2, Indochina | OCEAC | 510 (R) | 4.5 | |||||
| WRAIR | 191 (R) | 203 | 13 | Pyr, 212 (R) | 4.2 | |||
| D6, Sierra Leone | WRAIR | 9 | 37 | 20 | 5.3 | |||
| TM90C3B, Thailand | WRAIR | 114 (R) | 147 | 29 (R) | 1.9 | |||
a
IC50 were assessed after 48 h contact of infected RBC with the drug, except for cases in which the exposure time was 24 h (marked with an asterisk). S and R indicate susceptibility and resistance to the drug. The threshold IC50s for in vitro resistance to chloroquine (CQ), quinine (Qui), mefloquine (MFQ), pyrimethamine (Pyr), and cycloguanil (Cyc) were estimated to be >100, >800, >20, and >500 nM, respectively.