TABLE 2.
Activity of amino artemisinins against early- and late-stage gametocytesa
| Compound | IC50 (nM) |
|
|---|---|---|
| Early-stage gametocytes | Late-stage gametocytes | |
| MB | 95.0 ± 11.3 | 143.0 ± 16.7 |
| Artemisinin | 37.0 ± 4.0 | 77.6 ± 50.0 |
| DHA | 43.0 ± 3.9 | 33.66 ± 1.98 |
| Artesunate | 37.7 ± 2.0 | 136.2 ± 85.9 |
| Artemether | 62.8 ± 3.0 | 259.4 ± 80.0 |
| Artemisone | 1.94 ± 0.11 | 42.4 ± 3.3b |
| Artemiside | 16.4 ± 1.0 | 1.5 ± 0.5b |
| 10-Sulfamide | 15.0 ± 2.0 | 419.4 ± 59.5 |
| 10-Arylamine | 38.2 ± 9.0 | 16.42 ± 6.38 |
| 10-Piperazine | 54.91 ± 5.11 | 25.7 ± 17.5b |
| 10-Phenylurea | 83 ± 2 | 1.70 ± 0.99b |
a
The IC50s of MB and the 10-amino artemisinins against early-stage (stage I to III) and late-stage (stage IV and V) gametocytes were determined using the luciferase assay. Data are means from at least two independent biological replicates (n = 2 to 4) performed in technical triplicate ± SEM.
b
Data are from a 72-h incubation period.