TABLE 3.
Interaction of artemisinin and two novel endoperoxides with thapsigargin
| Starting concn (μM) of thapsigargina | Assays with artemisinin
|
Assays with compound 3a
|
Assays with compound 3c
|
|||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Artemisinin concn (μM) | Apparent IC50 (μM)
|
SFIC | Starting concn (μM) of compound 3a | Apparent IC50 (μM)
|
SFIC | Starting concn (μM) of compound 3c | Apparent IC50 (μM)
|
SFIC | ||||
| Artemisinin | Thapsigargin | Compound 3a | Thapsigargin | Compound 3c | Thapsigargin | |||||||
| 2.5 | 0.04 | 0.010 | 0.31 | 1.04 | 1.6 | 0.14 | 0.22 | 0.8 | 0.6 | 0.10 | 0.42 | 0.97 |
| 5.0 | 0.02 | 0.0072 | 0.83 | 0.83 | 0.8 | 0.14 | 0.93 | 0.8 | 0.3 | 0.068 | 1.12 | 0.77 |
| 10.0 | 0.01 | 0.0054 | 2.33 | 0.85 | 0.4 | 0.079 | 2.0 | 0.71 | 0.15 | 0.048 | 3.02 | 0.84 |
Twofold dilutions of the drugs combined in a fixed ratio were added to P. falciparum parasites (strain D10). The apparent IC50 values for each of the drugs were estimated and used to calculate the SFIC values. The results represent the mean values for an experiment performed in duplicate. The IC50 values for the individual drugs determined for this data set were 7.4 μM for thapsigargin, 0.010 μM for artemisinin, 0.18 μM for compound 3a, and 0.11 μM for compound 3c.