Activity of drugs against wild-type T. brucei, Δ tbat1 knockout cells, and a line selected in vitro for resistance to DB75
IC50 is defined as the 50% inhibitory concentration for cellular viability after 72 h of treatment with trypanocide using Alamar Blue as an indicator dye for metabolic activity. Resistance factor for each compound was calculated by dividing the IC50 value attained with the DB75R-CL1 or Δ tbat1cells by the value attained with wild-type T. brucei brucei 427 cells. All experiments were performed in duplicate on at least three independent occasions. S.E. were always below 20% of those given mean values.
Trypanocide | Wild-Type | Δtbat1 | DB75R-CL1 | ||||
|---|---|---|---|---|---|---|---|
| IC50 | IC50 | Resistance Factor | IC50 | Resistance Factor | |||
| μM | μM | μM | |||||
| DB75 | 0.08 | 0.85 | 10.6 | 1.6 | 20 | ||
| Diminazene aceturate | 0.09 | 1.6 | 17.8 | 1.9 | 21.1 | ||
| Pentamidine isethionate | 0.01 | 0.03 | 3 | 0.06 | 6 | ||
| Cymelarsan | 0.03 | 0.09 | 3 | 0.05 | 1.7 | ||
| Melarsoprol | 0.03 | 0.03 | 1 | 0.03 | 1 | ||
| Melarsen oxide | 0.01 | 0.02 | 1 | 0.01 | 1 | ||
| DAPI | 0.57 | 1.7 | 3 | 1.1 | 1.9 | ||
| Suramin | 0.02 | 0.02 | 1 | 0.02 | 1 | ||
| Isometamidium | 2.2 | 6.5 | 3 | 1.8 | 0.8 | ||
| Megazol | 0.09 | 0.1 | 1.1 | 0.06 | 0.7 | ||