TABLE 2.
Summary of properties associated with the pharmacological activity of bisthiazoliums against the two hematozoan parasites
| Parasite | IC50 for growth inhibition (nM) | T16 accumulation (CAR) into infected erythrocytes | T16 uptake into infected erythrocytes
|
Exchangeability | Proportion of T16 (%)
|
Interaction with FPIX/hemozoin | PC50 after 3 h | Kinetics for choline transport into free parasites
|
|||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Apparent Km (μM) | Vmax (pmol/107 infected cells/min) | Inside the intracellular parasite | In acidic food vacuole | Associated with hemozoinb | Apparent Km (μM) | Vmax (pmol 107 infected cells/min) | T16 inhibition (IC50) | ||||||
| Babesia divergens | 28 | >60 | 0.65 | 0.20 | No | ∼80 | Not applicable | Not applied (<1) | Not applied | Yes; specific (69 nM) | 8.5 ± 1.8 | 3.47 ± 1.22 | Yes (89 ± 20 nM) |
| Plasmodium falciparum | 1.9 | >600a | 0.73 ± 0.26 | Partial (until 40%) | 50-80 | ∼40a | >20 | Yes, likely to contribute to antimalarial activityc | Yes; specific (180 nM) | 25.0 ± 3.5c | 46 ± 2c | Yes (140 μM)c | |