Table 3.
Predicted intracellular localization of ten antimalarial drugs; concentration ratio to outside in lysosomes (Lys), cytosol (Cyt) and mitochondria (Mit); in bold: selective accumulation in lysosomes (> 5times above cytosol and mitochondria).
| Chemical | Lys | Cyt | Mit |
|---|---|---|---|
| Amodiaquine | 479 | 42.5 | 51.2 |
| Artemesinine | 10 | 10 | 10 |
| Chloroquine * | 582 – 5180** | 23 | 2.85 |
| Cycloguanil | 43.5 | 3.4 | 0.5 |
| Halofantrine | 23700 | 18100 | 83300 |
| Quinine | 48.3 | 5.5 | 3.1 |
| Mefloquine | 9.2 | 5.8 | 4.1 |
| Primacrine | 12.5 | 5.5 | 3.4 |
| Pyrimethamine | 72.1 | 12.6 | 12.0 |
| Pyrimethamine* | 127 | 10.3 | 9.2 |
| Quinine * | 138 | 8.7 | 6.4 |
| Quinidine * | 239 | 17.3 | 15.2 |
*
Calculated with the data provided by Newton and Kluza (1978); quinine and quinidine are structurally identical optical isomeres.
**
pH of lysosomes 5 or 6; an increase of lysosomal pH has been observed after adding chloroquine to cells (Poole and Ohkuma 1981).