Table 2.
Intracellular concentrations of AZT-TP or DXG-TP for activated or resting macrophages or PBM cells treated with 10 μM AZT-DXG at a ratio of 1:1a
| Cell type | Drugb | Active metabolite measured | Intracellular NRTI-TP(±SD) |
|
|---|---|---|---|---|
| μM | pmol/106 cells | |||
| PBM cells | ||||
| Activated | AZT | AZT-TP | 3.5 ± 0.9 | 1.1 ± 0.3 |
| Activated | AZT + DXG | AZT-TP | 2.7 ± 0.6 | 0.9 ± 0.2 |
| Activated | DXG | DXG-TP | 0.2 ± 0.1 | 0.06 ± 0.03 |
| Activated | AZT + DXG | DXG-TP | 0.25 ± 0.01 | 0.1 ± 0.003 |
| Resting | AZT | AZT-TP | 1.8 ± 0.4 | 0.6 ± 0.1 |
| Resting | AZT + DXG | AZT-TP | 1.4 ± 0.3 | 0.5 ± 0.1 |
| Resting | DXG | DXG-TP | 0.5 ± 0.2 | 0.2 ± 0.06 |
| Resting | AZT + DXG | DXG-TP | 0.54 ± 0.12 | 0.2 ± 0.03 |
| Macrophages | ||||
| Activated | AZT | AZT-TP | 0.3 ± 0.3 | 0.8 ± 0.8 |
| Activated | AZT + DXG | AZT-TP | 0.1 ± 0.05 | 0.3 ± 0.1 |
| Activated | DXG | DXG-TP | 0.05 ± 0.04 | 0.1 ± 0.1 |
| Activated | AZT + DXG | DXG-TP | 0.02 ± 0.008 | 0.05 ± 0.02 |
| Resting | AZT | AZT-TP | 0.1 ± 0.1 | 0.3 ± 0.3 |
| Resting | AZT + DXG | AZT-TP | 0.1 ± 0.01 | 0.3 ± 0.03 |
| Resting | DXG | DXG-TP | 0.04 ± 0.03 | 0.1 ± 0.08 |
| Resting | AZT + DXG | DXG-TP | 0.02 ± 0.01 | 0.05 ± 0.03 |
The presence of AZT did not antagonize DXG-TP levels in macrophages or PBM cells, independent of the activation state, and the presence of DXG did not antagonize AZT-TP levels in macrophages or PBM cells independent of the activation state.
AZT + DXG at a ratio of 1:1.