Table 4. Anti-HIV-1 activity of nucleoside analogues in Vpx expressing THP1 cells.
Nucleoside analogue | PMA− |
PMA+ |
||||||
---|---|---|---|---|---|---|---|---|
EC50 (μM)a [95% CI]b |
Fold | pc | EC50 (μM) [95% CI] |
Fold | p | |||
Vpx− | Vpx+ | Vpx− | Vpx+ | |||||
ACV | >200 | >200 | — | — | 1.08 [0.735–1.43] | 29.6 [2.62–56.5] | 27 | 0.0004 |
GCV | >200 | >200 | — | — | 0.632 [0.596–0.668] | >200 | >316 | <0.0001 |
CFB | 0.340 [0.118–0.563] | >1.6 | >5 | <0.0001 | 0.003 [0.002–0.004] | 0.012 [0.003–0.021] | 4 | 0.0017 |
d4T | 4.39 [3.76–5.02] | 13.3 [12.1–14.4] | 3 | 0.0001 | 1.49 [0.501–2.48] | 52.2 [33.0–71.5] | 35 | 0.0009 |
ddI | 1.04 [0.863–1.22] | 2.73 [1.40–4.07] | 3 | 0.0039 | 0.079 [0.061–0.096] | 4.34 [3.19–5.50] | 55 | 0.0005 |
ABC | 0.459 [0.399–0.519] | 0.622 [0.356–0.888] | 1 | 0.0619† | 0.038 [0.036–0.040] | 7.050 [4.67–9.43] | 187 | 0.0002 |
NVP | 0.244 [0.240–0.248] | 0.292 [0.067–0.517] | 1 | 0.1146† | 0.223 [0.196–0.250] | 0.235 [0.217–0.253] | 1 | 0.0379† |
RAL | 0.035 [0.017–0.053] | 0.043 [0.016–0.070] | 1 | 0.0683† | 0.038 [0.020–0.056] | 0.037 [0.002–0.072] | 1 | 0.9071† |
aEC50 is the effective concentration of drug that inhibits infection of cells by 50% measured as the percentage of GFP+ cells in Vpx− or Vpx+ populations. Values were calculated by non-linear regression for at least two independent experiments.
b95% confidence interval. Non-ambiguous values were subject to a replicate test.
cEC50 values for each replicate were used to perform an unpaired two-tailed t-test to determine differences between Vpx− and Vpx+ populations.
†Difference not statistically significant.