Table 2. Antiviral and Cytotoxicity Profilea.
| BiCycle Wild type strain NL4–3 | Hela |
PBMC
MTS |
Strain 11808 (PI)f | Strain 7401 (NRTI)f | Strain 12231 (NNRTI)f | Strain 11845 (INI)f | |||
|---|---|---|---|---|---|---|---|---|---|
| ID | EC50 (μM)b | CC50 (μM)b | SI-Helac | CC50 (μM)b | SI-PBMCd | EC50 (μM)b | EC50 (μM)b | EC50 (μM)b | EC50 (μM)b |
| 4 | 1.2 ± 0.7 | 3.6 ± 0.7 | 3 | 2.6 ± 1.7 | 2 | ||||
| 15 | 2.3 ± 2 | 4.2 ± 3.4 | 2 | 11 ± 6.0 | 5 | ||||
| 16 | 0.7 ± 0.1 | 3.2 ± 0.9 | 5 | 3.0 ± 1.4 | 4 | ||||
| 17 | 0.2 ± 0.1 | 0.6 ± 0.04 | 3 | 2.4 ± 1 | 12 | ||||
| 20 | 0.2 ± 0.1 | 2.7 ± 0.4 | 13 | 3.1 ± 0.8 | 16 | ||||
| 25 | 0.4 ± 0.3 | 6.0 ± 0.2 | 15 | 1.1 ± 0.1 | 3 | ||||
| 27 | 0.04 ± 0.03 | 3.0 ± 0.1 | 75 | 2.7 ± 0.1 | 75 | 0.056 ± 0.02 (1.4)e | 0.031 ± 0.02 (0.8)e | 0.11 ± 0.04 (2.8)e | 0.09 ± 0.04 (2.3)e |
| 28 | 0.1 ± 0.03 | 3.0 ± 0.5 | 30 | 2.5 ± 0.2 | 25 | 0.02 ± 0.01 (0.2)e | 0.01 ± 0.005 (0.1)e | 0.08 ± 0.06 (0.8)e | 0.07 ± 0.08 (0.7)e |
| 29 | 0.1 ± 0.05 | 2.1 ± 0.3 | 21 | 5 ± 2 | 50 | 0.16 ± 0.1 (1.6)e | 0.13 ± 0.08 (1.3)e | 0.21 ± 0.07 (2.0)e | 0.09 ± 0.02 (0.9)e |
a
Susceptibility to viral strains harbouring resistance to drug used in clinical practice.
b
Data are average ± SD for a least two independent experiments.
c
SI-Hela: HELA CC50/BiCycle EC50.
d
SI-PBMC: PBMC CC50/BiCycle EC50.
e
Fold change values indicate the ratio between IC50 values from drug-resistant and NL4–3 wild type reference strains.
f
NIH AIDS Reagent Program catalogue number of resistant strains (www.aidsreagent.org). PI, resistance to protease inhibitor; NRTI, resistance to nucleoside reverse transcriptase inhibitor; NNRTI, resistance to non-nucleoside reverse transcriptase inhibitor; INI, resistance to integrase inhibitor.