Table 4.
Anti-RSV activity of NIH351: Effect of 5′-monothiophosphate removal and antisense domain nucleotide sequence scrambling
| Oligonucleotide | Description | Structure/sequence | Neutral red assay
|
|
|---|---|---|---|---|
| EC50, μM | IC50, μM | |||
| NIH351 | 2-5A-gap-mer | 2-5A4-Bu2-AsAsAsAATGGGGCAAAsTsAsA | 0.08 ± 0.02 | >3.2 |
| NIH426 | Scrambled 2-5A-gap-mer | 2-5A4-Bu2-GsAsTsAGAAATAGAAAsGsCsA | 3.4 ± 1.5 | >3 |
| NIH489 | Dephospho-2-5A-gap-mer | A3-Bu2-AsAsAsAATGGGGCAAAsTsAsA | >10 | >10 |
| NIH320 | Gap-mer | AsAsAsAATGGGGCAAAsTsAsA | >10 | >10 |
Oligonucleotides were added to HEp-2 cells according to the protocol of Table 2 for 4 days by removal of medium and addition of fresh medium containing the appropriate oligonucleotide concentration. The assay was stopped at the end of day 6. Under these assay conditions, ribavirin showed an EC50 of <4 μM and an IC50 of 231 μM. EC50 and IC30 see legend to Table 2.