Table 2.
Anti-HIV-1 activities of I-11 and I-12 against wild-type strains, clinical isolated strains, and resistant strainsa.
| Strain | Cell | EC50 (μmol/L) |
CC50 (μmol/L) |
SI |
|||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| I-11 | I-12 | DB02 | NVP | I-11 | I-12 | DB02 | NVP | I-11 | I-12 | DB02 | NVP | ||
| HIV-1IIIB | C8166 | 0.0043 ± 0.0023 | 0.0189 ± 0.0058 | 0.0095 ± 0.0017 | 0.0274 ± 0.0068 | 94.48 ± 2.40 | >200 | >200 | >200 | 21,514 | >10,582 | >21,053 | >7299 |
| HIV-1Ba-L | TZM-b1 | 0.0485 ± 0.0068 | 0.1933 ± 0.0261 | 0.0377 ± 0.0231 | 0.1659 ± 0.0465 | 77.10 ± 3.68 | >200 | >200 | >200 | 1590 | >1035 | >5305 | >1206 |
| HIV-1TC-1 | PBMC | 0.0145 ± 0.0001 | 0.0554 ± 0.0112 | 0.0118 ± 0.0006 | 0.1992 ± 0.0487 | 46.84 ± 5.20 | >200 | >200 | >200 | 3230 | >3610 | >16,949 | >1004 |
| HIV-1WAN | PBMC | 0.0566 ± 0.0024 | 0.1651 ± 0.620 | 0.0151 ± 0.0025 | 0.0770 ± 0.0193 | 46.84 ± 5.20 | >200 | >200 | >200 | 828 | >1211 | >13,245 | >2597 |
| HIV-174Vb | C8166 | 0.0462 ± 0.0237 | 0.0881 ± 0.0179 | 0.0249 ± 0.0099 | 0.0768 ± 0.0193 | 94.48 ± 2.40 | >200 | >200 | >200 | 2045 | >2270 | >8032 | >2604 |
| HIV-1RF/V82F/184Vc | C8166 | 0.0541 ± 0.0231 | 0.2193 ± 0.0465 | 0.0465 ± 0.0089 | 0.0614 ± 0.0085 | 94.48 ± 2.40 | >200 | >200 | >200 | 951 | >912 | >4301 | >3257 |
| HIV-1A17d | C8166 | 2.77 ± 0.82 | 4.87 ± 2.71 | 6.01 ± 1.05 | 20.15 ± 3.10 | 94.48 ± 2.40 | >200 | >200 | >200 | 34 | >41 | >33 | >10 |
a
Mean activity of EC50 was exhibited by mean ± SD, n ≥ 3.
b
Mutation site of HIV-1RF/V82F/184V are V82F and M184V in protease encoding region in pol gene.
c
Mutation site of HIV-174V is L74V in reverse transcriptase (RT) encoding region in pol gene.
d
Mutation sites of HIV-1A17 are K103N and Y181C in RT encoding region in pol gene.