TABLE 1.
Range of anti-HIV activities of calanolide analogs in established human cell lines
| Virus (isolate) | Cellsa | EC50 (μM)b
|
||||
|---|---|---|---|---|---|---|
| Calanolide A | Costatolide | Dihydrocostatolide | Nevirapine | AZT | ||
| HIV-1 (IIIB) | CEM-SS | 0.08 | 0.2 | 0.1 | 0.1 | 0.003 |
| HIV-1 (RF) | CEM-SS | 0.1 | 0.7 | 0.6 | 0.2 | 0.004 |
| HIV-1 (SK1) | CEM-SS | 0.09 | 0.06 | 0.3 | 0.2 | 0.005 |
| HIV-2 (ROD) | CEM-SS | >10 | >10 | >10 | >38 | 0.005 |
| SIV (DeltaB670) | 174×CEM | >10 | >10 | >10 | >38 | 0.02 |
| HIV-1 (IIIB) | 174×CEM | 0.5 | 0.15 | 0.8 | 0.1 | 0.03 |
| HIV-1 (IIIB) | MT2 | 0.4 | 0.8 | 0.8 | 0.1 | 0.04 |
| HIV-1 (IIIB) | U937 | 0.2 | 0.3 | 0.8 | 0.3 | 0.003 |
| HIV-1 (IIIB) | AA5 | 0.2 | 1.4 | 0.6 | 0.7 | 0.01 |
| HIV-1 (WEJO) | PBMC | 0.03 | 0.2 | 0.2 | 0.06 | 0.02 |
| ROJO (SI) | PBMC | 0.07 | 1.5 | 0.5 | 0.3 | 0.01 |
| TEKI (SI) | PBMC | 0.3 | 0.2 | 0.5 | 0.1 | 0.05 |
| SLKA (SI) | PBMC | 0.3 | 0.03 | 0.3 | 0.2 | 0.02 |
| Clade A | PBMC | 0.07 | 0.1 | 0.5 | 0.06 | 0.008 |
| Clade B | PBMC | 0.2 | 0.2 | 0.4 | 0.07 | 0.01 |
| Clade C | PBMC | 0.02 | 0.09 | 0.06 | 0.05 | 0.007 |
| Clade D | PBMC | 0.06 | 0.2 | 0.2 | 0.1 | 0.01 |
| Clade E | PBMC | 0.03 | 0.4 | 0.5 | 0.007 | 0.01 |
| Clade F | PBMC | 0.04 | 0.1 | 0.1 | 0.2 | 0.05 |
| BaL | MM | 0.05 | 0.01 | 0.1 | 0.4 | 0.03 |
| ADA | MM | 0.07 | 0.05 | 0.1 | 0.2 | 0.01 |
a
Cellular phenotypes are as follows: CEM-SS, T cell; 174×CEM, T cell–B cell fusion; U937, macrophage; AA5, Epstein-Barr virus-infected B cell; PBMC, fresh PBMCs, MM, fresh peripheral blood monocytes.
b
EC50s are the mean for a minimum of three replicate evaluations. The reproducibilities of the EC50s obtained between replicate experiments in this highly optimized anti-HIV assay have been determined to be such that the standard errors averaged less than 10% of the respective mean value.