TABLE 2.
Effect of synthetic flavonoid dimers on pentamidine resistance of LeMDR1 mutantsa
| Compound | IC50 of pentamidine (μg/ml) ± SD
|
Mean IC50 (μg/ml) ± SD
|
|||
|---|---|---|---|---|---|
| LeMDR1−/− | Le wild type | LeV160 | Vinblastine (LeV160) | Puromycin (LeV160) | |
| No modulator | 18.9 ± 0.8 | 12.0 ± 0.8 | 9.0 ± 0.1 | 167.0 ± 3.6 | 16.0 ± 1.0 |
| 9a | 18.0 ± 1.0 | ND | ND | 170.0 ± 7.0 | ND |
| 9b | 9.4 ± 0.4 | ND | ND | 160.0 ± 6.0 | ND |
| 9c | 5.0 ± 0.3 | ND | 5.0 ± 0.4 | 134.0 ± 6.0 | 13.0 ± 0.5 |
| 9d | 4.6 ± 0.4 | 4.0 ± 0.3 | 4.7 ± 0.1 | 140.0 ± 2.3 | 15.0 ± 0.6 |
| 9e | 12.5 ± 0.1 | ND | 7.5 ± 0.3 | 170.0 ± 2.3 | 19.0 ± 0.4 |
| 9f | 12.5 ± 0.8 | ND | 7.2 ± 0.3 | 165.0 ± 2.3 | 17.0 ± 1.0 |
| 9h-1 | 8.2 ± 0.5 | ND | ND | 160.0 ± 8.0 | ND |
| 9i | 13.8 ± 0.7 | ND | 6.8 ± 0.2 | 165.0 ± 2.3 | 19.0 ± 0.8 |
| 9j | 20.9 ± 1.3 | ND | ND | 170.0 ± 4.0 | ND |
| 9k-1 | 20.9 ± 3.0 | ND | ND | 150.0 ± 6.0 | ND |
a
The IC50 values for each drug were determined by a MTS-based proliferation assay. Each IC50 value was derived from at least three independent experiments with triplicates in each experiment. ND, not determined.