Table 1.
Growth inhibitory effects of Act D in MDCKII cell lines over-expressing specific drug transporters.
| MDCKII-WT |
MDCKII-ABCB1 |
MDCKII-ABCC1 |
MDCKII-ABCC2 |
MDCKII-ABCG2 |
||||||
|---|---|---|---|---|---|---|---|---|---|---|
| GI50 (nM) | 95% CI | GI50 (nM) | 95% CI | GI50 (nM) | 95% CI | GI50 (nM) | 95% CI | GI50 (nM) | 95% CI | |
| Act D | 12.7 | – | 745 | (680.8, 905.3) | 25.7 | (18.3, 36.1) | 40.4 | (32.2, 50.7) | 14.0 | (11.7, 16.8) |
| Act D + verapamil | 4.4 | (3.31, 5.85) | 129 | (109.8, 150.5) | – | – | – | – | – | – |
| Act D + MK571 | 4.1 | (3.02, 5.55) | – | – | 5.90 | (3.35, 10.4) | 32.3 | 23.3, 44.7) | – | – |
| Act D + KO143 | 13.1 | (10.2, 16.9) | – | – | – | – | – | – | 13.0 | (10.3, 15.4) |
–, not applicable.
GI50 assessed by MTS assay after 72 h of drug exposure. Values are the mean of ≥3 experiments.