Table 1.
The Effect of Licochalcone A on Drug Resistance Mediated by ABCB1, ABCC1 or ABCG2
| Treatment | Concentration (μM) | Mean IC50a ± SD and (FRb) | |
|---|---|---|---|
| pcDNA-HEK293 [nM] | MDR19-HEK293 [nM] |
||
| Colchicine (ABCB1 substrate) | - | 8.42 ± 3.13 (1.0) | 97.58 ± 17.62 (1.0) |
| + licochalcone A | 0.5 | 8.67 ± 2.87 (1.0) | 94.92 ± 13.25 (1.0) |
| + licochalcone A | 1.0 | 7.99 ± 2.31 (1.1) | 114.81 ± 15.32 (0.8) |
| + licochalcone A | 2.0 | 8.90 ± 2.90 (0.9) | 121.20 ± 11.48 (0.8) |
| + licochalcone A | 3.0 | 9.03 ± 3.02 (0.9) | 105.41 ± 9.50 (0.9) |
| + tariquidar | 1.0 | 7.62 ± 2.36 (1.1) | 7.83 ± 1.37*** (12.5) |
| pcDNA-HEK293 [μM] |
MRP1-HEK293 [μM] |
||
| Etoposide (ABCC1 substrate) | - | 0.21 ± 0.04 (1.0) | 63.34 ± 7.92 (1.0) |
| + licochalcone A | 0.5 | 0.31 ± 0.07 (0.7) | 53.57 ± 4.65 (1.2) |
| + licochalcone A | 1.0 | 0.30 ± 0.07 (0.7) | 49.26 ± 4.31 (1.3) |
| + licochalcone A | 2.0 | 0.30 ± 0.06 (0.7) | 66.65 ± 12.38 (1.0) |
| + licochalcone A | 3.0 | 0.28 ± 0.06 (0.8) | 56.47 ± 7.41 (1.1) |
| + MK-571 | 25 | 0.16 ± 0.03 (1.0) | 11.87 ± 1.65*** (5.4) |
| pcDNA-HEK293 [nM] |
R482-HEK293 [nM] |
||
| Mitoxantrone (ABCG2 substrate) | - | 4.70 ± 0.99 (1.0) | 50.66 ± 6.88 (1.0) |
| + licochalcone A | 0.5 | 5.11 ± 1.01 (0.9) | 18.75 ± 2.69** (2.7) |
| + licochalcone A | 1.0 | 4.60 ± 0.91 (1.0) | 7.09 ± 0.82*** (7.1) |
| + licochalcone A | 2.0 | 4.74 ± 0.90 (1.0) | 7.83 ± 1.45*** (6.5) |
| + licochalcone A | 3.0 | 4.78 ± 0.93 (1.0) | 6.22 ± 0.85*** (8.1) |
| + Ko143 | 1.0 | 4.57 ± 0.91 (1.0) | 4.62 ± 0.52*** (10.9) |
| [nM] | [nM] | ||
| Topotecan (ABCG2 substrate) | - | 24.60 ± 5.98 (1.0) | 201.31 ± 25.89 (1.0) |
| + licochalcone A | 0.5 | 26.83 ± 6.50 (0.9) | 90.05 ± 13.54** (2.2) |
| + licochalcone A | 1.0 | 24.72 ± 5.57 (1.0) | 51.47 ± 10.61*** (3.9) |
| + licochalcone A | 2.0 | 25.89 ± 5.53 (1.0) | 44.11 ± 8.51*** (4.6) |
| + licochalcone A | 3.0 | 25.55 ± 5.49 (1.0) | 42.41 ± 8.71*** (4.7) |
| + Ko143 | 1.0 | 25.15 ± 5.75 (1.0) | 17.88 ± 2.31*** (11.3) |
a
IC50 values are mean ± SD calculated from dose-response curves obtained from three independent experiments.
b
FR,. fold-reversal values were obtained by dividing the IC50 values of cells treated with a particular drug in the absence of a modulator by the IC50 values of cells treated with the same drug in the presence of a modulator.
*
p < 0.05;
**
p < 0.01;
***
p < 0.001.