Table 2. The reversal efficacy of Icotinib in ABCG2-mediated drug resistance in ABCG2-transfected cell lines.
IC50 ± SDa (μM) | ||||||||
---|---|---|---|---|---|---|---|---|
Compounds | HEK293/pcDNA3.1 | (RF)b | ABCG2-482-R2 | (RF)b | ABCG2-482-G2 | (RF)b | ABCG2-482-T7 | (RF)b |
Mitoxantrone (μM) | 0.0557 ± 0.0028 | 1.0 | 0.5754 ± 0.0460 | 10.3 | 1.7045 ± 0.1364 | 30.6 | 1.1045 ± 0.0884 | 19.8 |
+ Icotinib 1.0 μM | 0.0533 ± 0.0037 | 1.0 | 0.3438 ± 0.0309* | 6.2 | 0.7934 ± 0.0714* | 14.3 | 0.5524 ± 0.0497* | 9.9 |
+ Icotinib 5.0 μM | 0.0503 ± 0.0040 | 0.9 | 0.0537 ± 0.0027* | 1.0 | 0.0701 ± 0.0035* | 1.3 | 0.0687 ± 0.0034* | 1.2 |
+ FTC 5.0 μM | 0.0491 ± 0.0022 | 0.9 | 0.0564 ± 0.0023* | 1.0 | 0.0645 ± 0.0026* | 1.2 | 0.0632 ± 0.0025* | 1.1 |
SN-38 (μM) | 0.0070 ± 0.00035 | 1.0 | 0.1885 ± 0.0151 | 27.1 | 0.2494 ± 0.0200 | 35.8 | 0.2095 ± 0.0168 | 30.1 |
+ Icotinib 1.0 μM | 0.0067 ± 0.0005 | 1.0 | 0.0612 ± 0.0055* |
8.8 | 0.0811 ± 0.0073* | 11.7 | 0.0750 ± 0.0068* | 10.8 |
+ Icotinib 5.0 μM | 0.0063 ± 0.0005 | 0.9 | 0.0087 ± 0.0004* | 1.2 | 0.0080 ± 0.0004* |
1.2 |
0.0077 ± 0.0005* | 1.1 |
+ FTC 5.0 μM | 0.0061 ± 0.0003 | 0.9 | 0.0075 ± 0.0003* | 1.1 | 0.0078 ± 0.0003* | 1.1 | 0.0078 ± 0.0003* | 1.1 |
Cisplatin (μM) | 1.6700 ± 0.0835 | 1.0 | 1.7045 ± 0.1364 | 1.0 | 1.6045 ± 0.1284 | 1.0 | 1.6704 ± 0.1336 | 1.0 |
+ Icotinib 5.0 μM | 1.5980 ± 0.1119 | 1.0 | 1.6662 ± 0.1500 | 1.0 | 1.5524 ± 0.1397 | 0.9 | 1.5500 ± 0.0775 | 0.9 |
+ FTC 5.0 μM | 1.5098 ± 0.1208 | 0.9 | 1.5801 ± 0.0790 | 0.9 | 1.6873 ± 0.0844 | 1.0 | 1.5400 ± 0.1001 | 0.9 |
IC50 values are represented the mean ± standard deviation (SD).
Resistance fold (RF) was calculated by the IC50 values for different substrates, and cisplatin of resistant cell lines, divided by the IC50 values for the respective control without the reversing agents, or the resistant cell lines in the presence or absence of Icotinib or FTC, divided by the IC50 values for different substrates, and cisplatin of respective control without the reversing agents.
. P < 0.05, versus the control group.