Table 2.
Compound | iBMECs | Inhibitor | Permeability (×10−6 cm/s) | Unpaired t-Test | Efflux Ratio | |
---|---|---|---|---|---|---|
A-B | B-A | p Value (BA vs. AB) | ||||
daunomycin | 33Q | - | 3.0 ± 0.1 | 3.9 ± 0.2 | <0.01 | 1.3 |
71Q | - | 2.6 ± 0.1 | 3.5 ± 0.3 | <0.05 | 1.3 | |
109Q | - | 2.8 ± 0.2 | 4.3 ± 0.2 | <0.001 | 1.5 | |
taxol | 33Q | - | 5.0 ± 0.2 | 6.9 ± 0.4 | <0.05 | 1.4 |
71Q | - | 3.5 ± 0.3 | 6.3 ± 0.2 | <0.01 | 1.8 | |
109Q | - | 6.7 ± 0.4 | 8.9 ± 0.4 | <0.05 | 1.3 | |
verapamil | 33Q | - | 14.0 ± 0.9 | 20.3 ± 0.8 | <0.001 | 1.5 |
71Q | - | 16.9 ± 0.3 | 19.2 ± 0.6 | ns | 1.1 | |
109Q | - | 16.7 ± 1.0 | 16.3 ± 1.1 | ns | 1.0 | |
vinblastine | 33Q | - | 1.2 ± 0.1 | 2.8 ± 0.2 | <0.01 | 2.3 |
+2 µM elacridar | 1.7 ± 0.1 * | 2.5 ± 0.2 | <0.05 | 1.5 | ||
71Q | - | 1.5 ± 0.2 | 2.7 ± 0.3 | <0.05 | 1.8 | |
+2 µM elacridar | 1.9 ± 0.1 | 2.0 ± 0.3 | ns | 1.0 | ||
109Q | - | 1.6 ± 0.1 | 3.1 ± 0.7 | ns | 1.9 | |
+2 µM elacridar | 2.9 ± 0.6 | 2.9 ± 0.4 | ns | 1.0 | ||
prazosin | 33Q | - | 3.8 ± 0.5 | 17.1 ± 1.0 | <0.001 | 4.5 |
+2 µM KO143 | 14.5 ± 1.3 ** | 15.2 ± 0.8 | ns | 1.0 | ||
71Q | - | 3.9 ± 0.6 | 16.2 ± 1.6 | <0.001 | 4.2 | |
+2 µM KO143 | 12.4 ± 0.9 ** | 17.1 ± 0.8 | <0.05 | 1.3 | ||
109Q | - | 5.2 ± 0.4 | 16.7 ± 1.2 | <0.001 | 3.2 | |
+2 µM KO143 | 7.6 ± 0.5 * | 11.9 ± 0.5 | <0.01 | 1.6 | ||
glutamate | 33Q | - | 4.1 ± 0.2 | 7.5 ± 0.5 | <0.05 | 1.8 |
71Q | - | 3.3 ± 0.1 | 6.8 ± 0.6 | <0.05 | 2.0 | |
109Q | - | 7.2 ± 0.7 | 9.0 ± 0.5 | ns | 1.3 | |
leucine | 33Q | - | 15.7 ± 1.7 | 19.4 ± 1.0 | ns | |
+10 µM JPH203 | 1.8 ± 0.3 *** | 2.2 ± 0.4 | ns | |||
71Q | - | 11.3 ± 0.7 | 17.3 ± 1.7 | ns | ||
+10 µM JPH203 | 1.8 ± 0.1 *** | 2.2 ± 0.1 | ns | |||
109Q | - | 19.5 ± 2.5 | 25.3 ± 1.7 | ns | ||
+10 µM JPH203 | 3.0 ± 0.3 *** | 5.7 ± 0.9 | ns | |||
glucose | 33Q | - +200 µM phloretin |
16.7 ± 0.9 6.3 ± 0.7 *** |
12.9 ± 2.5 5.2 ± 0.9 |
ns
ns |
|
71Q | - +200 µM phloretin |
18.6 ± 0.7 7.2 ± 1.5 ** |
17.9 ± 4.3 6.2 ± 1.0 |
ns
ns |
||
109Q | - +200 µM phloretin |
14.1 ± 1.6 6.5 ± 1.1 ** |
12.5 ± 0.9 5.8 ± 0.6 |
ns
ns |
||
lucifer yellow | 33Q | - | 0.23 ± 0.02 | 0.21 ± 0.04 | ns | 0.9 |
71Q | - | 0.37 ± 0.03 | 0.34 ± 0.06 | ns | 0.9 | |
109Q | - | 0.70 ± 0.03 | 0.70 ± 0.1 | ns | 1.0 |
Permeability of transported substrates across iBMECs in presence of different inhibitors. Coefficients in the A-B and in the B-A directions are reported as mean ± SD of at least 3 biological replicates along with respective efflux ratio. Statistical difference between both sides is reported as p-value; ns = no significant. The statistical analysis (Student’s t-test) for the difference of permeability for the compound alone or in the presence of an inhibitor is indicated by asterisks: *** p < 0.001, ** p < 0.01 and * p < 0.05.