TABLE 1

Kinetic parameters for the penetration across the monolayers of polarized cell lines expressing mouse Bcrp or Mdr1a and their corresponding control cells

Data were taken from Figs. 1 and 2. Permeabilities across GFP- and Bcrp-MDCK or parent LLC-PK1 and L-Mdr1a were determined by the slopes from 1 to 3 h in the transcellular transport. Flux ratios were calculated by the permeabilities in the basal-to-apical direction divided by those in the apical-to-basal direction and the value of flux ratio in the cell lines expressing mouse Bcrp or Mdr1a divided by that in their corresponding control cells defined as CFR. The results are shown as the mean value and S.E.

CompoundCell LinePermeabilityFlux RatioCFR
A to BB to A
μL/h/well
ErlotinibLLC-PK135.2 ± 1.538.3 ± 1.81.094.56
L-Mdr1a12.2 ± 0.9***60.7 ± 3.9**4.96
GFP-MDCK28.0 ± 0.431.5 ± 0.41.131.39
Bcrp-MDCK21.5 ± 0.3***33.5 ± 3.11.56
FlavopiridolLLC-PK126.6 ± 1.139.6 ± 1.71.494.71
L-Mdr1a9.57 ± 2.22***67.3 ± 9.8**7.03
GFP-MDCK36.4 ± 1.034.3 ± 0.50.9411.98
Bcrp-MDCK22.1 ± 0.9***41.2 ± 2.3*1.86
MitoxantroneLLC-PK14.23 ± 0.529.08 ± 0.632.151.39
L-Mdr1a4.79 ± 0.4114.3 ± 0.7**2.97
GFP-MDCK1.11 ± 0.334.26 ± 0.433.842.62
Bcrp-MDCK0.801 ± 0.068.06 ± 0.24**10.1
DantroleneLLC-PK122.5 ± 0.837.0 ± 1.91.640.982
L-Mdr1a24.3 ± 0.439.2 ± 3.31.61
GFP-MDCK29.9 ± 0.930.8 ± .71.031.86
Bcrp-MDCK22.1 ± 0.8**42.2 ± 1.3**1.91
QuinidineLLC-PK122.3 ± 0.822.9 ± 1.11.036.21
L-Mdr1a6.62 ± 0.58***42.2 ± 2.2**6.38
GFP-MDCK42.4 ± 3937.8 ± 1.00.8921.04
Bcrp-MDCK38.4 ± 3.635.6 ± 3.60.928

  • Asterisks represent statistically significant differences in the permeability between transporter-expressing cells and the corresponding control cells:

  • ↵* , P < 0.05;

  • ↵** , P < 0.01; and

  • ↵*** , P < 0.001.