Fig. 4
Drug-metabolizing activities and drug transport activities were examined in ELC-org-mono. The CYP3A4 (A) and CES2 (B) activities were measured. (C) The permeabilities of 3H-labeled digoxin (substrate for P-gp) in ELC-org-mono with or without 100 µM verapamil (P-gp inhibitor) were measured. The efflux ratio (Papp B to A/Papp A to B) of each group is shown above the bar. (D) The permeabilities of 3H-labeled estrone sulfate (substrate for BCRP) with or without 100 µM Ko143 (BCRP inhibitor) were measured. The efflux ratio (Papp B to A/Papp A to B) of each group is shown above the bar. (E) The PEPT1 activity was measured by evaluating the amount of 14C-labeled Glycyl sarcosine (substrate for PEPT1) uptake into the cells with or without 100 µM glibenclamide (PEPT1 inhibitor). All data represent the mean ± S.D. (n = 3, biological replicates). Statistical analyses were performed using the unpaired two-tailed Student’s t-test (*p < 0.05, ***p < 0.005)