TABLE 5

Basal-to-apical permeability (efflux) of 3,5-di-O-caffeoylquinic acid in the presence of ABC transporter inhibitors

Papp values in the basal-to-apical direction were determined by analysis of the apical solution after basal incubation (1 h) of 3,5-diCQA (500 μM) with differentiated monolayers (n = 6) and ABC transporter inhibitor (apical side) at 37°C and 5% CO2. Papp is expressed as ×10−6 ± S.D.

InhibitorTransporter AffectedaPermeability: Papp B→A%InhibitionbInhibitor Conc.: Current Study
cm/sμM
QuercetinMRP-2, BCRP, P-gp0.13 ± 0.036525
MK571MRP-20.21 ± 0.044625
CyclosporineP-gp0.25 ± 0.063510
ApigeninBCRP0.26 ± 0.043225
Control0.39 ± 0.03
  • Statistical significant reduction (P < 0.05) of 3,5-diCQA efflux compared with the control condition.

  • a Inhibitor specificity evaluated by Matsson et al. (2009).

  • b %Inhibition: [(Papp control − Papp inhibitor)/(Papp control × 100).