Evidence for a polarized efflux system for peptides in the apical membrane of Caco-2 cells.

The transport of two model peptides across confluent monolayers of human colon adenocarcinoma (Caco-2) cells was studied. In the case of AcPhe(NMePhe)2NH2, transport in the apical to basolateral direction was increased with increasing peptide concentration in the apical compartment. Transport was also increased in the presence of verapamil. In contrast, the flux of AcPheNH2 was neither concentration dependent nor affected by verapamil. Further, in the presence of verapamil, transport in the basolateral to apical direction was showed for AcPhe(NMePhe)2NH2 and again unchanged for AcPheNH2. These results are consistent with the presence of a saturable, apically polarized transport system in Caco-2 cells which serves to hinder transport in the apical to basolateral direction, increase flux in the basolateral to apical direction and shows substrate specificity for these model peptides.