Assessment of Malondialdehyde Belonging to Modulators and Substrates of the P-Glycoprotein Transporter Protein.

In the study on cells of the Caco-2 line, the affiliation of malondialdehyde (MDA) to modulators and substrates of P-glycoprotein (Pgp) was assessed, and the biological role of Pgp in conditions of oxidative stress (OS) was studied. MDA was used at concentrations of 10, 50, 100, and 150 μM; OS was simulated by incubation with hydrogen peroxide (H2O2) at concentrations of 0.1-100 μM for 24 h. The relative amount of Pgp was evaluated by the Western blot hybridization, and the activity was estimated by the transport of its substrate fexofenadine (HPLC with UV detection, HPLC MS/MS). In this study, it was shown that MDA at concentrations of 10 and 50 μM and exposure duration of 24 h increases the relative amount and activity of Pgp by acting through CAR and PXR, and MDA can be transported by Pgp. The induction of Pgp under the action of MDA during the development of OS can have a protective significance, ensuring the removal of the peroxidation product from cells into the extracellular space and thereby increasing the viability of cells.