Piperine’s Effect on Efflux Mechanism
In Caco-2 cells (human colon carcinoma cell lines), piperine has been found to inhibit the P-glycoprotein (P-gp)-mediated transport of drugs, such as digoxin and cyclosporine A.
It has also been indicated that dietary piperine could affect the plasma concentrations of P-gp and metabolizing enzyme CYP3A4 substrates in humans, in particular if the drugs are administered orally (Bharadwaj et al., 2002).
Also oral administration of piperine at a dose of 112 µg/kg for 14 days led to increased intestinal P-gp level with reduced hepatic P-gp, while the renal P-gp level were unaffected in rats (Han et al. 2008).