Evaluating the effect of gallic acid on the expression of drugs transporters in human hepatocytes

Abstract

Several plants have been used by their medical benefits. The responsible of these benefits are phytochemicals. Flavonoids have antioxidants, antifungal, antimicrobial proprieties and photoprotection activity. Gallic Acid is a phenolic acid that belong to the flavonoids group, this compound is abundant in strawberries, raspberries, black and green tea, and has been described antimicrobial and antifungal proprieties, as well as effects over drug metabolic enzymes. However, the mechanism of these effects has not been described. Membrane transporters have an important role in drug disposition. Since these flavonoids appear modify parameters such as absorption, distribution and metabolism of some drugs used in the treatment of some diseases, we analyze the effect of gallic acid over the expression of drugs transporters in hepatocytes. We treated HepG2 cells with different concentrations of gallic acid in order to establish the toxicological effects and the effect over proliferation of these cells by MTS assay, and then we observe the effect of the gallic acid over drugs transporters expression by inmunofluorescence detection. We observed that gallic acid has a toxicological effect in high concentrations and inhibits cell proliferation (0.1 and 1μM). However, gallic acid might induce the expression of drug transporters Pg‐P, OATP‐B and PEPT‐1 at low concentrations.