Folate is a water-soluble B vitamin with a crucial role in the synthesis and methylation of DNA and in the metabolism of several amino acids. In the present study we investigated whether beverages like wine, beer and tea, or some of their specific constituents, affect the intestinal uptake of (3)H-folic acid or (3)H-methotrexate (an antifolate). All tested beverages significantly inhibited the uptake of (3)H-folic acid by Caco-2 cells. Most of these beverages, with the exception of wines (not tested), also inhibited (3)H-methotrexate uptake in these cells. Additionally, ethanol, when tested separately, inhibited the uptake of both compounds. Some of the tested phenolic compounds, namely myricetin, epigallocatechin gallate (EGCG) and isoxanthohumol, markedly inhibited (3)H-folic acid uptake. Myricetin and EGCG also had a concentration-dependent inhibitory effect upon the uptake of (3)H-methotrexate by Caco-2 cells. Resveratrol, quercetin and kaempferol were able to inhibit the transport of both compounds, but only in the concentration of 100 microM. In conclusion, dietary constituents may impact on intestinal folate uptake, as here shown for phenolic compounds.