Transport mechanism and metabolism of olive oil hydroxytyrosol in Caco‐2 cells

3,4‐Dihydroxyphenylethanol (hydroxytyrosol; DPE) is the major phenolic antioxidant present in extra virgin olive oil, either in a free or esterified form. Despite its relevant biological effects, no data are available on its bioavailability and metabolism. The aim of the present study is to examine the molecular mechanism of DPE intestinal transport, using differentiated Caco‐2 cell monolayers as the model system. The kinetic data demonstrate that [14C]DPE transport occurs via a passive diffusion mechanism and is bidirectional; the calculated apparent permeability coefficient indicates that the molecule is quantitatively absorbed at the intestinal level. The only labelled DPE metabolite detectable in the culture medium by HPLC (10% conversion) is 3‐hydroxy‐4‐methoxyphenylethanol, the product of catechol‐O‐methyltransferase; when DPE is assayed in vitro with the purified enzyme a Kmvalue of 40 μM has been calculated.