A growing literature is dedicated to the understanding of carotenoid beneficial health effects. However, the absorption process of this broad family of molecules is still poorly understood. These highly lipophilic plant metabolites are usually weakly absorbed. It was long believed that β-carotene absorption (the principal provitamin A carotenoid in the human diet), and thus all other carotenoid absorption, was driven by passive diffusion through the brush border of the enterocytes. The identification of transporters able to facilitate carotenoid uptake by the enterocytes has challenged established statements. After a brief overview of carotenoid metabolism in the human upper gastrointestinal tract, a focus will be put on the identified proteins participating in the transport and the metabolism of carotenoids in intestinal cells and the regulation of these processes. Further progress in the understanding of the molecular mechanisms regulating carotenoid intestinal absorption is still required to optimize their bioavailability and, thus, their health effects.
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