Transport of resveratrol, a cancer chemopreventive agent, to cellular targets: plasmatic protein binding and cell uptake.
Resveratrol produced by several plants, berries and fruits, including grapes, is one of the best known natural food microcomponents with potent chemopreventive properties towards the most severe contemporary human diseases: cardiovascular sickness, cancer and neurodegenerative pathologies. Demonstration of its mechanism of action also implies the elucidation of the steps of bioavailability and bioabsorption in cells and tissues. In order to estimate the relationships between the amounts of resveratrol taken up by food or drink intake, and the several possible benefits illustrated from in vitro/in vivo experiments and from epidemiological studies, it is essential to demonstrate step by step the route of resveratrol from plasma to the cell active site. In plasma, resveratrol was shown to interact with lipoproteins. This commentary also contains previously unpublished results about interactions between resveratrol and albumin and the enhancement of this binding in presence of fatty acids. We have previously described that resveratrol uptake by hepatic cells involves two processes--a passive one and a carrier-mediated one. Thanks to this last process, resveratrol, while tightly bound to blood proteins, could be largely delivered to body tissues. The intracellular proteic targets of resveratrol remain to be identified.
Jannin
Brigitte
B
Laboratoire de Biologie Moléculaire et Cellulaire, Université de Bourgogne, 6 boulevard Gabriel, 21000 Dijon, France.
Menzel
Matthias
M
Berlot
Jean-Pierre
JP
Delmas
Dominique
D
Lançon
Allan
A
Latruffe
Norbert
N
D000818:Animals; D016588:Anticarcinogenic Agents / Q000493:pharmacokinetics*; D001692:Biological Transport / Q000502:physiology; D001798:Blood Proteins / Q000378:metabolism; D005227:Fatty Acids / Q000378:metabolism; D006801:Humans; D011485:Protein Binding; D000077185:Resveratrol; D012709:Serum Albumin / Q000378:metabolism*; D013267:Stilbenes / Q000493:pharmacokinetics*; D014407:Tumor Cells, Cultured
D016588:Anticarcinogenic Agents; D001798:Blood Proteins; D005227:Fatty Acids; D012709:Serum Albumin; D013267:Stilbenes; D000077185:Resveratrol