In Vitro Glucuronidation and Sulfation of ε-Viniferin, a Resveratrol Dimer, in Humans and Rats
Abstractε-Viniferin is a resveratrol dimer that possesses antioxidant or anti-inflammatory activities. However little is known about the metabolism of this oligostilbene. This study was thus undertaken as a first approach to identify and characterize the metabolites of ε-viniferin and to describe the kinetic profile of their appearance in humans and rats. The glucuronides and sulfates of ε-viniferin were first obtained by chemical hemi-synthesis and were fully characterized by UPLC-MS and NMR spectroscopy. Then, ε-viniferin was incubated with human or rat S9 liver fractions that led to the formation of four glucuronoconjugates and four sulfoconjugates. In both species, ε-viniferin was subjected to an intense metabolism as 70 to 80% of the molecule was converted to glucuronides and sulfates. In humans, the hepatic clearance of ε-viniferin (Vmax/Km) for glucuronidation and sulfation were 4.98 and 6.35 µL/min/mg protein, respectively, whereas, in rats, the hepatic clearance for glucuronidation was 20.08 vs. 2.59 µL/min/mg protein for sulfation. In humans, three major metabolites were observed: two glucuronides and one sulfate. By contrast, only one major glucuronide was observed in rats. This strong hepatic clearance of ε-viniferin in human and rat could explain its poor bioavailability and could help to characterize its active metabolites. View Full-Text
- Supplementary File 1:
PDF-Document (PDF, 155 KB)
Share & Cite This Article
Courtois, A.; Jourdes, M.; Dupin, A.; Lapèze, C.; Renouf, E.; Biais, B.; Teissedre, P.-L.; Mérillon, J.-M.; Richard, T.; Krisa, S. In Vitro Glucuronidation and Sulfation of ε-Viniferin, a Resveratrol Dimer, in Humans and Rats. Molecules 2017, 22, 733.
Courtois A, Jourdes M, Dupin A, Lapèze C, Renouf E, Biais B, Teissedre P-L, Mérillon J-M, Richard T, Krisa S. In Vitro Glucuronidation and Sulfation of ε-Viniferin, a Resveratrol Dimer, in Humans and Rats. Molecules. 2017; 22(5):733.Chicago/Turabian Style
Courtois, Arnaud; Jourdes, Michael; Dupin, Adeline; Lapèze, Caroline; Renouf, Elodie; Biais, Benoît; Teissedre, Pierre-Louis; Mérillon, Jean-Michel; Richard, Tristan; Krisa, Stéphanie. 2017. "In Vitro Glucuronidation and Sulfation of ε-Viniferin, a Resveratrol Dimer, in Humans and Rats." Molecules 22, no. 5: 733.
Note that from the first issue of 2016, MDPI journals use article numbers instead of page numbers. See further details here.