Gastrointestinal biotransformation of resveratrol in mice

Resveratrol, a stilbenoid compound present in various berries, has been associated with reduced risk of chronic diseases such as cancer, obesity and diabetes. Accumulated evidence indicates that biotransformation plays important roles in the biological activities of dietary compounds. We investigated the gastrointestinal biotransformation of resveratrol in mice fed with resveratrol for 5 weeks. LC‐MS analysis revealed that the major site of biotransformation for resveratrol was the small intestine, although there was a low degree of biotransformation occurring in the stomach. In the small intestine, resveratrol underwent phase I metabolism to produce dihydroresveratrol and piceatannol. Subsequently, resveratrol, dihydroresveratrol and piceatannol all underwent phase II metabolism to yield their corresponding sulfate and glucuronide conjugates. However, in the colon, resveratrol, dihydroresveratrol and piceatannol mainly existed in the non‐conjugated forms, presumably due to the deconjugation by colonic microbiota. Moreover, the level of dihydroresveratrol in the colon was much higher that of resveratrol, suggesting that dihydroresveratrol may be essential for potential beneficial biological effects in the colon, such as anti‐inflammation and anti‐carcinogenesis. In summary, our results provided detailed information on the metabolic fate of resveratrol in the gastrointestinal tract, which is important for better understanding of the health benefits of resveratrol. Support or Funding Information This study was supported by funding from USDA.