Intestinal pharmacokinetics of resveratrol and regulatory effects of resveratrol metabolites on gut barrier and gut microbiota

Bowei Zhang; Yingchuan Xu; Huan Lv; Wenwen Pang; Jin Wang; Hui Ma; Shuo Wang

doi:10.1016/j.foodchem.2021.129532

Intestinal pharmacokinetics of resveratrol and regulatory effects of resveratrol metabolites on gut barrier and gut microbiota

Food Chem. 2021 Mar 26:357:129532. doi: 10.1016/j.foodchem.2021.129532. Online ahead of print.

Authors

Bowei Zhang¹, Yingchuan Xu¹, Huan Lv¹, Wenwen Pang¹, Jin Wang¹, Hui Ma¹, Shuo Wang²

Affiliations

¹ Tianjin Key Laboratory of Food Science and Health, School of Medicine, Nankai University, Tianjin 300071, China.
² Tianjin Key Laboratory of Food Science and Health, School of Medicine, Nankai University, Tianjin 300071, China. Electronic address: wangshuo@nankai.edu.cn.

PMID: 33878586
DOI: 10.1016/j.foodchem.2021.129532

Abstract

Resveratrol, a dietary polyphenol, has a variety of intestinal bioactivities. However, its material basis remains unknown. This study examined the intestinal pharmacokinetics of resveratrol using HPLC-MS/MS. After oral ingestion in mice, resveratrol and its sulfation metabolites were identified in copious amount in the entire intestinal tract and feces. The glucuronidation metabolites were found in major quantity only in the small intestine. The amount of resveratrol and its metabolites in the total intestine peaked at 4 h, with a concentration of 200 ± 74.8 μM, which corresponded to 14.0% of the administrated dose. During in vitro fermentation, resveratrol-3-O-sulfate, but not resveratrol, significantly promoted the growth of Lactobacillus reuteri (10-fold higher). During the incubation with Caco-2 cells, resveratrol-3-O-sulfate significantly up-regulated the mRNA expressions of tight junction and mucin-related proteins. In conclusion, the intestinal concentration of resveratrol could partially support its intestinal bioactivities, which may be mediated through the actions of its metabolites.

Keywords: Gut barrier; Gut microbiota; Metabolism; Pharmacokinetics; Resveratrol.