Absorption and Metabolism Characteristics of Rutin in Caco-2 Cells

Xiaofang Zhang,Xiaopeng Shi,Jinhui Song,Shan Miao,Aidong Wen,Yan Li

doi:10.1155/2013/382350

Xiaofang Zhang, Xiaopeng Shi + Show 4 more

Open Access

https://doi.org/10.1155/2013/382350

Copy DOI

Abstract

The intestinal absorption and metabolism characteristics of the potentially beneficial polyphenol rutin were studied by measuring the intracellular accumulation and transport of rutin into Caco-2 cells with the sensitive and reliable analytical method of HPLC-coupled tandem mass spectrometry. Rutin and glucuronidated rutin were absorbed differently by the basolateral and apical membranes, and rutin showed differential permeability through the apical and basolateral sides. Approximately 33% of the rutin was metabolized to glucuronidated rutin, and the intracellular concentration of glucuronidated rutin was much lower than that of parent rutin. P-glycoprotein and multidrug-resistant proteins 2 and 3 were involved in the transmembrane transport and intracellular accumulation of rutin by Caco-2 cells. These results suggest that a specific transport system mediates rutin movement across the apical membrane in Caco-2 cells and that metabolic enzymes are important for this process.

Highlights

Polyphenols are found in many plants and are abundant in fruits and vegetables [1, 2]
Parent ions and product ions of rutin were selected from spectra after standard solutions were injected into a mass spectrometer in electrospray ionization (ESI) negative-ion mode [M-H]−
Our novel findings are as follows: (1) intracellular accumulation of rutin was observed in a time- and dosedependent manner in Caco-2 cells; (2) parent rutin was partly metabolized to glucuronidated rutin in Caco-2 cells; (3) the permeability values of parent rutin were different in the two opposite directions, and the amount of glucuronidated rutin transported was dependent on the direction; (4) P-gp and multidrug-resistant proteins (MRPs) were involved in the intracellular accumulation and transport by Caco-2 cells

Summary

Introduction

Polyphenols are found in many plants and are abundant in fruits and vegetables [1, 2]. These compounds have attracted much interest owing to clear evidence of their preventative effect in cardiovascular disease and cancer [3, 4]. Rutin has received much attention owing to its multiple biological effects, the limited understanding of its absorption characteristics and metabolic pathways makes it difficult to understand the reasons for its poor bioavailability. Intestinal metabolic enzymes, transporters, and even microflora were reported to be the main reasons for the poor bioavailability of natural polyphenols [8, 9]

Results

Discussion

Conclusion