Absorption and Metabolism Characteristics of Rutin in Caco‐2 Cells

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.

Matrix effects of the hydroethanolic extract and the butanol fraction of calyces from Physalis peruviana L. on the biopharmaceutics classification of rutin

“…As shown in Figure , rutin, pure and from BF, was susceptible to being transported outside of the cells, but when HEE was tested, the efflux of the marker was practically reversed. According to our results and previous reports, P‐gp will be involved in this efflux. Hence, the lower ER of rutin from HEE could be a consequence of the saturation of this transporter, that would be favoured by the more complex mixture of compounds present in crude extracts (comparatively to fractions) and by the higher starting concentration of HEE used in the experiments (equivalent to 10 μ m for HEE vs 5 μ m for BF).…”

Rutin as A Novel c-Met Inhibitory Lead for The Control of Triple Negative Breast Malignancies

“…The outcomes revealed that plasma flavonoids were significantly elevated in rutin-supplemented group, fortunately, without any adverse changes in blood chemistry or indices of liver function. Additionally, Zhang et al ., has reported the absorption and metabolism characteristics of rutin in the intestinal-derived Caco-2 cells (33) and the pharmacokinetics of rutin has been studied in rats after oral administration with the identification of its associated metabolites in urine and feces by Ou-yang et al (34). Furthermore, various antitumor studies have been reported for rutin in rodents.…”

Advances in plant-based inhibitors of P-glycoprotein

“…To add, rutin 4 ( Figure 2, Table 3) was isolated from Ruta graveolens grass naphtha 76 . Zhang et al 76 reported that rutin decreased the bioavailability of cyclosporine through activation of P-gp.…”

“…Zhang et al 76 reported that rutin decreased the bioavailability of cyclosporine through activation of P-gp. Thus, P-gp is involved in the transmembrane transport and intracellular accumulation of rutin in human colonic cancer cells (Caco-2).…”