Characterization of the intestinal absorption of morroniside from Cornus officinalis Sieb. et Zucc via a Caco-2 cell monolayer model

Abstract

Morroniside is a biologically active polyphenol found in Cornus officinalis Sieb. et Zucc (CO) that exhibits a broad spectrum of pharmacological activities, such as protecting nerves, and preventing diabetic liver damage and renal damage. However, little data are available regarding the mechanism of its intestinal absorption. Here, an in vitro human intestinal epithelial cell model of cultured Caco-2 cells was applied to study the absorption and transport of morroniside. The effects of donor concentration, pH and inhibitors were investigated. The bidirectional permeability of morroniside from the apical (AP) to the basolateral (BL) side and in the reverse direction was studied. When administered at three tested concentrations (5, 25 and 100 μM), the apparent permeability coefficient (P app ) values in the AP-to-BL direction ranged from 1.59 × 10 −6 to 2.66 × 10 −6 cm/s. In the reverse direction, BL-to-AP, the value was ranged from 2.67 × 10 −6 to 4.10 × 10 −6 cm/s. The data indicated that morroniside transport was pH-dependent. The permeability of morroniside was affected by treatment with various inhibitors, such as multidrug resistance protein inhibitors MK571 and indomethacin, as well as the breast cancer resistance protein inhibitor apigenin. The mechanisms of the intestinal absorption of morroniside may involve multiple transport pathways, such as the passive diffusion and efflux protein-mediated active transport especially involving multidrug resistance protein 2 and breast cancer resistance protein. After the addition of CO, the P app values in the AP-to-BL direction increased significantly, therefore, it can be assumed that some ingredients in the CO promote morroniside absorption in the small intestine.

Mycotoxins: Biotransformation and Bioavailability Assessment Using Caco-2 Cell Monolayer

“…The Caco-2 cell line is the most common and extensively used in vitro model to study the intestinal absorption of mycotoxins via the intestinal membrane enterocytes [ 2 , 10 , 187 , 188 ]. It was originally derived from a heterogeneous human epithelial colorectal adenocarcinoma cells established by Fogh and coworkers in 1977 [ 189 ].…”

Lipid-lowering effect and oral transport characteristics study of curculigoside

“…MRPs are another class of ABC transporters associated with drug efflux in Caco-2 cells. The MRP2 inhibitor MK571 inhibits the efflux of morroniside and sweroside in Caco-2 cells ( 38 ). In our study, the MRPs inhibitors, MK 571, benzbromarone and indomethacin had on significant effects on curculigoside efflux, which proved that MRPs were not involved in the absorption process of curculigoside.…”

Approaches, Strategies and Procedures for Identifying Anti-Inflammatory Drug Lead Molecules from Natural Products

“…The differentiated Caco-2 cells exhibit features that closely resemble small bowel enterocytes, including brush-border microvilli [ 228 , 229 ], and produce various cytokines, like IL-6, IL-8, IL-15 and TNF [ 230 , 231 , 232 ]. As such, Caco-2 cells are widely used in IBD research [ 233 , 234 ]. Zhang et al [ 235 ] investigated in vitro anti-inflammatory effects of Paenibacillus polymyxa Prazmowski exopolysaccharide (PYQ1-EPS) on TNF-induced inflammation in Caco-2 cells.…”