Characterization of the Intestinal Absorption of Morroniside from Cornus officinalis Sieb. et Zucc via a Caco-2 Cell Monolayer Model

Abstract

Morroniside is biologically active polyphenols found in Cornus officinalis Sieb. et Zucc (CO) which exhibits a broad spectrum of pharmacological activities, such as protecting nerves, preventing diabetic liver damageand renal damage. However, little data is available regarding its mechanism ofintestinal absorption. Here, ahuman intestinal epithelial cell model Caco-2 cell in vitro cultured was applied to study on the absorption and transport of morroniside, the effects of time, donor concentration,pH, temperature and inhibitors,the absorption and transport of morroniside were investigated.The bidirectional permeability of morroniside from the apical (AP) to the basolateral (BL) side and in the revese direction was studied. When administrated was setat three tested concentrations (5, 25 and 100M), the P app value in AP-to-BL direction was ranged from 1.59 to 2.66x10 -6 cm/s. Inthe reverse direction, BL-to-AP, the value was ranged from 2.67to 4.10 x10 -6 cm/s.The data indicated that morroniside transport was both pH- and temperature- dependent. The morronisides permeability process affected bytreatment with various inhibitors, such as the multidrug resistance protein inhibitors MK571 and benzbromarone, the breast cancer resistance protein inhibitor apigenin.It can be found that the mechanisms of intestinal absorption of morroniside may involve multiple transport pathways like passive diffusion as well as efflux protein-mediated active transportespecially the multidrug resistance protein2 and breast cancer resistance protein.After CO was added, P app AB increased significantly by about 125.26%, it can therefore be assumed that some ingredients in the crude material promote morronisides absorption in the small intestine.