Transport in Caco-2 cell monolayers of flavone C-glycosides from a neotropical blueberry

We previously reported the isolation of two flavone C-glycosides, orientin and vitexin, from the neotropical blueberry Anthopterus wardii, and reported their anti-inflammatory and inhibitory activities against IL-8 and MMP-1, respectively. The objective of this study was to investigate the transport of these flavone C-glycosides using a two-compartment transwell human intestinal epithelial cell Caco-2 monolayer system, simulating the intestinal barrier. Orientin and vitexin transport in the apical to basolateral direction across Caco-2 cell monolayers were determined. The amounts of the C-glycosides were quantitatively measured by HPLC-TOF-MS, and the apparent permeability coefficient (P_app) values were also calculated. Our results showed that both orientin and vitexin could permeate to the basolateral side. The P_app values for orientin and vitexin were ranged from 6.58 to 29.9×10^-5 and 1.58 to 2.58×10^-5 cm/s, respectively. Also, a small amount of vitexin was absorbed inside the epithelial cells. This is the first report of the transport of the anti-inflammatory components orientin and vitexin in human intestinal epithelial cell monolayers. Our findings provide scientific evidence suggesting the possible bioavailability of these components in vivo.