Planta Med 2012; 78 - PD79
DOI: 10.1055/s-0032-1320437

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

GGL Yue 1, 2, SB Wu 3, MH To 1, 2, G Flores 3, CBS Lau 1, 2, E Kennelly 3
  • 1Institute of Chinese Medicine
  • 2State Key Laboratory of Phytochemistry and Plant Resources in West China (CUHK), The Chinese University of Hong Kong, Shatin, New Territories, Hong Kong
  • 3Department of Biological Sciences, Lehman College and The Graduate Center, City University of New York, Bronx, NY 10468, USA

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 (Papp) values were also calculated. Our results showed that both orientin and vitexin could permeate to the basolateral side. The Papp 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.