Absorption and transportation characteristic of dihydrofurocoumarins from Rhizome et Radix Notopterygii in a model of Caco-2 cell monolayers

Abstract

Objective: To study the absorption and transportation characteristic of nodakenetin (NANI), nodakenin (ND), decuroside V (DEV), and forbesoside [6′-O-(trans-feruloyl)-nodakenin, FDE] isolated from Rhizome et Radix Notopterygii, which were classified four linear dihydrofurocouma-rins, in human intestinal epithelium. Methods: Caco-2 (the human colon adenocarcinoma cell lines) cell monolayers were used as an intestinal epithelial cell model. The permeability of the four coumarins from apical side (AP side) to basolateral side (BL side) or from BL side to AP side was evaluated. The concentration of the four coumarins was measured by HPLC coupled with UV detector. Transportation parameters and permeability coefficients (Papp) were then calculated, and Papp values were compared with the reported values for model compounds, propranolol, and atenolol. Results: The Papp values of NANI in the bi-directional transportation were quantitative degree of 1×106cm/s, which laid between propranolol often used as a control substance for high permeability and Atenolol often used as a control substance for poor permeability. Whereas Papp values of ND, DEV, and FDE were quantitative degree of 1×107cm/s, which was comparable with the Papp values of atenolol. The absorption and transportation of four coumarins were positive correlation to the concentration of 25-400 μmol/L. Conclusion: Four linear dihydrofurocoumarins can be absorbed across intestinal epithelial cells by passive diffusion mechanism. The NANI is moderately, while ND, DEV, and FDE are poorly absorbed compounds.