Absorption and transport characteristic of paeoniflorin and its derivatives in model of Caco-2 cell monolayers
10.7501/j.issn.0253-2670.2013.15.014
- Author:
Xiu-Wei YANG
1
Author Information
1. Department of Natural Medicines
- Publication Type:Journal Article
- Keywords:
Apparent permeability coefficients;
Benzoylpaeoniflorin;
Caco-2 cell monolayers;
Oxypaeoniflorin;
Paeoniflorin;
Pentaacetylpaeoniflorin;
Pentacacetyl-albiflorin;
Tetraacetylpaeoniflorin
- From:
Chinese Traditional and Herbal Drugs
2013;44(15):2097-2104
- CountryChina
- Language:Chinese
-
Abstract:
Objective: To study the absorption and transport characteristic of paeoniflorin (PF), oxypaeoniflorin (OP), benzoylpaeoniflorin (BP), tetraacetylpaeoniflorin (TP), pentaacetylpaeoniflorin (PP), and pentacacetylalbiflorin (PA) in human colon adenocarcinoma cell line Caco-2 cell monolayer model. Methods: The Caco-2 cell monolayers were used as an intestinal epithelial cell model. The permeability of the tested compounds from apical (AP) side to basolateral (BL) side or from BL side to AP side was evaluated. The concentration of the tested compounds was measured by HPLC coupled with UV detector. The transport parameters and apparent permeability coefficients (Papp) were calculated, and the Papp values were compared with the reported values for model compounds, Propranolol and Atenolol. Results: The Papp values of PF in the bi-directional transport and atenolol were at the quantitative degree of 10-7 cm/s. Whereas those of OP, BP, TP, PP, and PA were between atenolol and propranolol used as a control substance for low and high permeability, respectively. The absorption and transport of the tested compounds were concentration-dependent at the concentration range of 10-200 μmol/L for PF, OP, and BP, 10-150 μmol/L for TP and PA, and 10-100 μmol/L for PP. Conclusion: The six tested compounds could be absorbed across the intestinal epithelial cells by passive diffusion mechanism. PF is poorly absorbed compound and OP, BP, TP, PP, and PA are moderately absorbed compounds. BP has a role to promote atenolol uptake transporters in Caco-2 cell monolayer model.
