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Intestinal permeability of atractylenolides across the human Caco-2 cell monolayer model

Jie Guo, Wei Xu, Xiu­-Wei Yang*   

  1. State Key Laboratory of Natural and Biomimetic Drugs; Department of Natural Medicines, School of Pharmaceutical Sciences, Peking University Health Science Center, Beijing 100191, China
  • Received:2011-05-30 Revised:2011-08-10 Online:2011-09-20 Published:2011-09-20
  • Contact: Xiu-­Wei Yang*

Abstract:

The intestinal permeability of three sesquiterpene lactones, atractylenolide I, II, and III, was investigated using the human Caco-2 cell monolayer model. The bidirectional permeability of the three compounds from the apical (AP) to the basolateral (BL) side and in the reserved direction was studied. The three compounds were assayed using HPLC. The Papp values of atractylenolide I, II, and III were all at the level of 10-5 cm/s, suggesting high intestinal permeability and good absorption. The bidirectional transport of the three compounds was time- and concentration-dependent, and indicated the main mechanism of the passive diffusion of the three compounds across the intestinal epithelium membrane. Moreover, atractylenolide I might be partly actively transported.

Key words: Atractylenolide I, Atractylenolide II, Atractylenolide III, Caco-2 cell monolayer model, Intestinal permeability

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