title: The octanol/water distribution coefficients of ardipusilloside-I and its metabolites, and their permeation characteristics across Caco-2 cell monolayer.
abstract: BACKGROUND
  Ardipusilloside-I (ADS-I) is a triterpenoid saponin extracted from Chinese medicinal herb Ardisiapusill A. DC. Previous studies have demonstrated the potent anti-tumor activities of ADS-I both in vitro and in vivo, and its main metabolites (M1 and M2) from human intestinal bacteria. However, the physicochemical properties and intestinal permeation rate of ADS-I and its metabolites are not understood. In this study, the octanol/water distribution coefficients (logP) of ADS-I and metabolites were investigated using standard shake flask technique, and their permeability properties was investigated across Caco-2 cells monolayer.
  
  
  RESULTS
  The logP of ADS-I, M1 and M2 was -0.01, 0.95 ± 0.04, 1.57 ± 0.11, respectively. The Papp values of ADS-I, M1 and M2 (in 10 μmol/L) across Caco-2 cell monolayers from the apical (AP) to basolateral (BL) direction were 1.88 ± 0.21 × 10(-6) cm·s(-1), 4.30 ± 0.43 × 10(-6) cm·s(-1), 4.74 ± 0.47 × 10(-6) cm·s(-1), respectively.
  
  
  CONCLUSIONS
  Our data indicated that ADS-I has the poorer intestinal absorption than its metabolites (M1 and M2) in these experimental systems, suggesting that the metabolites of ADS-I may be the predominant products absorbed by the intestine when ADS-I is administered orally.
authors.affiliation: State Key Laboratory of Military Stomatology & National Clinical Research Center for Oral Diseases & Shaanxi Engineering Research Center for Dental Materials and Advanced Manufacture, Department of Pharmacy, School of Stomatology, The Fourth Military Medical University, Xi'an, 710032 Shaanxi China.
authors.forename: Wei-Yu
authors.initials: WY
authors.lastname: Cao
authors.affiliation: State Key Laboratory of Military Stomatology & National Clinical Research Center for Oral Diseases & Shaanxi Engineering Research Center for Dental Materials and Advanced Manufacture, Department of Pharmacy, School of Stomatology, The Fourth Military Medical University, Xi'an, 710032 Shaanxi China.
authors.forename: Bin
authors.initials: B
authors.lastname: Feng
authors.affiliation: State Key Laboratory of Military Stomatology & National Clinical Research Center for Oral Diseases & Shaanxi Engineering Research Center for Dental Materials and Advanced Manufacture, Department of Pharmacy, School of Stomatology, The Fourth Military Medical University, Xi'an, 710032 Shaanxi China.
authors.forename: Li-Fei
authors.initials: LF
authors.lastname: Cheng
authors.affiliation: State Key Laboratory of Military Stomatology & National Clinical Research Center for Oral Diseases & Shaanxi Engineering Research Center for Dental Materials and Advanced Manufacture, Department of Pharmacy, School of Stomatology, The Fourth Military Medical University, Xi'an, 710032 Shaanxi China.
authors.forename: Ying
authors.initials: Y
authors.lastname: Wang
authors.affiliation: State Key Laboratory of Military Stomatology & National Clinical Research Center for Oral Diseases & Shaanxi Engineering Research Center for Dental Materials and Advanced Manufacture, Department of Pharmacy, School of Stomatology, The Fourth Military Medical University, Xi'an, 710032 Shaanxi China.
authors.forename: Ji
authors.initials: J
authors.lastname: Wang
authors.affiliation: State Key Laboratory of Military Stomatology & National Clinical Research Center for Oral Diseases & Shaanxi Engineering Research Center for Dental Materials and Advanced Manufacture, Department of Pharmacy, School of Stomatology, The Fourth Military Medical University, Xi'an, 710032 Shaanxi China.
authors.forename: Xiao-Juan
authors.initials: XJ
authors.lastname: Wang
keywords: Ardipusilloside-I; Caco-2 cell monolayers; Intestinal absorption; LogP; Metabolites