The octanol/water distribution coefficients of ardipusilloside-I and its metabolites, and their permeation characteristics across Caco-2 cell monolayer
| Autor: | Li-Fei Cheng, Ji Wang, Ying Wang, Bin Feng, Xiao-Juan Wang, Wei-yu Cao |
|---|---|
| Jazyk: | angličtina |
| Předmět: |
chemistry.chemical_classification
Octanol Caco-2 cell monolayers Chromatography LogP Chemistry(all) 010405 organic chemistry Intestinal absorption General Chemistry Permeation 01 natural sciences In vitro 0104 chemical sciences 010404 medicinal & biomolecular chemistry chemistry.chemical_compound chemistry Caco-2 In vivo Monolayer Metabolites Research Article Ardipusilloside-I Triterpenoid saponin |
| Zdroj: | Chemistry Central Journal |
| ISSN: | 1752-153X |
| DOI: | 10.1186/s13065-016-0175-y |
| Popis: | 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. Conclusion 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. |
| Databáze: | OpenAIRE |
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