Abstract
BackgroundArdipusilloside-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.ResultsThe 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.ConclusionOur 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.
Highlights
Ardipusilloside-I (ADS-I) is a triterpenoid saponin extracted from Chinese medicinal herb Ardisiapusill A
LogP of ADS‐I and its metabolites in octanol/water The LogP of ADS-I and its metabolites were determined by using standard shake flask method and HPLCELSD technique
ADS-I has the highest polarity and molecular weight compared to M1 and M2, the lower logP value of ADS-I suggests that this compound has a poor absorption in human intestine after oral administration
Summary
Ardipusilloside-I (ADS-I) is a triterpenoid saponin extracted from Chinese medicinal herb Ardisiapusill A. 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. The octanol/water distribution coefficients (logP) of ADS-I and metabolites were investigated using standard shake flask technique, and their perme‐ ability properties was investigated across Caco-2 cells monolayer. Ardipusilloside-I (ADS-I) [1] is a major bioactive triterpenoid saponin isolated from Chinese medicinal herb Ardisiapusill A. The anti-tumor activity of this compound was first reported by Dr Wang’s group [2], followed by many preclinical studies, showing that ADS-I induces tumor cell apoptosis and inhibits tumor cell growth, invasion and metastasis both in vitro and in vivo [3,4,5,6].
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