Effects of saponins from the root bark of Aralia elata on the transport of chondroitin sulfate in Caco-2 cell monolayers and rats

Abstract

We investigated the intestinal absorption enhancing effect of the saponins from the root bark of Aralia elata (SRBAE) in Caco-2 cell monolayers and rats. SRBAE at concentrations of 0.04% and 0.08% (w/v) decreased the transepithelial electrical resistance (TEER) values and increased the paracellular uptake of chondroitin sulfates (CSs) having different molecular weights (MW 500, 4500, and 18000) in a dose-dependent manner. We also evaluated the cytotoxicity of SRBAE to determine its proper concentration as an absorption enhancer. MTT assay and trypan blue exclusion test indicated that the cytotoxicity of SRBAE at concentrations of 0.04% and 0.08% was negligible. CS (MW 18000) was orally administered with or without SRBAE to rats. The oral administration of SRBAE (250 mg/kg) in l h increased the intestinal absorption of CS, by 4.9-fold versus the control (CS alone). Histological examination of the gastrointestinal tissues showed that SRBAE did not cause any damage to tissues. In conclusion, our results suggest that SRBAE acts as an efficient absorption enhancer and makes it easier for hydrophilic molecules to penetrate the intestinal epithelium. © 2005 Pharmaceutical Society of Japan.