title: Esterification enhanced intestinal absorption of ginsenoside Rh2 in Caco-2 cells without impacts on its protective effects against H₂O₂-induced cell injury in human umbilical vein endothelial cells (HUVECs).
abstract: Ginsenoside Rh2 and its octyl ester derivative (Rh2-O) were investigated for their transcellular transport in the Caco-2 cell system and their protective effect against oxidative stress in human umbilical vein endothelial cells (HUVECs). Results showed that the transport rates for apical-to-basolateral (AP-BL) flux of Rh2 (0.21 × 10⁻⁶ cm/s) was enhanced by the synthesis of its esterified derivative Rh2-O (1.93 × 10⁻⁶ cm/s) over the concentrations of 10-50 μM. In addition, both Rh2 and its esterified derivative Rh2-O exhibited similar protective effects against oxidative damage induced by H₂O₂. Pretreatment of Rh2 and Rh2-O significantly decreased the activation of caspase-3 known to play a key role in H₂O₂-induced cell apoptosis. These results were consistent with that of a flow cytometry assay analyzing HUVECs apoptosis. The present study demonstrated that the absorption of ginsenoside Rh2 in vitro can be significantly enhanced by synthesis of its ester derivative. Meanwhile, no significant discrepancy between Rh2 and Rh2-O on their bioactivities against the oxidative damage induced by H₂O₂ was observed, which means that esterification of Rh2 might have a higher bioavailability than Rh2 in vitro without impacts on pharmaceutical actions.
authors: State Key Laboratory of Food Science and Technology, Institute for Advanced Study, Nanchang University , Nanchang, Jiangxi 330047, China.
authors: Bing
authors: B
authors: Zhang
authors: Hui
authors: H
authors: Ye
authors: Xue-Mei
authors: XM
authors: Zhu
authors: Jiang-Ning
authors: JN
authors: Hu
authors: Hong-Yan
authors: HY
authors: Li
authors: Rong
authors: R
authors: Tsao
authors: Ze-Yuan
authors: ZY
authors: Deng
authors: Yi-Nan
authors: YN
authors: Zheng
authors: Wei
authors: W
authors: Li
mesh_terms: D017209:Apoptosis / Q000187:drug effects*; D018938:Caco-2 Cells; D053148:Caspase 3 / Q000378:metabolism; D004951:Esterification; D036145:Ginsenosides / Q000737:chemistry* / Q000493:pharmacokinetics*; D061307:Human Umbilical Vein Endothelial Cells / Q000166:cytology / Q000187:drug effects* / Q000201:enzymology; D006801:Humans; D006861:Hydrogen Peroxide / Q000633:toxicity*; D007408:Intestinal Absorption / Q000187:drug effects; D020011:Protective Agents / Q000737:chemistry* / Q000493:pharmacokinetics*
chemical_list: D036145:Ginsenosides; D020011:Protective Agents; C055305:ginsenoside Rh2; D006861:Hydrogen Peroxide; D053148:Caspase 3