title: Esterification of Ginsenoside Rh2 Enhanced Its Cellular Uptake and Antitumor Activity in Human HepG2 Cells.
abstract: Our previous research had indicated that the octyl ester derivative of ginsenoside Rh2 (Rh2-O) might have a higher bioavailability than Rh2 in the Caco-2 cell line. The aim of this study was to investigate the cellular uptake and antitumor effects of Rh2-O in human HepG2 cells as well as its underlying mechanism compared with Rh2. Results showed that Rh2-O exhibited a higher cellular uptake (63.24%) than Rh2 (36.76%) when incubated with HepG2 cells for 24 h. Rh2-O possessed a dose- and time-dependent inhibitory effect against the proliferation of HepG2 cells. The IC50 value of Rh2-O for inhibition of HepG2 cell proliferation was 20.15 μM, which was roughly half the value of Rh2. Rh2-O induced apoptosis of HepG2 cells through a mitochondrial-mediated intrinsic pathway. In addition, the accumulation of ROS was detected in Rh2-O-treated HepG2 cells, which participated in the apoptosis of HepG2 cells. Conclusively, the findings above all suggested that Rh2-O as well as Rh2 inducing HepG2 cells apoptosis might involve similar mechanisms; however, Rh2-O had better antitumor activities than Rh2, probably due to its higher cellular uptake.
authors.affiliation: State Key Laboratory of Food Science and Technology, Institute for Advanced Study, Nanchang University , Nanchang, Jiangxi 330047, China.
authors.forename: Fang
authors.initials: F
authors.lastname: Chen
authors.affiliation: State Key Laboratory of Food Science and Technology, Institute for Advanced Study, Nanchang University , Nanchang, Jiangxi 330047, China.|College of Food Science, Nanchang University , Nanchang, Jiangxi 330047, China.
authors.forename: Ze-Yuan
authors.initials: ZY
authors.lastname: Deng
authors.affiliation: State Key Laboratory of Food Science and Technology, Institute for Advanced Study, Nanchang University , Nanchang, Jiangxi 330047, China.
authors.forename: Bing
authors.initials: B
authors.lastname: Zhang
authors.affiliation: College of Food Science, Nanchang University , Nanchang, Jiangxi 330047, China.
authors.forename: Zeng-Xing
authors.initials: ZX
authors.lastname: Xiong
authors.affiliation: College of Food Science, Nanchang University , Nanchang, Jiangxi 330047, China.
authors.forename: Shi-Lian
authors.initials: SL
authors.lastname: Zheng
authors.affiliation: College of Food Science, Nanchang University , Nanchang, Jiangxi 330047, China.
authors.forename: Chao-Li
authors.initials: CL
authors.lastname: Tan
authors.affiliation: State Key Laboratory of Food Science and Technology, Institute for Advanced Study, Nanchang University , Nanchang, Jiangxi 330047, China.|College of Food Science, Nanchang University , Nanchang, Jiangxi 330047, China.
authors.forename: Jiang-Ning
authors.initials: JN
authors.lastname: Hu
mesh_terms: D000970:Antineoplastic Agents / Q000737:chemistry* / Q000378:metabolism*; D001692:Biological Transport / Q000187:drug effects; D004951:Esterification; D036145:Ginsenosides / Q000737:chemistry* / Q000378:metabolism*; D056945:Hep G2 Cells; D006801:Humans; D015394:Molecular Structure
chemical_list: D000970:Antineoplastic Agents; D036145:Ginsenosides; C055305:ginsenoside Rh2
keywords: ROS; Rh2; apoptosis; cellular uptake; ginsenosides; mitochondria; octyl ester derivative