Differential antiangiogenic and anticancer activities of the active metabolites of ginsenoside Rg3

Epimers of ginsenoside Rg3 (Rg3) have a low bioavailability and are prone to deglycosylation, which produces epimers Rh2 (S–Rh2 R–Rh2) protopanaxadiol (S-PPD R-PPD). The aim this study was compare the efficacy potency these molecules as anti-cancer agents. Crystal violet staining used anti-proliferatory action on human epithelial breast cancer cell line, MDA-MB-231, umbilical vein endothelial cells (HUVEC) their potency. Cell death cycle were studied using flow cytometry mode live imaging. Anti-angiogenic effects drug loop formation assay. Molecular docking showed interaction with vascular growth factor receptor-2 (VEGFR2) aquaporin (AQP) water channels. VEGF bioassay VEGFR2, in vitro. HUVEC more sensitive line anti-proliferative S–Rh2, S-PPD R-PPD. induced necroptosis/necrosis MDA-MB-231 apoptosis HUVEC. S–Rh2 most potent inhibitor formation. In silico molecular predicted good binding score between or PPD ATP-binding pocket VEGFR2. that an allosteric modulator addition, SRh2 had scores AQP1 AQP5, both play roles migration proliferation. combination might be responsible for observed by Rg3.