Physcion 8- O -β-glucopyranoside induces apoptosis, suppresses invasion and inhibits epithelial to mesenchymal transition of hepatocellular carcinoma HepG2 cells

Abstract Background Aberrant increased expression of DNMT1 and resulting silence of tumor suppressor genes have been found in a variety of human malignancies and DNMT1 has been considered as a promising therapeutic target for cancer prevention and treatment. One of the main active ingredients of Rumex japonicus Houtt, physcion 8- O -β-glucopyranoside (PG), has been found to have antitumor activities. Materials and methods Human hepatocellular carcinoma (HCC) cell line HepG2 was examined. Cell proliferation was analyzed using MTT assay. The apoptosis, migration and invasion were determined by flow cytometry, wound healing and Transwell assay, respectively. The expression of signaling molecules were examined by RT-PCR and western blots. Results Our results provide experimental evidence that PG inhibits growth and suppresses invasion of HCC cells by downregulating DNMT1 via ROS-dependent AMP-activated protein kinase (AMPK)-mediated modulation of transcription factor Sp1. Conclusion our results revealed for the first time that PG inhibits growth and suppresses invasion of HCC, highlighting the anti-tumor activities of PG against HCC. However, further studies, including clinical trials, are needed to fully evaluate PG as a novel therapeutic in cancer prevention and treatment.