Riparsaponin isolated from Homonoia riparia Lour induces apoptosis of oral cancer cells.

Homonoia riparia Lour (Euphorbiaceae) is a known source of herbal medicine in China, and riparsaponin (RSP) is an active constituent isolated from H. riparia. The aim of the present study was to investigate the antitumor effect of RSP on human oral carcinoma cells and its potential underlying molecular mechanism. RSP was isolated from roots of H. riparia and identified using nuclear magnetic resonance. An MTT assay was used to evaluate the cytotoxicity of RSP on human oral carcinoma cells. Subsequently, DAPI staining was performed to investigate the apoptotic effect of RSP. To investigate the potential underlying molecular mechanism of action of RSP, western blotting was performed to determine the expression of cleaved caspase 3/9, B-cell lymphoma 2 (Bcl-2), Bcl-2-associated X protein (Bax), Bcl-2-associated death promoter (Bad), epithelial cadherin (E-CAD), c-MET, matrix metalloproteinase (MMP)-2 and MMP-9. RSP exhibited a significant anti-proliferative effect on oral carcinoma cells at concentrations between 10 and 200 µg/ml via apoptosis. Following treatment with RSP (20, 40 and 80 µg/ml), expression of cleaved caspase-3 (P<0.05, P<0.01 and P<0.01, respectively), cleaved caspase-9 (P<0.01), Bad (P<0.01), Bax (P<0.01), c-MET (P<0.01), MMP-2 (P<0.01) and MMP-9 (P<0.01) in oral carcinoma cells was increased significantly compared with the control group, whereas expression of Bcl-2 (P<0.01) and E-CAD (P<0.01) was decreased. These results suggest that RSP possessed notable antitumor activity against oral squamous cell carcinoma by inducing mitochondria-mediated apoptosis.