This study was conducted to explore the novel anticancer compounds from Chinese herbs. During the processof screening, to evaluate the potential chemopreventive effect of natural compounds, Xanthoxyletin was isolatedfrom Erythrina variegata. It has been reported that Xanthoxyletin possesses antibacterial, fungicidal, and algicidalproperties. In this study, we examined the antiproliferative effects of Xanthoxyletin against SGC-7901 cells andits ability to induce apoptosis and cell cycle arrest for the first time. We observed that its inhibitory effects oncells were associated with the DNA damage, apoptosis through mitochondrial dysfunction, and cell cycle arrestat S phase in a dose-dependent manner. Additionally, Xanthoxyletin also increased the production of reactiveoxygen species in SGC-7901 cells. These results suggest that Xanthoxyletin may be promising anticancer agentand has worth for further mechanistic and therapeutic studies against gastric cancer.