The 40% ethanol fraction (EF40) of the root extract possesses attractive anticancer properties with no toxicity to normal cells. EF40 reduces the expression of Nrf2, a protein found in many cancers, leading to the accumulation of reactive oxygen species (ROS) that cause cell cycle arrest and apoptosis. EF40 also inhibits NSCLC cell migration by downregulating MMPs and hnRNP-K. Mouse studies showed significant suppression of tumor growth and lung metastasis. EF40 could be a potential natural anti-NSCLC drug that requires further attention for its mechanisms and clinical applications.