Coptisine is another bioactive component of Rhizoma coptidis, and it exhibits antioxidation, anti-osteosarcoma, anti-inflammation, neuroprotection, and anti-cancer actions through preventing interleukin-1β (IL-1β) expression, activating Akt and c-Jun N-terminal kinase (JNK)/nuclear factor erythroid 2-related factor 2 (Nrf2)/NAD(P)H:quinine oxidoreductase 1 (NQO1) signaling pathways and inhibiting lipopolysaccharide (LPS)/toll-like receptor-4 (TLR-4)-mediated pathway [28–32]. This evidence concerns the gene NQO1 and cancer.