Luteolin significantly inhibited Nrf2 and its target genes [NADPH quinone oxidoreductase 1 (NQO1), heme oxygenase-1 (HO-1), and GSTα1/2] in resistant cells, while the combination of luteolin with different chemotherapeutics demonstrated synergistic effects in anti-cancer activities. The gene discussed is NQO1; the disease is cancer.