4′-Bromoflavone significantly induces quinone reductase (QR) activity in cultured murine hepatoma 1c1c7 cells (concentration to double activity: 10 nM) and effectively induces the α- and mu-isoforms of glutathione S-transferase in cultured H4IIE rat hepatoma cells with no observed toxicity[1]. 4′-Bromoflavone is a potent inhibitor of cytochrome P4501A1-mediated ethoxyresorufin-O-deethylase activity, with an IC 50 of 0.86 μM. In HepG2 or MCF-7 cells, 4′-Bromoflavone significantly reduces the covalent binding of metabolically activated benzo[a]pyrene to cellular DNA[1].

在短期饮食研究中，4′-Bromoflavone 以剂量依赖性方式提高了大鼠肝脏、乳腺、结肠、胃和肺中的醌还原酶（QR）活性以及谷胱甘肽水平。在雌性Sprague Dawley大鼠的研究中，4′-Bromoflavone 显著增强了QR活性（II相代谢酶）[1]。
在DMBA处理的雌性Sprague Dawley大鼠中，饮食给予 4′-Bromoflavone（2000和4000 mg/kg 饮食，从DMBA处理前1周至处理后1周）可显著抑制乳腺肿瘤的发生率和多发性，并明显延长肿瘤潜伏期[1]。