Imperatorin is reported as an anti-cancer medicine with many targets to induce cell apoptosis, such as enhancing p53 expression [1], inducing Mcl-1 degradation [2], activating activation of caspase-3, caspase-8, caspase-9 [3].
When tested with human cancer cell lines (SNU 449-liver cancer and HCT-15-colon cancer), imperatorin treatment promoted cell apoptosi in a dose-dependent manner via modulating expression of apotosis-related proteins [4]. In human embryonic kidney cells, imperatorin treatment significantly attenuated H2O2-induced ROS production [5]. When tested with human hepatoma HepG2 cells, administration of imperatorin inhibited cell proliferation in a time- and dose- dependent manner [3]. In human lung cancer H23 cells, imperatorin was shown to enhance the expression of p53 and induced cells apoptosis at sub-toxic concentrations [1].
In nude mouse model bearing HepG2 cells, treatment with imperatorin significantly suppressed tumor growth in a dose-dependent manner [3].
It is also reported that imperatorin inhibits voltage-gated K+ channels and ATP-sensitive K+ channels when tested with neuronal NG-108-15 cells [6].
References:
[1]. Choochuay, K., et al., Imperatorin sensitizes anoikis and inhibits anchorage-independent growth of lung cancer cells. J Nat Med, 2013. 67(3): p. 599-606.
[2]. Li, X., et al., Imperatorin induces Mcl-1 degradation to cooperatively trigger Bax translocation and Bak activation to suppress drug-resistant human hepatoma. Cancer Lett, 2014. 348(1-2): p. 146-55.
[3]. Luo, K.W., et al., Anticancer effects of imperatorin isolated from Angelica dahurica: induction of apoptosis in HepG2 cells through both death-receptor- and mitochondria-mediated pathways. Chemotherapy, 2011. 57(6): p. 449-59.
[4]. Rahman, A., et al., Growth inhibition of various human cancer cell lines by imperatorin and limonin from poncirus trifoliata rafin. Seeds. Anticancer Agents Med Chem, 2015. 15(2): p. 236-41.
[5]. Cao, Y., et al., Antioxidant effect of imperatorin from Angelica dahurica in hypertension via inhibiting NADPH oxidase activation and MAPK pathway. J Am Soc Hypertens, 2014. 8(8): p. 527-36.
[6]. Wang, Y.W., et al., Inhibitory effects of imperatorin on voltage-gated K(+) channels and ATP-sensitive K(+) channels. Pharmacol Rep, 2015. 67(1): p. 134-9.