Ellipticine is an alkaloid isolated from Apocyanaceae plants that exhibits antitumor activities by intercalating into DNA and/or inhibiting DNA topoisomerase II.1,2,3 It forms covalent adducts in DNA after being enzymatically activated with cytochrome P450 isoforms (e.g., CYP3A4, CYP1A1, or CYP1A2) or by peroxidases in target tissues.2,3 Ellipticine has been shown to inhibit the proliferation of human breast adenocarcinoma MCF-7 cells, leukemia HL-60 and CCRF-CEM cells, neuroblastoma IMR-32, UKF-NB-3, and UKF-NB-4 cells, and U87MG glioblastoma cells with IC50 values ranging from 0.27-4.7 ?M.2
1.Kohn, K.W., Waring, M.J., Glaubiger, D., et al.Intercalative binding of ellipticine to DNACancer Res.35(1)71-76(1975) 2.Stiborová, M., Poljakova, J., Martinkova, E., et al.Ellipticine cytotoxicity to cancer cell lines - a comparative studyInterdiscip. Toxicol.4(2)98-105(2011) 3.Aimová, D., Svobodová, L., Kotrbová, V., et al.The anticancer drug ellipticine is a potent inducer of rat cytochromes P450 1A1 and 1A2, thereby modulating its own metabolismDrug Metab. Dispos.35(10)1926-1934(2007)
















