Ellipticine HCl

Description: Ellipticine HCl, originally identified as a natural product, is a DNA-damaging agent acting as a prodrug whose pharmacological efficiencies and genotoxic side effects are dictated by activation with cytochrome P450 (CYP). Ellipticine is a potent antineoplastic agent exhibiting multiple mechanisms of action including DNA intercalating and inhibiting DNA topoisomerase II. Ellipticine can also act as an inhibitor or inducer of biotransformation enzymes, thereby modulating its own metabolism leading to its genotoxic and pharmacological effects. Treatment of all cells tested with ellipticine resulted in inhibition of cell growth and proliferation. This effect was associated with formation of two covalent ellipticine-derived DNA adducts, identical to those formed by 13-hydroxy- and 12-hydroxyellipticine, the ellipticine metabolites generated by CYP and peroxidase enzymes, in MCF-7, HL-60, CCRF-CEM, UKF-NB-3, UKF-NB-4 and U87MG cells, but not in neuroblastoma UKF-NB-3 cells. Therefore, DNA adduct formation in most cancer cell lines tested in this comparative study might be the predominant cause of their sensitivity to ellipticine treatment, whereas other mechanisms of ellipticine action also contribute to its cytotoxicity to neuroblastoma UKF-NB-3 cells.

References: Int J Mol Sci. 2014 Dec 25; 16(1):284-306; Interdiscip Toxicol. 2011 Jun; 4(2):98-105.

Related CAS#:519-23-3 (free base); 109628-38-8 (Hydroxyellipticine-1a); 51131-85-2 (9-Hydroxyellipticin free base); 52238-35-4 (9-hydroxyellipticine HCl); 105118-14-7 (Datelliptium chloride); 58337-35-2 (Celiptium, elliptinium acetate)