Ellipticine is a polyaromatic small molecule DNA intercalator, demonstrated to inhibit Topo II (DNA topoisomerase II) and to form covalent adducts with DNA. The formation of Ellipticine-DNA adducts is correlated to cytotoxicity and these adducts are suggested to interfere with DNA replication in the S phase. Antineoplastic effects are demonstrated with Ellipticine. Processing of Ellipticine by cytochrome p450 produces the adduct forming metabolites 13- and 12-hydroxyellipticine, and Ellipticine is described to inhibit cytochrome p450 CYP1A1 activity. Ellipticine was also shown to block p53 protein phosphorylation.
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PMID: # 28623690 Siebert, MN. et al. 2017. Aquat. Toxicol. 189: 142-149.
PMID: # 27769881 Siebert, MN. et al. 2017. Comp. Biochem. Physiol. B, Biochem. Mol. Biol. 203: 115-121.
PMID: # 28555524 Wen, HL. et al. 2017. Immunopharmacol Immunotoxicol. 39: 219-224.
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