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.
1. Froelich-Ammon, S.J., et al. 1995. J. Biol. Chem. 270: 14998-15004. PMID: 7797481 2. Ohashi, M., et al. 1995. Jpn. J. Cancer Res. 86: 819-827. PMID: 7591958 3. Chang, C.Y. and Puga, A. 1998. Mol. Cell. Biol. 18: 525-535. PMID: 9418899 4. Poljaková, J., et al. 2009. Biochem. Pharmacol. 77: 1466-1479. PMID: 19426684
Bright yellow solid
Soluble in DMSO, ethanol, and methanol. Insoluble in water.
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Poljakova et alPoljakova et al. (PubMed ID 19426684) found that ellipticine, an antineoplastic agent, formed covalent DNA adducts that conferred cytotoxicity to neurobalstoma cells.
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