Ellipticine (NSC 71795) is a powerful antineoplastic agent, leveraging multiple mechanisms for its antitumor, mutagenic, and cytotoxic effects. Its actions include DNA intercalation and inhibition of DNA topoisomerase II activity, as well as the creation of covalent DNA adducts through oxidation processes facilitated by cytochromes P450 (CYP) and peroxidases[1]. Ellipticine's capability to act both as an inhibitor and inducer of biotransformation enzymes further influences its metabolism, contributing to its genotoxic and pharmacological outcomes. Cellular exposure to Ellipticine results in inhibited growth and proliferation, linked to the formation of two specific covalent Ellipticine-derived DNA adducts[2].
Ellipticine HCl/玫瑰树碱盐酸盐 动物研究
Animal study
In various healthy organs (liver, kidney, lung, spleen, breast, heart, and brain) as well as in mammary adenocarcinoma DNA, treatment with Ellipticine leads to the generation of Ellipticine-derived DNA adducts. Notably, the levels of these adducts in adenocarcinomas are nearly double those found in normal mammary tissues. The upregulation of cytochrome b5 in the livers of rats treated with Ellipticine indicates its potential role in modulating the bioactivation and detoxification of Ellipticine via cytochrome P450 pathways[3].
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