Ellipticine and its analogues

Ellipticine, an alkaloid isolated from the leaves of Ochrosia elliptica and other Apocynaceae plants, is the prototype of intercalators based on the pyridocarbazole system and displays a broad spectrum of antitumor activity.6 Although at physiological pH values it can exist both as a neutral species and as a monocation (Fig. 7.2), it is the latter form that seems responsible for DNA intercalation, which leads to RNA polymerase inhibition. Other DNA-related enzymes that are inhibited by ellipticine include DNA polymerase, RNA methylase, and topoisomerase II, although it is not known whether these effects are a consequence of intercalation.

Ellipticine is also known to lead to cytochrome P450 (CYP)-dependent metabolites that are able to bind covalently to DNA.7in vitro experiments employing a peroxidase-H2O2 oxidizing system have shown that one of the metabolites from ellipticine, namely its 9-hydroxy derivative 7.1, oxidizes to quinonimine 7.28 but,

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