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IC50 = 0.99 μM for L1210 lymphocytic leukemia cells [1]

Plant alkaloid ellipticine shows antitumor, mutagenic and cytotoxic activities by inhibition of DNA topoisomerase II activity. DNA topoisomerase II regulates the overwinding or underwinding of DNA by cuting DNA double helix, passing another unbroken DNA helix through it, and then reannealing the cut strands.

In vitro: Treatment mammalian DNA topoisomerase II reaction mixture with ellipticine resulted in the stimulation of DNA cleavage. The drug-stimulation of DNA cleavage is related to the formation of a ternary complex between topoisomerase II, DNA, and ellipticine. Ellipticine dose not inhibit enzyme-mediated DNA religation, however, it stimulates DNA breakage by enhancing the forward rate of cleavage [2]. Ellipticine showed growth inhibition activity on L1210 lymphocytic leukemia cells with a IC50 of 0.99 μM [1].

In vivo: Ellipticine was evaluated in P. berghei infected mice in the 4-day suppressive test. Ellipticine had a 100% inhibition versus controls on days 5 and 7 at an oral dose of 50 mg/kg/day, and the mean survival time (MST) was more than 40 days [3].

Clinical trial: Several ellipticine derivatives have been validated in clinical trials, however, due to adverse side-effects, no progress has be reported.

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