Artemisinin

Artemisinin is an antimalarial agent with anticancer activity.^1,2 It is an iron(II) oxide-reactive endoperoxide that generates reactive oxygen species (ROS) upon cleavage of its endoperoxide bridge.³ It reduces the growth of various P. falciparum strains in vitro (IC₅₀s = 3.98-20.36 nM) and reduces parasitemia in mice infected with P. falciparum with a curative dose (CD₅₀) value of 140 mg/kg.^1,4 It also reduces P. berghei infection in mice (ED₅₀ = 5.6 mg/kg per day).⁵ Artemisinin (100-400 μM) induces cell cycle arrest in the G₀/G₁ phase and apoptosis and inhibits growth of SK-N-AS, BE(2)-C, SK-N-DZ, and SHEP1 neuroblastoma cells in a time- and concentration-dependent manner.² It also suppresses BE(2)-C cell colony formation in a soft agar assay and reduces tumor growth in a BE(2)-C mouse xenograft model. Formulations containing artemisinin have been used in combination therapies for the treatment of malaria.

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1. Akoachere, M., Buchholz, K., Fischer, E., et al. In vitro assessment of methylene blue on chloroquine-sensitive and -resistant Plasmodium falciparum strains reveals synergistic action with artemisinins. Antimicrob. Agents Chemother. 49(11), 4592-4597 (2005).

2. Zhu, S., Liu, W., Ke, X., et al. Artemisinin reduces cell proliferation and induces apoptosis in neuroblastoma. Oncol. Rep. 32(3), 1094-1100 (2014).

3. Ooko, E., Saeed, M.E.M., Kadioglu, O., et al. Artemisinin derivatives induce iron-dependent cell death (ferroptosis) in tumor cells. Phytomedicine 22(11), 1045-1054 (2015).

4. Robert, A., Benoit-Vical, F., Claparols, C., et al. The antimalarial drug artemisinin alkylates heme in infected mice. Proc. Natl. Acad. Sci. USA 102(38), 13676-13680 (2005).

5. Chawira, A.N., Warhurst, D.C., Robinson, B.L., et al. The effect of combinations of qinghaosu (artemisinin) with standard antimalarial drugs in the suppressive treatment of malaria in mice. Trans. R. Soc. Trop. Med. Hyg. 81(4), 554-558 (1987).