Artemisinin contains an endoperoxide moiety that can react with
iron to form cytotoxic
free radicals.
Cancer cells contain significantly more intracellular free
iron than normal cells and it has been shown that
artemisinin and its analogs selectively cause apoptosis in many
cancer cell lines. In addition,
artemisinin compounds have been shown to have anti-angiogenic, anti-inflammatory, anti-
metastasis, and growth inhibition effects. These properties make
artemisinin compounds attractive
cancer chemotherapeutic
drug candidates. However, simple
artemisinin analogs are less potent than traditional
cancer chemotherapeutic agents and have short plasma half-lives, and would require high dosage and frequent administration to be effective for
cancer treatment. More potent and target-selective
artemisinin-compounds are being developed. These include
artemisinin dimers and trimers,
artemisinin hybrid compounds, and tagging of
artemisinin compounds to molecules that are involved in the intracellular
iron-delivery mechanism. These compounds are promising potent anticancer compounds that produce significantly less side effect than traditional chemotherapeutic agents.