Targeted treatment of cancer with artemisinin and artemisinin-tagged iron-carrying compounds.
Artemisinin is a chemical compound that reacts with iron to form free radicals which can kill cells. Cancer cells require and uptake a large amount of iron to proliferate. They are more susceptible to the cytotoxic effect of artemisinin than normal cells. Cancer cells express a large concentration of cell surface transferrin receptors that facilitate uptake of the plasma iron-carrying protein transferrin via endocytosis. By covalently tagging artemisinin to transferrin, artemisinin could be selectively picked up and concentrated by cancer cells. Futhermore, both artemisinin and iron would be transported into the cell in one package. Once an artemisinin-tagged transferrin molecule is endocytosed, iron is released and reacts with artemisinin moieties tagged to transferrin. Formation of free radicals kills the cancer cell. The authors have found that artemisinin-tagged transferrin is highly selective and potent in killing cancer cells. Thus, artemisinin and artemisinin-tagged iron-carrying compounds could be developed into powerful anticancer drugs.
Lai
Henry
H
University of Washington, Department of Bioengineering, Box 357962, Seattle, Washington 98195-7962, USA. hlai@u.washington.edu
Sasaki
Tomikazu
T
Singh
Narendra P
NP
D000970:Antineoplastic Agents / Q000008:administration & dosage* / Q000494:pharmacology* / Q000627:therapeutic use; D037621:Artemisinins / Q000008:administration & dosage* / Q000494:pharmacology* / Q000627:therapeutic use; D016503:Drug Delivery Systems / Q000379:methods*; D006801:Humans; D007501:Iron / Q000008:administration & dosage / Q000378:metabolism / Q000494:pharmacology*; D009369:Neoplasms / Q000188:drug therapy* / Q000378:metabolism; D012717:Sesquiterpenes / Q000008:administration & dosage* / Q000494:pharmacology* / Q000627:therapeutic use
D000970:Antineoplastic Agents; D037621:Artemisinins; D012717:Sesquiterpenes; C031327:artemisinin; D007501:Iron