Selective toxicity of dihydroartemisinin and holotransferrin toward human breast cancer cells

Artemisinin becomes cytotoxic in the presence of ferrous iron. Since iron i nflux is high in cancer cells, artemisinin and its analogs selectively kill cancer cells under conditions that increase intracellular iron concentrati ons. We report here that after incubation with holotransferrin, which incre ases the concentration of ferrous iron in cancer cells, dihydroartemisinin, an analog of artemisinin, effectively killed a type of radiation-resistant human breast cancer cell in vitro. The same treatment had considerably les s effect on normal human breast cells. Since it is relatively easy to incre ase the iron content inside cancer cells in vivo, administration of artemis inin-like drugs and intracellular iron-enhancing compounds may be a simple, effective, and economical treatment for cancer. (C) 2001 Elsevier Science Inc. All rights reserved.