Artemisinin dimer anticancer activity correlates with heme-catalyzed reactive oxygen species generation and endoplasmic reticulum stress induction.

@article{Stockwin2009ArtemisininDA,
  title={Artemisinin dimer anticancer activity correlates with heme-catalyzed reactive oxygen species generation and endoplasmic reticulum stress induction.},
  author={Luke H. Stockwin and Bingnan Han and S Xiaofeng Yu and Melinda G. Hollingshead and Mahmoud A ElSohly and Waseem Gul and Desmond Slade and Ahmed Galal and Dianne L. Newton and Maja A Bumke},
  journal={International journal of cancer},
  year={2009},
  volume={125 6},
  pages={1266-75}
}
Analogs of the malaria therapeutic, artemisinin, possess in vitro and in vivo anticancer activity. In this study, two dimeric artemisinins (NSC724910 and 735847) were studied to determine their mechanism of action. Dimers were >1,000 fold more active than monomer and treatment was associated with increased reactive oxygen species (ROS) and apoptosis induction. Dimer activity was inhibited by the antioxidant L-NAC, the iron chelator desferroxamine and exogenous hemin. Similarly, induction of… CONTINUE READING

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