Ancient Chinese Salad Plant Transformed Into New Cancer-killing Compound
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The artemisinin compound takes advantage of cancer cell's high iron levels. Artemisinin is highly toxic in the presence of iron, but harmless otherwise. Cancer cells need a lot of iron to maintain the rapid division necessary for tumor growth.
Since too much free-floating iron is toxic, when cells need iron they construct a special protein signal on their surfaces. The body's machinery then delivers iron, shielded with a protein package, to these signals proteins. The cell then swallows this bundle of iron and proteins.
Artemisinin alone is fairly effective at killing cancer cells. It kills approximately 100 cancer cells for every healthy cell, about ten times better than current chemotherapies. To improve those odds, the researchers added a small chemical tag to artemisinin that sticks to the "iron needed here" protein signal. The cancer cell, unaware of the toxic compound lurking on its surface, waits for the protein machinery to deliver iron molecules and engulfs everything -- iron, proteins and toxic compound.
Once inside the cell, the iron reacts with artemisinin to release poisonous molecules called free radicals. When enough of these free
radicals accumulate, the cell dies.
"The compound is like a little bomb-carrying monkey riding on the back of a Trojan horse," said Henry Lai, UW bioengineering professor and
co-author of the study.
The compound is so selective for cancer cells partly due to their rapid multiplication, which requires high amounts of iron, and partly because cancer cells are not as good as healthy cells at cleaning up free-floating iron.
"Cancer cells get sloppy at maintaining free iron, so they are more sensitive to artemisinin," Sasaki said.
References:
Synthesis and anti-cancer activity of covalent conjugates of artemisinin and a transferrin-receptor targeting peptide
Steve Oh, Byung Ju Kim, Narendra P. Singh, Henry Lai, Tomikazu Sasaki; February 8, 2009
Anticancer Effect of AntiMalarial Artemisinin Compounds,
AK Das; 2015 Mar-Apr
The Effects of Artemisinin on the Cytolytic Activity of Natural Killer (NK) Cells,
Youn Kyung Houh, Kyung Eun Kim, Sunyoung Park, Dae Young Hur, Seonghan Kim, Daejin Kim, Sa Ik Bang, Yoolhee Yang, Hyun Jeong Park, and Daeho Cho; 2017 Jul
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