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Synthesis and anti-cancer activity of covalent conjugates of artemisinin and a transferrin-receptor targeting peptide. | LitMetric

AI Article Synopsis

  • - Artemisinin, derived from the plant Artemisia annua L., demonstrates a unique ability to fight cancer through a process that depends on iron.
  • - By attaching artemisinin to a peptide that targets transferrin receptors (HAIYPRH), it can be taken into cancer cells alongside iron, which activates its anti-cancer properties.
  • - The resulting artemisinin-peptide conjugates exhibit strong anti-cancer effects specifically on Molt-4 leukemia cells while being less harmful to normal cells.

Article Abstract

Artemisinin, a natural product isolated from Artemisia annua L., shows a unique anti-cancer activity by an iron dependent mechanism. Artemisinin was covalently conjugated to a transferrin-receptor targeting peptide, HAIYPRH that binds to a cavity on the surface of transferrin receptor. This enables artemisinin to be co-internalized with receptor-bound transferrin. The iron released from transferrin can activate artemisinin to generate toxic radical species to kill cells. The artemisinin-peptide conjugates showed potent anti-cancer activity against Molt-4 leukemia cells with a significantly improved cancer/normal cells selectivity.

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Source
http://dx.doi.org/10.1016/j.canlet.2008.08.031DOI Listing

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