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.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Antineoplastic Agents / chemistry
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Antineoplastic Agents / pharmacology*
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Artemisia / chemistry
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Artemisinins / chemical synthesis*
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Artemisinins / chemistry
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Artemisinins / pharmacology*
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Cells, Cultured
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Humans
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Leukemia / drug therapy*
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Leukemia / metabolism
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Leukemia / pathology
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Leukocytes / drug effects
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Leukocytes / metabolism
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Peptide Fragments / chemical synthesis
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Peptide Fragments / chemistry
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Peptide Fragments / pharmacology*
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Receptors, Transferrin / metabolism*
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Recombinant Fusion Proteins / pharmacology*
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Transferrin / metabolism
Substances
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Antineoplastic Agents
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Artemisinins
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Peptide Fragments
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Receptors, Transferrin
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Recombinant Fusion Proteins
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Transferrin
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artemisinin