Artemisinin is an anti-malarial drug with poor water solubility and oral absorption; so a variety of derivatives based on the parent nucleus have been developed.Compared with artemisinin , dihydroartemisinin (DHA) has a stronger anti-malaria activity, and has the advantages of high metabolic rate and better water solubility .Recent studies have discovered that DHA has a good inhibitory effect on tumor cells, which is closely related to the peroxide bridge in its molecular structure . Since tumor cells need more Fe 3+ than normal cells, there are a large number of transferrin receptors on the tumor cell membrane .DHA can break the peroxide bridge in the presence of Fe 2+, and the free radicals generated can play its lethal effect on tumor cells.In addition, DHA can promote endocytosis of transferrin receptor , and thus prevent cancer cells from taking Fe 3+from microenvironment .This article reviews the anti-tumor molecular mechanism of DHA , including accelerating oxidative damage , inducing apoptosis , inhibiting the growth , proliferation and invasion of tumor cells , reversing tumor multidrug resistance .

Artemisinin is an anti-malarial drug with poor water solubility and oral absorption; so a variety of derivatives based on the parent nucleus have been developed. Compared with artemisinin, dihydroartemisinin (DHA) has a stronger anti-malaria activity, and has the advantages of high metabolic rate and better water solubility. Recent studies have discovered that DHA has a good inhibitory effect on tumor cells, which is closely related to the peroxide bridge in its molecular structure. Since tumor cells need more Fethan normal cells, there are a large number of transferrin receptors on the tumor cell membrane. DHA can break the peroxide bridge in the presence of Fe, and the free radicals generated can play its lethal effect on tumor cells. In addition, DHA can promote endocytosis of transferrin receptor, and thus prevent cancer cells from taking Fefrom microenvironment. This article reviews the anti-tumor molecular mechanism of DHA, including accelerating oxidative damage, inducing apoptosis, inhibiting the growth, proliferation and invasion of tumor cells, reversing tumor multidrug resistance.
Antigens, CD ; drug effects ; metabolism ; Antineoplastic Agents ; pharmacokinetics ; pharmacology ; Apoptosis ; drug effects ; Artemisinins ; metabolism ; pharmacokinetics ; pharmacology ; Endocytosis ; drug effects ; Free Radicals ; chemical synthesis ; pharmacology ; Humans ; Iron ; metabolism ; Neoplasms ; drug therapy ; physiopathology ; Oxidative Stress ; drug effects ; Receptors, Transferrin ; drug effects ; metabolism