The mode of action of antimalarial endoperoxides.

The mechanism of action of artemisinin appears to involve two steps. In the first step, activation, intra-parasitic iron catalyses the cleavage of the endoperoxide bridge and the generation of free radicals. In the second step, alkylation, the artemisinin-derived free radical forms covalent bonds with parasite proteins.

[1]  Chang Ho Oh,et al.  Regiospecifically oxygen-18 labeled 1,2,4-trioxane: a simple chemical model system to probe the mechanism(s) for the antimalarial activity of artemisinin (qinghaosu). , 1992 .

[2]  W. Peters,et al.  The chemotherapy of rodent malaria. XLVII. Studies on pyronaridine and other Mannich base antimalarials. , 1992, Annals of tropical medicine and parasitology.

[3]  S. Meshnick,et al.  Alkylation of human albumin by the antimalarial artemisinin. , 1993, Biochemical pharmacology.

[4]  S. Meshnick,et al.  Artemisinin (qinghaosu): the role of intracellular hemin in its mechanism of antimalarial action. , 1991, Molecular and biochemical parasitology.

[5]  O. Levander,et al.  Qinghaosu, dietary vitamin E, selenium, and cod-liver oil: effect on the susceptibility of mice to the malarial parasite Plasmodium yoelii. , 1989, The American journal of clinical nutrition.

[6]  S. Meshnick,et al.  Iron-dependent free radical generation from the antimalarial agent artemisinin (qinghaosu) , 1993, Antimicrobial Agents and Chemotherapy.

[7]  A. Butler,et al.  Artemisinin (qinghaosu): a new type of antimalarial drug , 1992 .

[8]  B. Halliwell,et al.  Free radicals in biology and medicine , 1985 .

[9]  S. Meshnick,et al.  Qinghaosu-mediated oxidation in normal and abnormal erythrocytes. , 1989, The Journal of laboratory and clinical medicine.

[10]  D. Warhurst,et al.  The chemotherapy of rodent malaria, XL. The action of artemisinin and related sesquiterpenes. , 1986, Annals of tropical medicine and parasitology.

[11]  S. Krungkrai,et al.  The antimalarial action on Plasmodium falciparum of qinghaosu and artesunate in combination with agents which modulate oxidant stress. , 1987, Transactions of the Royal Society of Tropical Medicine and Hygiene.

[12]  S. Meshnick,et al.  Morphologic effects of artemisinin in Plasmodium falciparum. , 1993, The American journal of tropical medicine and hygiene.

[13]  S. Meshnick,et al.  Hemin-catalyzed decomposition of artemisinin (qinghaosu). , 1992, Biochemical pharmacology.

[14]  S. Meshnick,et al.  Activated oxygen mediates the antimalarial activity of qinghaosu. , 1989, Progress in clinical and biological research.

[15]  A. Chou,et al.  Ferriprotoporphyrin IX fulfills the criteria for identification as the chloroquine receptor of malaria parasites. , 1980, Biochemistry.