Document Detail


Iron-dependent free radical generation from the antimalarial agent artemisinin (qinghaosu).
MedLine Citation:
PMID:  8517699     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
Artemisinin is an important new antimalarial agent containing a bridged endoperoxide. The in vitro antimalarial activity of an artemisinin derivative, arteether, is antagonized by two iron chelators, pyridoxal benzoylhydrazone and 1,2-dimethyl-3-hydroxypyrid-4-one. Similarly, the acute toxicity of artemisinin in mice is antagonized by another chelator, deferoxamine-hydroxyethylstarch. A combination of artemisinin and hemin oxidizes erythrocyte membrane thiols in vitro, and this oxidation is also inhibited by an iron chelator. Thus, iron plays a role in the mechanisms of action and toxicity of artemisinin. The combination of artemisinin and hemin also decreases erythrocyte deformability. Iron probably catalyzes the generation of free radicals from artemisinin since alpha-tocopherol antagonizes the thiol-oxidizing activity of artemisinin and since a spin-trapped free radical signal can be seen by electron paramagnetic resonance only when artemisinin is incubated in the presence of iron.
Authors:
S R Meshnick; Y Z Yang; V Lima; F Kuypers; S Kamchonwongpaisan; Y Yuthavong
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't; Research Support, U.S. Gov't, P.H.S.    
Journal Detail:
Title:  Antimicrobial agents and chemotherapy     Volume:  37     ISSN:  0066-4804     ISO Abbreviation:  Antimicrob. Agents Chemother.     Publication Date:  1993 May 
Date Detail:
Created Date:  1993-07-22     Completed Date:  1993-07-22     Revised Date:  2009-11-18    
Medline Journal Info:
Nlm Unique ID:  0315061     Medline TA:  Antimicrob Agents Chemother     Country:  UNITED STATES    
Other Details:
Languages:  eng     Pagination:  1108-14     Citation Subset:  IM    
Affiliation:
Department of Epidemiology, University of Michigan School of Public Health, Ann Arbor 48109.
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MeSH Terms
Descriptor/Qualifier:
Animals
Antimalarials / antagonists & inhibitors,  pharmacology*,  therapeutic use
Artemisinins*
Drugs, Chinese Herbal / pharmacology*
Erythrocyte Deformability / drug effects
Free Radicals / metabolism
Iron / metabolism*
Iron Chelating Agents / pharmacology
Malaria, Falciparum / drug therapy,  parasitology
Male
Mice
Plasmodium falciparum / drug effects
Sesquiterpenes / antagonists & inhibitors,  pharmacology*,  therapeutic use
Grant Support
ID/Acronym/Agency:
AI26848/AI/NIAID NIH HHS; DK92111/DK/NIDDK NIH HHS
Chemical
Reg. No./Substance:
0/Antimalarials; 0/Artemisinins; 0/Drugs, Chinese Herbal; 0/Free Radicals; 0/Iron Chelating Agents; 0/Sesquiterpenes; 63968-64-9/artemisinine; 7439-89-6/Iron
Comments/Corrections

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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