Peroxide bond-dependent antiplasmodial specificity of artemisinin and OZ277 (RBx11160).
Using nonperoxidic analogs of artemisinin and OZ277 (RBx11160), the strong in vitro antiplasmodial activities of the latter two compounds were shown to be peroxide bond dependent. In contrast, the weak activities of artemisinin and OZ277 against six other protozoan parasites were peroxide bond independent. These data support the iron-dependent artemisinin alkylation hypothesis.
Kaiser
Marcel
M
Swiss Tropical Institute, Basel, Switzerland.
Wittlin
Sergio
S
Nehrbass-Stuedli
Angela
A
Dong
Yuxiang
Y
Wang
Xiaofang
X
Hemphill
Andrew
A
Matile
Hugues
H
Brun
Reto
R
Vennerstrom
Jonathan L
JL
D000818:Animals; D000962:Antimalarials / Q000494:pharmacology*; D037621:Artemisinins / Q000737:chemistry / Q000494:pharmacology*; D056890:Eukaryota / Q000145:classification / Q000187:drug effects*; D006573:Heterocyclic Compounds, 1-Ring / Q000737:chemistry / Q000494:pharmacology*; D007501:Iron / Q000378:metabolism; D021261:Parasitic Sensitivity Tests; D010545:Peroxides / Q000737:chemistry* / Q000494:pharmacology; D010963:Plasmodium falciparum / Q000187:drug effects; D012717:Sesquiterpenes / Q000737:chemistry / Q000494:pharmacology*; D013141:Spiro Compounds / Q000737:chemistry / Q000494:pharmacology*
D000962:Antimalarials; D037621:Artemisinins; D006573:Heterocyclic Compounds, 1-Ring; D010545:Peroxides; D012717:Sesquiterpenes; D013141:Spiro Compounds; C489136:arterolane; C055261:deoxyartemisinin; D007501:Iron