Study on the mechanism of action of artemether against schistosomes: the identification of cysteine adducts of both carbon-centred free radicals derived from artemether.
Reaction of the antimalarial and anti-schistosome drug artemether (1) and catalytic amount of ferrous ion in the presence of excess cysteine gave two adducts of cysteine and previous postulated primary and secondary carbon-centred free radicals besides their other rearrangement products. This piece of further evidence for the presence of carbon-centred radicals, especially the secondary carbon-centred free radical for the first time by the isolation of its coupling adduct, will be help to understand the mechanism of action of artemether and other qinghaosu derivatives against parasites.
Wu
Wen-Min
WM
State Key Laboratory of Bio-Organic and Natural Products Chemistry, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, China.
Chen
Yan-Li
YL
Zhai
Zili
Z
Xiao
Shu-Hua
SH
Wu
Yu-Lin
YL
D000818:Animals; D000962:Antimalarials / Q000737:chemistry; D000077549:Artemether; D037621:Artemisinins / Q000737:chemistry*; D003545:Cysteine / Q000737:chemistry; D005609:Free Radicals / Q000737:chemistry; D012556:Schistosomicides / Q000737:chemistry*; D012717:Sesquiterpenes / Q000737:chemistry*
D000962:Antimalarials; D037621:Artemisinins; D005609:Free Radicals; D012556:Schistosomicides; D012717:Sesquiterpenes; D000077549:Artemether; D003545:Cysteine