Trioxaquines and heme-artemisinin adducts inhibit the in vitro formation of hemozoin better than chloroquine.
Trioxaquines, potential antimalarial agents, and heme-artemisinin adducts, resulting from the alkylation of heme by artemisinin, were evaluated as inhibitors of beta-hematin formation in 10 M acetate medium at pH 5.
Loup
Christophe
C
Laboratoire de Chimie de Coordination, CNRS, 205 Route de Narbonne, 31000, Toulouse Cedex 4, France. christophe.loup@lcc-toulouse.fr
Lelièvre
Joël
J
Benoit-Vical
Françoise
F
Meunier
Bernard
B
D000478:Alkylation; D000818:Animals; D000962:Antimalarials / Q000494:pharmacology*; D037621:Artemisinins / Q000737:chemistry / Q000494:pharmacology*; D002738:Chloroquine / Q000494:pharmacology*; D004146:Dioxanes / Q000737:chemistry / Q000494:pharmacology*; D006418:Heme / Q000737:chemistry*; D006420:Hemeproteins / Q000037:antagonists & inhibitors* / Q000096:biosynthesis*; D010961:Plasmodium / Q000187:drug effects / Q000201:enzymology; D012717:Sesquiterpenes / Q000494:pharmacology; D013055:Spectrophotometry, Infrared
D000962:Antimalarials; D037621:Artemisinins; C503606:DU1301; D004146:Dioxanes; D006420:Hemeproteins; D012717:Sesquiterpenes; C020753:hemozoin; D006418:Heme; D002738:Chloroquine; C031327:artemisinin
Antimicrob Agents Chemother. 2007 Apr;51(4):1463-72
17242150
Proc Natl Acad Sci U S A. 2005 Sep 20;102(38):13676-80
16155128
Chembiochem. 2005 Apr;6(4):653-8
15744769
Biochim Biophys Acta. 1999 May 31;1454(1):31-7
10354512
Biochem Pharmacol. 1998 Mar 15;55(6):737-47
9586945
Exp Parasitol. 2000 Dec;96(4):249-56
11162378
Angew Chem Int Ed Engl. 2001 May 18;40(10):1954-1957
11385684
Antimicrob Agents Chemother. 2003 Mar;47(3):1175
12604568
Anal Biochem. 2004 Feb 1;325(1):85-91
14715288
Exp Parasitol. 2002 Apr;100(4):252-6
12128052
Trends Parasitol. 2001 Mar;17(3):122-6
11286794
Nature. 2000 Mar 16;404(6775):307-10
10749217
J Med Chem. 1999 Nov 4;42(22):4630-9
10579825
J Med Chem. 2000 Jan 27;43(2):283-91
10649984
Anal Biochem. 2005 Mar 15;338(2):306-19
15745752
J Inorg Biochem. 2002 Jul 25;91(1):19-26
12121758
Chem Biol. 2002 Mar;9(3):321-32
11927257
Antimicrob Agents Chemother. 1999 Mar;43(3):598-602
10049273
Chemistry. 2004 Apr 2;10(7):1625-36
15054749
FEBS Lett. 1994 Sep 19;352(1):54-7
7925942
J Am Chem Soc. 2007 Mar 7;129(9):2615-27
17290993