Trioxaquines and heme-artemisinin adducts inhibit the in vitro formation of hemozoin better than chloroquine.
نویسندگان
چکیده
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.
منابع مشابه
Heme - Artemisinin Adducts Inhibit the in vitro Formation of Hemozoin Better than Chloroquine
Christophe Loup Françoise Benoit-Vical Laboratoire de Chimie de Coordination CHU Rangueil CNRS Service de Parasitologie et Mycologie 205 Route de Narbonne 1 Av. Jean Poulhès 31000 Toulouse TSA 50032 phone: 00 33 5 61 33 31 48 31059 Toulouse cedex 9 fax.: 00 33 5 61 32 20 96 phone: 00 33 5 61 32 34 46 [email protected] fax.: 00 33 5 61 32 20 96 [email protected] AC...
متن کاملThe antimalarial trioxaquine DU 1301 alkylates heme in malaria - infected 1 mice 2 3
18 The in vivo alkylation of heme by the antimalarial trioxaquine DU1301 afforded covalent 19 heme-drug adducts that have been detected in the spleen of malaria-infected mice. This result 20 indicates that the alkylation capacity of trioxaquines in mammals infected by Plasmodium is 21 similar to that of artemisinin, a natural antimalarial trioxane-containing drug. 22 AC CE PT ED Copyright © 200...
متن کاملProtein complex directs hemoglobin-to-hemozoin formation in Plasmodium falciparum.
Malaria parasites use hemoglobin (Hb) as a major nutrient source in the intraerythrocytic stage, during which heme is converted to hemozoin (Hz). The formation of Hz is essential for parasite survival, but to date, the underlying mechanisms of Hb degradation and Hz formation are poorly understood. We report the presence of a ∼200-kDa protein complex in the food vacuole that is required for Hb d...
متن کاملThe interaction of artemisinin with malarial hemozoin.
[14C]Artemisinin was taken up by Plasmodium falciparum in culture and concentrated in hemozoin. In vitro, hemin and artemisinin were found to undergo a chemical reaction forming two major products which were isolated by high-performance liquid chromatography (HPLC). The m/z values of the two products were 856 and 871. Thin-layer chromatography (TLC) and HPLC of hemozoin isolated from [14C]artem...
متن کاملArtemisinin and heme.
A recent Letter to the Editor (R. K. Haynes, D. Monti, D. Taramelli, N. Basilico, S. Parapini, and P. Olliaro, Letter, Antimicrob. Agents Chemother. 47:1175, 2003) presented cogent evidence that artemisinin and its derivatives do not inhibit hemozoin formation in vitro. However, the authors misinterpret these data to conclude that “binding of artemisinins with Fe(III)PPIX is not necessary for a...
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ورودعنوان ژورنال:
- Antimicrobial agents and chemotherapy
دوره 51 10 شماره
صفحات -
تاریخ انتشار 2007