antischistosomal activity of trioxaquines in vivo efficacy and mechanism of action on schistosoma mansoniantischistosomal trioxaquines活动对曼氏裂体吸虫体内疗效和作用机理.pdf

Antischistosomal Activity of Trioxaquines: In Vivo Efficacy and Mechanism of Action on Schistosoma mansoni 1,2 ´ ˆ 1,2 1,2 3 ` 3 ´ ´ Julien Portela , Jerome Boissier *, Benjamin Gourbal , Vincent Pradines , Vincent Colliere , Frederic ´ 4 3,4 3 Cosledan , Bernard Meunier , Anne Robert * ´ ´ ´ 1 Universite de Perpignan Via Domitia, Perpignan, France, 2 CNRS, UMR 5244, Ecologie et Evolution des Interactions, Perpignan, France, 3 Laboratoire de Chimie de Coordination du CNRS, Toulouse, France, 4 Palumed, Castanet-Tolosan, France Abstract Schistosomiasis is among the most neglected tropical diseases, since its mode of spreading tends to limit the contamination to people who are in contact with contaminated waters in endemic countries. Here we report the in vitro and in vivo anti- schistosomal activities of trioxaquines. These hybrid molecules are highly active on the larval forms of the worms and exhibit different modes of action, not only the alkylation of heme. The synergy observed with praziquantel on infected mice is in favor of the development of these trioxaquines as potential anti-schistosomal agents. ` Citation: Portela J, Boissier J, Gourbal B, Pradines V, Colliere V, et al. (2012) Antischistosomal Activity of Trioxaquines: In Vivo Efficacy and Mechanism of Action on Schistosoma mansoni. PLoS Negl Trop Dis 6(2): e1474. doi:10.1371/journal.pntd.0001474 Editor: Timothy G. Geary, McGill University, Canada Received August 22, 201