Anthelminthic properties of mangostin and mangostin diacetate

Few anthelminthic drugs are available for human use despite the significant burden caused by helminth infections. We studied the activities of mangostin, a major bioactive xanthone isolated from the pericarp and fruit of Garcinia mangostana and of the synthetic derivative mangostin diacetate. Mangostin and mangostin diacetate lacked activity against the nematodes Heligmosomoides polygyrus (third-stage larvae (L3)), Ancylostoma ceylanicum L3, and Trichuris muris adults and showed only low activity against A. ceylanicum adults (IC(50)s of 91 mu g/ml) in vitro. Mangostin showed promising activities (IC50 of 2.9-15.6 mu g/ml) against the trematodes Schistosoma mansoni, Echinostoma caproni, and Fasciola hepatica in vitro. Single oral doses (400 mg/kg and 800 mg/kg) of the drugs achieved worm burden reductions ranging from 0 to 38% and 11-54% against S. mansoni and E. caproni in vivo, respectively. Pharmacokinetic studies would be helpful to understand the differences observed between in vitro and in vivo activities and lacking dose-response relationships. (C) 2012 Elsevier Ireland Ltd. All rights reserved.