title: Clonorchicidal properties of the synthetic trioxolane OZ78.
abstract: Because the synthetic trioxolane OZ78 is active against the liver fluke Fasciola hepatica, we were motivated to investigate the in vivo and in vitro activity against another liver fluke, namely Clonorchis sinensis. Rats infected with C. sinensis for 2 and 5 wk were treated orally with single doses of OZ78 (75, 150, or 300 mg/kg). Worm burden reductions were assessed against untreated control rats. Scanning electron microscopy (SEM) was used to observe adult C. sinensis after recovery from rats 1-3 days posttreatment with a single 300 mg/kg oral dose of OZ78 and after in vitro exposure to concentrations of 1, 10, and 100 microg/ml of OZ78. A single 300 mg/kg oral dose of OZ78 resulted in worm burden reductions of 78.5% and 98.5% against juvenile and adult C. sinensis, respectively. SEM observations revealed tegumental surface alterations, including blebbing and sloughing. OZ78 emerges as a new compound with a broad spectrum of activity against major foodborne trematode infections.
authors.affiliation: Swiss Tropical Institute, Basel, Switzerland. jennifer.keiser@unibas.ch
authors.forename: Jennifer
authors.initials: J
authors.lastname: Keiser
authors.forename: Shu-Hua
authors.initials: SH
authors.lastname: Xiao
authors.forename: Yuxiang
authors.initials: Y
authors.lastname: Dong
authors.forename: Jürg
authors.initials: J
authors.lastname: Utzinger
authors.forename: Jonathan L
authors.initials: JL
authors.lastname: Vennerstrom
mesh_terms: D000218:Adamantane / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology; D000818:Animals; D000871:Anthelmintics / Q000008:administration & dosage / Q000138:chemical synthesis / Q000494:pharmacology*; D003003:Clonorchiasis / Q000188:drug therapy* / Q000469:parasitology; D003004:Clonorchis sinensis / Q000187:drug effects* / Q000254:growth & development / Q000648:ultrastructure; D008297:Male; D008855:Microscopy, Electron, Scanning; D021261:Parasitic Sensitivity Tests; D051381:Rats; D017207:Rats, Sprague-Dawley
chemical_list: D000871:Anthelmintics; C518172:OZ78 compound; D000218:Adamantane