{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,10,8]],"date-time":"2026-10-08T07:02:45Z","timestamp":1791442965170,"version":"4.3.3"},"reference-count":36,"publisher":"American Society for Microbiology","issue":"9","license":[{"start":{"date-parts":[[2014,9,1]],"date-time":"2014-09-01T00:00:00Z","timestamp":1409529600000},"content-version":"tdm","delay-in-days":0,"URL":"https:\/\/journals.asm.org\/non-commercial-tdm-license"}],"content-domain":{"domain":["journals.asm.org"],"crossmark-restriction":true},"short-container-title":["Antimicrob Agents Chemother"],"published-print":{"date-parts":[[2014,9]]},"abstract":"<jats:title>ABSTRACT<\/jats:title><jats:p>A racemic mixture of<jats:italic>R<\/jats:italic>and<jats:italic>S<\/jats:italic>enantiomers of praziquantel (PZQ) is currently the treatment of choice for schistosomiasis. Though the<jats:italic>S<\/jats:italic>enantiomer and the metabolites are presumed to contribute only a little to the activity of the drug, in-depth side-by-side studies are lacking. The aim of this study was to investigate the<jats:italic>in vitro<\/jats:italic>activities of PZQ and its main metabolites, namely,<jats:italic>R<\/jats:italic>- and<jats:italic>S-cis<\/jats:italic>- and<jats:italic>R<\/jats:italic>- and<jats:italic>S-trans<\/jats:italic>-4\u2032-hydroxypraziquantel, against adult worms and newly transformed schistosomula (NTS). Additionally, we explored the<jats:italic>in vivo<\/jats:italic>activity and hepatic shift (i.e., the migration of the worms to the liver) produced by each PZQ enantiomer in mice. Fifty percent inhibitory concentrations of<jats:italic>R<\/jats:italic>-PZQ,<jats:italic>S<\/jats:italic>-PZQ, and<jats:italic>R-trans<\/jats:italic>- and<jats:italic>R-cis<\/jats:italic>-4\u2032-hydroxypraziquantel of 0.02, 5.85, 4.08, and 2.42 \u03bcg\/ml, respectively, for adult<jats:named-content xmlns:xlink=\"http:\/\/www.w3.org\/1999\/xlink\" content-type=\"genus-species\" xlink:type=\"simple\">S. mansoni<\/jats:named-content>were determined<jats:italic>in vitro. S-trans<\/jats:italic>- and<jats:italic>S-cis<\/jats:italic>-4\u2032-hydroxypraziquantel were not active at 100 \u03bcg\/ml. These results are consistent with microcalorimetry data and studies with NTS.<jats:italic>In vivo<\/jats:italic>, single 400-mg\/kg oral doses of<jats:italic>R<\/jats:italic>-PZQ and<jats:italic>S<\/jats:italic>-PZQ achieved worm burden reductions of 100 and 19%, respectively. Moreover, worms treated<jats:italic>in vivo<\/jats:italic>with<jats:italic>S<\/jats:italic>-PZQ displayed an only transient hepatic shift and returned to the mesenteric veins within 24 h. Our data confirm that<jats:italic>R<\/jats:italic>-PZQ is the main effector molecule, while<jats:italic>S<\/jats:italic>-PZQ and the metabolites do not play a significant role in the antischistosomal properties of PZQ.<\/jats:p>","DOI":"10.1128\/aac.02741-14","type":"journal-article","created":{"date-parts":[[2014,7,1]],"date-time":"2014-07-01T14:43:52Z","timestamp":1404225832000},"page":"5466-5472","update-policy":"https:\/\/doi.org\/10.1128\/asmj-crossmark-policy-page","source":"Crossref","is-referenced-by-count":104,"title":["Activity of Praziquantel Enantiomers and Main Metabolites against Schistosoma mansoni"],"prefix":"10.1128","volume":"58","author":[{"given":"Isabel","family":"Meister","sequence":"first","affiliation":[{"name":"Department of Medical Parasitology and Infection Biology, Swiss Tropical and Public Health Institute, Basel, Switzerland"},{"name":"University of Basel, Basel, Switzerland"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Katrin","family":"Ingram-Sieber","sequence":"additional","affiliation":[{"name":"Department of Medical Parasitology and Infection Biology, Swiss Tropical and Public Health Institute, Basel, Switzerland"},{"name":"University of Basel, Basel, Switzerland"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Noemi","family":"Cowan","sequence":"additional","affiliation":[{"name":"Department of Medical Parasitology and Infection Biology, Swiss Tropical and Public Health Institute, Basel, Switzerland"},{"name":"University of Basel, Basel, Switzerland"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Matthew","family":"Todd","sequence":"additional","affiliation":[{"name":"School of Chemistry, Faculty of Science, University of Sydney, Sydney, Australia"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Murray N.","family":"Robertson","sequence":"additional","affiliation":[{"name":"School of Chemistry, Faculty of Science, University of Sydney, Sydney, Australia"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Claudia","family":"Meli","sequence":"additional","affiliation":[{"name":"Merck Serono, Global Early Development, Global Non Clinical Safety Merck\u2014Living Innovation RBM S.p.A.\u2014Istituto di Ricerche Biomediche A. 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