Please use this identifier to cite or link to this item: http://hdl.handle.net/2440/114929
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dc.contributor.authorSundaraneedi, M.en
dc.contributor.authorEichenberger, R.en
dc.contributor.authorAl-Hallaf, R.en
dc.contributor.authorYang, D.en
dc.contributor.authorSotillo, J.en
dc.contributor.authorRajan, S.en
dc.contributor.authorWangchuk, P.en
dc.contributor.authorGiacomin, P.en
dc.contributor.authorKeene, F.en
dc.contributor.authorLoukas, A.en
dc.contributor.authorCollins, J.en
dc.contributor.authorPearson, M.en
dc.date.issued2018en
dc.identifier.citationInternational Journal for Parasitology: Drugs and Drug Resistance, 2018; 8(1):1-7en
dc.identifier.issn2211-3207en
dc.identifier.issn2211-3207en
dc.identifier.urihttp://hdl.handle.net/2440/114929-
dc.description.abstractOver 4.5 billion people are at risk of infection with soil transmitted helminths and there are concerns about the development of resistance to the handful of frontline nematocides in endemic populations. We investigated the anti-nematode efficacy of a series of polypyridylruthenium(II) complexes and showed they were active against L3 and adult stages of Trichuris muris, the rodent homologue of the causative agent of human trichuriasis, T. trichiura. One of the compounds, Rubb12-mono, which was among the most potent in its ability to kill L3 (IC50 = 3.1 ± 0.4 μM) and adult (IC50 = 5.2 ± 0.3 μM) stage worms was assessed for efficacy in a mouse model of trichuriasis by administering 3 consecutive daily oral doses of the drug 3 weeks post infection with the murine whipworm Trichuris muris. Mice treated with Rubb12-mono showed an average 66% reduction (P = 0.015) in faecal egg count over two independent trials. The drugs partially exerted their activity through inhibition of acetylcholinesterases, as worms treated in vitro and in vivo showed significant decreases in the activity of this class of enzymes. Our data show that ruthenium complexes are effective against T. muris, a model gastro-intestinal nematode and soil-transmitted helminth. Further, knowledge of the target of ruthenium drugs can facilitate modification of current compounds to identify analogues which are even more effective and selective against Trichuris and other helminths of human and veterinary importance.en
dc.description.statementofresponsibilityMadhu Sundaraneedi, , Ramon M. Eichenberger, Rafid Al-Hallaf, Dai Yang, Javier Sotillo, Siji Rajan, Phurpa Wangchuk, Paul R. Giacomin, F. Richard Keene, Alex Loukas, J. Grant Collinsa, Mark S. Pearsonen
dc.language.isoenen
dc.publisherElsevieren
dc.rights© 2017 The Authors. Published by Elsevier Ltd on behalf of Australian Society for Parasitology. This is an open access article under the CC BY-NC-ND license (http://creativecommons.org/licenses/BY-NC-ND/4.0/).en
dc.subjectAcetylcholinesterase; Anthelmintic; Ruthenium complex; Trichuris murisen
dc.titlePolypyridylruthenium(II) complexes exert in vitro and in vivo nematocidal activity and show significant inhibition of parasite acetylcholinesterasesen
dc.typeJournal articleen
dc.identifier.rmid0030078541en
dc.identifier.doi10.1016/j.ijpddr.2017.11.005en
dc.identifier.pubid389070-
pubs.library.collectionPhysics publicationsen
pubs.library.teamDS05en
pubs.verification-statusVerifieden
pubs.publication-statusPublisheden
dc.identifier.orcidKeene, F. [0000-0001-7759-0465]en
Appears in Collections:IPAS publications
Physics publications

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