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Chloroquine-containing organoruthenium complexes are fast-acting multistage antimalarial agents

dc.contributor.authorMacedo, Taís S.
dc.contributor.authorColina-Vegas, Legna
dc.contributor.authorda Paixão, Marcelo
dc.contributor.authorNavarro, Maribel
dc.contributor.authorBarreto, Breno C.
dc.contributor.authorOliveira, Poliana C. M.
dc.contributor.authorMacabira, Simone G.
dc.contributor.authorMachado, Marta
dc.contributor.authorPrudêncio, Miguel
dc.contributor.authorD'Alessandro, Sarah
dc.contributor.authorBasilico, Nicoletta
dc.contributor.authorMoreira, Diogo R. M.
dc.contributor.authorBatista, Alzir A.
dc.contributor.authorSoares, Milena B. P.
dc.date.accessioned2022-02-22T17:33:01Z
dc.date.available2022-02-22T17:33:01Z
dc.date.issued2016
dc.description© Cambridge University Press 2016pt_PT
dc.description.abstractWe report the pharmacological activity of organoruthenium complexes containing chloroquine (CQ) as a chelating ligand. The complexes displayed intraerythrocytic activity against CQ-sensitive 3D7 and CQ-resistant W2 strains of Plasmodium falciparum, with potency and selectivity indexes similar to those of CQ. Complexes displayed activity against all intraerythrocytic stages, but moderate activity against Plasmodium berghei liver stages. However, unlike CQ, organoruthenium complexes impaired gametocyte viability and exhibited fast parasiticidal activity against trophozoites for P. falciparum. This functional property results from the ability of complexes to quickly induce oxidative stress. The parasitaemia of P. berghei-infected mice was reduced by treatment with the complex. Our findings demonstrated that using chloroquine for the synthesis of organoruthenium complexes retains potency and selectivity while leading to an increase in the spectrum of action and parasite killing rate relative to CQ.pt_PT
dc.description.sponsorshipThis research was funded by FAPESB (grant PET0042/2013, Brazil) to M.B.P.S, FAPESP (grant 14/10516-7, Brazil) to A.A.B. and Fundação para a Ciência e Tecnologia (grant PTDC/SAU-MIC/117060/2010 Portugal) to M.P. A.A.B. and M.B.P.S. are recipients of senior fellowships by CNPq (Brazil)pt_PT
dc.description.versioninfo:eu-repo/semantics/publishedVersionpt_PT
dc.identifier.citationParasitology (2016), 143, 1543-1556pt_PT
dc.identifier.doi10.1017/S0031182016001153pt_PT
dc.identifier.eissn1469-8161
dc.identifier.issn0031-1820
dc.identifier.urihttp://hdl.handle.net/10451/51460
dc.language.isoengpt_PT
dc.peerreviewedyespt_PT
dc.publisherCambridge University Presspt_PT
dc.relationUtilization of host cell resources by the malaria parasite in the liver
dc.relation.publisherversionhttps://www.cambridge.org/core/journals/parasitology#pt_PT
dc.subjectMalariapt_PT
dc.subjectPlasmodium bergheipt_PT
dc.subjectPlasmodium falciparumpt_PT
dc.subjectChloroquinept_PT
dc.subjectOrganoruthenium complexespt_PT
dc.subjectOxidative stresspt_PT
dc.titleChloroquine-containing organoruthenium complexes are fast-acting multistage antimalarial agentspt_PT
dc.typejournal article
dspace.entity.typePublication
oaire.awardTitleUtilization of host cell resources by the malaria parasite in the liver
oaire.awardURIinfo:eu-repo/grantAgreement/FCT/3599-PPCDT/PTDC%2FSAU-MIC%2F117060%2F2010/PT
oaire.citation.endPage1556pt_PT
oaire.citation.issue12pt_PT
oaire.citation.startPage1543pt_PT
oaire.citation.titleParasitologypt_PT
oaire.citation.volume143pt_PT
oaire.fundingStream3599-PPCDT
person.familyNamePrudêncio
person.givenNameMiguel
person.identifierhttps://scholar.google.pt/citations?user=zduN6wsAAAAJ&hl=pt-PT&oi=ao
person.identifier.ciencia-id5511-16ED-48E0
person.identifier.orcid0000-0003-1746-6029
person.identifier.scopus-author-id6603561872
project.funder.identifierhttp://doi.org/10.13039/501100001871
project.funder.nameFundação para a Ciência e a Tecnologia
rcaap.rightsrestrictedAccesspt_PT
rcaap.typearticlept_PT
relation.isAuthorOfPublication80e4e74d-bf34-4a71-8530-cc3280543b65
relation.isAuthorOfPublication.latestForDiscovery80e4e74d-bf34-4a71-8530-cc3280543b65
relation.isProjectOfPublication8729af9d-d073-49fe-b1ba-11bd63ab7a14
relation.isProjectOfPublication.latestForDiscovery8729af9d-d073-49fe-b1ba-11bd63ab7a14

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