In vitro and in vivo anthelmintic activity of (-)-6,6 '-dinitrohinokinin against schistosomula and juvenile and adult worms of Schistosoma mansoni

Página do item simplificado
dc.contributor.authorPereira, Ana C.
dc.contributor.authorSilva, Marcio L. A. e
dc.contributor.authorSouza, Julia Medeiros
dc.contributor.authorLaurentiz, Rosangela S. de [UNESP]
dc.contributor.authorRodrigues, Vanderlei
dc.contributor.authorJanuario, Ana H.
dc.contributor.authorPauletti, Patricia M.
dc.contributor.authorTavares, Denise C.
dc.contributor.authorDa Silva Filho, Ademar A.
dc.contributor.authorCunha, Wilson R.
dc.contributor.authorBastos, Jairo K.
dc.contributor.authorMagalhaes, Lizandra G.
dc.contributor.institutionUniv Franca
dc.contributor.institutionUniversidade Estadual Paulista (Unesp)
dc.contributor.institutionUniversidade de São Paulo (USP)
dc.contributor.institutionUniv Fed Juiz de Fora
dc.date.accessioned2018-11-26T16:16:29Z
dc.date.available2018-11-26T16:16:29Z
dc.date.issued2015-09-01
dc.description.abstractThe chemotherapy of schistosomiasis relies on the use of praziquantel. However, concerns over drug resistance have encouraged the search for new drug leads. This paper is the first report on the in vitro and in vivo activity of (-)-6,6'-dinitrohinokinin (DNK) against Schistosoma mansoni. In vitro, the lethal concentrations for 50% of parasites (LC50) of DNK against adult worms were 103.9 +/- 3.6 and 102.5 +/- 4.8 mu M at 24 and 72 h, respectively. Scanning electron microscopy images showed extensive tegumental alterations such as peeling and smaller numbers of tubercles in the spine of adult worms. DNK also elicited high mortality of schistosomula, with LC50 values of 57.4 +/- 2.3, 32.5 +/- 0.9, and 20.4 +/- 1.2 mu M at 24, 48, and 72 h, respectively. DNK displayed moderate activity against the juvenile liver parasite, with an LC50 value of 179.5 +/- 2.3 mu M at 72 h. This compound reduced the total number of eggs by over 83%, and it affected the development of eggs produced by adult worms. The selectivity index showed that at 24 h, DNK was 8.5 and 15.4 times more toxic to the adult worms and schistosomula than to Chinese hamster lung fibroblast cells, respectively. Treatment of infected mice with DNK moderately decreased worm burden (33.8-52.3%), egg production (40.7-60.0%), and spleen and liver weights. Together, our results indicated that DNK presents moderate in vitro and in vivo activities against S. mansoni, and it might therefore be interesting to explore the structure-activity relationship of the antischistosomal activity of this compound. (C) 2015 Elsevier B.V. All rights reserved.en
dc.description.affiliationUniv Franca, Nucleo Pesquisas Ciencias Exatas & Tecnol, BR-14404600 Franca, SP, Brazil
dc.description.affiliationUniv Estadual Paulista, Fac Engn Ilha Solteira, Dept Fis & Quim, BR-15385000 Ilha Solteira, SP, Brazil
dc.description.affiliationUniv Sao Paulo, Fac Med Ribeirao Preto, Dept Bioquim & Imunol, BR-14049900 Ribeirao Preto, SP, Brazil
dc.description.affiliationUniv Fed Juiz de Fora, Fac Farm Juiz de Fora, Dept Ciencias Farmaceut, BR-36036900 Juiz De Fora, MG, Brazil
dc.description.affiliationUniv Sao Paulo, Fac Farm Ribeirao Preto, Dept Ciencias Farmaceut, BR-14030000 Ribeirao Preto, SP, Brazil
dc.description.affiliationUnespUniv Estadual Paulista, Fac Engn Ilha Solteira, Dept Fis & Quim, BR-15385000 Ilha Solteira, SP, Brazil
dc.description.sponsorshipConselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)
dc.description.sponsorshipFundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)
dc.description.sponsorshipIdFAPESP: Process FAPESP: 1998/14956-7
dc.description.sponsorshipIdFAPESP: Process FAPESP: 2010/17378-8
dc.description.sponsorshipIdFAPESP: Process FAPESP: 2011/10179-2
dc.description.sponsorshipIdFAPESP: Process FAPESP: 2009/15207-4
dc.format.extent195-201
dc.identifierhttp://dx.doi.org/10.1016/j.actatropica.2015.06.005
dc.identifier.citationActa Tropica. Amsterdam: Elsevier Science Bv, v. 149, p. 195-201, 2015.
dc.identifier.doi10.1016/j.actatropica.2015.06.005
dc.identifier.fileWOS000359957500026.pdf
dc.identifier.issn0001-706X
dc.identifier.lattes7989837727910759
dc.identifier.orcid0000-0002-5240-4870
dc.identifier.urihttp://hdl.handle.net/11449/160730
dc.identifier.wosWOS:000359957500026
dc.language.isoeng
dc.publisherElsevier B.V.
dc.relation.ispartofActa Tropica
dc.rights.accessRightsAcesso aberto
dc.sourceWeb of Science
dc.subjectLignan
dc.subject(-)-6,6 '-Dinitrohinokinin
dc.subjectSchistosoma mansoni
dc.titleIn vitro and in vivo anthelmintic activity of (-)-6,6 '-dinitrohinokinin against schistosomula and juvenile and adult worms of Schistosoma mansonien
dc.typeArtigo
dcterms.licensehttp://www.elsevier.com/about/open-access/open-access-policies/article-posting-policy
dcterms.rightsHolderElsevier B.V.
unesp.author.lattes7989837727910759[4]
unesp.author.orcid0000-0002-5240-4870[4]

Arquivos

Pacote Original
Agora exibindo 1 - 1 de 1
Imagem de Miniatura
Nome:
WOS000359957500026.pdf
Tamanho:
654.09 KB
Formato:
Adobe Portable Document Format
Descrição:
Baixar

Coleções

Artigos - Física e Química - FEIS