ChloroquineV1, Ncbi, Merge, bibRecord, 000261

In vitro and in vivo antischistosomal activity of ferroquine derivatives.

Identifieur interne : 000261 ( Ncbi/Merge ); précédent : 000260; suivant : 000262

In vitro and in vivo antischistosomal activity of ferroquine derivatives.

Auteurs : Jennifer Keiser [Suisse] ; Mireille Vargas ; Riccardo Rubbiani ; Gilles Gasser ; Christophe Biot

Source :

Parasites & vectors [ 1756-3305 ] ; 2014.

RBID : pubmed:25190030

Descripteurs français

KwdFr :
- Aminoquinoléines (), Aminoquinoléines (pharmacologie), Animaux, Cellules HeLa, Composés du fer II (), Composés du fer II (pharmacologie), Femelle, Humains, Schistosoma mansoni (), Schistosomiase à Schistosoma mansoni (traitement médicamenteux), Schistosomicides (pharmacologie), Souris, Structure moléculaire.
MESH :
- pharmacologie : Aminoquinoléines, Composés du fer II, Schistosomicides.
- traitement médicamenteux : Schistosomiase à Schistosoma mansoni.
- Aminoquinoléines, Animaux, Cellules HeLa, Composés du fer II, Femelle, Humains, Schistosoma mansoni, Souris, Structure moléculaire.

English descriptors

KwdEn :
- Aminoquinolines (chemistry), Aminoquinolines (pharmacology), Animals, Female, Ferrous Compounds (chemistry), Ferrous Compounds (pharmacology), HeLa Cells, Humans, Metallocenes, Mice, Molecular Structure, Schistosoma mansoni (drug effects), Schistosomiasis mansoni (drug therapy), Schistosomicides (pharmacology).
MESH :
- chemical , chemistry : Aminoquinolines, Ferrous Compounds.
- chemical , pharmacology : Aminoquinolines, Ferrous Compounds, Schistosomicides.
- drug effects : Schistosoma mansoni.
- drug therapy : Schistosomiasis mansoni.
- Animals, Female, HeLa Cells, Humans, Metallocenes, Mice, Molecular Structure.

Abstract

Schistosomiasis is a neglected tropical disease and drug-repurposing is a useful strategy to fill its exhausted drug development pipeline. The ferrocenyl analogue of chloroquine, ferroquine, is an antimalarial in late-stage drug development. The aim of the present work was to study the antischistosomal activity of ferroquine against Schistosoma mansoni adult worms and newly transformed schistosomula (NTS) in vitro and in vivo. Hydroxyl-ferroquine and ruthenoquine were included to study the potential role of reactive oxygen species in the antischistosomal activity. Chloroquine and mefloquine, the later described for its antischistosomal properties, served as comparators.

DOI: 10.1186/1756-3305-7-424
PubMed: 25190030

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pubmed:25190030

Le document en format XML

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<term>Female</term>
<term>Ferrous Compounds (chemistry)</term>
<term>Ferrous Compounds (pharmacology)</term>
<term>HeLa Cells</term>
<term>Humans</term>
<term>Metallocenes</term>
<term>Mice</term>
<term>Molecular Structure</term>
<term>Schistosoma mansoni (drug effects)</term>
<term>Schistosomiasis mansoni (drug therapy)</term>
<term>Schistosomicides (pharmacology)</term>
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<keywords scheme="KwdFr" xml:lang="fr"><term>Aminoquinoléines ()</term>
<term>Aminoquinoléines (pharmacologie)</term>
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<term>Cellules HeLa</term>
<term>Composés du fer II ()</term>
<term>Composés du fer II (pharmacologie)</term>
<term>Femelle</term>
<term>Humains</term>
<term>Schistosoma mansoni ()</term>
<term>Schistosomiase à Schistosoma mansoni (traitement médicamenteux)</term>
<term>Schistosomicides (pharmacologie)</term>
<term>Souris</term>
<term>Structure moléculaire</term>
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<front><div type="abstract" xml:lang="en">Schistosomiasis is a neglected tropical disease and drug-repurposing is a useful strategy to fill its exhausted drug development pipeline. The ferrocenyl analogue of chloroquine, ferroquine, is an antimalarial in late-stage drug development. The aim of the present work was to study the antischistosomal activity of ferroquine against Schistosoma mansoni adult worms and newly transformed schistosomula (NTS) in vitro and in vivo. Hydroxyl-ferroquine and ruthenoquine were included to study the potential role of reactive oxygen species in the antischistosomal activity. Chloroquine and mefloquine, the later described for its antischistosomal properties, served as comparators.</div>
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<DateCompleted><Year>2015</Year>
<Month>04</Month>
<Day>15</Day>
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<DateRevised><Year>2019</Year>
<Month>12</Month>
<Day>10</Day>
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<Article PubModel="Electronic"><Journal><ISSN IssnType="Electronic">1756-3305</ISSN>
<JournalIssue CitedMedium="Internet"><Volume>7</Volume>
<PubDate><Year>2014</Year>
<Month>Sep</Month>
<Day>04</Day>
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<Title>Parasites & vectors</Title>
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<ArticleTitle>In vitro and in vivo antischistosomal activity of ferroquine derivatives.</ArticleTitle>
<Pagination><MedlinePgn>424</MedlinePgn>
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<Abstract><AbstractText Label="BACKGROUND" NlmCategory="BACKGROUND">Schistosomiasis is a neglected tropical disease and drug-repurposing is a useful strategy to fill its exhausted drug development pipeline. The ferrocenyl analogue of chloroquine, ferroquine, is an antimalarial in late-stage drug development. The aim of the present work was to study the antischistosomal activity of ferroquine against Schistosoma mansoni adult worms and newly transformed schistosomula (NTS) in vitro and in vivo. Hydroxyl-ferroquine and ruthenoquine were included to study the potential role of reactive oxygen species in the antischistosomal activity. Chloroquine and mefloquine, the later described for its antischistosomal properties, served as comparators.</AbstractText>
<AbstractText Label="FINDINGS" NlmCategory="RESULTS">All metal complexes were shown to be moderately cytotoxic on human cervix HeLa cancer cells and human fetal lung fibroblasts MRC-5. 72 hours post-incubation NTS exposed to 33.3 µM ruthenoquine had died, while ferroquine and hydroxyl-ferroquine treated worms were strongly affected. No activity was observed treating NTS with chloroquine at 33.3 µM. Incubation of adult S. mansoni with 33.3 µM of the organometallic derivatives were highly affected in viability but were still alive 72 hours post-incubation. Mefloquine showed the highest activity against NTS and adult S. mansoni. Low total worm burden reductions of 0-36% were observed following oral administration of 200-800 mg/kg of the ferroquine derivatives to S. mansoni-infected mice.</AbstractText>
<AbstractText Label="CONCLUSIONS" NlmCategory="CONCLUSIONS">The organometallic compounds evaluated in this study revealed moderate in vitro activity against both larval and adult stages of S. mansoni but low in vivo activity. No correlation can be drawn between the antimalarial and antischistosomal activity of chloroquine analogues and oxidative shock does not seem to play a role in the activity of these compounds against S. mansoni.</AbstractText>
</Abstract>
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<ForeName>Jennifer</ForeName>
<Initials>J</Initials>
<AffiliationInfo><Affiliation>Department of Medical Parasitology and Infection Biology, Swiss Tropical and Public Health Institute, Basel, Switzerland. jennifer.keiser@unibas.ch.</Affiliation>
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<ForeName>Mireille</ForeName>
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<ForeName>Riccardo</ForeName>
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<ForeName>Christophe</ForeName>
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	Serveur d'exploration Chloroquine
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Serveur d'exploration Chloroquine

In vitro and in vivo antischistosomal activity of ferroquine derivatives.

In vitro and in vivo antischistosomal activity of ferroquine derivatives.

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