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In vitro and in vivo activity of benzocphenanthridines against Leishmania amazonensis

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dc.contributor.author Castillo, Denis
dc.contributor.author Sauvain, Michel
dc.contributor.author Rivaud, Marion
dc.contributor.author Jullian, Valerie
dc.date.accessioned 2020-06-10T18:12:14Z
dc.date.available 2020-06-10T18:12:14Z
dc.date.issued 2014
dc.identifier.uri https://hdl.handle.net/20.500.12866/8065
dc.description.abstract Seven benzo[c]phenanthridines, synthetic or isolated from Zanthoxylum rhoifolium root bark, were evaluated against Leishmania amazonensis axenic amastigotes. Five of them were considered leishmanicidal, with IC50 values ranging from 0.03 to 0.54 microM, and were evaluated on intramacrophagic amastigotes of L. amazonensis. Chelerythrine displayed the best activity (IC50=0.5 microM), which was in the same range as the reference compound amphotericin B (IC50=0.4 microM). In vivo studies with chelerythrine, avicine, and fagaridine on a model of mice cutaneous leishmaniasis resulted in the identification of fagaridine as the most active compound. Fagaridine decreased the parasitic burden more than 50% at the 3rd and 6th weeks after the end of treatment. en_US
dc.language.iso eng
dc.publisher Thieme Medical Publishers
dc.relation.ispartof urn:issn:1612-1805
dc.rights info:eu-repo/semantics/restrictedAccess
dc.rights.uri https://creativecommons.org/licenses/by-nc-nd/4.0/deed.es
dc.subject Animals en_US
dc.subject Benzophenanthridines/chemistry/isolation & purification/pharmacology en_US
dc.subject Cell Survival/drug effects en_US
dc.subject Disease Models, Animal en_US
dc.subject Female en_US
dc.subject Humans en_US
dc.subject Inhibitory Concentration 50 en_US
dc.subject Leishmania/drug effects en_US
dc.subject Leishmaniasis, Cutaneous/drug therapy/parasitology en_US
dc.subject Macrophages/drug effects en_US
dc.subject Mice en_US
dc.subject Mice, Inbred BALB C en_US
dc.subject Parasitic Sensitivity Tests en_US
dc.subject Phenanthridines/chemistry/isolation & purification/pharmacology en_US
dc.subject Plant Bark/chemistry en_US
dc.subject Plant Extracts/chemistry/isolation & purification/pharmacology en_US
dc.subject Plant Roots/chemistry en_US
dc.subject Plants, Medicinal en_US
dc.subject Zanthoxylum/chemistry en_US
dc.title In vitro and in vivo activity of benzocphenanthridines against Leishmania amazonensis en_US
dc.type info:eu-repo/semantics/article
dc.identifier.doi https://doi.org/10.1055/s-0034-1382826
dc.subject.ocde https://purl.org/pe-repo/ocde/ford#3.02.00 es_PE
dc.subject.ocde https://purl.org/pe-repo/ocde/ford#1.06.03
dc.subject.ocde https://purl.org/pe-repo/ocde/ford#1.04.01
dc.subject.ocde https://purl.org/pe-repo/ocde/ford#1.04.07
dc.subject.ocde https://purl.org/pe-repo/ocde/ford#3.01.05

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