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New findings on Simalikalactone D, an antimalarial compound from Quassia amara L. (Simaroubaceae)

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dc.contributor.author Bertani, S.
dc.contributor.author Houël, E.
dc.contributor.author Jullian, V.
dc.contributor.author Bourdy, G.
dc.contributor.author Valentin, A.
dc.contributor.author Stien, D.
dc.contributor.author Deharo, E.
dc.date.accessioned 2022-01-18T19:26:46Z
dc.date.available 2022-01-18T19:26:46Z
dc.date.issued 2012
dc.identifier.uri https://hdl.handle.net/20.500.12866/10856
dc.description.abstract Quassia amara L. (Simaroubaceae) is a species widely used as tonic and is claimed to be an efficient antimalarial all over the Northern part of the Amazon basin. Quassinoid compound Simalikalactone D (SkD) has been shown to be one of the molecules responsible for the antiplasmodial activity of a watery preparation made out of juvenile fresh leaves of this plant. Because of its strong antimalarial activity, we decided to have a further insight of SkD pharmacological properties, alone or in association with classical antimalarials. At concentrations of up to 200 μM, we showed herein that SkD did not exert any apoptotic or necrotic activities in vitro on lymphoblastic cells. However, an antiproliferative effect was evident at concentrations higher than 45. nM. SkD was inefficient at inhibiting heme biomineralization and the new permeability pathways induced by the parasite in the host erythrocyte membrane. With respect to Plasmodium falciparum erythrocytic stages, SkD was almost inactive on earlier and later parasite stages, but potently active at the 30th h of parasite cycle when DNA replicates in mature trophozoites. In vitro combination studies with conventional antimalarial drugs showed that SkD synergizes with atovaquone (ATO). The activity of ATO on the Plasmodium mitochondrial membrane potential was enhanced by SkD, which on its own had a poor effect on this cellular parameter. en_US
dc.language.iso eng
dc.publisher Elsevier
dc.relation.ispartofseries Experimental Parasitology
dc.rights info:eu-repo/semantics/restrictedAccess
dc.rights.uri https://creativecommons.org/licenses/by-nc-nd/4.0/deed.es
dc.subject Humans en_US
dc.subject article en_US
dc.subject controlled study en_US
dc.subject in vitro study en_US
dc.subject non|priority journal en_US
dc.subject Plasmodium en_US
dc.subject unclassified drug en_US
dc.subject Plasmodium falciparum en_US
dc.subject antimalarial agent en_US
dc.subject chloroquine en_US
dc.subject Cell Line en_US
dc.subject doxycycline en_US
dc.subject Antimalarials en_US
dc.subject host parasite interaction en_US
dc.subject parasite development en_US
dc.subject protozoal DNA en_US
dc.subject monotherapy en_US
dc.subject developmental stage en_US
dc.subject Plant Extracts en_US
dc.subject trophozoite en_US
dc.subject artemether en_US
dc.subject Inhibitory Concentration 50 en_US
dc.subject amodiaquine en_US
dc.subject apoptosis en_US
dc.subject atovaquone en_US
dc.subject bruceantin en_US
dc.subject brusatol en_US
dc.subject cell death en_US
dc.subject cell membrane permeability en_US
dc.subject Cell Membrane Permeability en_US
dc.subject cycloguanil en_US
dc.subject DNA replication en_US
dc.subject erythrocyte membrane en_US
dc.subject Erythrocyte Membrane en_US
dc.subject Erythrocytes en_US
dc.subject lymphoblast en_US
dc.subject mefloquine en_US
dc.subject mitochondrial membrane potential en_US
dc.subject phytochemistry en_US
dc.subject Plant Leaves en_US
dc.subject plant medicinal product en_US
dc.subject Plasmodium yoelii en_US
dc.subject Quassia en_US
dc.subject quassia amara en_US
dc.subject Quassia amara en_US
dc.subject Quassinoid en_US
dc.subject Quassins en_US
dc.subject quinine en_US
dc.subject simalikalactone d en_US
dc.subject Simalikalactone d en_US
dc.subject Simaroubaceae en_US
dc.title New findings on Simalikalactone D, an antimalarial compound from Quassia amara L. (Simaroubaceae) en_US
dc.type info:eu-repo/semantics/article
dc.identifier.doi https://doi.org/10.1016/j.exppara.2012.02.013
dc.subject.ocde https://purl.org/pe-repo/ocde/ford#3.03.07
dc.relation.issn 1090-2449


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