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Leishmanicidal compounds and potent PPARγ activators from Renealmia thyrsoidea

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dc.contributor.author Cabanillas Amado, Billy Joel
dc.contributor.author Le Lamer, Anne-Cecile
dc.contributor.author Olagnier, David
dc.contributor.author Castillo Pareja, Denis Helan
dc.contributor.author Arévalo Zelada, Jorge Luis
dc.contributor.author Valadeau, Celine
dc.contributor.author Coste, Agnes
dc.contributor.author Pipy, Bernard
dc.contributor.author Bourdy, Genevieve
dc.contributor.author Sauvain, Michel Henri Auguste
dc.contributor.author Fabre, Nicolas
dc.date.accessioned 2020-06-10T18:12:13Z
dc.date.available 2020-06-10T18:12:13Z
dc.date.issued 2014
dc.identifier.uri https://hdl.handle.net/20.500.12866/8056
dc.description.abstract ETHNOPHARMACOLOGICAL RELEVANCE: Leaves and rhizomes of Renealmia thyrsoidea (Ruiz & Pav.) Poepp. & Endl. traditionally used in the Yanesha pharmacopoeia to treat skin infections such as leishmaniasis ulcers, or to reduce fever were chemically investigated to identify leishmanicidal compounds, as well as PPARgamma activators. METHODS: Compounds were isolated through a bioassay-guided fractionation and their structures were determined via detailed spectral analysis. The viability of Leishmania amazonensis axenic amastigotes was assessed by the reduction of tetrazolium salt (MTT), the cytotoxicity on macrophage was evaluated using trypan blue dye exclusion method, while the percentage of infected macrophages was determined microscopically in the intracellular macrophage-infected assay. The CD36, mannose receptor (MR) and dectin-1 mRNA expression on human monocytes-derived macrophages was evaluated by quantitative real-time PCR. RESULTS: Six sesquiterpenes (1-6), one dihydrobenzofuranone (7) and four flavonoids (8-11) were isolated from the leaves. Alongside, two flavonoids (12-13) and five diarylheptanoids (14-18) were identified in the rhizomes. Leishmanicidal activity against Leishmania amazonensis axenic amastigotes was evaluated for all compounds. Compounds 6, 7, and 11, isolated from the leaves, showed to be the most active derivatives. Diarylheptanoids 14-18 were also screened for their ability to activate PPARgamma nuclear receptor in macrophages. Compounds 17 and 18 bearing a Michael acceptor moiety strongly increased the expression of PPARgamma target genes such as CD36, Dectin-1 and mannose receptor (MR), thus revealing interesting immunomodulatory properties. CONCLUSIONS: Phytochemical investigation of Renealmia thyrsoidea has led to the isolation of leishmanicidal compounds from the leaves and potent PPARgamma activators from the rhizomes. These results are in agreement with the traditional uses of the different parts of Renealmia thyrsoidea. en_US
dc.language.iso eng
dc.publisher Elsevier
dc.relation.ispartofseries Journal of Ethnopharmacology
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 Antiprotozoal Agents/isolation & purification/pharmacology en_US
dc.subject Humans en_US
dc.subject Leishmania mexicana/drug effects en_US
dc.subject Leishmanicidal activity en_US
dc.subject Macrophages/drug effects en_US
dc.subject Male en_US
dc.subject Medicinal plants en_US
dc.subject Medicine, Traditional en_US
dc.subject Mice en_US
dc.subject Mice, Inbred BALB C en_US
dc.subject Peru en_US
dc.subject Plant Extracts/pharmacology en_US
dc.subject Plant Leaves en_US
dc.subject PPAR gamma/drug effects/metabolism en_US
dc.subject PPARgamma en_US
dc.subject Real-Time Polymerase Chain Reaction en_US
dc.subject Renealmia thyrsoidea en_US
dc.subject Rhizome en_US
dc.subject Zingiberaceae en_US
dc.subject Zingiberaceae/chemistry en_US
dc.title Leishmanicidal compounds and potent PPARγ activators from Renealmia thyrsoidea en_US
dc.type info:eu-repo/semantics/article
dc.identifier.doi https://doi.org/10.1016/j.jep.2014.09.010
dc.subject.ocde https://purl.org/pe-repo/ocde/ford#3.01.05
dc.relation.issn 1872-7573


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