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https://hdl.handle.net/20.500.12955/1975
Título : | Biodereplication of antiplasmodial extracts: application of the amazonian medicinal plant piper coruscans kunth |
Autor : | Vásquez Ocmín, Pedro Gallard, Jean François Van Baelen, Anne Cécile Leblane, Karine Cojean, Sandrine Mouray, Elisabeth Grellier, Philippe Amasifuen Guerra, Carlos Alberto Beniddir, Mehdi A. Evanno, Laurent Figadère, Bruno Maciuk, Alexandre |
Fecha de publicación : | 7-nov-2022 |
Publicado en: | Molecules |
Resumen : | Improved methodological tools to hasten antimalarial drug discovery remain of interest, especially when considering natural products as a source of drug candidates. We propose a biodereplication method combining the classical dereplication approach with the early detection of potential antiplasmodial compounds in crude extracts. Heme binding is used as a surrogate of the antiplasmodial activity and is monitored by mass spectrometry in a biomimetic assay. Molecular networking and automated annotation of targeted mass through data mining were followed by mass-guided compound isolation by taking advantage of the versatility and finely tunable selectivity offered by centrifugal partition chromatography. This biodereplication workflow was applied to an ethanolic extract of the Amazonian medicinal plant Piper coruscans Kunth (Piperaceae) showing an IC50 of 1.36 ug/mL on the 3D7 Plasmodium falciparum strain. It resulted in the isolation of twelve compounds designated as potential antiplasmodial compounds by the biodereplication workflow. Two chalcones, aurentiacin (1) and cardamonin (3), with IC50 values of 2.25 and 5.5 uM, respectively, can be considered to bear the antiplasmodial activity of the extract, with the latter not relying on a heme-binding mechanism. This biodereplication method constitutes a rapid, efficient, and robust technique to identify potential antimalarial compounds in complex extracts such as plant extracts. |
Palabras clave : | Piper coruscans Kunth (Piperaceae) Biodereplication Heme binding Mass Spectrometry Plasmodium |
metadata.dc.subject.agrovoc: | Piperaceae Replication Spectrometry Plasmodium |
Editorial : | MDPI |
Citación : | Vásquez, P.; Gallard, J.; Van Baelen, A.; Leblanc, K.; Cojean, S.; Mouray, E.; Grellier, P.; Guerra, C.; Beniddir, M.; Evanno, L.; et al. Biodereplication of antiplasmodial extracts: application of the amazonian medicinal plant piper coruscans kunth. Molecules 2022, 27, 7638. doi: 10.3390/molecules27217638 |
URI : | https://hdl.handle.net/20.500.12955/1975 |
metadata.dc.identifier.doi: | https://doi.org/10.3390/molecules27217638 |
ISSN : | 1420-3049 |
metadata.dc.subject.ocde: | https://purl.org/pe-repo/ocde/ford#4.05.00 |
Aparece en las colecciones: | Artículos científicos |
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Vásquez-et-al_2022_Medicinal_Plants.pdf | 3,01 MB | Adobe PDF | Visualizar/Abrir |
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