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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)
Heme binding
Mass Spectrometry
metadata.dc.subject.agrovoc: Piperaceae
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
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