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Biodereplication approach for antimalarial drugs in complex extracts mixtures: active compounds from the insect Pyrrhocoris apterus

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dc.contributor.author Vasquez-Ocmin, P es_PE
dc.contributor.author Suyyagh-Albouz, S es_PE
dc.contributor.author Cojean, S es_PE
dc.contributor.author Beniddir, M es_PE
dc.contributor.author Loiseau, P es_PE
dc.contributor.author Figadere, B es_PE
dc.contributor.author Maciuk, A es_PE
dc.date.accessioned 2024-05-30T23:13:38Z
dc.date.available 2024-05-30T23:13:38Z
dc.date.issued 2016
dc.description Consejo Nacional de Ciencia y Tecnología (CONCYTEC) is acknowledged for PhD funding of Pedro Vásquez-Ocmín; Karine Leblanc for supporting in MS analyses.
dc.description.abstract Malaria remains the most important global public health problem, with an estimated 214 million cases and 438 000 deaths in 2015, principally under 5-years old children [1]. Antimalarial drugs resistance permanent rising calls for new active molecules research against Plasmodium. The principal antimalarial drugs mechanism consists in interrupted heme crystallization in parasite erythrocytic phase, perturbating his waste-sorting strategy [2]. With a target-based approach, we developed a method which identifies heme-active molecule adduct in a complex extract (m/z for heme = 616) by mass spectroscopy (Q-TOF MS). This in vitro miniaturized biodereplication is based on a medium mimicking the parasite digestive vacuole (pH = 4.8) [3]. Application of the method was realized on a methanolic extract of Pyrrhocoris apterus insect (Pyrrhocoridae) (IC50 of extract = 80 ng/mL, Plasmodium falciparum 3D7 chloroquine-sensible strain). Active compounds were identified by m/z adduct (X + 616) using molecular networking4. Successive fractionation of active fractions was performed by several chromatography methods and structural identification was performed by 600 MHz NMR.
dc.description.sponsorship Consejo Nacional de Ciencia, Tecnología e Innovación Tecnológica - Concytec
dc.identifier.doi https://doi.org/10.1055/s-0036-1596283
dc.identifier.isi 411789300107
dc.identifier.uri https://hdl.handle.net/20.500.12390/1025
dc.language.iso eng
dc.publisher Thieme
dc.rights info:eu-repo/semantics/openAccess
dc.subject https://purl.org/pe-repo/ocde/ford#3.01.05
dc.subject.ocde https://purl.org/pe-repo/ocde/ford#3.01.05
dc.title Biodereplication approach for antimalarial drugs in complex extracts mixtures: active compounds from the insect Pyrrhocoris apterus
dc.type info:eu-repo/semantics/conferenceObject
dspace.entity.type Publication
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