A5033068243- Malaria Research and Control
- Traditional and Medicinal Uses of Annonaceae
- Synthesis and biological activity
- Synthesis and Catalytic Reactions
- Research on Leishmaniasis Studies
- Synthesis and Biological Evaluation
- Trypanosoma species research and implications
- Alkaloids: synthesis and pharmacology
- Phenothiazines and Benzothiazines Synthesis and Activities
- Mosquito-borne diseases and control
- Computational Drug Discovery Methods
- HIV/AIDS drug development and treatment
- X-ray Diffraction in Crystallography
- Phytochemistry and Biological Activities
- Crystallization and Solubility Studies
- Natural product bioactivities and synthesis
- Ferrocene Chemistry and Applications
- Click Chemistry and Applications
- Endoplasmic Reticulum Stress and Disease
- Marine Sponges and Natural Products
- Essential Oils and Antimicrobial Activity
- Chemical synthesis and alkaloids
- Chemical Synthesis and Analysis
- Plant biochemistry and biosynthesis
- Microbial Natural Products and Biosynthesis
Centre National de la Recherche Scientifique
2015-2025
Muséum national d'Histoire naturelle
2007-2025
Molécules de Communication et Adaptation des Micro-organismes
2013-2023
Sorbonne Université
1993-2022
Université Paris Cité
2015
Evolution des Régulations Endocriniennes
2004-2014
Institut Pasteur de Lille
2000-2008
Université de Lille
2000-2005
Institut de Biologie de Lille
2000-2003
Institut de Biologie Physico-Chimique
1993-1996
Forty bis(9-amino-6-chloro-2-methoxyacridines), in which acridine moieties are joined by alkanediamines, polyamines, or polyamines substituted a side chain, were synthesized and tested for their vitro activity upon the erythrocytic stage of Plasmodium falciparum, trypomastigote Trypanosoma brucei, amastigote cruzi Leishmania infantum as well cytotoxic effects MRC-5 cells. Results clearly showed importance nature linker its chain antiparasitic activity, cytotoxicity, cellular localization....
Three series of monoquinolines consisting a 1,4-bis(3-aminopropyl)piperazine linker and large variety terminal groups were synthesized. Our aim was to prove that in related bisquinoline, it is the second quinoline moiety responsible for cytotoxicity not an absolute requirement overcoming resistance chloroquine (CQ). Eleven compounds displayed higher selectivity index (ratio CC50/IC50 activity) than CQ, one them cured mice infected by Plasmodium berghei.
The biological activities of essential oils from three plants grown in Cameroon: Ocimum basilicum, canum, and Cymbopogon citratus were tested against Plasmodium falciparum mature-stage larvae Anopheles funestus. Gas chromatography gas - mass spectrometry analyses showed that the main compounds are geranial, 1,8-cineole linalool C. citratus, O. canum respectively. Larvicidal tests carried out according to protocol recommended by World Health Organization oil leaves is most active An. funestus...
Three new monoterpene indole alkaloids (1-3) have been isolated from the bark of Geissospermum laeve, together with known (-)-leuconolam (4), geissolosimine (5), and geissospermine (6). The structures 1-3 were elucidated by analysis their HRMS NMR spectroscopic data. absolute configuration geissolaevine (1) was deduced comparison experimental theoretically calculated ECD spectra. isolation workflow guided a molecular networking-based dereplication strategy using an in-house database...
Flagella are important for eukaryote cell motility, including in sperm, and vital life cycle progression of many unicellular eukaryotic pathogens. The "9+2" axoneme most motile flagella comprises nine outer doublet two central-pair singlet microtubules. T-shaped radial spokes protrude from the doublets towards central pair necessary effective beating. We asked if there were spoke adaptations associated with parasite lineage-specific properties apicomplexans trypanosomatids. Following an...
Radioiodinated recombinant human interleukin DA (HILDA)/leukemia inhibitory factor (LIF) purified from conditioned medium of Chinese hamster ovary transfected cells enabled the identification specific receptor sites on a variety cell types. Using low concentrations (up to 500 pM) ligand iodinated at high radioactivity, affinity receptors (equilibrium dissociation constant Kd in range 30-100 were first demonstrated. They expressed levels by peripheral blood monocytes but not lymphocytes, NK...
Abstract The increasing resistance of Plasmodium falciparum to the most commonly used antimalarial drugs makes it necessary identify new therapeutic targets. telomeres parasite could constitute an attractive target. They are composed repetitions a degenerate motif ( 5′ GGGTTYA 3′ , where Y is T or C), different from human one GGGTTA ). In this report we investigate possibility targeting with G‐quadruplex ligands. Through solution hybridisation assays provide evidence existence telomeric...
Spilanthes spp. are used as traditional herbal medicines in Africa and India to treat malaria. Yet, date, there no data on the active constituents or most effective extraction methods for this indication. The isolated alkylamides, spilanthol undeca‐2 E ‐ene‐8,10‐diynoic acid isobutylamide, found S. acmella Murr., were shown have IC 50 s of 16.5 μg/mL 41.4 Plasmodium falciparum strain PFB 5.8 16.3 chloroquine resistant P. K1 strain, respectively. Further investigations revealed that at...
The synthesis and antiplasmodial evaluation of new hybrids combining the pharmacophore structures artemisinin, ciprofloxacin or norfloxacin, 7-chloroquinoline are reported in this study. first step for all syntheses is obtainment key piperazine esters intermediates bearing drugs norfloxacin. Using these platforms, 18 final compounds were synthesized through a multistep procedure with overall yields ranging between 8 20%. All screened their activity against chloroquine-resistant Plasmodium...
Piptadenia pervillei Vatke (Fabaceae) was selected from a screening programme devoted to the search of naturally-occuring antimalarial compounds plants Madagascar. Bioassay-guided fractionation ethyl acetate extract leaves led isolation four phenolic compounds, (+)-catechin (1), 5-gallate (2), 3-gallate (3) and gallate (4). Structures were determined by NMR mass spectroscopy. Compounds 2 3 displayed highest in vitro activity against chloroquine-resistant strain FcB1 Plasmodium falciparum...
Plasmodium falciparum M1 family aminopeptidase is currently considered as a promising target for anti-malarial chemotherapy. Several series of inhibitors developed by various research groups display IC50/Ki values down to nM range on native PfA-M1 or recombinant forms and block the parasite development in culture at µM sub-µM concentrations. A handful these has been tested murine models malaria shown anti plasmodial vivo activity. However, most do also other neutral malarial aminopeptidase,...
Theionbrunonines A and B (1 2), the first examples of monoterpene bisindole alkaloids linked by a thioether bridge, were isolated from stems Mostuea brunonis, guided molecular networking-based dereplication strategy. Their structures elucidated combination spectroscopic data ECD calculations. plausible biosynthetic pathway for 1 2 was postulated. 2) showed moderate antiplasmodial activities in micromolar range against strain FcB1 Plasmodium falciparum no cytotoxic activity MRC-5 cell line at 20 μM.
Five new monoterpene indole alkaloids (1–5), including four serpentinine-related bisindoles and one alstonine derivative monomer, have been isolated from the aerial parts of Picralima nitida. Their structures were elucidated by analysis their HRMS NMR spectroscopic data, absolute configurations deduced comparison experimental simulated ECD spectra. In addition, two known compounds (6 7), previously undescribed P. nitida, also purified. The compound isolation workflow was guided a molecular...
A series of novel hybrids artemisinin (ART) with either a phytormone endoperoxide G factor analogue (GMeP) or chloroquine (CQ) and conjugates the same compounds polyamines (PAs), spermidine (Spd), homospermidine (Hsd) were synthesized their antiplasmodial activity was evaluated using CQ-resistant P. falciparum FcB1/Colombia strain. The ART-GMeP hybrid 5 9 10 which are Spd Hsd two molecules ART one molecule GMeP, most potent IC50 values 2.6, 8.4, 10.6 nM, respectively. also presented highest...
Abstract Background and objectives: Blood transfusions can transmit parasitic infections, such as those caused by Plasmodium (malaria), Trypanosoma cruzi (Chagas' disease), Babesia (babesiosis). A higher degree of blood transfusion safety would be reached if methods were available for inactivating parasites. Materials methods: We evaluated the effectiveness photosensitization using lipophilic pheophorbide red light illumination to eradicate cells infected with falciparum, divergens, in whole...
The diversity of the cultivable microbiota marine sponge Phorbas tenacior frequently found in Mediterranean Sea was investigated, and its potential as a source antimicrobial, antioxidant antiplasmodial compounds evaluated. bacterial community studied by isolation, cultivation 16S rRNA gene sequencing. Twenty-three strains were isolated identified Proteobacteria (α or γ classes) Actinobacteria phyla. Furthermore, three different morphotypes localized extracellularly within tissues revealed...