Search results for: Françoise Benoit‐Vical

Items from 1 to 15 out of 15 results

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Gold(I) complexes bearing phosphole ligands: Synthesis and antimalarial activity

Kévin Fourmy, Maryse Gouygou, Odile Dechy-Cabaret, Françoise Benoit-Vical

Comptes Rendus Chimie > 2017 > 20 > 4 > 333-338

A series of gold(I)-monophosphole complexes have been synthesized and characterized. The introduction of a nitrogen moiety in the complex structure was envisioned either by choosing the bis(trifluoromethanesulfonyl)imidate ligand as the X-ligand or by preparing a new pyrrolidinophosphole ligand as the L-ligand. All the complexes have been evaluated in vitro for their antimalarial activity. These gold–phosphole...

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Antiplasmodial activities of gold(I) complexes involving functionalized N-heterocyclic carbenes

Catherine Hemmert, Arba Pramundita Ramadani, Luca Boselli, Álvaro Fernández Álvarez, more

Bioorganic & Medicinal Chemistry > 2016 > 24 > 13 > 3075-3082

A series of twenty five molecules, including imidazolium salts functionalized by N-, O- or S-containing groups and their corresponding cationic, neutral or anionic gold(I) complexes were evaluated on Plasmodium falciparum in vitro and then on Vero cells to determine their selectivity. Among them, eight new compounds were synthesized and fully characterized by spectroscopic methods. The X-ray structures...

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Plasmodium falciparum: multifaceted resistance to artemisinins

Lucie Paloque, Arba P. Ramadani, Odile Mercereau-Puijalon, Jean-Michel Augereau, more

Malaria Journal > 2016 > 15 > 1 > 1-12

Plasmodium falciparum resistance to artemisinins, the most potent and fastest acting anti-malarials, threatens malaria elimination strategies. Artemisinin resistance is due to mutation of the PfK13 propeller domain and involves an unconventional mechanism based on a quiescence state leading to parasite recrudescence as soon as drug pressure is removed. The enhanced P. falciparum quiescence...

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Evaluation of antiplasmodial and antileishmanial activities of herbal medicine Pseudelephantopus spiralis (Less.) Cronquist and isolated hirsutinolide-type sesquiterpenoids

Cynthia Girardi, Nicolas Fabre, Lucie Paloque, Arba Pramundita Ramadani, more

Journal of Ethnopharmacology > 2015 > 170 > Complete > 167-174

Pseudelephantopus spiralis (Less.) Cronquist is distributed in the Caribbean, Mesoamerica and Latin America. Preparations of the plant are traditionally used in Latin America for the treatment of various diseases including fever, malaria, and spleen or liver inflammations.Aerial parts of P. spiralis were extracted with either ethanol or distilled water. Seven hirsutinolide-type sesquiterpenoids were...

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Influence of Amodiaquine on the Antimalarial Activity of Ellagic Acid: Crystallographic and Biological Studies

Ewa Żesławska, Barbara Oleksyn, Aude Fabre, Françoise Benoit‐Vical

Chemical Biology & Drug Design > 84 > 6 > 669 - 675

In the search for new antimalarial drugs, design of hybrid molecules is recommended to improve biological activity and to decrease the risk of parasite resistance development. Ellagic acid, as an inhibitor of Plasmodium glutathione, presents an original mode of action and thus appears as a promising antiplasmodial compound. A new complex (AQ–EA) consisting of the well‐known antimalarial drug, amodiaquine,...

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Synthesis, structures, and antimalarial activities of some silver(I), gold(I) and gold(III) complexes involving N-heterocyclic carbene ligands

Catherine Hemmert, Aymeric Fabié, Aude Fabre, Françoise Benoit-Vical, more

European Journal of Medicinal Chemistry > 2013 > 60 > C > 64-75

A series of mono-and dinuclear silver(I) and mononuclear gold(I) complexes containing bis(N-heterocyclic carbene) (NHC) or N-functionalized NHC ligands were synthesized and fully characterized by spectroscopic methods and, in some cases, by single crystal X-ray diffraction. The in vitro antiplasmodial and antifungal activities of a previously described family of N-functionalized bis(imidazolium) proligands...

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Indole and aminoimidazole moieties appear as key structural units in antiplasmodial molecules

Charlotte Passemar, Mariette Saléry, Patrice Njomnang Soh, Marie-Denise Linas, more

Phytomedicine > 2011 > 18 > 13 > 1118-1125

From a library of compounds of natural sources, a big series of molecules was chosen by random sampling to evaluate their in vitro antimalarial activity against Plasmodium falciparum and their antifungal activity against Candida sp. From 184 molecules tested, no molecules were active against Candida sp. (MIC>10μg/ml) whereas 13 clearly showed high antiplasmodial activity in vitro, with an IC ...

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Resistance to antimalarial compounds: Methods and applications

Benoit Witkowski, Antoine Berry, Françoise Benoit-Vical

Drug Resistance Updates > 2009 > 12 > 1-2 > 42-50

Considerable progress has been made in antimalarial research; however, much more effort is required to develop new antimalarials which overcome plasmodial resistance to clinically available drugs and limit the emergence of resistance. In particular, research must focus on understanding the mechanisms by which Plasmodium falciparum impedes the action of these drugs.In this review, we discuss the different...

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Pfs 16 pivotal role in Plasmodium falciparum gametocytogenesis: A potential antiplasmodial drug target

Antoine Berry, Caroline Deymier, Mathieu Sertorio, Benoît Witkowski, more

Experimental Parasitology > 2009 > 121 > 2 > 189-192

Mature gametocytes, the sexual stage of Plasmodium falciparum, ensure the continued transmission of malaria from the human host to the mosquito vector. Even if gametocytes are not implicated in the malaria physiopathology it is crucial to the spread of malaria. Gametocytes are to be a key target for drugs used against Plasmodium in public health. The expression levels of 4 sexual-stage specific genes,...

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Modifications of the chemical structure of terpenes in antiplasmodial and antifungal drug research

David Olagnier, Philippe Costes, Antoine Berry, Marie-Denise Linas, more

Bioorganic & Medicinal Chemistry Letters > 2007 > 17 > 22 > 6075-6078

Pure natural monoterpenes were evaluated in vitro for their antiplasmodial activities against Plasmodium falciparum. Chemically modified terpenes were also tested to see whether the introduction of an alkyne, a cyclopropane, a diene, or a cyclopentenone moiety had an influence on the biological activity. The IC ₅₀ obtained on a chloroquine-resistant strain of Plasmodium (FcM29-Cameroon) showed...

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Are West African plants a source of future antimalarial drugs?

Patrice Njomnang Soh, Françoise Benoit-Vical

Journal of Ethnopharmacology > 2007 > 114 > 2 > 130-140

Ethnopharmacology is a very interesting resource in which new therapies may be discovered. In the case of malaria, two major antimalarial drugs widely used today came originally from indigenous medical systems, that is quinine and artemisinin, from Peruvian and Chinese ancestral treatments, respectively. There is an urgent need for the discovery of new drugs due to the critical epidemiological situation...

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The key role of heme to trigger the antimalarial activity of trioxanes

Anne Robert, Françoise Benoit-Vical, Bernard Meunier

Coordination Chemistry Reviews > 2005 > 249 > 17-18 > 1927-1936

Artemisinin is an efficient antimalarial drug containing a 1,2,4-trioxane, which is able to alkylate heme both in vitro and in vivo, giving rise to covalent heme–artemisinin coupling products. The low valent iron(II) protoporphyrin-IX, which is the prosthetic group of hemoglobin, induces the homolysis of the peroxide bond of artemisinin by an inner-sphere electron transfer. The generated alkoxy radical...

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Pfcrt K76T mutation and its associations in imported Plasmodium falciparum malaria cases

Antoine Berry, Aurélia Vessière, Richard Fabre, Françoise Benoit-Vical, more

Infection, Genetics and Evolution > 2004 > 4 > 4 > 361-364

Over 3 years (1999-2002), 305 cases of falciparum malaria were diagnosed in Toulouse, France. After retrospective analysis, only 131 patients entered the study. The diagnosis of malaria was ensured by optical methods (QBC(TM) then thin smear examination), the results of which were checked from 1999 to mid-2001 by a conventional PCR method, replaced at that time by a real-time PCR using LightCycler(TM)...

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Antiplasmodial and antifungal activities of iridal, a plant triterpenoid

Françoise Benoit-Vical, Christine Imbert, Jean-Paul Bonfils, Yves Sauvaire

Phytochemistry > 2003 > 62 > 5 > 747-751

Iridal, a triterpenoidic compound extracted from Iris germanica L., was previously shown to have an interesting activity on two cultured human tumor cell lines (A2780 and K562). In the present work, this same product was tested in vitro on Plasmodium falciparum chloroquine-resistant and -sensitive strains, in vivo on P. vinckei, and on some Candida albicans and C. parapsilosis strains too. The IC...

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Antiplasmodial activity of plant extracts used in west African traditional medicine

Alexis Valentin, Mustofa, Françoise Benoit-Vical, Yves Pélissier, more

Journal of Ethnopharmacology > 2000 > 73 > 1-2 > 145 - 151

Five plants originating from Ivory Coast were selected after an ethnobotanical survey, Alchornea cordifolia, Mitragyna inermis, Nauclea diderrichii, Pterocarpus santalinoides, and Terminalia glaucescens. Traditional healers for the treatment of malaria commonly used these plants. Extracts of these plants were tested on three strains of Plasmodium falciparum, FcB1-Colombia and FcM29-Cameroon (chloroquine-resistant...

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