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2020-09-17 - Colloque/Présentation - communication orale - Anglais - 22 page(s)

Wells Mathilde , Hambye Stéphanie , Blankert Bertrand , "Discovery strategies for novel antiplasmodial compounds from the venom of Bufo toads" in Venoms and Toxins, Oxford, Royaume-uni, 2020

  • Codes CREF : Analyse et contrôle pharmaceutique (DI3450), Chimie analytique (DI1314), Sciences pharmaceutiques (DI3400), Techniques séparatives (DI2729)
  • Unités de recherche UMONS : Analyse pharmaceutique (M130)
  • Instituts UMONS : Institut des Sciences et Technologies de la Santé (Santé)

Abstract(s) :

(Anglais) Malaria remains a major concern for health organizations around the world. In 2018, the World Health Organization reported more than 228 million cases and 405.000 deaths. With more than 80 countries affected, approximately 3 billion people are at risk of infection. The emergence and transmission of resistances to most antimalarial drugs are a real worry. The need for new therapeutic candidates represents an absolute necessity. In more recent years, animal venoms and secretions have sparked a growing interest for scientists. In fact, toad venoms constitute a rich source of molecules with many potential therapeutic activities. The goal of this work is to develop a bio-guided fractionation process and the subsequent discovery of new drug candidates against malaria from toad venom. Several Bufo species are considered during this work. Three species are currently being studied: Rhinella marina, Bufo bufo and Incillius alvarius. The extraction process from the air-dried venom is based on a four-solvent system assisted by sonication. After each extraction, the crude extracts are analyzed by TLC and LC-MS to obtain a chemical profile. For the fractionation step, flash chromatography is considered as a first approach to obtain rough fractions that will also be characterized and then biologically studied. In the first fractionation round, 3 to 4 fractions are obtained. The following step will consist in producing subfractions of the fractions displaying interesting therapeutic properties. For this purpose, further preparative techniques will be considered such as flash chromatography and semi-preparative LC. Each crude extract and the subsequently obtained fractions are tested for their antiplasmodial activity (3D7 and W2 strains) using the SYBR-Green I assay and microscopy. Their cytotoxicities are also assessed on a panel of human cell lines. The samples that display antiplasmodial activities will be further analyzed and structurally characterized by MS and NMR.


Mots-clés :
  • (Anglais) toad
  • (Anglais) venom
  • (Anglais) malaria