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2019-05-20 - Colloque/Présentation - communication orale - Anglais - page(s)

Wells Mathilde , Van Koninckxloo-Van Bever Aurore, Hambye Stéphanie , Blankert Bertrand , "Extraction and characterization of potential new antimalarial compounds from toad venom" in 20th Forum of Pharmaceutical Sciences, Brussels, Belgium, 2019

  • Codes CREF : Analyse et contrôle pharmaceutique (DI3450), Chimie analytique (DI1314), Sciences pharmaceutiques (DI3400)
  • 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 2017, the World Health Organization reported more 219 million cases and 435.000 deaths. With 87 countries affected, it is estimated that more than 800 million people are at risk of infection. The emergence and transmission of resistances to most antimalarial drugs are a real worry. Thus, the need for new therapeutic candidates represents an absolute necessity [1]. In more recent years, animals’ venoms and secretions have sparked a growing interest in scientists. In fact, toad venoms constitute a rich source of molecules, mainly bufadienolides, with many potential therapeutic activities [2]. The objective of this on-going project is to develop a bioguided fractionation process and the subsequent discovery of new drug candidates against malaria from toad venom. Raw extract characterization: The extraction process from the air-dried gland secretions of Rhinella marina consists of a ultrasonication-assisted solvent extraction. Up till now, three different solvents have been tested: methanol, ethyl acetate and a methanol/ethyl acetate mixture (1:1). The venom composition is subject to variabilities between batches depending on the animal’s habitat and its diet primarily. After each extraction, the raw extracts are analyzed by LC-MS to have an overview of the compounds present in the sample. Fractionation process: For this step, flash chromatography is considered as a first approach to obtain rough fractions that will be analyzed by LC-MS and then studied biologically. Flash chromatography offers a fast and simple separation process that can be applied to complex natural products. Biological activity: Each raw extract and the subsequently obtained fractions are tested for their antiplasmodial activity (3D7 strain) using the pLDH assay and the microscopic evaluation. Their cytotoxicity is also assessed on human cell lines (HeLa). The samples that display an antiplasmodial activity will be further analyzed (LC-MS) and structurally characterized by 1H-NMR. References [1] WHO World Malaria Report, 2018. [2] Rodriguez, C., et al., Toxins and pharmacologically active compounds from species of the family Bufonidae (Amphibia, Anura), Journal of Ethnopharmacology, 2017 (198), 235 – 254.