Synthèse et évaluation de l'activité anti-Leishmania d'anthranoïdes issus du genre Psorospermum (Hypericaceae) utilisé en médecine traditionnelle camerounaise

Abstract : The study of plants belonging to the Psorospermum genus, led us to isolate several anthranoïd compounds, among which 9 vismiones, from an extract of P. glaberrimum bark. The latter have shown strong anti-Leishmania activity. In order to check if the anti-Leishmania activity of the extracts correlates with their vismiones content, a dosage of the vismiones in several organs of various Psorospermum species has been carried out using LC-FTMS. Organic synthesis work has allowed: 1) to obtain a wide variety of vismione analogues in order to better understand which structural subunit is responsible for the anti-Leishmania activity; 2) to synthesize an analogue showing an optimised activity as well as an enhanced stability compared to natural vismiones; 3) set up a route for the total synthesis of vismione, which has never been achieved yet. The anti-Leishmania activities of the synthesized analogues, as well as their cytotoxicity were evaluated. Finally, preliminary investigations on the mode of action of vismiones were carried out on a plant model which has a biosynthetic pathway essential for the survival of the parasite. These investigations led us to further study the intrinsic fluorescence properties of the vismiones, which potentially make them interesting tools as fluorescent probes.
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Nicolas Wasser. Synthèse et évaluation de l'activité anti-Leishmania d'anthranoïdes issus du genre Psorospermum (Hypericaceae) utilisé en médecine traditionnelle camerounaise. Chimie organique. Université de Strasbourg, 2018. Français. ⟨NNT : 2018STRAF055⟩. ⟨tel-02146020⟩

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