Reference : Heparin-Coated Liposomes Improve Antiplasmodial Activity and Reduce the Toxicity of P...
Scientific journals : Article
Human health sciences : Pharmacy, pharmacology & toxicology
http://hdl.handle.net/2268/248988
Heparin-Coated Liposomes Improve Antiplasmodial Activity and Reduce the Toxicity of Poupartone B
English
Ledoux, Allison mailto [Université de Liège - ULiège > Département de pharmacie > Pharmacognosie >]
Coelho Cristino Mamede, Lucia Cristina mailto [Université de Liège - ULiège > Département de pharmacie > Pharmacognosie >]
Palazzo, Claudio [University of Liege > Pharmacy > Laboratory of Pharmaceutical Technology and Biopharmacy > >]
Furst, Tania [University of Liege > Pharmacy > Laboratory of Pharmaceutical Technology and Biopharmacy > >]
Jansen, Olivia mailto [Université de Liège - ULiège > Département de pharmacie > Pharmacognosie >]
De Tullio, Pascal mailto [Université de Liège - ULiège > Département de pharmacie > Chimie pharmaceutique >]
Kagisha, Vedaste mailto [Université de Liège - ULiège > > CIRM >]
Pendeville-Samain, Hélène mailto [Université de Liège - ULiège > > Platform Zebrafish facility & transgenics >]
Fillet, Marianne mailto [Université de Liège - ULiège > Département de pharmacie > Analyse des médicaments >]
Piel, Géraldine mailto [Université de Liège - ULiège > Département de pharmacie > Développement de nanomédicaments >]
Frederich, Michel mailto [Université de Liège - ULiège > Département de pharmacie > Pharmacognosie >]
18-May-2020
Planta Medica International Open
thieme
7
e
73–80
Yes (verified by ORBi)
International
2509-6656
New York
USA
[en] poupartone ; Malaria ; Poupartia borbonica
[en] Poupartone B is an alkyl cyclohexenone derivative isolated from Poupartia borbonica. This compound demonstrated promising antimalarial activity (IC50 < 1 μg/mL), however, it was not de- void of toxicity. Thus, to reduce the adverse side effects of this natural bioactive molecule, a delivery strategy involving a na- nostructure was formulated. Additionally, poupartone B-load- ed liposomes were coated with heparin, a glycosaminoglycan that is known to target proteins on the surface of Plasmodium falciparum-infected red blood cells. The quantification of the compound in the formulation was performed by HPLC-DAD, while heparin was quantitated by 1H NMR spectroscopy. The liposomes’ antiplasmodial activity was tested on artemisinin- resistant P. falciparum isolate, and toxicity was evaluated on human HeLa cells and zebrafish embryos. Throughout this re- search, the formulation demonstrated higher antiplasmodial activities against both P. falciparum strains and a significant decrease of in vitro toxicity. The formulation improved the se- lectivity index 2 times in vitro and proved to be 3 times less toxic than the compound alone in the zebrafish embryo acute toxicity test. Hence, the use of this strategy to deliver natural products in Plasmodium-infected cells, particularly those with a narrow therapeutic margin, is proposed.
Center of Interdisciplinary Research on Medicines
Researchers
http://hdl.handle.net/2268/248988
10.1055/a-1158-0569
Open access
NA

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