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Repurposing Heparin as Antimalarial: Evaluation of Multiple Modifications Toward In Vivo Application

September 2, 2020 - 11:45 -- Open Access
Lantero E, Aláez-Versón CR, Romero P, Sierra T, Fernàndez-Busquets X
Pharmaceutics 2020, 12(9), 825

Heparin is a promising antimalarial drug due to its activity in inhibiting Plasmodium invasion of red blood cells and to the lack of resistance evolution by the parasite against it, but its potent anticoagulant activity is preventing the advance of heparin along the clinical pipeline. We have determined, in in vitro Plasmodium falciparum cultures, the antimalarial activity of heparin-derived structures of different origins and sizes, to obtain formulations having a good balance of in vitro safety (neither cytotoxic nor hemolytic), low anticoagulant activity (≤23 IU/mL according to activated partial thromboplastin time assays), and not too low antimalarial activity (IC50 at least around 100 µg/mL).

Heparin Administered to Anopheles in Membrane Feeding Assays Blocks Plasmodium Development in the Mosquito

August 5, 2020 - 16:24 -- Open Access
Lantero E, Fernandes J, Aláez-Versón CR, Gomes J, Silveira H, Nogueira F, Fernàndez-Busquets X
Biomolecules. 2020 Aug 1;10(8):E1136

Innovative antimalarial strategies are urgently needed given the alarming evolution of resistance to every single drug developed against Plasmodium parasites. The sulfated glycosaminoglycan heparin has been delivered in membrane feeding assays together with Plasmodium berghei-infected blood to Anopheles stephensi mosquitoes.

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