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Alsinol, an arylamino alcohol derivative active against Plasmodium, Babesia, Trypanosoma, and Leishmania: Past and new outcomes

Arias Maria Héléna, Quiliano Miguel, Bourgeade-Delmas Sandra, Fabing Isabelle, Chantal Isabelle, Berthier David, Minet Cécile, Eparvier Véronique, Sorres Jonathan, Stien Didier, Galiano Lucía, Aldana Ignacio, Valentin Alexis, Garavito Giovanny, Deharo Eric. 2020. Alsinol, an arylamino alcohol derivative active against Plasmodium, Babesia, Trypanosoma, and Leishmania: Past and new outcomes. Parasitology Research, 119 : pp. 3503-3515.

Journal article ; Article de recherche ; Article de revue à facteur d'impact
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Url - éditeur : https://rdcu.be/b6YqS

Abstract : Malaria, babesiosis, trypanosomosis, and leishmaniasis are some of the most life-threatening parasites, but the range of drugs to treat them is limited. An effective, safe, and low-cost drug with a large activity spectrum is urgently needed. For this purpose, an aryl amino alcohol derivative called Alsinol was resynthesized, screened in silico, and tested against Plasmodium, Babesia, Trypanosoma, and Leishmania. In silico Alsinol follows the Lipinski and Ghose rules. In vitro it had schizontocidal activity against Plasmodium falciparum and was able to inhibit gametocytogenesis; it was particularly active against late gametocytes. In malaria-infected mice, it showed a dose-dependent activity similar to chloroquine. It demonstrated a similar level of activity to reference compounds against Babesia divergens, and against promastigotes, and amastigotes stages of Leishmania in vitro. It inhibited the in vitro growth of two African animal strains of Trypanosoma but was ineffective in vivo in our experimental conditions. It showed moderate toxicity in J774A1 and Vero cell models. The study demonstrated that Alsinol has a large spectrum of activity and is potentially affordable to produce. Nevertheless, challenges remain in the process of scaling up synthesis, creating a suitable clinical formulation, and determining the safety margin in preclinical models.

Mots-clés Agrovoc : Babesia, Leishmania, Plasmodium falciparum, Trypanosoma, Protozoa, Parasitose, Contrôle de maladies, Efficacité, Expérimentation in vitro, Expérimentation in vivo

Mots-clés complémentaires : Arylamino alcohol, alsinol, Expérimentation in silico

Mots-clés libres : Antiprotozoan, Alsinol, Trypanosoma, Leishmania sp., Plasmodium falciparum gametocytes, Babesia

Classification Agris : L73 - Animal diseases
000 - Other themes

Champ stratégique Cirad : CTS 4 (2019-) - Santé des plantes, des animaux et des écosystèmes

Auteurs et affiliations

  • Arias Maria Héléna, Universidad Nacional de Colombia (COL)
  • Quiliano Miguel, Universidad Peruana de Ciencias Aplicadas (PER)
  • Bourgeade-Delmas Sandra, IRD (FRA)
  • Fabing Isabelle, CNRS (FRA)
  • Chantal Isabelle, CIRAD-BIOS-UMR INTERTRYP (FRA) ORCID: 0000-0002-3429-484X
  • Berthier David, CIRAD-BIOS-UMR INTERTRYP (FRA) ORCID: 0000-0002-3283-6588
  • Minet Cécile, CIRAD-BIOS-UMR INTERTRYP (FRA) ORCID: 0000-0002-9287-1481
  • Eparvier Véronique, CNRS (FRA)
  • Sorres Jonathan, CNRS (FRA)
  • Stien Didier, CNRS (FRA)
  • Galiano Lucía, Universidad de Navarra (ESP)
  • Aldana Ignacio, Universidad de Navarra (ESP)
  • Valentin Alexis, IRD (FRA)
  • Garavito Giovanny, Universidad Nacional de Colombia (COL) - auteur correspondant
  • Deharo Eric, Université Toulouse III Paul Sabatier (FRA)

Source : Cirad-Agritrop (https://agritrop.cirad.fr/596370/)

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