RT info:eu-repo/semantics/article T1 Assessment of the antiprotozoal activity of Pulicaria inuloides extracts, an Algerian medicinal plant: leishmanicidal bioguided fractionation A1 Fadel, Hamza A1 Sifaoui, Ines A1 López Arencibia, Atteneri A1 Reyes Batlle, María A1 Hajaji, Soumaya A1 Chiboub, Olfa A1 Jiménez Díaz, Ignacio Antonio A1 López Bazzocchi, Isabel A1 Lorenzo Morales, Jacob A1 Benayache, Samir A1 Piñero Barroso, José Enrique K1 Pulicaria inuloides K1 Leishmania K1 Trypanosoma K1 Acanthamoeba K1 Bioguided fractionation AB The lack of an effective chemotherapy for treatment of protozoan disease urges a wide investigation for active compounds, andplant-derived compounds continue to provide key leads for therapeutic agents. The current study reports the in vitro antiprotozoalevaluation of the Algerian medicinal plant Pulicaria inuloides against Leishmania amazonensis, Trypanosoma cruzi, andAcanthamoeba castellanii str. Neff. All the extracts from the aerial part showed to be present a higher leishmanicidal activitythan anti-Acanthamoeba or Trypanosoma. Therefore, bioguided fractionation of the active CHCl3 extract led to the isolation andcharacterization of the flavonol, quercetagetin-3,5,7,3′-tetramethyl ether (1) as the main component. The structure of compound 1was established by extensive 1D and 2D NMR spectroscopic analysis (COSY, HSQC, HMBC, and ROESY experiments),chemical transformation (derivatives 2 and 3), and comparison with data in the literature. Compound 1 and derivatives 2 and3 were further evaluated against the promastigote and amastigote stage of L. amazonensis. Compounds 1–3 exhibited moderateleishmanicidal activity with IC50 values ranging from 0.234 to 0.484 mM and from 0.006 to 0.017 mM for the promastigote andamastigote forms, respectively, as well as low toxicity levels on macrophages (CC50 ranging from 0.365 to 0.664 mM). Thisstudy represents the first report of the antiprotozoal evaluation of Pulicaria inuloides, and the results highlight this species as apromising source of leishmanicidal agents. YR 2018 FD 2018 LK http://riull.ull.es/xmlui/handle/915/36068 UL http://riull.ull.es/xmlui/handle/915/36068 LA en DS Repositorio institucional de la Universidad de La Laguna RD 24-nov-2024