title: In vitro and in vivo activity of major constituents from Pluchea carolinensis against Leishmania amazonensis.
abstract: The search for new therapeutic agents from natural sources has been a constant for the treatment of diseases such as leishmaniasis. Herein, in vitro and in vivo pharmacological activities of pure major phenolic constituents (caffeic acid, chlorogenic acid, ferulic acid, quercetin, and rosmarinic acid) from Pluchea carolinensis against Leishmania amazonensis are presented. Pure compounds showed inhibitory activity against promastigotes (IC50 = 0.2-0.9 μg/mL) and intracellular amastigotes (IC50 = 1.3-2.9 μg/mL). Four of them were selected after testing against macrophages of BALB/c mice: caffeic acid, ferulic acid, quercetin, and rosmarinic acid, with selective indices of 11, 17, 10, and 20, respectively. Ferulic acid, rosmarinic acid, and caffeic acid controlled lesion size development and parasite burden in footpads from BALB/c experimentally infected mice, after five injections of compounds by intralesional route at 30 mg/kg every 4 days. Pure compounds from P. carolinensis demonstrated antileishmanial properties.
authors.affiliation: Laboratory of Microbiology, Parasitology and Hygiene (LMPH), Faculty of Pharmaceutical, Biomedical and Veterinary Sciences, Antwerp University, Antwerp, Belgium.
authors.forename: Elly
authors.initials: E
authors.lastname: Montrieux
authors.forename: Wilmer H
authors.initials: WH
authors.lastname: Perera
authors.forename: Marley
authors.initials: M
authors.lastname: García
authors.forename: Louis
authors.initials: L
authors.lastname: Maes
authors.forename: Paul
authors.initials: P
authors.lastname: Cos
authors.forename: Lianet
authors.initials: L
authors.lastname: Monzote
mesh_terms: D000818:Animals; D000981:Antiprotozoal Agents / Q000494:pharmacology*; D019659:Asteraceae / Q000737:chemistry*; D002109:Caffeic Acids / Q000494:pharmacology; D002478:Cells, Cultured; D002934:Cinnamates / Q000494:pharmacology; D003373:Coumaric Acids / Q000494:pharmacology; D053630:Depsides / Q000494:pharmacology; D005260:Female; D007894:Leishmania mexicana / Q000187:drug effects*; D007896:Leishmaniasis / Q000188:drug therapy*; D008264:Macrophages / Q000469:parasitology; D051379:Mice; D008807:Mice, Inbred BALB C; D011794:Quercetin / Q000031:analogs & derivatives / Q000494:pharmacology; D000097123:Rosmarinic Acid
chemical_list: D000981:Antiprotozoal Agents; D002109:Caffeic Acids; D002934:Cinnamates; D003373:Coumaric Acids; D053630:Depsides; D011794:Quercetin; D000097123:Rosmarinic Acid; C012526:quercitrin; C004999:ferulic acid; C040048:caffeic acid