title: Dual-stage triterpenoids from an African medicinal plant targeting the malaria parasite.
abstract: Sixteen triterpenoids (1-16), previously isolated from the aerial parts of the African medicinal plant Momordica balsamina or obtained by derivatization, were evaluated for their activity against liver stages of Plasmodium berghei, measuring the luminescence intensity in Huh-7 cells infected with a firefly luciferase-expressing P. berghei line, PbGFP-Luccon. Toxicity of compounds (1-16) was assessed on the same cell line through the fluorescence measurement of cell confluency. The highest activity was displayed by a derivative bearing two acetyl residues, karavoate B (7), which led to a dose-dependent decrease in the P. berghei infection rate, exhibiting a very significant activity at the lowest concentration employed (1 μM) and no toxicity towards the Huh-7 cells. It is noteworthy that, in previous studies, this compound was found to be a strong inhibitor of blood-stages of Plasmodium falciparum, thus displaying a dual-stage antimalarial activity.
authors.affiliation: iMed.ULisboa, Faculdade de Farmácia, Universidade de Lisboa, Av. Prof. Gama Pinto, 1649-003 Lisboa, Portugal.
authors.forename: Cátia
authors.initials: C
authors.lastname: Ramalhete
authors.affiliation: IMM, Faculdade de Medicina, Universidade de Lisboa, 1649-028 Lisboa, Portugal.
authors.forename: Filipa P
authors.initials: FP
authors.lastname: da Cruz
authors.affiliation: CEMEC, Universidade Pedagógica, Faculdade de Ciências Naturais e Matemática, 21402161 Maputo, Mozambique.
authors.forename: Silva
authors.initials: S
authors.lastname: Mulhovo
authors.affiliation: CQM, Universidade da Madeira, 9020-105 Funchal, Portugal.
authors.forename: Inês J
authors.initials: IJ
authors.lastname: Sousa
authors.affiliation: CQM, Universidade da Madeira, 9020-105 Funchal, Portugal; BioLab, Instituto Universitario Antonio Gonzalez, CIBICAN, Universidad de La Laguna, 38206 La Laguna, Spain.
authors.forename: Miguel X
authors.initials: MX
authors.lastname: Fernandes
authors.affiliation: IMM, Faculdade de Medicina, Universidade de Lisboa, 1649-028 Lisboa, Portugal.
authors.forename: Miguel
authors.initials: M
authors.lastname: Prudêncio
authors.affiliation: iMed.ULisboa, Faculdade de Farmácia, Universidade de Lisboa, Av. Prof. Gama Pinto, 1649-003 Lisboa, Portugal. Electronic address: mjuferreira@ff.ul.pt.
authors.forename: Maria-José U
authors.initials: MJ
authors.lastname: Ferreira
mesh_terms: D000962:Antimalarials / Q000737:chemistry* / Q000302:isolation & purification / Q000494:pharmacology; D002460:Cell Line; D002470:Cell Survival / Q000187:drug effects; D006801:Humans; D029775:Momordica / Q000737:chemistry* / Q000378:metabolism; D035261:Plant Components, Aerial / Q000737:chemistry / Q000378:metabolism; D010946:Plants, Medicinal / Q000737:chemistry / Q000378:metabolism; D010963:Plasmodium falciparum / Q000187:drug effects; D014315:Triterpenes / Q000737:chemistry* / Q000302:isolation & purification / Q000494:pharmacology
chemical_list: D000962:Antimalarials; D014315:Triterpenes
keywords: Antimalarials; Dual stage; Momordica balsamina; Plasmodium berghei; Triterpenoids