title: Antileishmanial activity of the hydroalcoholic extract of Miconia langsdorffii, isolated compounds, and semi-synthetic derivatives.
abstract: The in vitro activity of the crude hydroalcoholic extract of the aerial parts of Miconia langsdorffii Cogn. was evaluated against the promastigote forms of L. amazonensis, the causative agent of cutaneous leishmaniasis in humans. The bioassay-guided fractionation of this extract led to identification of the triterpenes ursolic acid and oleanolic acid as the major compounds in the fraction that displayed the highest activity. Several ursolic acid semi-synthetic derivatives were prepared, to find out whether more active compounds could be obtained. Among these ursolic acid-derived substances, the C-28 methyl ester derivative exhibited the best antileishmanial activity.
authors.affiliation: Núcleo de Pesquisa em Ciências Exatas e Tecnológicas da Universidade de Franca, Av. Dr. Armando Salles de Oliveira 201-Parque Universitário, CEP 14404-600, Franca, SP, Brazil.
authors.forename: Juliana A
authors.initials: JA
authors.lastname: Peixoto
authors.forename: Márcio Luis
authors.initials: ML
authors.lastname: Andrade E Silva
authors.forename: Antônio E M
authors.initials: AE
authors.lastname: Crotti
authors.forename: Rodrigo
authors.initials: R
authors.lastname: Cassio Sola Veneziani
authors.forename: Valéria M M
authors.initials: VM
authors.lastname: Gimenez
authors.forename: Ana H
authors.initials: AH
authors.lastname: Januário
authors.forename: Milton
authors.initials: M
authors.lastname: Groppo
authors.forename: Lizandra G
authors.initials: LG
authors.lastname: Magalhães
authors.forename: Fransérgio F
authors.initials: FF
authors.lastname: Dos Santos
authors.forename: Sérgio
authors.initials: S
authors.lastname: Albuquerque
authors.forename: Ademar A
authors.initials: AA
authors.lastname: da Silva Filho
authors.forename: Wilson R
authors.initials: WR
authors.lastname: Cunha
mesh_terms: D000818:Animals; D000981:Antiprotozoal Agents / Q000737:chemistry* / Q000494:pharmacology*; D001681:Biological Assay / Q000379:methods; D007891:Leishmania / Q000187:drug effects*; D035322:Melastomataceae / Q000737:chemistry*; D015394:Molecular Structure; D009828:Oleanolic Acid / Q000737:chemistry / Q000494:pharmacology; D010936:Plant Extracts / Q000737:chemistry* / Q000494:pharmacology*; D014315:Triterpenes / Q000737:chemistry / Q000494:pharmacology; D000097245:Ursolic Acid
chemical_list: D000981:Antiprotozoal Agents; D009828:Oleanolic Acid; D010936:Plant Extracts; D014315:Triterpenes; D000097245:Ursolic Acid