title: Antileishmanial sesquiterpene lactones from Pseudelephantopus spicatus, a traditional remedy from the Chayahuita Amerindians (Peru). Part III.
abstract: BACKGROUND
  The study of traditional remedies used by the Chayahuita, an ethnic group from the Peruvian Amazonia, has prompted us to investigate in detail the ethanolic extract of Pseudelephantopus spicatus (Juss. ex Aubl.) C.F. Baker, which has demonstrated strong biological activity towards Leishmania amazonensis. Our goal was to discover the active compound of this plant-based remedy.
  
  
  METHODS
  A bioguided fractionation of the crude extract was undertaken based on the biological activity recorded against Leishmania amazonensis axenic amastigotes in in vitro bioassays.
  
  
  RESULTS
  Three strongly to moderately active compounds were isolated: two hirsutinolides (the 8,13-diacetyl-piptocarphol and the 8-acetyl-13-O-ethyl-piptocarphol) and ursolic acid. IC(50) against Leishmania amazonensis axenic amastigotes are respectively 0.2, 0.37 and 0.99 μM (while IC(50) of amphotericin B is 0.41 μM). These compounds have never been isolated from this plant species, and germacranolides have never been identified as potential antileishmanial agents.
  
  
  CONCLUSIONS
  The compounds isolated from Pseudelephantopus spicatus account for the antileishmanial activity of the plant, thus giving support to its use by the Chayahuita in Peru.
authors.affiliation: CNRS - UMR Ecofog, Université des Antilles et de la Guyane, BP792, 97337 Cayenne cedex, France. guillaume.odonne@gmail.com
authors.forename: G
authors.initials: G
authors.lastname: Odonne
authors.forename: G
authors.initials: G
authors.lastname: Herbette
authors.forename: V
authors.initials: V
authors.lastname: Eparvier
authors.forename: G
authors.initials: G
authors.lastname: Bourdy
authors.forename: R
authors.initials: R
authors.lastname: Rojas
authors.forename: M
authors.initials: M
authors.lastname: Sauvain
authors.forename: D
authors.initials: D
authors.lastname: Stien
mesh_terms: D000666:Amphotericin B / Q000494:pharmacology; D019659:Asteraceae / Q000737:chemistry; D005591:Chemical Fractionation; D004305:Dose-Response Relationship, Drug; D006801:Humans; D007199:Indians, South American; D020128:Inhibitory Concentration 50; D007783:Lactones / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D007891:Leishmania / Q000187:drug effects* / Q000254:growth & development; D008519:Medicine, Traditional; D010568:Peru; D035261:Plant Components, Aerial; D010936:Plant Extracts / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D010946:Plants, Medicinal; D012717:Sesquiterpenes / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D014315:Triterpenes / Q000494:pharmacology; D014344:Trypanocidal Agents / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D000097245:Ursolic Acid
chemical_list: D000666:Amphotericin B; D007783:Lactones; D010936:Plant Extracts; D012717:Sesquiterpenes; D014315:Triterpenes; D014344:Trypanocidal Agents; D000097245:Ursolic Acid