TY - JOUR AU - Odonne, G. AU - Herbette, G. AU - Eparvier, V. AU - Bourdy, G. AU - Rojas, R. AU - Sauvain, M. AU - Stien, D. PY - 2011// TI - Antileishmanial sesquiterpene lactones from Pseudelephantopus spicatus, a traditional remedy from the Chayahuita Amerindians (Peru). Part III T2 - J. Ethnopharmacol. JO - Journal of Ethnopharmacology SP - 875 EP - 879 VL - 137 IS - 1 KW - Asteraceae KW - Chayahuita KW - Hirsutinolides KW - Leishmaniasis KW - Peru KW - Pseudelephantopus spicatus KW - Traditional remedy KW - 8 KW - 13 diacetylpiptocarphol KW - acetyl 13 o ethylpiptocarphol KW - amphotericin B KW - antileishmanial agent KW - plant extract KW - Pseudelephantopus spicatus extract KW - sesquiterpene lactone derivative KW - unclassified drug KW - ursolic acid KW - amastigote KW - article KW - biological activity KW - Ic 50 KW - in vitro study KW - Leishmania KW - medicinal plant KW - nonhuman KW - traditional medicine KW - Leishmania amazonensis N2 - Ethnopharmacological relevance: 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. Materials and 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. IC50 against Leishmania amazonensis axenic amastigotes are respectively 0.2, 0.37 and 0.99 μM (while IC50 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. © 2011 Elsevier Ireland Ltd All rights reserved. SN - 03788741 (Issn) UR - http://www.scopus.com/inward/record.url?eid=2-s2.0-80052031355&partnerID=40&md5=3d857edf1641fb5e735e08bdf7a40b5c N1 - Export Date: 21 October 2011; Source: Scopus; Coden: Joetd; doi: 10.1016/j.jep.2011.07.008; Language of Original Document: English; Correspondence Address: Odonne, G.; Bureau du CNRS en Guyane, CNRS – UPS 2561, 2 Avenue Gustave Charlery, 97300 Cayenne, France; email: guillaume.odonne@gmail.com; Chemicals/CAS: amphotericin B, 1397-89-3, 30652-87-0; ursolic acid, 77-52-1 ID - Odonne_etal2011 ER -