Active sesquiterpene lactones against Leishmania amazonensis and Leishmania braziliensis

Andrea M. Sosa, Susana Amaya, Efrain Salamanca Capusiri, Miguel Gilabert, Alicia Bardón, Alberto Giménez, Nancy R. Vera, Susana A. Borkosky

Research output: Contribution to journalArticlepeer-review

15 Scopus citations

Abstract

Seventeen sesquiterpene lactones (SLs) isolated from five species of the tribe Vernonieae were evaluated for their in vitro activity against promastigotes of Leishmania amazonensis and Leishmania braziliensis. Additionally, a quantitative structure activity relationship has been made, since all these natural compounds were found to have potent to mild antileishmanial properties. The most active compounds against L. braziliensis were 16 and 17 (IC50 values 1.45 and 1.34 μM, respectively), followed by compound 15 with IC50 value of 1.60 μM against L. amazonensis. The three glaucolide-type SLs (4−6) were the least active against both parasites. The computational study allowed us to establish that lipophilicity and polarisability play an important role in the antiparasitic activity. This is the first report of the known germacradiendiolides 16 and 17 from Elephantopus mollis. The activity data of the compounds 1−17 assayed against Leishmania parasites are reported here for the first time.

Original languageEnglish
Pages (from-to)2611-2615
Number of pages5
JournalNatural Product Research
Volume30
Issue number22
DOIs
StatePublished - 16 Nov 2016

Bibliographical note

Publisher Copyright:
© 2016 Informa UK Limited, trading as Taylor & Francis Group.

Keywords

  • Leishmania amazonensis
  • Leishmania braziliensis
  • Vernonieae
  • antileishmanial activity
  • sesquiterpene lactones

Fingerprint

Dive into the research topics of 'Active sesquiterpene lactones against Leishmania amazonensis and Leishmania braziliensis'. Together they form a unique fingerprint.

Cite this