Active sesquiterpene lactones against Leishmania amazonensis and Leishmania braziliensis

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.

Keywords:

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

Acknowledgement

Authors would like to thank Dr Nora Muruaga for the identification of the plant material.