Active sesquiterpene lactones against Leishmania amazonensis and Leishmania braziliensis. Issue 22 (16th November 2016)

• Record Type: Journal Article
• Authors: Sosa, Andrea M.; Amaya, Susana; Salamanca Capusiri, Efrain; Gilabert, Miguel; Bardón, Alicia; Giménez, Alberto; Vera, Nancy R.; Borkosky, Susana A.
• Is Part Of: Natural product research. Volume 30:Issue 22(2016)
• Page Start: 2611
• Page End: 2615
• Publication Date: 2016-11-16
• Subjects: Vernonieae -- sesquiterpene lactones -- antileishmanial activity -- Leishmania amazonensis -- Leishmania braziliensis; Natural products -- Periodicals; Natural products -- Research -- Periodicals; Biological Factors -- Periodicals; Biological Products -- Periodicals; 547
• DOI: 10.1080/14786419.2015.1126260
• Languages: English
• ISSNs: 1478-6419

Abstract

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 were16 and17 (IC50 values 1.45 and 1.34 μM, respectively), followed by compound15 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 germacradiendiolides16 and17 from Elephantopus mollis . The activity data of the compounds1 −17 assayed against Leishmania parasites are reported here for the first time. Abstract :