Active sesquiterpene lactones against Leishmania amazonensis and Leishmania braziliensis

作者：Sosa Andrea M; Amaya Susana; Salamanca Capusiri Efrain; Gilabert Miguel; Bardon Alicia; Gimenez Alberto; Vera Nancy R; Borkosky Susana A^*

来源：Natural Product Research, 2016, 30(22): 2611-2615.

DOI：10.1080/14786419.2015.1126260

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

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 1.34M, respectively), followed by compound 15 with IC50 value of 1.60M 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.

• 出版日期2016