Planta Med 2014; 80 - PD64
DOI: 10.1055/s-0034-1382485

Leishmanicidal sesquiterpene lactones from Tithonia diversifolia

SR Ambrósio 1, 2, JS de Toledo 3, CHG Borges 1, V Manfrim 3, DG Cerri 3, AK Cruz 3, FB Da Costa 2
  • 1Universidade de Franca, Franca, Brazil
  • 2AsterBioChem Research Team, Faculdade de Ciências Farmacêuticas de Ribeirão Preto, USP, Ribeirão Preto, Brazil
  • 3Faculdade de Medicina de Ribeirão Preto, USP, Ribeirão Preto, Brazil

Sesquiterpene lactones (SLs) are recognized as a class of natural compounds with a wide spectrum of biological activities, including against Leishmania spp. In this work, a SL rich extract from Tithonia diversifolia (SLRE) was tested against promastigote forms of L. braziliensis. This result revealed that SLRE is a rich source of potent leishmanicidal compounds (LD50= 1.5 ± 0.50 µg/mL). Therefore eight sesquiterpene lactones from SLRE were investigated and three of them (1 – 3) showed potent leishmanicidal effect with high level of selectivity, displaying LD50 values (ranging from 21.2 ± 8.0 to 37.4 ± 7.1µM) similar to that observed for positive control (hygromycin B; 15.1 ± 0.9µM). Due to these results, compounds 1 – 3 were evaluated at their LD50 concentrations on intracellular amastigotes. After 48 hours of treatment these SLs reduced the internalization of parasites in about 58, 51 and 27%, respectively, in comparison with negative control. The results described herein bring new perspectives in the study of STL and may provide promising leads for the development of new drugs against leishmaniasis.

Fig. 1

The authors thank to FAPESP for funds and grants (process number 2014/04281 – 7)