IQUIMEFA   05518
INSTITUTO QUIMICA Y METABOLISMO DEL FARMACO
Unidad Ejecutora - UE
artículos
Título:
TRYPANOCIDAL ACTIVITY OF SMALLANTHUS SONCHIFOLIUS. IDENTIFICATION OF ACTIVE SESQUITERPENE LACTONES BY BIOASSAY-GUIDED FRACTIONATION
Autor/es:
FRANK FERNANDA; ULLOA JERÓNIMO; CAZORLA SILVIA; MARAVILLA GRETA; MALCHIODI EMILIO; GRAU ALFREDO; MARTINO VIRGINIA; CATALÁN CÉSAR; MUSCHIETTI LILIANA
Revista:
EVIDENCE-BASED COMPLEMENTARY AND ALTERNATIVE MEDICINE
Editorial:
OXFORD UNIV PRESS
Referencias:
Lugar: Oxford; Año: 2013 vol. 2013 p. 1 - 8
ISSN:
1741-427X
Resumen:
In order to find novel plant-derived biologically active compounds against Trypanosoma cruzi, we isolated, from the organic extract of Smallanthus sonchifolius, the sesquiterpene lactones enhydrin (1), uvedalin (2), and polymatin B (3) by bioassay-guided fractionation technique.These compounds showed a significant trypanocidal activity against the epimastigote forms of the parasite with IC50 values of 0.84 uM(1), 1.09 uM(2), and 4.90 uM(3). After a 24 h treatmentwith 10 ug/mL of enhydrin or uvedalin, parasites were not able to recover their replication rate. Compounds 1 and 2 showed IC50 values of 33.4 uM and 25.0 uM against T. cruzi trypomastigotes, while polymatin B was not active. When the three compounds were tested against the intracellular forms of T. cruzi, they were able to inhibit the amastigote replication with IC50 of 5.17 uM, 3.34 uM, and 9.02 uM for 1, 2, and 3, respectively. The cytotoxicity of the compounds was evaluated in Vero cells obtaining CC50 values of 46.5 uM (1), 46.8 uM (2), and 147.3 uM (3) and the selectivity index calculated. According to these results, enhydrin and uvedalin might have potentials as agents against Chagas disease and could serve as lead molecules to develop new drugs.