Trypanocidal and leishmanicidal activities of flavonoids from Argentine medicinal plants.
In vitro trypanocidal and leishmanicidal activities of the flavonoids hispidulin, from Ambrosia tenuifolia, and santin, from Eupatorium buniifolium, are reported. A sensitive technique that takes advantage of ((3)H)thymidine uptake by dividing trypanosomatids has been adjusted for quantification of the parasiticidal effect of the natural products. The IC(50) values for hispidulin and santin on Trypanosoma cruzi epimastigotes were 46.7 and 47.4 muM, respectively. On trypomastigotes, the IC(50) values were 62.3 microM for hispidulin and 42.1 microM for santin. Hispidulin was more active than santin on promastigotes of Leishmania mexicana (IC(50) = 6.0 microM versus 32.5 microM). No cytotoxic activity was observed on lymphoid cells, making hispidulin and santin potential lead compounds for the development of new natural drugs. This is the first report on the trypanocidal and leishmanicidal activities of these flavonoids and on the presence of santin in E. buniifolium.
Sülsen
Valeria P
VP
Cátedra de Farmacognosia, (IQUIMEFA)-(UBA-CONICET), Facultad de Farmacia y Bioquímica, Universidad de Buenos Aires, Buenos Aires, Argentina.
Cazorla
Silvia I
SI
Frank
Fernanda M
FM
Redko
Flavia C
FC
Anesini
Claudia A
CA
Coussio
Jorge D
JD
Malchiodi
Emilio L
EL
Martino
Virginia S
VS
Muschietti
Liliana V
LV
D031164:Ambrosia / Q000737:chemistry*; D000818:Animals; D001118:Argentina; D004353:Drug Evaluation, Preclinical; D036602:Eupatorium / Q000737:chemistry*; D005260:Female; D047309:Flavones / Q000494:pharmacology* / Q000633:toxicity; D005419:Flavonoids / Q000494:pharmacology* / Q000633:toxicity; D020128:Inhibitory Concentration 50; D007894:Leishmania mexicana / Q000187:drug effects* / Q000254:growth & development / Q000302:isolation & purification; D008297:Male; D051379:Mice; D008807:Mice, Inbred BALB C; D013601:T-Lymphocytes / Q000187:drug effects; D013936:Thymidine / Q000493:pharmacokinetics; D014316:Tritium; D014349:Trypanosoma cruzi / Q000187:drug effects* / Q000254:growth & development / Q000302:isolation & purification
D047309:Flavones; D005419:Flavonoids; D014316:Tritium; C104803:santin; C055957:hispidulin; D013936:Thymidine