Antiparasitic Activity of Diterpenoids Against Trypanosoma cruzi

作者:Alegre Gomez Sergio; Sainz Paula; Fatima Simoes M; Rijo Patricia; Moiteiro Cristina; Gonzalez Coloma Azucena; Martinez Diaz Rafael A*
来源:Planta Medica, 2017, 83(3-4): 306-311.
DOI:10.1055/s-0042-115646

摘要

Twenty-seven diterpenes, including abietanes, labdanes, abeoabietanes, halimanes, and pimaranes, have been evaluated against epimastigote and intracellular amastigote forms of Trypanosoma cruzi and also against LC5 and NCTC cell lines. Royleanones (3, 4, and 5) and a further abietane (12), obtained by purification of Plectranthus spp. extracts, were the most active compounds on epimastigotes, showing IC50 values similar (1.73 mu g/mL, 12) or even lower (0.39, 0.99, and 1.20 mu g/mL, 3, 4, and 5 respectively) than the positive control nifurtimox (2.3 mu g/mL). On intracellular amastigotes, abietanes 3, 4, and 5 showed a significant activity with IC50 values of 0.83, < 0.31, and 0.62 mu g/mL, respectively, but were less potent than the positive control nifurtimox (IC50 < 0.16 mu g/mL). Compounds 3, 4, and 5 were not cytotoxic to LC5 and NCTC 929 cells at 1 mu g/mL.

  • 出版日期2017-2