Antiparasitic Activity of Diterpenoids Against Trypanosoma cruzi

Planta Med. 2017 Feb;83(3-04):306-311. doi: 10.1055/s-0042-115646. Epub 2016 Sep 6.

Abstract

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 µg/mL, 12) or even lower (0.39, 0.99, and 1.20 µg/mL, 3, 4, and 5 respectively) than the positive control nifurtimox (2.3 µg/mL). On intracellular amastigotes, abietanes 3, 4, and 5 showed a significant activity with IC50 values of 0.83, < 0.31, and 0.62 µg/mL, respectively, but were less potent than the positive control nifurtimox (IC50 < 0.16 µg/mL). Compounds 3, 4, and 5 were not cytotoxic to LC5 and NCTC 929 cells at 1 µg/mL.

MeSH terms

  • Animals
  • Antiparasitic Agents / chemistry
  • Antiparasitic Agents / pharmacology*
  • Cell Line
  • Diterpenes / chemistry
  • Diterpenes / pharmacology*
  • Humans
  • Inhibitory Concentration 50
  • Mice
  • Plant Extracts / chemistry
  • Plant Extracts / pharmacology
  • Plectranthus / chemistry
  • Trypanosoma cruzi / drug effects*

Substances

  • Antiparasitic Agents
  • Diterpenes
  • Plant Extracts