Bioactive Isocedrenes from Perezia multiflora

Planta Med. 2021 Mar;87(3):201-208. doi: 10.1055/a-1298-4706. Epub 2020 Nov 23.

Abstract

Four isocedrenes (1: - 4: ), including one new compound (2: ), were isolated from an ethanolic extract of the aerial parts of Perezia multiflora by bioactivity-guided fractionation. For compounds 1: and 3: , a revised stereochemical assignment is proposed based on molecular modeling studies using DFT-NMR calculations. Antiparasitic activity of the four compounds was evaluated using an in vitro culture of Plasmodium falciparum and axenic amastigotes of Leishmania infantum. IC50 values ranged from 0.81 to 16.1 µM (P. falciparum) and 0.16 to 2.03 µM (L. infantum). Toxicity was evaluated against J774A.1 mouse macrophages or human macrophages generated from THP-1 monocytic cells (IC50 values ranging from 0.16 to 2.64 µM). Compound 4: exhibited weak selectivity against P. falciparum with a selectivity index (SI = CC50/IC50) of 3. No selectivity was observed for compounds 1: - 3: against both parasites.

MeSH terms

  • Antiprotozoal Agents*
  • Asteraceae*
  • Humans
  • Leishmania infantum*
  • Malaria, Falciparum*
  • Plasmodium falciparum

Substances

  • Antiprotozoal Agents