Bioactive Isocedrenes from Perezia multiflora

Sandra Bourgeade-Delmas (1) , Christiane André-Barrès (2, 3) , Jeanne Lucas , Manon Trinel , Denis Castillo Pareja , Valérie Jullian (1)

1 PHARMA-DEV - Pharmacochimie et Biologie pour le Développement
2 CNRS - Centre National de la Recherche Scientifique
3 SPCMIB - Synthèse et Physico-Chimie de Molécules d'Intérêt Biologique

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 com- pounds 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 gener- ated from THP-1 monocytic cells (IC50 values ranging from 0.16 to 2.64μM). 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.

Mots clés: Leishmania; Plasmodium; sesquiterpenes; isocedrenes; Asteraceae; Perezia multiflora

Domaines: Chimie thérapeutique

Sandra Bourgeade-Delmas, Christiane André-Barrès, Jeanne Lucas, Manon Trinel, Denis Castillo Pareja, et al.. Bioactive Isocedrenes from Perezia multiflora. Planta Medica, 2021, 87 (03), pp.201-208. ⟨10.1055/a-1298-4706⟩. ⟨hal-03020846⟩