Bioactive Isocedrenes from Perezia multiflora

Bourgeade-Delmas S.; André-Barrès C.; Lucas J.; Trinel M.; Castillo Pareja D.; Jullian V. · Planta Medica (2020) · DOI: 10.1055/a-1298-4706

Resumen

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. IC 50values 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 (IC 50values ranging from 0.16 to 2.64 μM). Compound 4 exhibited weak selectivity against P. falciparum with a selectivity index (SI = CC 50/IC 50) of 3. No selectivity was observed for compounds 1 - 3 against both parasites.

Instituciones: Universidad Peruana Cayetano Heredia