Planta Med 2021; 87(03): 201-208
DOI: 10.1055/a-1298-4706
Biological and Pharmacological Activity
Original Papers

Bioactive Isocedrenes from Perezia multiflora

Sandra Bourgeade-Delmas
1  UMR 152 Pharmadev, Université de Toulouse, IRD, UPS, Toulouse, France
,
Christiane André-Barrès
2  UMR 5068 LSPCMIB, Université de Toulouse, CNRS, UPS, Toulouse, France
,
Jeanne Lucas
1  UMR 152 Pharmadev, Université de Toulouse, IRD, UPS, Toulouse, France
,
Manon Trinel
1  UMR 152 Pharmadev, Université de Toulouse, IRD, UPS, Toulouse, France
,
Denis Castillo Pareja
3  Laboratorios de Investigación y Desarrollo, Facultad de Ciencias y Filosofía, Universidad Peruana Cayetano Heredia, Lima, Peru
,
1  UMR 152 Pharmadev, Université de Toulouse, IRD, UPS, Toulouse, France
3  Laboratorios de Investigación y Desarrollo, Facultad de Ciencias y Filosofía, Universidad Peruana Cayetano Heredia, Lima, Peru
› Institutsangaben

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.

Supporting Information



Publikationsverlauf

Eingereicht: 08. Juli 2020

Angenommen nach Revision: 17. Oktober 2020

Publikationsdatum:
23. November 2020 (online)

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