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.
journal_name
Planta Medjournal_title
Planta medicaauthors
Bourgeade-Delmas S,André-Barrès C,Lucas J,Trinel M,Castillo Pareja D,Jullian Vdoi
10.1055/a-1298-4706subject
Has Abstractpub_date
2020-11-23 00:00:00eissn
0032-0943issn
1439-0221pub_type
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