Bioactive Isocedrenes from Perezia multiflora
Sandra Bourgeade-Delmas1, Christiane André-Barrès2, Jeanne Lucas1
1UMR 152 Pharmadev, Université de Toulouse, IRD, UPS, Toulouse, France.
Planta Medica
|November 24, 2020
Summary
Four isocedrenes from Perezia multiflora showed antiparasitic activity against Plasmodium falciparum and Leishmania infantum. One compound displayed weak selectivity, while others lacked significant selectivity due to toxicity.
Area of Science:
- Natural Product Chemistry
- Medicinal Chemistry
- Parasitology
Background:
- Perezia multiflora is a plant source of bioactive compounds.
- Isocedrenes are a class of sesquiterpenes with potential biological activities.
- Parasitic infections like malaria and leishmaniasis require new therapeutic agents.
Purpose of the Study:
- To isolate and characterize isocedrenes from Perezia multiflora.
- To evaluate the antiparasitic activity and toxicity of isolated compounds.
- To propose revised stereochemical assignments for selected compounds.
Main Methods:
- Bioactivity-guided fractionation of ethanolic extract of Perezia multiflora.
- Isolation and structural elucidation of four isocedrenes, including one new compound.
- In vitro antiparasitic assays against Plasmodium falciparum and Leishmania infantum.
- Cytotoxicity assays using mouse and human macrophages.
- Molecular modeling studies (DFT-NMR) for stereochemical assignment.
Main Results:
- Four isocedrenes were isolated, with one being a new compound.
- Antiparasitic activity was observed with IC50 values ranging from 0.81 to 16.1 µM (P. falciparum) and 0.16 to 2.03 µM (L. infantum).
- Compound 4 showed weak selectivity against P. falciparum (SI=3), while compounds 1-3 lacked selectivity due to toxicity (IC50 values 0.16-2.64 µM).
- Revised stereochemical assignments were proposed for compounds 1 and 3.
Conclusions:
- Ethanolic extract of Perezia multiflora contains isocedrenes with antiparasitic potential.
- Compound 4 exhibits limited therapeutic potential against P. falciparum due to toxicity.
- Further investigation into structure-activity relationships and toxicity mechanisms is warranted.
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