Title
New clerodane diterpenoids from Laetia procera (Poepp.) Eichler (Flacourtiaceae), with antiplasmodial and antileishmanial activities
Date Issued
15 November 2005
Access level
metadata only access
Resource Type
journal article
Author(s)
Jullian V.
Bonduelle C.
Valentin A.
Acebey L.
Duigou A.G.
Prévost M.F.
Universidad Paul Sabatier
Abstract
Extracts of Laetia procera (Flacourtiaceae) displayed significant in vitro activity against Plasmodium falciparum. P. falciparum bioassay guided fractionation of a trunk bark extract of this plant led to the isolation of six clerodane diterpenoids (1-6) and a butanolide (7). Five of these compounds are new and called Laetiaprocerine A-D (3-6) and Laetianolide A (7). Their structures were established on the basis of 1D and 2D NMR experiments. Absolute configurations of 1 and 2 were determined by a modified Mosher's method and the absolute configuration of 5 by chemical correlation. The clerodane diterpenoids displayed activities against P. falciparum with an IC50 down to 0.5 μM on FCb1 and F32 strains, and also cytotoxicity toward human tumor cell line MCF7. The most active compound showed a selectivity index of 6.8. Some of these compounds also displayed activities against Leishmania amazonensis amastigote axenic stages and promastigote. © 2005 Elsevier Ltd. All rights reserved.
Start page
5065
End page
5070
Volume
15
Issue
22
Language
English
OCDE Knowledge area
Química medicinal
Scopus EID
2-s2.0-26044431994
PubMed ID
Source
Bioorganic and Medicinal Chemistry Letters
ISSN of the container
0960894X
Sponsor(s)
This work was supported by the ACI Pal+, French Ministry of Research. We thank Dr. Christian Moretti (US 084 Biodival, IRD) for organizing the plant supply and for fruitful discussions.
Sources of information: Directorio de Producción Científica Scopus