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. 2011 Oct 28;74(10):2174-80.
doi: 10.1021/np200499d. Epub 2011 Oct 13.

Antiplasmodial and antiproliferative pseudoguaianolides of Athroisma proteiforme from the Madagascar Dry Forest

Affiliations

Antiplasmodial and antiproliferative pseudoguaianolides of Athroisma proteiforme from the Madagascar Dry Forest

Ende Pan et al. J Nat Prod. .

Abstract

Investigation of extracts from the plant Athroisma proteiforme (Humbert) Mattf. (Asteraceae) for antimalarial activity led to the isolation of the five new sesquiterpene lactones 1-5 together with centaureidin (6). The structures of the new compounds were deduced from analyses of physical and spectroscopic data, and the absolute configuration of compound 1 was confirmed by an X-ray crystallographic study. Athrolides C (3) and D (4) both showed antiplasmodial activities with IC50 values of 6.6 (3) and 7.2 μM (4) against the HB3 strain and 5.5 (3) and 4.2 μM (4) against the Dd2 strain of the malarial parasite Plasmodium falciparum. The isolates 1-6 also showed antiproliferative activity against A2780 human ovarian cancer cells, with IC50 values ranging from 0.4 to 2.5 μM.

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Figures

Figure 1
Figure 1
a) Key COSY (bold) and HMBC (arrows) correlations for 1. b) Key NOESY correlations for 1.
Figure 2
Figure 2
Anisotropic displacement ellipsoid drawing of 1
Figure 3
Figure 3
a) Key COSY (bold) and HMBC (arrows) correlations for 3. b) Key NOESY correlations for 3.

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