Antiplasmodial and Antiproliferative Pseudoguaianolides of Athroisma proteiforme from the Madagascar Dry Forest

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 <b>1</b>–<b>5</b> together with centaureidin (<b>6</b>). The structures of the new compounds were deduced from analyses of physical and spectroscopic data, and the absolute configuration of compound <b>1</b> was confirmed by an X-ray crystallographic study. Athrolides C (<b>3</b>) and D (<b>4</b>) both showed antiplasmodial activities with IC₅₀ values of 6.6 (<b>3</b>) and 7.2 μM (<b>4</b>) against the HB3 strain and 5.5 (<b>3</b>) and 4.2 μM (<b>4</b>) against the Dd2 strain of the malarial parasite Plasmodium falciparum. The isolates <b>1</b>–<b>6</b> also showed antiproliferative activity against A2780 human ovarian cancer cells, with IC₅₀ values ranging from 0.4 to 2.5 μM