Isolation and identification of antiplasmodial sesquiterpene lactones from Oncosiphon piluliferum

Oncosiphon piluliferum (Asteraceae) is used traditionally to treat a variety of ailments, mainly fevers. This prompted the screening of this plant for antiplasmodial properties. The dichloromethane extract of the aerial parts of the plant showed activity in vitro against the chloroquine-sensitive (IC50 2.6 μg/ml) and the chloroquine-resistant (IC50 3.1 μg/ml) strains of Plasmodium falciparum. Through conventional chromatographic techniques and bioassay-guided fractionation, sesquiterpene lactones of the germacranolide and eudesmanolide type displaying significant in vitro antiplasmodial activity (IC50 values ranging from 0.4 to 4.4 μg/ml) were isolated and identified by spectroscopic data. In addition, the cytotoxic effects of the active compounds against Chinese Hamster Ovarian (CHO) cells were evaluated and the compounds were found to be toxic to mammalian cells at similar concentrations. Structure-activity relationships were assessed. © 2007 Elsevier Ireland Ltd. All rights reserved.