Antiplasmodial activities of sesquiterpene lactone from Carpesium cernum

Abstract

The whole plant of genus Carpesium is used in traditional medicine as an anti-pyretic, analgesic and vermifugic, including a topical application for sores and inflammation. Previous experiments on Carpesium rosulatum suggested that the antiplasmodial effect was due to the existence of ineupatorolide A. In present paper, screening of Carpesium species from South Korea showed that this plant refers to which species had promising antiplasmodial activity. Subsequently, this species was selected for bioassay-guided fractionation in order to identify the active principles. Fractionation of the ethyl acetate extract of the whole plants by chromatographic techniques yielded four characterised sesquiterpenoid lactones which exhibited antiplasmodial activity against Plasmodium falciparum. This being the first time that this has been reported from Carpesium cernum. The antiplasmodial activity of the isolated compounds was determined against the Plasmodium falciparum.

Natural Products Published in 2009 from Plants Traditionally Used to Treat Malaria

“…(Euphorbiaceae) and displayed antiplasmodial activity (IC 50 values of 8.7 and 9.9 µM, respectively) against K1 [25]. Fractionation of the ethyl acetate extract of Carpesium cernuum L. (Asteraceae) yielded four characterised sesquiterpenoid lactones among which 11(13)-dehydroivaxillin (57) and 11-epi-ivaxillin (58) exhibited antiplasmodial activity against D10 with IC 50 values of 2.0 and 9.3 µM [34]. In vivo antiplasmodial activity of 57 showed a suppression of parasitemia of 58.6 % with a dose of 2 mg/kg/day in the four-day test [35].…”

Antiplasmodial Sesquiterpenoid Lactones from Trichospira verticillata: Structure Elucidation by Spectroscopic Methods and Comparison of Experimental and Calculated ECD Data

“…Sesquiterpenoid lactones are a series of well-known compounds that have been reported to have various bioactivities, including antiplasmodial, antiproliferative, and antifungal activities. − Several bioactive germacranolide-type sesquiterpenoid lactones have been isolated recently, most often from the Asteraceae family. , Previous structure–activity relationship studies indicated that the α,β-unsaturated γ-lactone unit, which could target cysteine residues in proteins by acting as a Michael acceptor, is important for the bioactivity of germacranolides . This α,β-unsaturated γ-lactone unit is present in all four trichospirolides A–D, but their activities are varied due to modifications in the 10-membered ring.…”

Effects of the topical application of an ethyl acetate fraction from Vernonia scorpioides on excisional wounds infected with Staphylococcus aureus in rats

“…In the tribe Vernonieae (family: Asteraceae) sesquiterpene lactones (Lopes, 1991) are found, for which the different biological effects are described. The data suggest that these compounds have anti-inflammatory and anti-ulcer (Feltenstein et al, 2004), anti-malarial (Chung & Moon, 2009), and antibacterial (Ntutelaa et al, 2009, Saroglou et al, 2010 properties. These results could be related to the α,β-unsaturated carbonyl groups in these compounds, which seems to be important for their cytotoxicity (Lee et al, 1971).…”