Abstract
Two new helenanolide sesquiterpene lactones, 1 and 2, as well as one known related structure, 11alpha,13-dihydrohelenalin-[2-(1-hydroxyethyl)acrylate] (3), together with 4'-beta-d-O-glucopyranosyl-luteolin and ethyl 2,5-dihydroxycinnamate were isolated from an ethyl acetate extract of leaves of Vernoniopsis caudatawith potent antiplasmodial activity (IC50 1.6 microg/mL) in a preliminary biological screen. The structures of the new compounds were determined by spectroscopic techniques. The three sesquiterpene lactones 1-3 displayed strong in vitro antiplasmodial activity, with IC50 values of 1, 0.19, and 0.41 microM, respectively. However, these compounds also exhibited considerable cytotoxicity on KB cells (IC50 < 1 microM in each case).
Publication types
-
Research Support, Non-U.S. Gov't
MeSH terms
-
Antimalarials / chemistry
-
Antimalarials / isolation & purification*
-
Antimalarials / pharmacology
-
Antineoplastic Agents, Phytogenic / chemistry
-
Antineoplastic Agents, Phytogenic / isolation & purification*
-
Antineoplastic Agents, Phytogenic / pharmacology
-
Asteraceae / chemistry*
-
Drug Screening Assays, Antitumor
-
Humans
-
Inhibitory Concentration 50
-
KB Cells
-
Lactones / chemistry
-
Lactones / isolation & purification*
-
Lactones / pharmacology
-
Madagascar
-
Plant Leaves / chemistry
-
Plants, Medicinal / chemistry*
-
Sesquiterpenes / chemistry
-
Sesquiterpenes / isolation & purification*
-
Sesquiterpenes / pharmacology
-
Sesquiterpenes, Guaiane
-
Tumor Cells, Cultured
Substances
-
Antimalarials
-
Antineoplastic Agents, Phytogenic
-
Lactones
-
Sesquiterpenes
-
Sesquiterpenes, Guaiane
-
helenalin-((2-hydroxyethyl-3-methyl)acrylate)
-
helenalin-(2-(1-hydroxyethyl)acrylate)