title: Furfuran lignans and a flavone from Artemisia gorgonum Webb and their in vitro activity against Plasmodium falciparum.
abstract: The chemical composition of the aerial parts of the Cape Verdean endemic shrub Artemisia gorgonum Webb (Asteraceae) was careful investigated, which led to the isolation and identification of six known furfuran lignans: eudesmin (1), magnolin (2), epimagnolin A (3), aschantin (4), kobusin (5), sesamin (6) and a flavone: artemetin (7). Compounds 1-7 were evaluated in vitro for their cytotoxicity in a screening panel consisting of various mammalian tumor cell lines, for their antimalarial activity against chloroquine-resistant Plasmodium falciparum (FcB1 strain) and for their cytotoxicity against murine normal cells (CFU-GM). While no promising cytotoxicity against human tumor cells were noticed, marginal potency and selectivity was found for compounds 1-5 against murine colon 38. Besides, compounds 2-7 showed mild antiplasmodial activities, 6 and 7 being the most active compounds (IC(50) 3.37 and 3.50 μg/ml respectively) without noticeable toxicity on mammalian normal cells. This is the first report of antiplasmodial activity for furfuran lignans and the first isolation of 1-7 from Artemisia gorgonum.
authors: Université de Nice-Sophia Antipolis, Laboratoire de Chimie des Molécules Bioactives et des Arômes, UMR 6001 CNRS, Faculté des Sciences, 28 Avenue Valrose, 06108 Nice Cedex 2, France.
authors: Risoleta
authors: R
authors: Ortet
authors: Soizic
authors: S
authors: Prado
authors: Erik L
authors: EL
authors: Regalado
authors: Frederick A
authors: FA
authors: Valeriote
authors: Joseph
authors: J
authors: Media
authors: Judith
authors: J
authors: Mendiola
authors: Olivier P
authors: OP
authors: Thomas
mesh_terms: D000818:Animals; D000962:Antimalarials / Q000302:isolation & purification* / Q000494:pharmacology; D019306:Artemisia / Q000737:chemistry*; D045744:Cell Line, Tumor; D002851:Chromatography, High Pressure Liquid; D047309:Flavones / Q000302:isolation & purification* / Q000494:pharmacology; D006801:Humans; D066298:In Vitro Techniques; D017705:Lignans / Q000302:isolation & purification* / Q000494:pharmacology; D010963:Plasmodium falciparum / Q000187:drug effects*; D021241:Spectrometry, Mass, Electrospray Ionization
chemical_list: D000962:Antimalarials; D047309:Flavones; D017705:Lignans