title: Antiplasmodial, antitrypanosomal, and cytotoxic activities of prenylated flavonoids isolated from the stem bark of Artocarpus styracifolius.
abstract: In continuation of our efforts to find new antimalarial drugs, a systematic IN VITRO evaluation using a chloroquine resistant strain of PLASMODIUM FALCIPARUM (FcB1) was undertaken on extracts prepared from various parts of Vietnamese plants. The ethyl acetate extract obtained from the stem bark of ARTOCARPUS STYRACIFOLIUS (Moraceae) exhibited strong antiplasmodial activity (87 % at 10 µg/mL) whereas weak cytotoxicity was observed in a human fibroblast cell line (MRC-5). Phytochemical investigation of this extract led to isolation of two new prenylated flavonoids, styracifolins A and B ( 1 and 2), as well as the known artoheterophyllin A ( 3) and B ( 4), artonins A ( 5), B ( 6), and F ( 7), and heterophyllin ( 8). Structures of 1 and 2 were elucidated by spectroscopic methods and through comparison with data reported in the literature. Compounds 1- 8 exhibited antiplasmodial activities with IC (50) values ranging from 1.1 µM to 13.7 µM, and compounds 1, 2, 6, and 8 showed significant antitrypanosomal activities.
authors.affiliation: Institut de Chimie des Substances Naturelles, Gif-sur-Yvette, France.
authors.forename: Mélanie
authors.initials: M
authors.lastname: Bourjot
authors.forename: Cécile
authors.initials: C
authors.lastname: Apel
authors.forename: Marie-Thérèse
authors.initials: MT
authors.lastname: Martin
authors.forename: Philippe
authors.initials: P
authors.lastname: Grellier
authors.forename: Van Hung
authors.initials: VH
authors.lastname: Nguyen
authors.forename: Françoise
authors.initials: F
authors.lastname: Guéritte
authors.forename: Marc
authors.initials: M
authors.lastname: Litaudon
mesh_terms: D000962:Antimalarials / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D031622:Artocarpus / Q000737:chemistry*; D002460:Cell Line; D002738:Chloroquine / Q000494:pharmacology; D003603:Cytotoxins / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D004351:Drug Resistance; D005419:Flavonoids / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D006801:Humans; D020128:Inhibitory Concentration 50; D010936:Plant Extracts / Q000737:chemistry; D010963:Plasmodium falciparum / Q000187:drug effects*; D054876:Prenylation; D014344:Trypanocidal Agents / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D014346:Trypanosoma brucei brucei / Q000187:drug effects*
chemical_list: D000962:Antimalarials; D003603:Cytotoxins; D005419:Flavonoids; D010936:Plant Extracts; D014344:Trypanocidal Agents; D002738:Chloroquine