Antiplasmodial, antitrypanosomal, and cytotoxic activities of prenylated flavonoids isolated from the stem bark of Artocarpus styracifolius.

Mélanie Bourjot , Cécile Apel (1) , Marie-Thérèse Martin (1) , Philippe Grellier , van Hung Nguyen (1) , Françoise Guéritte (1) , Marc Litaudon (1)

1 ICSN - Institut de Chimie des Substances Naturelles

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.

Domaines: Chimie organique

Mélanie Bourjot, Cécile Apel, Marie-Thérèse Martin, Philippe Grellier, van Hung Nguyen, et al.. Antiplasmodial, antitrypanosomal, and cytotoxic activities of prenylated flavonoids isolated from the stem bark of Artocarpus styracifolius.. Planta Medica, 2010, 76 (14), pp.1600-4. ⟨10.1055/s-0030-1249777⟩. ⟨hal-00529976⟩