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

Planta Med. 2010 Oct;76(14):1600-4. doi: 10.1055/s-0030-1249777. Epub 2010 Apr 8.

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.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antimalarials / chemistry
  • Antimalarials / isolation & purification
  • Antimalarials / pharmacology*
  • Artocarpus / chemistry*
  • Cell Line
  • Chloroquine / pharmacology
  • Cytotoxins / chemistry
  • Cytotoxins / isolation & purification
  • Cytotoxins / pharmacology*
  • Drug Resistance
  • Flavonoids / chemistry
  • Flavonoids / isolation & purification
  • Flavonoids / pharmacology*
  • Humans
  • Inhibitory Concentration 50
  • Plant Extracts / chemistry
  • Plasmodium falciparum / drug effects*
  • Prenylation
  • Trypanocidal Agents / chemistry
  • Trypanocidal Agents / isolation & purification
  • Trypanocidal Agents / pharmacology*
  • Trypanosoma brucei brucei / drug effects*

Substances

  • Antimalarials
  • Cytotoxins
  • Flavonoids
  • Plant Extracts
  • Trypanocidal Agents
  • Chloroquine