In vitro activity of artemisinin, its derivatives, and pyronaridine against different strains of Plasmodium falciparum

Trans R Soc Trop Med Hyg. 1990 Sep-Oct;84(5):635-7. doi: 10.1016/0035-9203(90)90129-3.

Abstract

The activities of artemisinin (qinghaosu), dihydroartemisinin (dihydroqinghaosu), artemether and pyronaridine were tested in a 48 h in vitro assay against 3 chloroquine-sensitive and one chloroquine-resistant strains of Plasmodium falciparum. Growth inhibition was modelled with a sigmoid Emax model. All compounds markedly inhibited the growth of all strains although, for the chloroquine-resistant strain, merozoites were detected at concentrations as high as 10(-4) M of artemisinin, dihydroartemisinin and artemether. Dihydroartemisinin, artemether and pyronaridine appeared to be more potent than artemisinin, with EC50 values of 4.7-23 nM, 0.98-6.1 nM and 4.4-18 nM respectively, while the EC50 value of artemisinin was 3-108 nM against all 4 strains.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antimalarials / pharmacology*
  • Artemether
  • Artemisinins*
  • Dose-Response Relationship, Drug
  • Drug Resistance
  • In Vitro Techniques
  • Naphthyridines / pharmacology*
  • Plasmodium falciparum / drug effects*
  • Plasmodium falciparum / growth & development
  • Sesquiterpenes / pharmacology*

Substances

  • Antimalarials
  • Artemisinins
  • Naphthyridines
  • Sesquiterpenes
  • artenimol
  • artemisinin
  • Artemether
  • pyronaridine