Low antiplasmodial activity of alkaloids and amides from the stem bark of Zanthoxylum rubescens (Rutaceae)

Parasite. 2007 Jun;14(2):161-4. doi: 10.1051/parasite/2007142161.

Abstract

The stem bark of Zanthoxylum rubescens (syn. Fagara rubescens) is used for treating fevers associated with malaria in the Ivory Coast. Three alkaloids: N-nornitidine, 7,9-dimethoxy-2,3-methylenedioxybenzophenanthridine, and bis[6-5,6-dihydrochelerythrinyl)] ether; and two amides: zanthomamide and lemairamide, were isolated from the stem bark of this plant. These compounds were screened in vitro against the chloroquine-sensitive 3D7 strain and the chloroquine-resistant FCM29 strain of P. falciparum. N-nornitidine was found to be inactive. 7,9-dimethoxy-2,3-methylenedioxybenzophenanthridine, lemairamide and zanthomamide showed weak activity with average IC50 values ranging from 45.6 microM to 149.9 microM. Bis[6-15,6-dihydrochelerythrinyl)] ether was the most active of the tested compounds with mean IC50s of 14.9 +/- 1.4 microM in FCM29 strain and 15.3 +/- 3.4 microM in 3D7 strain (approximately 58 to approximately 1130 times less active than chloroquine respectively). The anti-Plasmodium activities of the tested alkaloids of Z. rubescens were low; and do not encourage the use of this plant as antimalarial.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Alkaloids / isolation & purification
  • Alkaloids / therapeutic use
  • Amides / isolation & purification
  • Amides / therapeutic use
  • Animals
  • Antimalarials / therapeutic use*
  • Chloroquine / therapeutic use
  • Dose-Response Relationship, Drug
  • Humans
  • Inhibitory Concentration 50
  • Malaria, Falciparum / drug therapy*
  • Plant Extracts / therapeutic use*
  • Plasmodium falciparum / drug effects*
  • Treatment Outcome
  • Zanthoxylum / chemistry*

Substances

  • Alkaloids
  • Amides
  • Antimalarials
  • Plant Extracts
  • Chloroquine