Antitrypanosomal alkaloids from Polyalthia suaveolens (Annonaceae): their effects on three selected glycolytic enzymes of Trypanosoma brucei

Bioorg Med Chem Lett. 2010 Jun 15;20(12):3495-8. doi: 10.1016/j.bmcl.2010.04.145. Epub 2010 May 6.

Abstract

In continuation of our study on medicinal plants of Cameroon, stem barks of Polyalthia suaveolens were phytochemically studied. This investigation yielded a new indolosesquiterpene alkaloid, named polysin (1) and four hitherto known alkaloids (2-5). Polysin (1) appeared as a competitive reversible inhibitor (K(i)=10 microM) of phosphofructo kinase (PFK) of Trypanosoma brucei with respect to fructose-6-phosphate (K(i)/K(M)=0.05) and could be used in the design of new trypanocidal drugs. The other isolated compounds (2-5) also exhibited interesting inhibitory effects on selected glycolytic enzymes (PFK, glyceraldehyde-3-phosphate dehydrogenase and aldolase).

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Alkaloids / chemistry
  • Alkaloids / isolation & purification
  • Alkaloids / pharmacology*
  • Cameroon
  • Enzyme Inhibitors / pharmacology
  • Glycolysis / drug effects
  • Phosphofructokinases / antagonists & inhibitors
  • Phytotherapy
  • Plants, Medicinal / chemistry
  • Polyalthia / chemistry*
  • Sesquiterpenes
  • Trypanocidal Agents / chemistry
  • Trypanocidal Agents / isolation & purification
  • Trypanocidal Agents / pharmacology*
  • Trypanosoma brucei brucei / drug effects
  • Trypanosoma brucei brucei / enzymology*
  • Trypanosoma brucei brucei / metabolism

Substances

  • Alkaloids
  • Enzyme Inhibitors
  • Sesquiterpenes
  • Trypanocidal Agents
  • Phosphofructokinases