Potent and selective antiplasmodial activity of the cyanobacterial alkaloid nostocarboline and its dimers

Bioorg Med Chem Lett. 2008 Aug 1;18(15):4413-5. doi: 10.1016/j.bmcl.2008.06.049. Epub 2008 Jun 19.

Abstract

The quaternary beta-carbolinium alkaloid nostocarboline from the cyanobacterium Nostoc 78-12A and 10 bis-cationic dimeric derivatives were evaluated against four protozoan parasites and low micromolar values against Trypanosoma brucei, submicromolar values against Leishmania donovani and low nanomolar values against Plasmodium falciparum K1 were determined. Selectivity against rat myoblasts (L6 cells) was found to be up to >2500-fold.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Alkaloids / chemistry
  • Alkaloids / isolation & purification*
  • Alkaloids / pharmacology*
  • Animals
  • Antiprotozoal Agents* / chemical synthesis
  • Antiprotozoal Agents* / chemistry
  • Antiprotozoal Agents* / isolation & purification
  • Antiprotozoal Agents* / pharmacology
  • Carbolines* / chemical synthesis
  • Carbolines* / chemistry
  • Carbolines* / isolation & purification
  • Carbolines* / pharmacology
  • Combinatorial Chemistry Techniques
  • Disease Models, Animal
  • Leishmania donovani / drug effects
  • Malaria / drug therapy
  • Molecular Structure
  • Myoblasts / drug effects
  • Nostoc / chemistry*
  • Parasitic Sensitivity Tests
  • Plasmodium falciparum / drug effects
  • Rats
  • Trypanosoma / drug effects

Substances

  • Alkaloids
  • Antiprotozoal Agents
  • Carbolines
  • nostocarboline