Research Highlights

Herb route to malaria cure

Biplab Das

doi:10.1038/nindia.2008.326 Published online 28 November 2008

An active compound has shown promising anti-malarial activity in mice infected with Plasmodium yoelii, used as a model of human malaria1. Known as bis-trioxane 12a, the compound could be a potential drug candidate for malaria chemotherapy.

In recent years, artemisinin and its derivatives produced from the Chinese herb Artemisia annua have helped overcome multi-drug resistant malaria. The key to artemisinin's success is the presence of the organic compound 1,2,4-trioxanes. Given the poor bioavailability of artemisinin and its derivatives, the researchers sought ways to synthetically produce 1,2,4-trioxanes.

Resorting to a slightly modified photo-oxygenation method, the researchers prepared bis-and tris-1,2,4-trioxanes. They assessed the anti-malarial activity of 24 bis-trioxanes and 3 tris-trioxanes in mice infected with multi-drug resistant P. yoelii.

The researchers found that bis-trioxane 12a is the most active compound of the all compounds tested. It was slightly more active than arteether, a derivative of artemisinin.

"To the best of our knowledge, this is the first report on antimalarial bis- and tris-trioxanes," says lead researcher Chandan Singh from the division of medicinal and process chemistry and division of parasitology of Central Drug Research Institute, Lucknow.


References

  1. Singh, C. et al. Novel Bis- and Tris-1,2,4-trioxanes: Synthesis and Antimalarial Activity against Multidrug-Resistant Plasmodium yoelii in Swiss Mice. J. Med. Chem. doi:  10.1021/jm801006v (2008)