Sunday 21 September, 2014

New family of antimalarial compounds both prevents and cures disease

Published On: Fri, Nov 18th, 2011 | Genomics | By BioNews

In a new study, an international team of scientists claim to have discovered a family of chemical compounds that could lead to a new generation of antimalarial drugs capable of not only alleviating symptoms but also preventing the deadly disease.

Stephan Meister and his team from the Genomics Institute of the Novartis Research Foundation (GNF) and The Scripps Research Institute have demonstrated that the class of compounds was more effective against malaria than some commercially available drugs.

To find compounds to act against the Plasmodium parasite, which causes malaria, the team screened thousands of candidates that were already known to act against malaria parasites in the blood.

Elizabeth Winzeler, a Scripps Research associate professor said that only 15 percent looked as if they might also work in the liver, a strong indication, that “a lot of compounds that are active against blood stages probably aren’t going to do anything about eliminating malaria.”

The group then identified the strongest candidates for drug development by mining the data for groups of related compounds that all showed activity in the liver. In the end, they settled on a cluster related to the chemical imidazolopiperazine.

“When we analyzed all of the data, we saw that multiple members of this imidazolopiperazine family were active in blood and liver stages,’ Winzeler said.

The group used an automated system of their own design to see how these new compounds fared against malaria parasites incubated in liver cells in the lab.

An imaging apparatus took multiple images of each collection of cells over time, and a computer script analysed those images to see how well the various compounds inhibited the growth of the parasites.

The team was finally able to develop compounds that could be taken orally and would stay in the blood long enough to be a viable candidate for drug development, and when it was given to mice, it provided complete protection against the parasite in the liver, and worked better in the blood than some commercially available drugs.

The study has been recently published in Science Express.

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