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Saccharin improves activity against two tumour-associated enzymes

Wed, 12/18/2019 - 14:38
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A study led by researchers from the University of Florence, Florence, Italy, have reported that artificial sweetener derivatives can improve activity against two tumour-associated enzymes. The study, ‘”A Sweet Combination”: Developing Saccharin and Acesulfame K Structures for Selectively Targeting the Tumor-Associated Carbonic Anhydrases IX and XII’, published in American Chemical Society' Journal of Medicinal Chemistry.

Saccharin binds to and inhibits an enzyme called carbonic anhydrase (CA) IX, which helps cancer cells survive in the acidic, oxygen-poor microenvironments of many tumours. In contrast, healthy cells make different - but very similar - versions of this enzyme called CA I and II. Saccharine and another artificial sweetener, called acesulfame K, can selectively bind to CA IX over CA I and II, making them possible anti-cancer drugs with minimal side effects.

Researchers Drs Alessio Nocentini and Claudiu Supuran, and colleagues wondered whether they could make versions of the artificial sweeteners that show even more potent and selective inhibition of CA IX and another tumour-associated enzyme, CA XII.

The team designed and synthesized a series of 20 compounds that combined the structures of saccharin and acesulfame K and also added various chemical groups at specific locations. Some of these compounds showed greater potency and selectivity toward CA IX and XII than the original sweeteners. In addition, some killed lung, prostate or colon cancer cells grown in the lab but were not harmful to normal cells.

These findings indicate that the widely used artificial sweeteners could be promising leads for the development of new anti-cancer drugs, the researchers stated.