Saccharin could sweeten the deal for cancer-fighting drugs

A form of saccharin, an artificial sweetener, could lead to the development of drugs to battle aggressive cancers (Photo: Doug Dollemore/American Chemical Society)

Whether it be advice from a dentist or preparing their body for beach season, there's a host of reasons people might reach for an artificial sweetener rather than sugar – though its cancer-fighting properties are unlikely to be one of them. But new research shows that the common sugar substitute known as saccharin could hamper the growth of particular cancers, with scientists claiming it could form the basis for new kinds of drug treatments.

Earlier research has established a protein called carbonic anhydrase IX (CA IX) as a potential target for drug treatments. This protein is present in a number of highly aggressive cancers, such as breast, lung, liver, kidney pancreas and brain. It works by regulating pH levels both in and surrounding cancer cells, giving them the ability to grow and spread to other parts of the body.

But a complication with this approach is that (CA IX) is very similar to 14 other carbonix anydrase proteins found in the body, which help keep everything in working order. Working out how CA IX could be targeted while leaving the beneficial proteins intact had proven a difficult task, but then a team of Italian scientists discovered that saccharin boasts exactly this capability, binding selectively to (CA IX) to hinder its activity.

The latest development comes at the hands of an international team of scientists who sought to build on this knowledge. They created a compound containing a molecule of glucose with similar chemical properties to saccharin, finding that it was 1,000 times more likely to bind to CA IX, and also reduced the amount of saccharin required to effectively inhibit the protein.

The researchers are now using X-ray crystallography to examine more closely how saccharin binds to CA IX and how the process could be improved by fine-tuning saccharin-based compounds to increase its cancer-fighting ability. What makes the CA IX protein such a promising target for cancer treatments is the fact that it is not found in healthy human cells, aside from the gastrointestinal tract. This could one day mean lower dosages and drugs with fewer side effects.

"It never ceases to amaze me how a simple molecule, such as saccharin, something many people put in their coffee everyday, may have untapped uses, including as a possible lead compound to target aggressive cancers," says Robert McKenna, Ph.D., from the University of Florida and one of the project's researchers. "This result opens up the potential to develop a novel anti-cancer drug that is derived from a common condiment that could have a lasting impact on treating several cancers."

The research is set to be presented on Tuesday at a meeting of the American Chemical Society.

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