12 January - 20 June 2016

Saccharin/Cyclamate blends inhibit bitter taste receptor activation

A study, conducted by researchers from the German Institute of Human Nutrition, Potsdam-Rehbruecke, and published in Cell Chemical Biology, has solved the 60-year-old mystery as to why a blend of saccharin and cyclamate has less of a bitter off-taste than either of the two constituents.

A study, conducted by researchers from the German Institute of Human Nutrition, Potsdam-Rehbruecke, and published in Cell Chemical Biology, has solved the 60-year-old mystery as to why a blend of saccharin and cyclamate has less of a bitter off-taste than either of the two constituents.

While the food industry has been using non-calorific, high-potency sweeteners to replace sugars for many years, the bitter off-tastes produced can limit their usefulness. Blends of two or more sweeteners have been used to try and reduce such undesirable flavours and the authors of the current study, Behrens et al., note that one of the earliest such blends was that of saccharin and cyclamate. Originally discovered in 1955, this achieves a high level of sweetness with a reduced bitter taste. The mechanism by which this happened however, was unknown until now.

Behrens et al. note that previous studies found that saccharin and cyclamate activate human bitter taste receptors (TAS2Rs). Cyclamate activates TAS2R1 and TAS2R38 at concentrations of 30 mM, above its sweet taste saturation level (2.2 mM).  As saccharin however activates TAS2R31 and TAS2R43 at concentrations of 0.17 mM and 0.08 mM respectively, below that of its sweet taste saturation (0.2 mM), Behrens et al "therefore concentrated on the TAS2R stimulating activity of saccharin".

Using T-REX 293 cells transfected with TAS2R constructs, Behrens et al. stimulated TAS2R31- and TAS2R43-expressing cells with sodium saccharin at 10.0 mM and sodium cyclamate at various concentrations and found ”strong reductions” of the saccharin response for both receptors. As they only saw a complete block for TAS2R43 signals and not for TAS2R31, they repeated the experiment using 3.0 mM sodium saccharin. This allowed them to calculate an IC50 concentration (the inhibitor concentration which reduces response by 50%) of sodium cyclamate at 16.2±9.0 mM for TAS2R31 and 4.8±0.4 mM for TAS2R43 thus showing TAS2R43 to be more sensitive to sodium cyclamate inhibition that TASR31.

Following these investigations and given "the structural similarity of cyclamate and saccharin", Behrens et al. also wondered if saccharin might similarly inhibit cyclamate activation of TAS2Rs. The researchers note that cyclamate requires higher concentrations to reliably activate the TAS2R1 receptor but found that sodium saccharin blocked TAS2R1 activation at concentrations between 1 and 10 mM.  Behrens et al. state that as this is above the sweet receptor saturation level for saccharin and at concentrations which saccharin tastes bitter, "this phenomenon may not contribute to the superior taste of cyclamate /saccharin blends in the general population” but indicates that for those less sensitive to bitter saccharin tastes, “blends with higher saccharin concentrations may show improved taste".

The researchers note that as previous studies have suggested that combinations of non-calorific sweeteners might provide "synergistic activation" of sweet receptors, they also investigated this but found that blends of saccharin and cyclamate did not elicit additional responses from sweetness receptors over and above that of the constituents.

In discussion, Behrens et al. reiterate that cyclamate can inhibit the two bitter taste receptors activated by saccharin and that saccharin can supress activation of the bitter taste receptors activated by cyclamate. They state that this mutual suppression of bitter taste receptors "accounts for the improved perceptual properties of non-caloric sweetener blends" and note that their findings may enable bitter-masking substance blends to be formulated even from compounds which alone, taste bitter.

RSSL's Product and Ingredient Innovation Team, has considerable experience in re-formulating products to provide more healthy options including low salt, low sugar versions and using pre- and probiotics.  Using RSSL can help speed up your development cycle considerably.  Download RSSL’s White Paper: Working with Intense Sweeteners.  To find out more please contact Customer Services telephone 0118 918 4076 or e-mail enquiries@rssl.com

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