saccharin
compound / compound-saccharin
サッカリン
Saccharin is an artificial sweetener that produces an aversive bitter aftertaste at high concentrations. An agonist of the TAS2R31 and TAS2R43 bitter taste receptors.
On this page (6 sections)
Reading the bitterness
In a study of 60 white subjects, the response of bitter aftertaste to saccharin and acesulfame K was associated with TAS2R31 variants. Initially, 30 markers across the receptor gene cluster were associated at P < 0.001, but haplotype analysis showed that most of these associations were apparent effects arising from strong linkage with TAS2R31. Cell-based testing confirmed that 4 TAS2R31 variants have independent effects on receptor response.
In HEK293T cells expressing TAS2R43, a response to 2.5 mM sodium saccharin occurred, and the menthol-like cooling compound (R)-(-)-carvone inhibited that response in a dose-dependent manner. This is a result measuring the calcium response of heterologously expressing cells, not an experiment directly assessing the reduction in bitter aftertaste felt by humans.
A review introduces an interaction in which cyclamate inhibits TAS2R31 and TAS2R43, the receptors that respond to saccharin, while saccharin also inhibits TAS2R1 and TAS2R38, the receptors that respond to cyclamate. This is a description explaining the reduction in bitter aftertaste when the two are used together, but it is not a result newly measured by the review, and the text of the original cited source has not been confirmed.
Sources for this overview
Genomic, genetic and functional dissection of bitter taste responses to artificial sweeteners
Checked for this overview: Separated the haplotype analysis addressing 60 subjects, 30 markers, P < 0.001, and high linkage disequilibrium from the cell-based testing that confirmed the independent effects of the 4 variants.
Checked for this overview: Matched TAS2R43-expressing cells, 2.5 mM sodium saccharin, and inhibition by (R)-(-)-carvone with the limitation that this is a cell-based experiment.
Checked for this overview: Matched the mutual receptor inhibition between saccharin and cyclamate with the limitation that this is a secondary citation from a review.
Structured claims — open a section to read each claim's confidence, evidence and limits
Mechanism and receptors (3)
Scope: Full-gene sequencing of TAS2R30-46 in 60 white subjects, taste responses to both sweeteners, and in vitro assays of receptor alleles. 30 markers were initially associated at P < 0.001
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receptor-tas2r31 —mediates_variation_in_bitterness_of→ compound-saccharinScope: Layer: cell. Ca2+ imaging and luminescence assays in HEK293T cells with heterologous expression of TAS2R43.
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compound-saccharin —activates→ receptor-tas2r43Scope: Layer: cell. A review description organizing findings based on heterologous human bitter-receptor expression assays (TAS2R31, TAS2R43, TAS2R1, TAS2R38).
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compound-saccharin —has_perceived_bitterness_suppressed_by→ "When used together with cyclamate, mutual inhibition occurs: cyclamate inhibits TAS2R31 and TAS2R43, the receptors that saccharin stimulates, and saccharin inhibits TAS2R1 and TAS2R38, the receptors that cyclamate activates. This yields a sweetness perception with a weaker bitter aftertaste than either sweetener alone."