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Review
. 2013;16(7):399-451.
doi: 10.1080/10937404.2013.842523.

Sucralose, a synthetic organochlorine sweetener: overview of biological issues

Susan S Schiffman  1 , Kristina I Rother
Affiliations
Free PMC article
Review

Sucralose, a synthetic organochlorine sweetener: overview of biological issues

Susan S Schiffman et al. J Toxicol Environ Health B Crit Rev. 2013.
Free PMC article

Abstract

Sucralose is a synthetic organochlorine sweetener (OC) that is a common ingredient in the world's food supply. Sucralose interacts with chemosensors in the alimentary tract that play a role in sweet taste sensation and hormone secretion. In rats, sucralose ingestion was shown to increase the expression of the efflux transporter P-glycoprotein (P-gp) and two cytochrome P-450 (CYP) isozymes in the intestine. P-gp and CYP are key components of the presystemic detoxification system involved in first-pass drug metabolism. The effect of sucralose on first-pass drug metabolism in humans, however, has not yet been determined. In rats, sucralose alters the microbial composition in the gastrointestinal tract (GIT), with relatively greater reduction in beneficial bacteria. Although early studies asserted that sucralose passes through the GIT unchanged, subsequent analysis suggested that some of the ingested sweetener is metabolized in the GIT, as indicated by multiple peaks found in thin-layer radiochromatographic profiles of methanolic fecal extracts after oral sucralose administration. The identity and safety profile of these putative sucralose metabolites are not known at this time. Sucralose and one of its hydrolysis products were found to be mutagenic at elevated concentrations in several testing methods. Cooking with sucralose at high temperatures was reported to generate chloropropanols, a potentially toxic class of compounds. Both human and rodent studies demonstrated that sucralose may alter glucose, insulin, and glucagon-like peptide 1 (GLP-1) levels. Taken together, these findings indicate that sucralose is not a biologically inert compound.

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Figures

FIGURE 1.
FIGURE 1.
Thin-layer radiochromatographic profile of methanolic fecal extracts following both intravenous (iv) and oral administration of 14C-sucralose: (a) 0–24 h fecal sample from a male rat given an iv dose of 14C-sucralose (2 mg/kg); (b) 0–24 h fecal sample from a male rat maintained on a diet containing 30,000 ppm sucralose for 85 wk before receiving an oral dose of 14C-sucralose (100 mg/kg). An enlargement of the peak profile is given to the right. (TLC traces from Sims et al., 2000).
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