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Non-Nutritive Sweeteners Acesulfame Potassium and Sucralose Are Competitive Inhibitors of the Human P-glycoprotein/Multidrug Resistance Protein 1 (PGP/MDR1). Nutrients 2023 Feb 23;15(5)

Date

03/12/2023

Pubmed ID

36904118

Pubmed Central ID

PMC10005754

DOI

10.3390/nu15051118

Scopus ID

2-s2.0-85149772752 (requires institutional sign-in at Scopus site)   1 Citation

Abstract

Non-nutritive sweeteners (NNS) are popular sugar replacements used in foods, beverages, and medications. Although NNS are considered safe by regulatory organizations, their effects on physiological processes such as detoxification are incompletely understood. Previous studies revealed that the NNS sucralose (Sucr) altered P-glycoprotein (PGP) expression in rat colon. We also demonstrated that early-life exposure to NNS Sucr and acesulfame potassium (AceK) compromises mouse liver detoxification. Building upon these initial discoveries, we investigated the impact of AceK and Sucr on the PGP transporter in human cells to assess whether NNS influence its key role in cellular detoxification and drug metabolism. We showed that AceK and Sucr acted as PGP inhibitors, competing for the natural substrate-binding pocket of PGP. Most importantly, this was observed after exposure to concentrations of NNS within expected levels from common foods and beverage consumption. This may suggest risks for NNS consumers, either when taking medications that require PGP as the primary detoxification transporter or during exposure to toxic compounds.

Author List

Danner L, Malard F, Valdes R, Olivier-Van Stichelen S

Author

Stephanie Olivier-Van Stichelen PhD Assistant Professor in the Biochemistry department at Medical College of Wisconsin




MESH terms used to index this publication - Major topics in bold

Animals
Humans
Mice
Non-Nutritive Sweeteners
Rats
Thiazines