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
03/12/2023Pubmed ID
36904118Pubmed Central ID
PMC10005754DOI
10.3390/nu15051118Scopus ID
2-s2.0-85149772752 (requires institutional sign-in at Scopus site)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 SAuthor
Stephanie Olivier-Van Stichelen PhD Assistant Professor in the Biochemistry department at Medical College of WisconsinMESH terms used to index this publication - Major topics in bold
AnimalsHumans
Mice
Non-Nutritive Sweeteners
Rats
Thiazines
