Effects of Natural Polyphenols on the Expression of Drug Efflux Transporter P-Glycoprotein in Human Intestinal Cells
Overview
Affiliations
The drug efflux transporter P-glycoprotein, which is encoded by (), plays important roles in drug absorption, distribution, and elimination. We previously reported that dietary polyphenols such as quercetin, curcumin, honokiol, magnolol, caffeic acid phenetyl ester (CAPE), xanthohumol, and anacardic acid inhibit P-glycoprotein-mediated drug transport. In the present study, we investigated the effects of polyphenols on the expression of P-glycoprotein using human intestinal epithelial LS174T cells and a reporter plasmid expressing 10.2 kbp of the upstream regulatory region of . Honokiol, magnolol, CAPE, xanthohumol, and anacardic acid activated the promoter in LS174T cells, and the cellular uptake of rhodamine 123 and calcein-AM, fluorescent substrates of P-glycoprotein, decreased in polyphenol-treated LS174T cells. These results suggest that dietary natural polyphenols can induce the drug efflux transporter P-glycoprotein and have the potential to promote food-drug interactions.
Zhang Y, Weh K, Tripp B, Clarke J, Howard C, Sunilkumar S Pharmaceuticals (Basel). 2023; 16(12).
PMID: 38139823 PMC: 10747310. DOI: 10.3390/ph16121697.
Myint O, Wattanapongpitak S, Kothan S, Udomtanakunchai C, Tima S, Tungjai M Toxicol Rep. 2022; 9:1443-1451.
PMID: 36518452 PMC: 9742882. DOI: 10.1016/j.toxrep.2022.06.017.
Villota H, Santa-Gonzalez G, Uribe D, Henao I, Arroyave-Ospina J, Barrera-Causil C Nutrients. 2022; 14(22).
PMID: 36432565 PMC: 9693551. DOI: 10.3390/nu14224880.
Magnolol and Honokiol Inhibited the Function and Expression of BCRP with Mechanism Exploration.
Yu C, Li P, Chen S, Lin S, Hou Y Molecules. 2021; 26(23).
PMID: 34885972 PMC: 8659015. DOI: 10.3390/molecules26237390.
Potential Herb-Drug Interactions in the Management of Age-Related Cognitive Dysfunction.
Auxtero M, Chalante S, Abade M, Jorge R, Fernandes A Pharmaceutics. 2021; 13(1).
PMID: 33478035 PMC: 7835864. DOI: 10.3390/pharmaceutics13010124.