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1.
Drug Metab Pharmacokinet ; 50: 100499, 2023 Jun.
Article in English | MEDLINE | ID: mdl-36907086

ABSTRACT

Understanding the physiological effects of food ingredients on bodily functions is crucial for the development of foods for specified health use (FoSHU) and functional foods. To investigate this, intestinal epithelial cells (IECs) have been widely studied as they are most frequently exposed to the highest concentrations of food ingredients. Among the various functions of IECs, in this review, we have discussed glucose transporters and their involvement in preventing metabolic syndromes such as diabetes. Phytochemicals are also discussed, as they significantly inhibit glucose and fructose absorption via sodium-dependent glucose transporter 1 (SGLT1) and glucose transporter 5 (GLUT5), respectively. Additionally, we have focused on the barrier functions of IECs against xenobiotics. Phytochemicals induce detoxification of metabolizing enzymes via pregnane X receptor or aryl hydrocarbon receptor activation, which suggests that food ingredients can enhance barrier function. This review will provide insights into the role of food ingredients and glucose transporters, as well as detoxification metabolizing enzymes in IECs, and help guide future research on these aspects.


Subject(s)
Food Ingredients , Intestines , Epithelial Cells/metabolism , Glucose/metabolism , Glucose/pharmacology
2.
Nutrients ; 13(10)2021 Sep 26.
Article in English | MEDLINE | ID: mdl-34684383

ABSTRACT

Rapid postprandial blood glucose elevation can cause lifestyle-related diseases, such as type II diabetes. The absorption of food-derived glucose is primarily mediated by sodium/glucose cotransporter 1 (SGLT1). Moderate SGLT1 inhibition can help attenuate postprandial blood glucose elevation and prevent lifestyle-related diseases. In this study, we established a CHO cell line stably expressing human SGLT1 and examined the effects of phytochemicals on SGLT1 activity. Among the 50 phytochemicals assessed, tangeretin and cardamonin inhibited SGLT1 activity. Tangeretin and cardamonin did not affect the uptake of L-leucine, L-glutamate, and glycyl-sarcosine. Tangeretin, but not cardamonin, inhibited fructose uptake, suggesting that the inhibitory effect of tangeretin was specific to the monosaccharide transporter, whereas that of cardamonin was specific to SGLT1. Kinetic analysis suggested that the suppression of SGLT1 activity by tangeretin was associated with a reduction in Vmax and an increase in Km, whereas suppression by cardamonin was associated with a reduction in Vmax and no change in Km. Oral glucose tolerance tests in mice showed that tangeretin and cardamonin significantly suppressed the rapid increase in blood glucose levels. In conclusion, tangeretin and cardamonin were shown to inhibit SGLT1 activity in vitro and lower blood glucose level in vivo.


Subject(s)
Blood Glucose/metabolism , Chalcones/pharmacology , Flavones/pharmacology , Intestines/physiology , Sodium-Glucose Transporter 1/antagonists & inhibitors , Administration, Oral , Amino Acids/metabolism , Animals , CHO Cells , Caco-2 Cells , Chalcones/chemistry , Cricetulus , Flavones/chemistry , Fructose/metabolism , Humans , Kinetics , Mice, Inbred ICR , Phytochemicals/pharmacology , Sarcosine/metabolism , Sodium/metabolism , Sodium-Glucose Transporter 1/metabolism
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