title: The role of sodium-dependent glucose transporter 1 and glucose transporter 2 in the absorption of cyanidin-3-o-β-glucoside in Caco-2 cells.
abstract: Anthocyanins have multiple biological activities of benefit to human health. While a few studies have been conducted to evaluate the bioavailability of anthocyanins, the mechanisms of their absorption mechanism remain ill-defined. In the present study, we investigated the absorption mechanism of cyanidin-3-O-β-glucoside (Cy-3-G) in human intestinal epithelial (Caco-2) cells. Cy-3-G transport was assessed by measuring the absorptive and efflux direction. Inhibition studies were conducted using the pharmacological agents, phloridzin, an inhibitor of sodium-dependent glucose transporter 1 (SGLT1), or phloretin, an inhibitor of glucose transporter 2 (GLUT2). The results showed that phloridzin and phloretin significantly inhibited the absorption of Cy-3-G. In addition, Caco-2 cells transfected with small interfering RNA (siRNA) specific for SGLT1 or GLUT2 showed significantly decreased Cy-3-G absorption. These siRNA transfected cells also showed a significantly decreased rate of transport of Cy-3-G compared with the control group. These findings suggest that Cy-3-G absorption is dependent on the activities of SGLT1 and GLUT2 in the small intestine and that SGLT1 and GLUT2 could be a limiting step for the bioavailability of Cy-3-G.
authors.affiliation: School of Public Health, Guangdong Medical College, Dongguan 523808, China. crystal031015@163.com.
authors.forename: Tang-Bin
authors.initials: TB
authors.lastname: Zou
authors.affiliation: Guangdong Provincial Key Laboratory of Food, Nutrition and Health, Department of Nutrition, School of Public Health, Sun Yat-Sen University, Guangzhou 510080, China. crystal031015@163.com.
authors.forename: Dan
authors.initials: D
authors.lastname: Feng
authors.affiliation: School of Public Health, Guangdong Medical College, Dongguan 523808, China. 1572@gdmc.edu.cn.
authors.forename: Gang
authors.initials: G
authors.lastname: Song
authors.affiliation: School of Public Health, Guangdong Medical College, Dongguan 523808, China. chineseli@163.com.
authors.forename: Hua-Wen
authors.initials: HW
authors.lastname: Li
authors.affiliation: School of Public Health, Guangdong Medical College, Dongguan 523808, China. gdmcthw@126.com.
authors.forename: Huan-Wen
authors.initials: HW
authors.lastname: Tang
authors.affiliation: Guangdong Provincial Key Laboratory of Food, Nutrition and Health, Department of Nutrition, School of Public Health, Sun Yat-Sen University, Guangzhou 510080, China. lingwh@mail.sysu.edu.cn.
authors.forename: Wen-Hua
authors.initials: WH
authors.lastname: Ling
mesh_terms: D000872:Anthocyanins / Q000493:pharmacokinetics*; D018938:Caco-2 Cells; D002460:Cell Line; D004847:Epithelial Cells / Q000187:drug effects* / Q000378:metabolism; D005960:Glucosides / Q000493:pharmacokinetics*; D006801:Humans; D007408:Intestinal Absorption / Q000187:drug effects*; D007413:Intestinal Mucosa / Q000166:cytology*; D010693:Phloretin / Q000494:pharmacology; D010695:Phlorhizin / Q000494:pharmacology; D034741:RNA, Small Interfering / Q000187:drug effects; D051269:Sodium-Glucose Transporter 1 / Q000378:metabolism*; D051297:Sodium-Glucose Transporter 2 / Q000378:metabolism*
chemical_list: D000872:Anthocyanins; D005960:Glucosides; D034741:RNA, Small Interfering; D051269:Sodium-Glucose Transporter 1; D051297:Sodium-Glucose Transporter 2; C462279:cyanidin-3-O-beta-glucopyranoside; D010695:Phlorhizin; D010693:Phloretin