Abstract

Cyanidin-3-O-glucoside (C3G) is a widespread anthocyanin derivative, which has been reported in vitro to exert potent antioxidant, antiglycation and α-glucosidase inhibition effects. Nevertheless, the physiological relevance of such properties remains uncertain considering its significant instability in gastrointestinal conditions. A simulated digestion procedure was thus instigated to assess the influence of gastric and intestinal media on its chemical integrity and biological activities. HPLC analyses of digested C3G samples confirmed the striking impact of intestinal conditions, as attested by a decomposition ratio of 70%. In contrast, with recovery rates of around 90%, antiglycation, as well as DPPH and ABTS scavenging assays, uniformly revealed a noteworthy persistence of its antiglycoxidant capacities. Remarkably, a prominent increase of its α-glucosidase inhibition activity was even observed after the intestinal phase, suggesting that classical in vitro evaluations might underestimate C3G antidiabetic potential. Consequently, the present data provide novel and specific insights on C3G’s digestive fate, suggesting that the gastrointestinal tract does not profoundly affect its positive action on oxidative and carbonyl stresses. More specifically, it also tends to support its regulating effects on postprandial hyperglycemia and its potential usefulness for diabetes management.

Highlights

  • Cyanidin glycosides have been reported to exhibit protective and therapeutic potentials in diabetes and associated complications [18]. In addition to their antiglycoxidant properties, their potent inhibitory effects on α-glucosidase might contribute to their antidiabetic action by controlling postprandial hyperglycemia [18,19]

  • NPG), pancreatin from porcine pancreas (8 × USP specification), pepsin from porcine gastric mucosa, bovine serum albumin (BSA), 2,2-diphenyl-1-picrylhydrazyl (DPPH), 2,2′-azino-bis(3-ethylbenzothiazoline-6sulfonic acid) diammonium salt (ABTS), D-ribose, Folin–Ciocalteu’s reagent, gallic acid, 63 of 10 hydroxy-2,5,7,8-tetramethylchromane-2-carboxylic acid (Trolox), sodium chloride, calcium chloride dihydrate, potassium chloride, magnesium chloride hexahydrate, potassium phosphate monobasic, sodium bicarbonate and ammonium carbonate were purchased from Sigma–Aldrich

  • HPLC analyses were performed with a LaChrom Elite system (VWR-Hitachi, Radnor, PA, USA) consisting of two L7100 pumps, a L7200 autosampler, a L2450 diode array detector (DAD) and EZ Chrom Elite software (Agilent Technologies, Santa Clara, CA, USA)

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Summary

Introduction

Publisher’s Note: MDPI stays neutral with regard to jurisdictional claims in published maps and institutional affiliations. Cyanidin glycosides have been reported to exhibit protective and therapeutic potentials in diabetes and associated complications [18] In addition to their antiglycoxidant properties, their potent inhibitory effects on α-glucosidase might contribute to their antidiabetic action by controlling postprandial hyperglycemia [18,19]. In vitro assessments of the biological activities of natural compounds and plant extracts is a first and fundamental step to endorse their potential physiological effects Such kinds of evaluations might not fully guarantee their actual benefits on human health since bioaccessibility, bioavailability and metabolization processes are not considered. The substantial sensitivity of anthocyanin constituents towards gastrointestinal conditions has been reported by several evaluations [20,21], highlighting the necessity of investigating the impact of the digestive tract on their biological properties. Spectrophotometric and fluorometric assays were achieved to validate the persistence of its radical scavenging, antiglycative and α-glucosidase inhibitory properties in digestive media

Reagents
Gastric
Sample Management
Spectrometric and Fluorometric Evaluations
HPLC Analysis
Statistical Analyses
Chemical Analyses of Digested C3G Samples
Impact of In Vitro Digestion on α-Glucosidase Inhibition Properties of C3G
A Review of Factors Affecting Anthocyanin Bioavailability

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