In Vitro and In Vivo Antihyperglycemic Effect of 2 Amadori Rearrangement Compounds, Arginyl‐Fructose and Arginyl‐Fructosyl‐Glucose

Abstract

During the heat processing of raw ginseng to produce red ginseng, amino acid derivatives such as arginyl-fructose (AF) and arginyl-fructosyl-glucose (AFG) are formed at high levels, through amadori rearrangement, the early step of Maillard reaction, from arginine and glucose or maltose, respectively. However, very limited information is available about the effect of the structural difference between AF and AFG on various biological activities. This is the first report of the mode of action and effect of AF and AFG on the type 2 diabetes management related inhibition of postprandial hyperglycemia in vitro and in animal model. In our previous study, standards AF and AFG were chemically synthesized and in this study their inhibitory activities against rat intestinal α-glucosidases and porcine pancreatic α-amylase were investigated in vitro. The IC(50) value of the in vitro inhibitory activity of AF and AFG on rat intestinal sucrase was high and in similar levels (6.40 and 6.20 mM, respectively). Additionally, a mild pancreatic α-amylase inhibitory activity was observed, with IC(50) values 36.30 and 37.60 mM for AF and AFG, respectively. The effect of AF and AFG on the postprandial blood glucose increase after meal was investigated in Sprague Dawley rats fed on starch or sucrose meals. Both amadori compounds significantly reduced the postprandial blood glucose levels after starch or sucrose loading. These results indicate that AF and AFG, Maillard reaction products, may have antidiabetic effect by suppressing carbohydrate absorption in the gastrointestinal level, and thereby reducing the postprandial increase of blood glucose.

Antihyperglycemic effect of short-term arginyl-fructose supplementation in subjects with prediabetes and newly diagnosed type 2 diabetes: randomized, double-blinded, placebo-controlled trial

“…Ha et al reported that AF had an antihyperglycemic effect and inhibited postprandial hyperglycemia in vitro and in vivo [8]. They demonstrated that AF has strong sucrase and α-amylase inhibitory activity in vitro.…”

“…Amino acid derivatives such as AF and AFG are widely distributed in KRG [5–7]. Previous studies reported that commercial red ginseng products could have AF and AFG levels ranging from 0.35 − 2.51 % and 0.25 − 2.64 %, respectively [8, 9]. The ginsenosides, which are better-known KRG components, have a content ranging from 0.5 − 1.1 % [8, 10].…”

“…These Amadori rearrangement compounds (AF and AFG) significantly reduced postprandial blood glucose levels after starch or sucrose loading in rats. AF and AFG displayed mild inhibitory activity against pancreatic α-amylase [8] and moderate levels of cellular antioxidant activity [11]. Although AF and AFG have potential as pharmacological agents for glycemic control, there are no clinical trials assessing the effects of AF and AFG on blood glucose regulation.…”

Stimulation of Phenolics, Antioxidant and α-Glucosidase Inhibitory Activities During Barley (Hordeum vulgare L.) Seed Germination

“…After centrifugation (12,000 × g, 30 min, 4°C), the resulting supernatant was used for the assay. Sucrase inhibition activity assay was slightly modified from a method described by Ha et al [20]. The activity was determined by pre-incubating a sample solution and rat α-glucosidase solution (100 μL) in 0.…”

Gene-Diet Interactions in Type 2 Diabetes: The Chicken and Egg Debate

“…Arginyl-fructose, which is widely distributed in red ginseng, has antidiabetic effects attributed to it by suppressing carbohydrate absorption in the gastrointestinal tract [152]. Arginyl-fructose has potential as a pharmacological agent for glycemic control since it significantly reduces postprandial blood glucose levels in rodents and humans.…”