Cyanidin-3-rutinoside alleviates postprandial hyperglycemia and its synergism with acarbose by inhibition of intestinal α-glucosidase

The inhibitory activity on intestinal α-glucosidase by cyanidin-3-rutinoside was examined in vitro and in vivo. The IC50 values of cyanidin-3-rutinoside against intestinal maltase, and sucrase were 2,323 ± 14.8 and 250.2 ± 8.1 µM, respectively. The kinetic analysis revealed that intestinal sucrase was inhibited by cyanidin-3-rutinoside in a mixed-type manner. The synergistic inhibition also found in combination of cyanidin-3-rutinoside with acarbose against intestinal maltase and sucrase. The oral administration of cyanidin-3-rutinoside (100 and 300 mg/kg) plus maltose or sucrose to normal rats, postprandial plasma glucose was markedly suppressed at 30–90 min after loading. Furthermore, the normal rats treated with acarbose and cyanidin-3-rutinoside (30 mg/kg) showed greater reduction of postprandial plasma glucose than the group treated with acarbose alone. These results suggest that cyanidin-3-rutinoside retards absorption of carbohydrates by inhibition of α-glucosidase which may be useful as a potential inhibitor for prevention and treatment of diabetes mellitus

Inhibitory Activities of Cyanidin and Its Glycosides and Synergistic Effect with Acarbose against Intestinal α-Glucosidase and Pancreatic α-Amylase

Cyanidin and its glycosides are naturally dietary pigments which have been indicated as promising candidates to have potential benefits to humans, especially in the prevention and treatment of diabetes mellitus. We investigated the structure activity relationships of cyanidin and its glycosides to inhibit intestinal α-glucosidases and pancreatic α-amylase in vitro. The results found that cyanidin and its glycosides are more specific inhibitors of intestinal sucrase than intestinal maltase. Cyanidin-3-galactoside and cyanidin-3-glucoside were the most potent inhibitors against intestinal sucrase and pancreatic α-amylase with IC50 values of 0.50 ± 0.05 and 0.30 ± 0.01 mM, respectively. Our findings indicate that the structural difference between glucose and galactose at the 3-O-position of cyanidin was an important factor for modulating the inhibition of intestinal sucrase and pancreatic α-amylase. The combination of cyandin-3-glucoside, cyanidin-3- galactoside or cyanidin-3,5-diglucosides with a low concentration of acarbose showed synergistic inhibition on intestinal maltase and sucrase. The synergistic inhibition was also found for a combination of cyanidin or cyanidin-3-glucoside with a low concentration of acarbose. The findings could provide a new insight into a use for the naturally occurring intestinal α-glucosidase and pancreatic α-amylase inhibitors for the prevention and treatment of diabetes and its complications

Cinnamic Acid and Its Derivatives Inhibit Fructose-Mediated Protein Glycation

Cinnamic acid and its derivatives have shown a variety of pharmacologic properties. However, little is known about the antiglycation properties of cinnamic acid and its derivatives. The present study sought to characterize the protein glycation inhibitory activity of cinnamic acid and its derivatives in a bovine serum albumin (BSA)/fructose system. The results demonstrated that cinnamic acid and its derivatives significantly inhibited the formation of advanced glycation end products (AGEs) by approximately 11.96–63.36% at a concentration of 1 mM. The strongest inhibitory activity against the formation of AGEs was shown by cinnamic acid. Furthermore, cinnamic acid and its derivatives reduced the level of fructosamine, the formation of Nɛ-(carboxymethyl) lysine (CML), and the level of amyloid cross β-structure. Cinnamic acid and its derivatives also prevented oxidative protein damages, including effects on protein carbonyl formation and thiol oxidation of BSA. Our findings may lead to the possibility of using cinnamic acid and its derivatives for preventing AGE-mediated diabetic complications

Effect of butanol fraction from Cassia tora L. seeds on glycemic control and insulin secretion in diabetic rats

Cassia tora L. seeds have previously been reported to reduce blood glucose level in human and animals with diabetes. In the present study, the effects of Cassia tora L. seed butanol fraction (CATO) were studied on postprandial glucose control and insulin secretion from the pancreas of the normal and diabetic rats. Diabetes was induced by an i.p. injection of Streptozotocin (55 mg/kg BW) into the male Sprague-Dawley rats. The postprandial glucose control was monitored during a 240 min-period using a maltose loading test. In normal rats, rats fed CATO (20 mg/100 g BW/d) showed lower postprandial glucose levels in all the levels from 30 min up to 180 min than those in the control rats without CATO (p<0.05). In diabetic rats, those levels in the CATO group seemed to be lower during the 30~180 min, but only glucose level at 30 min showed significant difference compared to that in the control group. Moreover, CATO delayed the peak time of the glucose rise in both normal and diabetic rats in the glucose curves. On the other hand, when CATO was administered orally to the diabetic rats for 5 days, 12 hr fasting serum glucose level was decreased in the diabetic rats (p<0.05). Degree of a decrease in 12 hr fasting serum insulin levels was significantly less in the diabetic CATO rats as compared to diabetic control rats. On the last day of feeding, β cells of the pancreas were stimulated by 200 mg/dL glucose through a 40 min-pancreas perfusion. Amounts of the insulin secreted from the pancreas during the first phase (11~20 min) and the second phase (21~40 min) in the CATO fed diabetic rats were significantly greater than those in the diabetic control group (p<0.05). These findings indicated that constituents of Cassia tora L. seeds have beneficial effect on postprandial blood glucose control which may be partially mediated by stimulated insulin secretion from the pancreas of the diabetic rats

Influence of the methanolic extract from Abutilon indicum leaves in normal and streptozotocin-induced diabetic rats

The methanolic leaf extract of Abutilon indicum (AI) was investigated for hypoglycemic effect in normal and streptozotocin-induced diabetic rats. The chemical screening of the extract showed that phenoliccompounds and flavonoid contents were 1.04 ± 0.01 mg/g and 59.92 ± 3.88 g/g extract, respectively. A single oral administration of the extract at a dose of 500 mg/kg significantly decreased the bloodglucose concentrations in both normal and diabetic rats after 2 h administration. Metformin was used as the reference drug and reduced the blood glucose only in diabetic rats. To clarify the involvedmechanism, normal rats were orally administered with sucrose and maltose at a dose of 3 g/kg with or without AI extract. The postprandial elevation in the blood glucose concentrations at 30 min after theadministration of sucrose with the extract was significantly suppressed when compared with the control group. No significant change in blood glucose concentrations was observed in maltose-loading rats. An in vitro study indicated that AI extract inhibited -glucosidases, the disaccharide-digesting enzyme in the small intestine. The extract showed a potent sucrase inhibitory activity with IC50 of 2.45 ±0.13 mg/ml while the extract was less potent on the maltase inhibition. The results suggested that the extract from AI extract would be effective for lowering and suppressing elevation of blood glucose

Inhibition of advanced glycation end products by red grape skin extract and its antioxidant activity

BACKGROUND: The objective of the present study was to determine the phytochemical content and the protective effect of red grape skin extract (RGSE) against fructose-mediated protein oxidation. In addition, RGSE was screened for its potential as an antioxidant using various in vitro models. METHODS: Antioxidant activity was measured by 2,2-diphenyl-1-picrylhydrazyl (DPPH), hydroxyl radical scavenging activity, superoxide radical scavenging activity, trolox equivalent antioxidant capacity, ferric reducing antioxidant power (FRAP), ferrous ion chelating power. The total phenols content was measured by Folin–Ciocalteu assay, the flavonoids content by the AlCl(3) colorimetric method. Antiglycation activity was determined using the formation of AGE fluorescence intensity, N(ϵ)-(carboxymethyl)lysine, and the level of fructosamine. The protein oxidation was examined using the level of protein carbonyl content and thiol group. RESULTS: The results showed that the content of total phenolics, flavonoids and total anthocyanins in RGSE was 246.3 ± 0.9 mg gallic acid equivalent/g dried extract, 215.9 ± 1.3 mg catechin equivalent/g dried extract, and 36.7 ± 0.8 mg cyanidin-3-glucoside equivalent/g dried extract, respectively. In the DPPH radical scavenging activity, hydroxyl radical scavenging activity, and superoxide radical scavenging activity, RGSE had the IC(50) values of 0.03 ± 0.01 mg/ml, 5.40 ± 0.01 mg/ml, and 0.58 ± 0.01 mg/ml, respectively. In addition, RGSE had trolox equivalent antioxidant capacity assay (395.65 ± 1.61 mg trolox equivalent/g dried extract), ferric reducing antioxidant power (114.24 ± 0.03 mM FeSO(4)/g dried extract), and ferrous ion chelating power (3,474.05 ± 5.55 mg EDTA/g dried extract), respectively. The results showed that RGSE at different concentrations (0.031–0.500 mg/ml) has significantly inhibited the formation of AGEs in terms of the fluorescence intensity of glycated BSA during 4 weeks of study. The RGSE markedly decreased the level of fructosamine, which is directly associated with the reduction of AGE formation and N(ϵ)-(carboxymethyl)lysine (CML). The results demonstrated the significant effect of RGSE on preventing protein oxidative damages, including effects on the thiol and protein carbonyl oxidation. CONCLUSIONS: The present study revealed that RGSE would exert beneficial effects by virtue of its antioxidants and antiglycation. The findings could provide a new insight into the naturally occurring antiglycation properties of RGSE for preventing AGE-mediated diabetic complication

In Vitro Inhibitory Effects of Cyandin-3-rutinoside on Pancreatic α-Amylase and Its Combined Effect with Acarbose

The inhibitory activity on pancreatic α-amylase by cyanidin-3-rutinoside was examined in vitro. The IC50 value of cyanidin-3-rutinoside against pancreatic α-amylase was 24.4 ± 0.1 μM. The kinetic analysis revealed that pancreatic α-amylase was inhibited by cyanidin-3-rutinoside in a non-competitive manner. The additive inhibition of a combination of cyanidin-3-rutinoside with acarbose against pancreatic α-amylase was also found. These results provide the first evidence for the effect of cyanidin-3-rutinoside in a retarded absorption of carbohydrates by inhibition of pancreatic α-amylase which may be useful as a potential inhibitor for prevention and treatment of diabetes mellitus