Berberine suppresses intestinal disaccharidases with beneficial metabolic effects in diabetic states, evidences from in vivo and in vitro study
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Disaccharidase
Acarbose
Sucrase
Maltase
Alpha-glucosidase
The inhibitory effect on human and rat intestinal disaccharidase by the extractive from the leaves of Morus alba (ELM) containing 0.24 % 1-deoxynojirimycin equivalent and its inhibitory activities were investigated by the modified Dahlqvist method. In the presence of 1000-fold diluted ELM solution, the sucrase activity of four human samples was inhibited by 96 % and that of maltase and isomaltase by 95 and 99 %, respectively. The activities of trehalase and lactase were inhibited by 44 and 38 %, respectively. The human disaccharidase activities varied from sample to sample because the samples were obtained from different resected regions after surgery. However, the ratio of the inhibitory effect for sucrase, maltase, isomaltase, trehalase and lactase was very similar among the four samples, and also that of resembled rat intestinal disaccharides. The inhibitory constant of the 1-deoxynojirimycin equivalent for sucrase, maltase and isomaltase was 2.1 x 10(-4), 2.5 x 10(-4) and 4.5 x 10(-4) mm, respectively, and these inhibitory activities were shown, using rat brush border membrane vesicles, to be competitive. These results demonstrate that digestion is inhibited when an appropriate amount of ELM is orally ingested with sucrose or polysaccharide in man. When ELM was orally administered in a sucrose solution to fasted rats, the elevation in blood glucose was significantly suppressed, depending on the concentration of ELM given. These results suggest that ELM could be used as an ingredient in health foods and in foods that help to prevent diabetes.
Disaccharidase
Sucrase
Maltase
Trehalase
Alpha-glucosidase
Lactase
Digestion
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The activities of lactase, sucrase, maltase and gamma-glutamyl transferase (gamma-GT) were determined in homogenates of rat jejunal mucosa 24 h after acute administrations of D-galactosamine (GALN) (1.855 mmol/kg; i.p. injection) and alpha-naphthyl-isocyanate (ANIT) (0.540 mmol/kg; given by gastric tube). The animals were fasted either 24 h or 72 h prior to sacrifice. In rats fasted only 24 h, GALN treatment resulted in a pronounced decrease in lactase and in a moderate elevation of sucrase and maltase. ANIT clearly reduced lactase and, to a lesser extent, sucrase, while it increased maltase. Seventy-two hour fasting has a modifying role. All disaccharidase activities tended to decrease, except for maltase in the ANIT treated group, where an increase was recorded. gamma-GT showed no significant changes after either GALN or ANIT treatment in rats fasted 24 h. However, the 72-hour food deprivation diminished it in ANIT intoxication. It is obvious that the intestinal enzymes are influenced by the hepatic damage produced by GALN and ANIT.
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Disaccharidase
Maltase
Lactase
Alpha-glucosidase
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α -glucosidase inhibitors are utilized in the treatment of type II diabetes mellitus (DM). The inhibition of intestinal α -glucosidase would delay the digestion and absorption of carbohydrates and consequently suppress postprandial hyperglycemia. Thai medicinal plants are widely used in the treatment of diabetes mellitus. An attempt to verify their Inhibitory effect on α-glucosidase from two different sources are reported herein. Among of them, the methanolic extract of Amomum xanthioides showed significant inhibitory activity against α-glucosidase, the sucrase and maltase from rat intestine with IC 50 value 3.10 4.20 and α glucosidase from baker's yeast with IC 50 values of 26.6 which is 25 times greater than the standard anti diabetic drug, acarbose. The preliminary observation provides the basis for further examination of Thai medicinal plants as supplement food and DM drug toward the treatment and prevention of diabetes.
Acarbose
Maltase
Sucrase
Alpha-glucosidase
Digestion
Disaccharidase
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Disaccharidase
Sucrase
Maltase
Alpha-glucosidase
Lactase
Husk
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Summary The purpose of this study was to examine the short‐term effects of 75, 100 and 150 mg of acarbose mixed in 100 g standard laboratory chow on specific intestinal disaccharidase activities and on hyperglycaemia in diabetic CBA strain mice on standard diet. The small intestine was excised and divided into three segments, from pylorus to duodenum, and two equal lengths of the jejunum and ileum of control and diabetic mice with or without added acarbose. Specific maltase and sucrase activities were determined using maltose and sucrose as substrates respectively. Increased specific activities of maltase and sucrase were detected in the intestines of CBA mice on standard laboratory diet seven days after alloxan‐induced diabetes. Feeding for 7 days with 75, 100 or 150 mg acarbose uniformly mixed in 100 g standard laboratory chow, induced a decrease in the specific maltase and sucrase activities, compared with diabetic mice on standard laboratory diet. Feeding with 75 mg acarbose mixed in 100 g standard laboratory chow caused a statistically significant decrease of maltase in the duodenum and of sucrase in duodenum and jejunum, without a antihyperglycaemic effect. Feeding with 100 or 150 mg caused statistically significant decreases in specific maltase and sucrase activities in duodenum, jejunum and ileum. An antihyperglycaemic effect was observed only in the group of diabetic mice fed with 100 mg acarbose. This indicates that the antihyperglycaemic effect of acarbose involves factors other than these, related only to its inhibitory effect on disaccharidase activities.
Acarbose
Disaccharidase
Sucrase
Maltase
Jejunum
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The specific effect of dietary sugars on jejunal disaccharidase activity in seven normal nonfasted male volunteers was studied. The sugars tested were sucrose, maltose, lactose, glucose, fructose, and galactose. Comparisons were made of the effects of each sugar in an isocaloric liquid diet.
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Maltase
Sucrase
Alpha-glucosidase
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Hexagalloylglucose (3-O-digalloyl-1,2,4,6-tetra-O-galloyl-β-D-glucose), which was isolated from the methanol extract of the galls of Quercus infectoria, significantly inhibited α-glycosidases such as sucrase, maltase and isomaltase. Its inhibitory activity was comparable to acarbose being used as a hypoglycemic agent, while the inhibitory activity on α-amylase was approximately 10 times lower than that of acarbose. The results indicate that, when compared to acarbose, hexagalloylglucose might reduce the side effects by reducing inhibition of α-amylase.
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Alpha-glucosidase
Maltase
Sucrase
Arbutin
Alpha-amylase
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Disaccharidase activities in intestinal metaplasia - contribution of lysosomal brush border enzymes.
Maltase, sucrase, and lactase were measured at pH 4 and pH 6 in normal and intestinalized gastric mucosa. In the normal mucosa the low activities of maltase and lactase seemed to be entirely due to lysosomal enzymes with acid pH-optimum. In intestinal metaplasia, brush border maltase and sucrase, but not lactase, appeared. On the other hand, there was a significant increase in lysosomal lactase (beta-galactosidase) activity.
Disaccharidase
Sucrase
Maltase
Lactase
Brush border
Intestinal metaplasia
Alpha-glucosidase
Intestinal mucosa
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Acarbose
Sucrase
Maltase
Alpha-glucosidase
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α-Glucosidase, an enzyme that plays a crucial role in glucose absorption in the intestine, is a key therapeutic intervention in the management of diabetes mellitus. The inhibition of this enzyme is critical for controlling postprandial hyperglycemia. The present study aims to investigate the stability of phenolic content, total flavonoid content, and α-glucosidase inhibition activities of six Thai folk anti-diabetes remedies by in vitro simulated gastrointestinal digestion methods, as well as to evaluate their synergistic effect with acarbose. The TFD-04 decoction and 90% EtOH extract showed higher total phenolic and flavonoid content (86.83 mg GAE/g extract, 10.00 mg QE/g extract) and (75.32 mg GAE/g extract, 12.45 mg QE/g extract), respectively. The α-glucosidase inhibitory activities (maltase and sucrase) of TFD-04 were found maximum in decoction and GD-decoction with IC50 values of 0.25±0.02 and 0.78±0.04 mg/mL, respectively, when compared with acarbose with statistical significance (P< 0.05). The IC50 values of 0.59±0.02 and 1.59±0.02 mg/mL, respectively. In addition, the decoction extract of TFD-04 showed the most potent synergistic inhibitory effect with acarbose. A kinetic analysis showed that TFD-04 showed uncompetitive inhibition against intestinal maltase. This study suggests that decoction extracts of TFD-04 may serve as effective anti-hyperglycemic remedies in the field of diabetic therapy.
Acarbose
Sucrase
Maltase
Decoction
Alpha-glucosidase
IC50
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