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Query: UMLS:C0011849 (diabetes)
 277,896 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

The evidence for the effect of polyphenol components of berries on digestive enzymes is reviewed. Anthocyanins inhibit alpha-glucosidase activity and can reduce blood glucose levels after starch-rich meals, a proven clinical therapy for controlling type II diabetes. Ellagitannins inhibit alpha-amylase activity and there is potential for synergistic effects on starch degradation after ingestion of berries such as raspberries and strawberries, which contain substantial amounts of ellagitannins and anthocyanins. A range of berry polyphenols (e.g. flavonols, anthocyanidins, ellagitannins and proanthocyanidins) can inhibit protease activities at levels which could affect protein digestion in the gastrointestinal tract. In contrast, potential for the inhibition of gastrointestinal lipase activity, a proven therapeutic target for the control of obesity through reduced fat digestion, may be limited to proanthocyanidins. Taking into account the manifold possible synergies for inhibition of starch, protein and/or lipid digestion by the spectrum of polyphenol components present within berry species, the inhibition of digestive enzymes by dietary polyphenols may represent an under-reported mechanism for delivering some of the health benefits attributed to a diet rich in fruit and vegetables.
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PMID:The inhibitory effects of berry polyphenols on digestive enzymes. 1649 5

Extracts of six selected Malaysian plants with a reputation of usefulness in treating diabetes were examined for alpha-amylase inhibition using an in vitro model. Inhibitory activity studied by two different protocols (with and without pre-incubation) showed that Phyllanthus amarus hexane extract had alpha-amylase inhibitory properties. Hexane and dichloromethane extracts of Anacardium occidentale, Lagerstroemia speciosa, Averrhoa bilimbiPithecellobium jiringa and Parkia speciosa were not active when tested without pre-incubation. Extraction and fractionation of Phyllanthus amarus hexane extract led to the isolation of dotriacontanyl docosanoate, triacontanol and a mixture of oleanolic acid and ursolic acid. Dotriacontanyl docosanoate and the mixture of oleanolic acid and ursolic acid are reported from this plant species for the first time. All compounds were tested in the alpha-amylase inhibition assay and the results revealed that the oleanolic acid and ursolic acid (2:1) mixture was a potent alpha-amylase inhibitor with IC(50)=2.01 microg/ml (4.41 microM) and that it contributes significantly to the alpha-amylase inhibition activity of the extract. Three pure pentacyclic triterpenoids, oleanolic acid, ursolic acid and lupeol were shown to inhibit alpha-amylase.
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PMID:alpha-Amylase inhibitory activity of some Malaysian plants used to treat diabetes; with particular reference to Phyllanthus amarus. 1667 67

The hypoglycaemic efficacy of sumac (Rhus coriaria L.) and black cumin (Bunium persicum Boiss) extracts were investigated through inhibition of a glycoside hydrolase: alpha-amylase. On the basis of our result ethyl acetate extract of sumac may have interest in the treatment and prevention of hyperglycaemia, diabetes and obesity, with an IC50 value of 28.7 microg mL-1.
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PMID:Hypoglycaemic activity of two spices extracts: Rhus coriaria L. and Bunium persicum Boiss. 1675 27

Inhibitors targeting pancreatic alpha-amylase and intestinal alpha-glucosidases delay glucose production following digestion and are currently used in the treatment of Type II diabetes. Maltase-glucoamylase (MGA), a family 31 glycoside hydrolase, is an alpha-glucosidase anchored in the membrane of small intestinal epithelial cells responsible for the final step of mammalian starch digestion leading to the release of glucose. This paper reports the production and purification of active human recombinant MGA amino terminal catalytic domain (MGAnt) from two different eukaryotic cell culture systems. MGAnt overexpressed in Drosophila cells was of quality and quantity suitable for kinetic and inhibition studies as well as future structural studies. Inhibition of MGAnt was tested with a group of prospective alpha-glucosidase inhibitors modeled after salacinol, a naturally occurring alpha-glucosidase inhibitor, and acarbose, a currently prescribed antidiabetic agent. Four synthetic inhibitors that bind and inhibit MGAnt activity better than acarbose, and at comparable levels to salacinol, were found. The inhibitors are derivatives of salacinol that contain either a selenium atom in place of sulfur in the five-membered ring, or a longer polyhydroxylated, sulfated chain than salacinol. Six-membered ring derivatives of salacinol and compounds modeled after miglitol were much less effective as MGAnt inhibitors. These results provide information on the inhibitory profile of MGAnt that will guide the development of new compounds having antidiabetic activity.
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PMID:Inhibition of recombinant human maltase glucoamylase by salacinol and derivatives. 1681 95

Water soluble cranberry-based phytochemical combinations with oregano, rosemary, and Rhodiola rosea were evaluated for total phenolic content, related antioxidant activity and inhibition of diabetes management-related alpha -glucosidase, pancreatic alpha-amylase inhibition, and hypertension-related ACE-I inhibitory activities. Water extracts of oregano had 114.9 mg/g DW of phenolics which was highest among all the extracts tested, whereas the 75% cranberry with 25% oregano combinations had the highest phenolics (38.9 mg/g DW) among all the combinations tested. The water extracts of oregano had the highest DPPH radical inhibition activity (73.6 %), whereas among combinations the 75% cranberry and 25% oregano had the highest DPPH radical inhibition activity (50.8 %). These results indicated a correlation between total phenolic content and antioxidant activity. The water extracts of pure Rhodiola rosea had the highest alpha -glucosidase inhibition, whereas the 75% cranberry and 25% Rhodiola rosea combination had the highest inhibition among the combinations. In the case of alpha -amylase inhibition the water extracts of Rhodiola rosea had the highest inhibition, whereas the 75% cranberry with 25% Rhodiola rosea combination had the highest inhibition among the combinations. All the water extracts tested indicated that they had anti-ACE-I inhibitory activity. More specifically, among the water extracts 100% cranberry had the highest ACE-I inhibitory activity and among the combination the 75% cranberry with 25% rosemary had the highest ACE-I inhibitory activity. The analysis of alpha -glucosidase,alpha -amylase, and ACE-I inhibitory activities suggested that inhibition depend on the phenolic profile of each unique extract and by bringing together synergistic combinations to cranberry, health beneficial functionality was enhanced. This enhanced functionality in terms of high alpha -glucosidase and alpha -amylase inhibitory activities indicate the potential for diabetes management, and high ACE-I inhibitory activity indicates the potential for hypertension management.
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PMID:Potential of cranberry-based herbal synergies for diabetes and hypertension management. 1683 38

There is a need for novel drugs for the treatment of infectious diseases, autoimmunity and cancer. Cyclic peptides constitute a class of compounds that have made crucial contributions to the treatment of certain diseases. Penicillin, Vancomycin, Cyclosporin, the Echinocandins and Bleomycin are well-known cyclic peptides. Cyclic peptides, compared to linear peptides, have been considered to have greater potential as therapeutic agents due to their increased chemical and enzymatic stability, receptor selectively, and improved pharmacodynamic properties. They have been used as synthetic immunogens, transmembrane ion channels, antigens for Herpes Simplex Virus, potential immunotherapeutic vaccines for diabetes and Experimental Autoimmune Encephalomyelitis - an animal model of Multiple Sclerosis, as inhibitors against alpha-amylase and as protein stabilizers. Herein, we review important cyclic peptides as therapeutic agents in disease.
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PMID:Round and round we go: cyclic peptides in disease. 1691 50

A purified pancreatic alpha-amylase inhibitor (alpha-AI) from white beans (Phaseolus vulgaris) was administered orally (100 mg/kg body weight dissolved in 9 g NaCl/l) for 22 d to non-diabetic (ND) and type 2 diabetic (neonatal diabetes models n0-STZ and n5-STZ) male Wistar rats. Mean glycaemia (mmol/l) declined from day 4 of the alpha-AI administration in ND rats (5.48 (sem 0.08) v. 4.39 (sem 0.13); P<0.05), n0-STZ diabetic rats (7.94 (sem 0.42) v. 5.56 (sem 0.32); P<0.01) and n5-STZ diabetic rats (17.34 (sem 2.58) v. 11.93 (sem 1.96)), until the end of treatment: ND (5.22 (sem 0.21) v. 3.97 (sem 0.06); P<0.01); n0-STZ (8.10 (sem 0.19) v. 5.21 (sem 0.30); P<0.01); and n5-STZ (16.36 (sem 2.14) v. 7.69 (sem 1.34); P<0.01). There was a decrease in water intake (ml/d) in the alpha-AI-treated diabetic rats: n0-STZ (30 (sem 0.10) v. 22 (sem 1.50); P<0.01) and n5-STZ (76 (sem 5.04) v. 57 (sem 4.85); P<0.01). Food intake (g/d) decreased in all three groups: ND (23 (sem 0.31) v. 20 (sem 0.03); P<0.05); n0-STZ (22 (sem 0.55) v. 16 (sem 0.98); P<0.01); and n5-STZ (31 (sem 0.58) v. 23 (sem 1.20); P<0.01). The enterocyte sucrase and maltase activities (U/g proteins) were high (P<0.01) in the untreated diabetic rats, n0-STZ (45 (sem 4) and 152 (sem 10), respectively) and n5-STZ (67 (sem 12) and 151 (sem 10), respectively) with respect to the ND rats (24 (sem 2) and 74 (sem 10), respectively). After alpha-AI treatment, enzyme activities declined in both diabetic rats, n0-STZ (21 (sem 2) and 85 (sem 11); P<0.01) and n5-STZ (28 (sem 7) and 75 (sem 19); P<0.05), to values close to those in the ND rats. In conclusion, alpha-AI significantly reduced glycaemia in both the ND and diabetic animals and reduced the intake of food and water, and normalized the elevated disaccharidase levels of the diabetic rats.
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PMID:White bean amylase inhibitor administered orally reduces glycaemia in type 2 diabetic rats. 1692 60

Diabetes mellitus (DM) is associated with pancreatic atrophy and compromised digestion of carbohydrates as a result of exocrine pancreatic insufficiency and lower alpha-amylase synthesis and secretion. The reduced production of digestive enzymes is likely to be caused by deregulated protein metabolism. The relative concentrations and phosphorylation of signaling proteins associated with protein translation, such as PKB, p70S6K1, 4E-BP1, ERK1/2, and also some of those implicated in protein breakdown, such as ubiquitin and NF-kappaB, in the pancreas of streptozotocin (STZ)-induced type I diabetic pancreas were measured using Western blotting. There were significant decreases in the levels of total PKB, p70S6K, 4E-BP1, ERK1/2, and NF-kappaB in the diabetic pancreas compared to control. In contrast, the phosphorylation of p70S6K1, 4E-BP1, ERK1/2, and protein ubiquitination increased significantly compared to controls. Together, these results indicate that STZ-induced DM leads to reduced levels of enzymes mediating protein synthesis while their phosphorylation is actually increased, perhaps in an attempt to maintain protein homeostasis, which is further compromised by heightened ubiquitin-dependent protein breakdown. It is likely that these factors are responsible for pancreatic atrophy, enzyme synthesis, and net protein loss in DM.
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PMID:Signaling proteins associated with diabetic-induced exocrine pancreatic insufficiency in rats. 1715 24

During the past decade, many salivary parameters have been used to characterize disease states. Ghrelin (GAH) is recently-discovered peptide hormone secreted mainly from the stomach but also produced in a number of other tissues including salivary glands. The aim of this work was to examine the relationship between active (aGAH) and inactive (dGAH) ghrelin in the saliva and other salivary parameters in type II diabetic patients and healthy controls. Salivary parameters were assessed in a single measurement of unstimulated whole saliva from 20 obese and 20 non-obese type II diabetes patients, and in 22 healthy controls. Total protein and alpha-amylase were determined by colorimetric methods, and glucose by the glucose-oxidase method. Saliva aGAH and dGAH levels were measured using a commercial radioimmunoassay (RIA) kit. Salivary concentrations of aGAH and dGAH ghrelin were more markedly decreased in obese diabetic subjects than in the two other groups. Glucose and alpha-amylase levels were higher in diabetic subjects than in controls. Furthermore, there were correlations between GAH levels and BMI, and between GAH and blood pressure. However, there was no marked variability in saliva flow rates among the groups. These results indicate that measurement of salivary GAH and its relationship to other salivary parameters might help to provide insight into the role of ghrelin in diabetes.
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PMID:A comparison of ghrelin, glucose, alpha-amylase and protein levels in saliva from diabetics. 1724 79

An investigation was made to reveal the possible involvement of thyroid hormones in the progression of diabetes mellitus in response to an atherogenic diet; CCT (4% cholesterol, 1% cholic acid and 0.5% 2-thiouracil). Following the intake of CCT diet for 14 consecutive days a decrease in the serum levels of insulin, both the thyroid hormones, triiodothyronine (T(3)) and thyroxine (T(4)); hepatic glycogen content, hepatic type-1 iodothyronine 5'-mono-deiodinase (5'D) and serum alpha-amylase activities were observed, while there was an increase in the levels of serum glucose and nitrite and in lipid peroxidation of heart, liver and kidney tissues as well as in serum. However, simultaneous administration of L-thyroxine (500 microg/kg/day, s.c.) to CCT-diet fed animals resulted in the amelioration of all the aforesaid adverse changes including that of serum glucose, insulin, alpha-amylase, hepatic glycogen content and nitrite levels, suggesting the involvement of thyroid hormones in the progression of CCT-diet induced diabetes mellitus.
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PMID:Atherogenic diet induced diabetes mellitus: involvement of thyroid hormones. 1762 31


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