Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts: Gene/Protein Disease Symptom Drug Enzyme Compound   Target Concepts: Gene/Protein Disease Symptom Drug Enzyme Compound

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Query: EC:3.2.1.20 (alpha-glucosidase)
4,237 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

The alpha-glucosidase inhibitor acarbose has been successfully used in diabetic patients to decrease the postprandial rise in blood glucose. The aim of the present experiments was to investigate the fate and effects of acarbose along the small intestine using a slow-marker perfusion technique. In 8 healthy volunteers, jejunal and ileal loads of acarbose, glucose, and total carbohydrates were determined following a liquid, 400-kcal formula meal containing either 200 mg of acarbose or placebo. Preprandial and postprandial plasma concentrations of glucose and several polypeptide hormones were determined. Recovery of acarbose during 4 h was 65% +/- 9% (mean +/- SEM) of ingested dose in the ileum but 94% +/- 9% in the jejunum, indicating that the compound was neither degraded nor absorbed by the intestine to a major degree. After acarbose administration, ileal loads of glucose and total carbohydrates were considerably higher, whereas postprandial plasma concentrations of glucose, insulin, and gastric inhibitory polypeptide were lower when compared with placebo. The retardation of carbohydrate digestion to be inferred from these findings is confirmed by significantly elevated plasma concentrations of enteroglucagon after acarbose administration compared with placebo administration.
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PMID:Fate and effects of the alpha-glucosidase inhibitor acarbose in humans. An intestinal slow-marker perfusion study. 328 63

Retardation of meal carbohydrate absorption by inhibition of starch degradation improves glucose tolerance in normal and diabetic humans. To determine the effects of Bay-m-1099, a new alpha-glucosidase inhibitor, on insulin requirements and prandial glucose tolerance in patients with insulin-dependent diabetes mellitus (IDDM), plasma glucose, triglyceride, and free insulin concentrations were measured after ingestion of a standard breakfast, lunch, and dinner in nine patients with IDDM in a single-blind, randomized, crossover design. A 20% reduction in insulin was given 30 minutes before the meals when the subjects received Bay-m-1099 (50 mg). This resulted in the AUC for plasma insulin to be significantly less with Bay-m-1099 (AUC, 8.2 +/- 1.3 vs. 12.8 +/- 1.6 microU/ml/min with placebo; P less than 0.01). Despite this reduction in plasma insulin levels, postprandial plasma glucose concentrations were reduced for the breakfast (73 +/- 15 vs. 112 +/- 14 mg/dl/min with placebo; P less than 0.01) and dinner (23 +/- 8 vs. 4 +/- 1 mg/dl/min with placebo; P less than 0.05) meal with Bay-m-1099. Bay-m-1099 did not affect postprandial plasma triglycerides and was well tolerated, the major side effect being flatulence (4/9) and mild diarrhea (4/9). We conclude that inhibition of intestinal alpha-glucosidases by Bay-m-1099 in IDDM reduces meal insulin requirements by at least 20% and that such an agent could be useful in the management of diabetes mellitus by reducing hyperinsulinemia.
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PMID:A new alpha-glucosidase inhibitor (Bay-m-1099) reduces insulin requirements with meals in insulin-dependent diabetes mellitus. 331 50

The present study aimed at investigating the metabolic effects and tolerance of two desoxynojirimycin derivatives with alpha-glucosidase inhibitory properties (BAY m 1099 and BAY o 1248). The study was performed in a double-blind cross-over manner on 7 insulin-treated outpatient diabetics (6 males, 1 female; mean age 43 +/- 14 years; mean duration of diabetes 5.8 +/- 4.2 years; all within +/- 10% of their ideal body weight). The usual diet containing 24.5 +/- 8 g dietary fibers and 52 +/- 22 g simple sugars was maintained throughout the study. After a 7-day run-in period, 4 consecutive periods of 7 days were considered for each patient. The patients were randomly allocated for 1 week to BAY o 1248 (20 mg with breakfast) or Bay m 1099 (50 mg with breakfast and dinner). After a 7-day wash-out period the patients underwent the alternate treatment. At the end of each period, the patients were admitted to the Metabolic Ward for detailed metabolic and hormonal investigations. No significant changes were observed in the daily insulin requirements (45 +/- 15 U/day). HbA1c did not change significantly. Residual insulin secretion was low (plasma C-peptide: 0.077 +/- 0.09 and 0.154 +/- 0.15 pmol/ml during fasting and 2 hours post-breakfast, respectively); it was not modified by the treatments. Increments in blood glucose were significantly lower after breakfast with both drugs. No differences were observed in plasma free insulin. A marked increase in breath hydrogen was observed after lunch with BAY o 1248 only. Clinical and biological tolerance was excellent for both compounds.(ABSTRACT TRUNCATED AT 250 WORDS)
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PMID:Assessment of the clinical efficacy and tolerance of two new alpha-glucosidase inhibitors in insulin-treated diabetics. 331 59

1. alpha-Glucosidase inhibitors delay carbohydrate absorption and have been proposed as adjunctive therapy for diabetes mellitus. 2. To determine the effects of two new alpha-glucosidase inhibitors, Bay-m-1099 and Bay-o-1248, on meal carbohydrate and lipid tolerance, plasma glucose, insulin and triglyceride levels were measured at 15-60 min intervals over 12 h after ingestion of a standard breakfast, lunch and dinner of identical composition in 31 normal volunteers. 3. The volunteers were randomized to receive either Bay-m-1099 (50 or 25 mg) or placebo prior to each meal, or the single administration of Bay-o-1248 (20 or 10 mg) or placebo prior to breakfast. 4. Only Bay-m-1099 at the 50 mg dose reduced significantly the postprandial increase in plasma insulin levels after each meal when compared with placebo (25, 36, 54% at breakfast, lunch, and dinner, respectively; P less than 0.05). Both drugs were well tolerated, with side effects limited to complaints of flatulence. 5. Thus, with the dosage schedule employed, Bay-m-1099, but not Bay-o-1248, significantly reduced postprandial increments in plasma insulin.
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PMID:The effect of two new alpha-glucosidase inhibitors on metabolic responses to a mixed meal in normal volunteers. 332 89

To examine prolonged alpha-glucosidase inhibition on blood glucose control, Acarbose, a potent alpha-glucosidase inhibitor, was administered for six months to insulin-dependent diabetic patients. Acarbose administration significantly diminished postprandial blood glucose increases by 20-30% and reduced insulin requirements by about 40% in these patients. Symptoms related to its use almost disappeared after the first month of treatment. These results suggest that prolonged alpha-glucosidase inhibition improves glucose tolerance in patients with insulin-dependent diabetes mellitus. Thus, an agent like acarbose might be a useful adjunct to insulin in the treatment of diabetic patients.
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PMID:Effects of prolonged (6 months) alpha-glucosidase inhibition on blood glucose control and insulin requirements in patients with insulin-dependent diabetes mellitus. 351 13

BAYo1248 and BAYm1099 are two new alpha-glucosidase inhibitors. Postprandial glucose tolerance was significantly improved and postprandial insulin requirements were significantly reduced as compared to placebo after breakfast and lunch when 20 mg BAYo1248 were administered prior to breakfast and after breakfast, lunch and dinner when 50 mg BAYm1099 were given prior to all three main meals. Postprandial breath H2 concentrations were mildly increased when these alpha-glucosidase inhibitors were given and no patient complained of any adverse effects (such as flatulence, abdominal pain or diarrhea). BAYo1248 and BAYm1099 might be useful adjuncts to insulin in the treatment of patients with insulin-dependent diabetes mellitus.
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PMID:Effects of two new alpha-glucosidase inhibitors on glycemic control in patients with insulin-dependent diabetes mellitus. 352 Jan 33

Bay m 1099 is a newly developed inhibitor of intestinal alpha-glucosidase. Its ability to lower postprandial plasma glucose, serum insulin and C-peptide levels in Type II diabetics has been investigated. Fifteen obese Type II diabetic patients with inadequate metabolic control during sulphonylurea treatment received a standardized diet and were treated either with Bay m 1099, b.d. (100 mg before breakfast and dinner) or placebo for 3 days, according to a double-blind cross-over design. The postprandial blood glucose level was significantly lower during Bay m 1099 treatment compared to placebo after breakfast and dinner (AUC after breakfast p less than 0.001). The reduced postprandial hyperglycaemia was associated with a decrease in meal stimulated serum insulin and C-peptide levels. Thus, Bay m 1099 may be a useful addition in the treatment of Type II diabetic patients.
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PMID:Effects of the alpha-glucosidase inhibitor 1 desoxynojirimycin (Bay m 1099) on postprandial blood glucose, serum insulin and C-peptide levels in type II diabetic patients. 352 20

We investigated the hormonal and metabolic response to a 100-g sucrose load given 15 min after adaptation to moderate-intensity (50% VmaxO2) long-duration (4-h) exercise in healthy volunteers. The effect of a 100-mg dose of the alpha-glucosidase inhibitor Acarbose ingested with the sucrose load was also investigated. "Naturally labeled [13C] sucrose" was used to follow the conversion to expired-air CO2 of the sugar ingested by isotope-ratio mass spectrometry. Circulating hormone and metabolite data were obtained in nine subjects, and indirect calorimetry and stable isotope methodology were applied to six of them. Under placebo, 93 +/- 4 g sucrose were entirely oxidized during the 4 h of exercise, total carbohydrate utilization was 235 +/- 14 g, endogenous carbohydrate utilization was 142 +/- 13 g, and total lipid oxidation was 121 +/- 7 g. A single oral dose of 100 mg Acarbose ingested with the sucrose load did not significantly modify total carbohydrate (239 +/- 2 g/4 h) or lipid (122 +/- 6 g/4 h) oxidation. In contrast, sucrose oxidation was reduced to 53 +/- 6 g/4 h and endogenous carbohydrate utilization increased to 186 +/- 7 g/4 h. Reduction of the rises in blood glucose and fructose and of the increases in plasma insulin and C peptide under Acarbose confirmed these effects, whereas lower circulating levels of alanine suggested a higher rate of gluconeogenesis. These data show that a 100-g glucose load ingested soon after initiation of exercise is a perfect available metabolic substrate.(ABSTRACT TRUNCATED AT 250 WORDS)
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PMID:Utilization of oral sucrose load during exercise in humans. Effect of the alpha-glucosidase inhibitor acarbose. 353 Aug 58

The role of thyroxine and insulin in the regulation of proliferation and differentiation of the immature duodenal epithelium of the fetal mouse was investigated using an organ culture method with a serum-free medium. Thyroxine (10 nM) stimulates specifically the activity of maltase. Insulin (125 mU/mL) remains without effect on the maturation of all hydrolytic functions studied. Each hormone significantly increases the percentages of brush border enzyme activities liberated in the medium and reduces the amount of glucose released in the medium. In the presence of dexamethasone (76 nM) the effect of thyroxine on maltase activity is still observed. Finally, thyroxine and insulin do not modify the labelling index in the duodenal crypts of the explants in the presence or absence of dexamethasone. These findings indicate that thyroxine and insulin can act directly on the development of the fetal mouse duodenum at the end of gestation. Nevertheless, their implication in prenatal development of the gut functions appears to be of minor importance.
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PMID:Role of thyroxine and insulin on the development of the fetal mouse duodenum in organ culture. 353 89

Miglitol is an alpha-glucosidase inhibitor which lowers blood glucose and insulin concentrations in healthy volunteers after a starch meal. It also lowers blood glucose concentrations after a starch meal in patients with non-insulin-dependent diabetes mellitus, but under these circumstances insulin is unaffected. We have studied the effect of miglitol after a glucose load in six healthy male volunteers. Although one would expect an alpha-glucosidase inhibitor to have no effect on blood glucose concentrations after a glucose load, miglitol produced a significant decrease in blood glucose concentrations after the absorption peak. This could be due to enhancement of insulin effects or to depression of anti-insulin factors.
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PMID:Miglitol may have a blood glucose lowering effect unrelated to inhibition of alpha-glucosidase. 354 25


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