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)

Antiobesity and antidiabetic actions of the alpha-glucosidase inhibitor AO-128 were examined using genetically obese-diabetic rats, Wistar fatty. Ten-week-old, male fatty rats were kept on CE-2 diet containing 10 or 25 ppm of AO-128 for 4 weeks. The average drug intake was calculated to be 0.74 or 1.78 mg/kg/day from the average food intake, respectively. The intestinal maltase and sucrase activities were decreased by AO-128 in a dose-related fashion. Food intake of fatty rats treated with AO-128 was decreased throughout the experiment. This decrease in food intake could hardly be explained only by diarrhea which occurred for the first 5 days of the administration of AO-128. AO-128 normalized hyperglycemia and markedly reduced hypertriglyceridemia and hyperinsulinemia in fatty rats. In addition, AO-128 decreased body weight gain, food efficiency, epididymal adipose tissue weight, carcass weight, and body fat deposition. These findings indicate that AO-128 may be useful for treating human obesity and diabetes.
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PMID:AO-128, alpha-glucosidase inhibitor: antiobesity and antidiabetic actions in genetically obese-diabetic rats, Wistar fatty. 869 66

Prophylactic insulin treatment prevents the development of hyperglycemia in animal models of insulin-dependent diabetes mellitus. Acarbose is a new antidiabetic drug which improves hyperglycemia by inhibiting alpha-glucosidase. In the present study, we determined the preventive effect of acarbose against multiple low-dose streptozotocin (MLDSTZ)-induced diabetes mellitus. The male ICR mice were fed acarbose (40 mg/100 g) containing powdered chow before the start of STZ administration. The mice were sacrificed at 3 and 10 days after the final STZ injection. MLDSTZ decreased serum immunoreactive insulin (IRI) levels and increased plasma glucose levels. Acarbose administration tended to decrease plasma glucose and serum IRI levels were significantly reduced in vehicle-treated mice. Acarbose administration significantly attenuated the degree of inflammation and destruction in pancreatic islets after MLDSTZ administration. In conclusion, acarbose-induced attenuation of acute hyperglycemia following MLDSTZ partially prevents the severity of pancreatic islet damage.
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PMID:Acarbose partially prevents the development of diabetes mellitus by multiple low-dose streptozotocin administration. 887 71

Since impaired glucose tolerance (IGT) is a major risk factor for non-insulin-dependent diabetes mellitus (NIDDM), some kinds of intervention aiming to prevent or to delay the onset of NIDDM in subjects with IGT might be considered. Besides life style modification, drug therapy which could correct insulin deficiency and insulin resistance, might prevent progression to NIDDM. One agent is an alpha-glucosidase inhibitor, which delays the absorption of glucose from the intestine. The resulting decrease in postprandial hyperglycemia and hyperinsulinemia could theoretically decrease insulin resistance in IGT subjects and, it is hoped, prevent or delay progression to NIDDM. Metformin, an antihyperglycemic drug of the biguanide class, may be effective in subjects with IGT by reducing hepatic glucose output, enhancing insulin sensitivity, or through other mechanisms such as weight loss. New insulin sensitizers, such as troglitazone and pioglitazone, improve insulin-mediated glucose disposal by enhancing tissue sensitivity to the actions of insulin and reversing the insulin resistance, characteristic of NIDDM. Sulfonylureas might be another candidates of drug intervention to IGT whose insulin secretory abilities are markedly reduced. As far as the question, "Can NIDDM be prevented or delayed?" is concerned, a prospective study using life style modification or above-mentioned drugs, should be performed on long-term basis.
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PMID:[Drug therapy in subjects with impaired glucose tolerance]. 891 39

Alpha-glucosidase inhibitor can suppress postprandial hyperglycemia by delaying the absorption of carbohydrates in the intestine, and may be useful in obese patients with non-insulin-dependent diabetes mellitus (NIDDM) and preserved insulin secretion. We encountered an obese elderly patient with NIDDM in whom gait disturbance had developed after cerebral hemorrhage and who suffered from ileus after treatment with voglibose. The patient had received voglibose which is reported to cause fewer abdominal symptoms than acarbose, for 15 days. The patient, a 63-year-old woman, was given a diagnosis of NIDDM in February 1995, and was treated with a sulfonylurea agent. However, her glycemic control remained poor and she was admitted to our hospital in April 1995. Her body mass index was 30.5 kg/m2 and laboratory investigation revealed a fasting plasma glucose level of 211 mg/dl, a postprandial (2 h) plasma glucose level of 288 mg/dl, HbAlc of 9.9%, a fasting insulin level of 9 microU/ml, urinary C-peptide excretion of 95.7 micrograms/ day, and an coefficient of variation of R-R value of 2.1%. Fifteen days after glibenclamide was replaced by to voglibose, abdominal pain, nausea, constipation, and ausculatory sounds of gurgling developed, and niveau were noted on an abdominal roentgenogram which indicated that simple ileus had developed. Voglibose was discontinued and the patient was treated with an enema and hot air. She recovered from simple ileus on the next day. This patient had had two abdominal surgeries and a cerebral hemorrhage, and her daily physical activities were limited, which might have contributed to ileus. In elderly patients with NIDDM, a history of abdominal surgery and the amount of daily exercise must be considered when deciding whether or not to give alpha-glucosidase inhibitors.
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PMID:[Occurrence of ileus after voglibose treatment in an elderly diabetic patient with gait disturbance caused by cerebral hemorrhage]. 892

Postprandial hyperglycemia and elevations in glycated hemoglobin A1c (HbA1c) levels have been associated with long-term complications of diabetes. Because not all patients with type II, or non-insulin-dependent diabetes mellitus (NIDDM), respond adequately to diet, exercise, or treatment with oral sulfonylurea drugs, alternate therapies have been investigated. Acarbose, the first alpha-glucosidase inhibitor available in the United States, exerts its activity in the gastrointestinal tract. By reversibly inhibiting the enzymatic cleavage of complex carbohydrates to simple absorbable sugars, treatment with acarbose results in a reduction in postprandial blood glucose and, subsequently, reductions in HbA1c levels. Acarbose may be given as monotherapy with diet or in combination with diet and a sulfonylurea drug. The results of several controlled clinical studies conducted in the United States are reviewed here. Acarbose, in doses of up to 100 mg three times daily for periods of up to 16 weeks, was statistically significantly superior to placebo with respect to the mean reduction in HbA1c levels and mean 1-hour postprandial glucose levels. Adverse events were nonsystemic and primarily gastrointestinal in nature. Acarbose represents a new approach to the management of NIDDM, modulating gastrointestinal carbohydrate metabolism to control postprandial hyperglycemia and to maximize long-term glycemic control.
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PMID:Acarbose: a review of US clinical experience. 908 5

The present study was conducted in order to examine the effect of acarbose, a potent alpha-glucosidase inhibitor, on renal function in rats with mild streptozotocin-diabetes. Male Wistar rats were made mildly diabetic by intravenous injection of streptozotocin (40 mg/kg) and were supplied a standard solid chow containing 0.1% acarbose for 8 weeks. Diabetic rats showed mild hyperglycemia under non-fasting condition and their urine albumin excretion (UAE) rate was markedly increased compared to non-diabetic control rats, while acarbose treatment resulted in a significant suppression of blood glucose level and UAE in diabetic rats. Examination by electron microscope revealed that the number of anionic sites in the lamina rara externa per 1000 nm of glomerular basement membrane (GBM) was significantly decreased in diabetic rats compared to control value (15.7 +/- 0.9 vs. 20.9 +/- 0.3 P < 0.001), whereas, significant recovery (19.6 +/- 0.6 P < 0.01) was observed after 8 weeks of acarbose treatment. In conclusion, acarbose treatment suppressed blood glucose level of mildly-insulin deficient animal model without insulin treatment and prevented from a reduction in the number of anionic sites in GBM which might ameliorate an increased permeability of GBM leading to albuminuria.
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PMID:Effect of an alpha-glucosidase inhibitor on glomerular basement membrane anionic sites in streptozotocin induced mildly diabetic rats. 927 79

Type 2 diabetes mellitus is a common, chronic disease affecting nearly 6% of the adult US population. It remains a leading cause of morbidity and mortality in Wisconsin as well as the country. Multiple lines of evidence show that controlling blood glucose in patients with type 2 diabetes can significantly decrease the development of and/or progression of microvascular complications as well as the macrovascular complications of diabetes. There are now four different classes of oral medications which are available to treat diabetes-sulfonylureas, biguanides, thiazolidinediones, and alpha-glucosidase inhibitors. Each class works differently to treat the underlying defects of diabetes which include impaired insulin secretion, insulin resistance and exaggerated postprandial hyperglycemia. This article will compare and contrast the different agents available, including appropriate use of each agent as monotherapy and in combination therapy. It will also discuss use of insulin in the patient who has failed oral therapy. Rational use of these tools, tailored for the individuals metabolic abnormalities, should allow for good glycemic control in the majority of patients with type 2 diabetes mellitus. Relaxation, massage, opium, and moderate exercise were among the recommended options for treatment of diabetes mellitus nearly 100 years ago. In the late nineteenth century, diabetes was a poorly characterized disorder, which was increasing in prevalence even at that time. Today, the underlying defects contributing to the development of type 2 diabetes are better understood, and include peripheral insulin resistance, relative pancreatic beta-cell insufficiency, increased hepatic glucose output, and an exaggerated postprandial glucose excursion. However, despite our better understanding of the disease, the prevalence of type 2 diabetes continues to increase in the US, now afflicting over 6% of the population. As our population ages and the proportion of obese people increases, we can expect to see a marked increase in the prevalence of diabetes in the future. Fortunately, our treatment options for type 2 diabetes have expanded remarkably within the last few years. Along with these new treatment options comes the exciting, although likely expensive, possibility of prevention of type 2 diabetes in at risk individuals.
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PMID:Therapy for type 2 diabetes mellitus. 954 Apr 50

The hypoglycemic effect and the alpha-glucosidase activity inhibition of acarbose (AC:alpha-glucosidase inhibitor) were investigated in normal and KK-Ay mice, an animal model of noninsulin-dependent diabetes mellitus (NIDDM). AC improved hyperglycemia after an oral administration of maltose or sucrose, dose dependently in normal mice (1, 10, and 50mg/kg body weight) and in KK-Ay mice (50mg/kg). Furthermore, AC (50mg/kg) significantly inhibited maltase and sucrase activities in the small intestines of normal and KK-Ay mice (inhibitory efficacy: sucrase > maltase). The enzymatic inhibition in KK-Ay mice is stronger than in normal mice. However, AC (50 mg/kg) did not suppress the blood glucose in oral lactose tolerance and did not inhibit the lactase activity in either normal or KK-Ay mice. These findings indicate that the AC effect on the inhibition of alpha-glucosidase activity is selective for sucrase and maltase in normal and NIDDM mice.
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PMID:Effect of acarbose (alpha-glucosidase inhibitor) on disaccharase activity in small intestine in KK-Ay and ddY mice. 974 58

The effect of acarbose, an alpha-glucosidase inhibitor, on postprandial glucose and lipid metabolism was investigated in patients with type 2 diabetes mellitus. Twenty patients (10 men and 10 women) with type 2 diabetes mellitus were studied. A test meal was taken with or without 100 mg of acarbose. The levels of plasma glucose, and serum immunoreactive insulin, lipids, apolipoproteins, and remnant-like particle cholesterol were investigated. Acarbose inhibited the postprandial increase of both plasma glucose and serum immunoreactive insulin. Acarbose also significantly suppressed the increase of serum triglycerides at 60, 90, and 120 min (P < 0.05 to P < 0.01), and the increase of serum remnant-like particle cholesterol at 60 and 120 min (P < 0.05). Acarbose inhibited the postprandial decline of apolipoprotein C-II, and decreased the postprandial serum apolipoprotein C-III level. These results suggest that acarbose may improve postprandial hyperlipidemia as well as postprandial hyperglycemia in patients with type 2 diabetes mellitus.
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PMID:Effect of acarbose on postprandial lipid metabolism in type 2 diabetes mellitus. 976 72

Diabetes mellitus is the most common endocrine disease, accounting for over 200 million people affected worldwide. It is characterized by a lack of insulin secretion and/or increased cellular resistance to insulin, resulting in hyperglycemia and other metabolic disturbances. People with diabetes suffer from increased morbidity and premature mortality related to cardiovascular, microvascular and neuropathic complications. The Diabetes Control and Complication Trial (DCCT) has convincingly demonstrated the relationship of hyperglycemia to the development and progression of complications and showed that improved glycemic control reduced these complications. Although the DCCT exclusively studied patients with Type 1 diabetes, there is ample evidence to support the belief that the same relationship between metabolic control and clinical outcome exists in patients with Type 2 diabetes. Therefore, a major effort should be made to develop and implement more effective treatment regimes. This article reviews those novel drugs that have been recently introduced for the management of Type 2 diabetes, or that have reached an advanced level of study and will soon be proposed for preliminary clinical trials. They include: (i) compounds that promote the synthesis/secretion of insulin by the beta-cell; (ii) inhibitors of the alpha-glucosidase activity of the small intestine; (iii) substances that enhance the action of insulin at the level of the target tissues; and (iv) inhibitors of free fatty acid oxidation.
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PMID:Novel therapeutic strategies for the treatment of type 2 diabetes. 981 70


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