Home  麻辣烫主人  我的博客   LOMO空间  资源下载   在线视听  在线翻译  宝贝计划   减肥方法  几米绘本

葡萄糖苷酶 抑制剂 Glucosidase Inhibitor

Mannosidase   AGE   Tyrosinase   Arrestin    TRAF6    Alzheimer Diseases    Diabetes   TCM    Parkinson

α-葡萄糖苷酶（α-glucosidase，EC 3. 2. 1. 20）是一类能够从含有α-葡萄糖苷键底物的非还原端催化水解α-葡萄糖基的酶的总称、包括麦芽糖酶（α-D-glucosidase glucohydrolase EC 3. 2. 1. 20）、异麦芽糖酶（dextrin 6-α-D-glucanchydolase，EC 3. 2. 1. 10）、蔗糖酶（sucrase，α-D-glucohydrolase，EC 3. 2. 1. 48）和海藻糖酶（trehalase，α-trehalase glucohydrolase，EC 3. 2. 1. 28）等，这些酶首先从猪肠粘膜中分离得到，随后从人体组织中也制备得到。α-葡萄糖苷酶广泛分布于生物体中，在机体的代谢过程中起着非常重要的作用，参与食物消化、糖蛋白的生物合成，多糖及糖复合物的合成与分解代谢等许多生物过程。如果这些α-糖苷酶的酶活力受到了影响，体内的正常代谢就会破坏。糖尿病、肥胖症、高血脂、炎症、癌变、免疫反应和病毒感染等都和细胞表面的复合糖质有密切关系，而复合糖质的形成又和α-葡萄糖苷酶的存在有一定的联系。因此，开发出适当的α-葡萄糖苷酶抑制剂类药物，调节α-葡萄糖苷酶的活性，可以治疗很多疾病，具有广阔的应用前景。

中药材拉丁文     免费文献资源      生物医药招聘      真空爱情记录     每周Science

1. Dibutyl phthalate, an alpha-glucosidase inhibitor from Streptomyces melanosporofaciens.
Dibutyl phthalate was found to inhibit alpha-glucosidase, alpha- and beta-mannosidases and beta-glucosidase, in that order of inhibition strength. Dibutyl phthalate was shown to be a reversible, slow-binding, noncompetitive inhibitor of yeast alpha-glucosidase with a K(i) value of 3.9 microM ... Read More »
» Published in J Biosci Bioeng. 2000;89(3):271-3.

2. alpha-Glucosidase inhibitors have a prolonged antiviral effect against hepatitis B virus through the sustained inhibition of the large and middle envelope glycoproteins.
Previous work has shown that the secretion of enveloped hepatitis B virus (HBV) DNA and the HBV middle envelope protein (MHBs) are sensitive to glucosidase inhibition. Here, it is shown that HBV DNA secretion remains depressed after the removal of the glucosidase inhibitor and long after glucosidase function returns to normal. For example, glyco-processing and the secretion of alpha-1 anti-trypsin returned to normal within 3 h of the removal of the glucosidase inhibitor. In contrast, the secretion of HBV did not return to normal for more than 7 days after the removal of the inhibitor. ... Read More »
» Published in Antivir Chem Chemother. 2006;17(5):259-67.

3. Long-Term Effect Of Alpha-Glucosidase Inhibitor On Late Dumping Syndrome
Dumping syndrome commonly occurs after gastrectomy. The late dumping, which is one of the dumping syndromes, is due to postprandial hypoglycaemia caused by an excessive insulin secretion after a sharp rise in plasma glucose. Several treatments, including operation, dietary fibre and somatostatin, have been attempted to relieve dumping symptoms. These treatments take effect through modulation of plasma insulin and glucose levels, but their efficacy is still under consideration. Alpha-glucosidase inhibitor attenuates the postprandial increase of plasma glucose levels and is widely used for ... Read More »
» Published in J Gastroenterol Hepatol. 1998 Dec;13(12):1201-6.

4. Synthesis of andrographolide derivatives: a new family of alpha-glucosidase inhibitors.
Andrographolide (1), the cytotoxic agent of the plant Andrographis paniculata, was subjected to semi-synthetic studies leading to a series of new derivatives, a novel family of glucosidase inhibitors. Nicotination of 3,19-hydroxyls in 15-alkylidene andrographolide derivatives (9) was favorable to alpha-glucosidase inhibition activity. Among them, 15-p-chlorobenzylidene-14-deoxy-11,12-didehydro-3,19-dinicotinateandrographolide (11c) was a very potent inhibitor against alpha-glucosidase with an IC50 value of 6 microM. However, all compounds concerned for beta-glucosidase showed no inhibition. ... Read More »
» Published in Bioorg Med Chem. 2007 Jun 15;15(12):4247-55. Epub 2007 Mar 24.

5. No Effect Of An Alpha-Glucosidase Inhibitor On Glucose Metabolism In Patients With Non-Insulin-Dependent Diabetes Mellitus And Low Function Of Pancreatic Beta Cells
Twenty patients with non-insulin-dependent diabetes mellitus who had been receiving appropriate dietary treatment for 3 months but whose glucose metabolism needed further improvement were treated with an alpha-glucosidase inhibitor. Treatment with the alpha-glucosidase inhibitor (0.6 mg/day) for 4 weeks, had no significant effect on blood glucose levels 2 h after breakfast or on glycosylated haemoglobin levels ... Read More »
» Published in J Int Med Res. 1995 Jul-Aug;23(4):294-8.

6. Effect Of An Alpha-Glucosidase Inhibitor Combined With Sulphonylurea Treatment On Glucose Metabolism In Patients With Non-Insulin-Dependent Diabetes Mellitus
Ten patients with non-insulin-dependent diabetes mellitus who were being treated with a sulphonylureal compound but whose glucose metabolism needed further improvement were given a combination of their usual sulphonylurea treatment and an alpha-glucosidase inhibitor. Treatment with the alpha-glucosidase inhibitor (0.6 mg/day), in addition to glibenclamide (7.5 mg/day in two patients; 5.0 mg/day in four; 2.5 mg/day in one) or tolbutamide (500 mg/day in three patients) for 4 weeks, improved hyperglycaemia after meals from 237-247 mg/dl to 192 mg/dl, and reduced glycosylated haemoglobin levels ... Read More »
» Published in J Int Med Res. 1995 Jul-Aug;23(4):279-83.

7. Stabilising normal and mis-sense variant alpha-glucosidase.
alpha-Glucosidase (EC 3.2.1.3) is a lysosomal enzyme that hydrolyses alpha-1,4- and alpha-1,6-linkages of glycogen to produce free glucose. A deficiency in alpha-glucosidase activity results in glycogen storage disorder type II (GSD II), also called Pompe disease. Here, d-glucose was shown to be a competitive inhibitor of alpha-glucosidase and when added to culture medium at 6.0 g/L increased the production of this protein by CHO-K1 expression cells and stabilised the enzyme activity. D-Glucose also prevented alpha-glucosidase aggregation/precipitation and increased protein yield in a modified ... Read More »
» Published in FEBS Lett. 2006 Aug 7;580(18):4365-70. Epub 2006 Jul 10.

8. Probing the aglycon binding site of a beta-glucosidase: a collection of C-1-modified 2,5-dideoxy-2,5-imino-D-mannitol derivatives and their structure-activity relationships as competitive inhibitors.
A range of new C-1 modified derivatives of the powerful glucosidase inhibitor 2,5-dideoxy-2,5-imino-D-mannitol has been synthesised and their biological activities probed with the beta-glucosidase from Agrobacterium sp. Ki values are compared with those of previously prepared close relatives. Findings suggest dramatic effects exerted by the aglycon binding site on substrate/inhibitor binding ... Read More »
» Published in Bioorg Med Chem. 2004 Jul 1;12(13):3485-95.

9. Effect Of Alpha-Glucosidase Inhibitor In Combination With Sulphonylurea Compounds On Lipid Profile In Patients With Non-Insulin-Dependent Diabetes Mellitus
The effects of administration of an alpha-glucosidase inhibitor and a sulphonylurea compound on lipid profile were investigated in patients with non-insulin-dependent diabetes mellitus, (NIDDM) previously treated with sulphonylurea compounds alone, but in whom metabolic control was inadequate. A group of patients (n = 10) were treated with the alpha-glucosidase inhibitor at a dose of 0.2 mg, three times daily, for 4 weeks. Treatment significantly reduced the post-prandial glucose level and the serum total cholesterol level. In addition, there were non-significant reductions in the triglyceride ... Read More »
» Published in J Int Med Res. 1995 Nov-Dec;23(6):492-6.

10. The Effect Of A Very Low Dose Of Tolbutamide Combined With An Alpha-Glucosidase Inhibitor In Non-Insulin-Dependent Diabetes Mellitus
The effect of adding a very low dose of a sulphonylurea (tolbutamide) to the treatment of 10 patients with noninsulin-dependent diabetes mellitus (NIDDM) was investigated. Patients took 0.1 mg tds of an alpha-glucosidase inhibitor orally for 8 weeks, and 50 mg tds of the sulphonylurea, tolbutamide, for the last 4 weeks of this period. The glycosylated haemoglobin level was significantly reduced during the combined treatment period compared with the level after treatment with alpha-glucosidase inhibitor alone (P = 0.035), although not compared with the pretreatment level. There were no ... Read More »
» Published in J Int Med Res. 1996 Sep-Oct;24(5):433-7.