Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts:   Target Concepts:
Query: EC:3.2.1.20 (alpha-glucosidase)
 4,237 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Non-insulin-dependent diabetes mellitus (NIDDM, type 2 diabetes) is a heterogeneous disease resulting from a dynamic interaction between defects in insulin secretion and insulin action. There are various pharmacological approaches to improving glucose homeostasis, but those currently used in clinical practice either do not succeed in restoring normoglycaemia in most patients or fail after a variable period of time. For glycaemic regulation, 4 classes of drugs are currently available: sulphonylureas, biguanides (metformin), alpha-glucosidase inhibitors (acarbose) and insulin, each of which has a different mode and site of action. These standard pharmacological treatments may be used individually for certain types of patients, or may be combined in a stepwise fashion to provide more ideal glycaemic control for most patients. Adjunct treatments comprise a few pharmacological approaches which may help to improve glycaemic control by correcting some abnormalities frequently associated with NIDDM, such as obesity (serotoninergic anorectic agents) and hyperlipidaemia (benfluorex). There is intensive pharmaceutical research to find new drugs able to stimulate insulin secretion (new sulphonylurea or nonsulphonylurea derivatives, glucagon-like peptide-1), improve insulin action (thiazolidinediones, lipid interfering agents, glucagon antagonists, vanadium compounds) or reduce carbohydrate absorption (miglitol, amylin analogues, glucagon-like peptide-1). Further studies should demonstrate the superiority of these new compounds over the standard antidiabetic agents as well as their optimal mode of administration, alone or in combination with currently available drugs.
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PMID:Drug treatment of non-insulin-dependent diabetes mellitus in the 1990s. Achievements and future developments. 927

Most patients with type 2 (non-insulin-dependent) diabetes mellitus require pharmacotherapy, initially as monotherapy and subsequently in combination, as adjuncts to diet and exercise. Exogenous insulin is ultimately required in a substantial proportion, reflecting the progressive natural history of the disease. Sulphonylureas and biguanides have been employed for over 4 decades as oral antidiabetic agents, but they have a limited capacity to provide long term glycaemic control and can cause serious adverse effects. Thus, more efficacious and tolerable antidiabetic agents are required. Recent years have witnessed the introduction of agents with novel modes of action, that is, the alpha-glucosidase inhibitors acarbose and miglitol (which reduce postprandial hyperglycaemia) and the first of the thiazolidinedione insulinsensitising drugs--troglitazone and rosiglitazone. Although the former has been withdrawn in some countries due to adverse effects, another 'glitazone' pioglitazone is expected to be approved in the near future. Other recently introduced drugs include glimepiride and the meglitinide insulin secretagogue, repaglinide. Attention is also focusing increasingly on combination therapy using insulin together with sulphonylureas, metformin or troglitazone. Rapid-acting insulin analogues are now being used as alternatives to conventional insulins; their role in the management of type 2 diabetes mellitus is presently uncertain but reports of a reduced frequency of hypoglycaemia are encouraging. The development of new drugs aims to counter the principal metabolic defects of the disorder, respectively, relative insulin deficiency and insulin resistance. Novel classes of rapid-acting secretagogues under evaluation include the morphilinoguanide BTS 67582 and the meglitinides mitiglinide (KAD 1229) and senaglinide (A-4166). Succinate ester derivatives represent a potential novel approach to improving beta-cell function through enhancement of insulin biosynthesis and secretion. Enhancement of nutrient-induced insulin secretion is a mechanism with several putative targets within the beta-cell; potentiators of insulin secretion include glucagon-like peptide-1 and its analogues, phosphodiesterase inhibitors and the imidazoline derivative PMS 812 (S 21663). The amylin agonist pramlintide slows gastric emptying and suppression of glucagon secretion. Non-thiazolidinedione insulin-sensitising agents include the gamma-receptor agonist G 1262570X (GG 570) and D-chiro-inositol. Insulin analogues with prolonged action and inhaled insulin preparations are also under investigation. Insulin-mimetic agents include organic vanadium compounds. Whether newer agents will offer clinically relevant efficacy and tolerability advantages over existing therapies remains to be determined.
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PMID:Recent developments and emerging therapies for type 2 diabetes mellitus. 1082 Jun 47

Five classes of oral hypoglycaemic drugs and two trace minerals used to treat diabetes mellitus in humans are reviewed and current knowledge on the use of these drugs in diabetic dogs and cats is presented. Oral sulphonylurea drugs stimulate insulin secretion and have been used successfully to treat diabetes in cats but not dogs. Preliminary studies evaluating the efficacy of the biguanide, metformin, in diabetic cats have not been promising. Pharmacokinetic studies have been performed in healthy cats, but clinical studies evaluating the efficacy of the insulin-sensitising drugs, thiazolidinediones, have not been reported. Treatment with the alpha-glucosidase inhibitor, acarbose, improved control of glycaemia in diabetic dogs; similar studies have not been reported in cats. Although chromium picolinate did not improve control of glycaemia in diabetic dogs, vanadium has improved control of the abnormality in diabetic cats.
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PMID:Oral medications for treating diabetes mellitus in dogs and cats. 1110 86

The pharmacological approaches to the treatment of type 2 diabetes mellitus were reviewed. Special attention was paid to the new therapeutic agents that are able to decrease plasma glucose levels. The possible mechanisms of the hypoglycemic effects are discussed. Briefly, repaginide, nateglinede and alpha-glucosidase inhibitors prevent postprandial hypoclycemia while thiazaolidinediones improve the sensitivity to insulin and vanadium compounds act as an insulin action enhancer.
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PMID:[Modern approaches to pharmacotherapy of diabetes mellitus type II]. 1250 8

The synthesis, spectroscopic, enzyme-inhibition, and free-radical-scavenging properties of a series of vanadium(IV) complexes, compounds 1-10, were investigated. These complexes exhibit a dimeric structure with hydrazide ligands coordinated in a bidentate fashion. All complexes are stable in the solid state, but exhibit varying degrees of stability in solution. In coordinating solvent such as DMSO, stepwise binding of two solvent molecules at the 6th positions trans to the V double bond O bond of the dimeric unit is observed. The dimeric compounds are converted to monomeric species in which both solvent molecules and the hydrazide ligands are coordinated to the V(IV) center. The free hydrazide ligands 11-20 were inactive against alpha-glucosidase, but the V(IV) complexes showed varying degrees of inhibition, depending on the type of ligand. The DPPH-radical-scavenging activities of 1-20 were determined, which indicated that steric and/or electronic effects responsible for changes in geometry play important roles in terms of antioxidant potential.
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PMID:Synthesis, spectroscopy, and biological properties of vanadium(IV)-hydrazide complexes. 1820 28

Vanadium compounds are being investigated as potential therapeutic agents in the treatment of many health problems, primarily diabetes. We aimed to provide the effect of N(1)-4-hydroxysalicylidene-N(4)-salicylidene-S-methyl-isothiosemicarbazidato-oxovanadium(IV) (VOL) on small intestinal injury in experimental male diabetic rats. Four groups were created of 3.0-3.5-month-old rats. The rats were made diabetic by a single dose of streptozotocin (STZ) at 65 mg/kg and grouped as follows: control animals, VOL-given control animals, STZ-induced diabetic animals and STZ-induced diabetic animals given VOL. A daily dose of 0.2 mM/kg vanadium complex was administered orally for 12 days after the inducement of diabetes. On the 12th day, small intestine tissue samples were taken. According to the data obtained from the biochemical analysis, reduced glutathione (GSH) level, catalase (CAT), glutathione peroxidase (GPx), glutathione-S-transferase (GST), superoxide dismutase (SOD), Na+/K+-ATPase and paraoxanase (PON) activities were increased, whereas sialic acid (SA), xanthine oxidase (XO) and disaccharidases (maltase and saccharidase) activities were decreased in the small intestine tissue of VOL-treated diabetic rats. Microscopic examinations revealed a remarkable decrease in the mucosal necrotic areas, discontinuity in the brush border, deterioration of the villi integrity and oedema inside the villi, but with a mild decrease in the inflammatory cells, deterioration and loss of integrity of the gland in the small intestine of VOL-treated diabetic rats. Moreover, VOL treatment markedly decreased the proliferation of villus cells and especially inflammatory cells in the small intestine of diabetic rats. According to the obtained data, the administration of VOL is a potentially convenient strategy to reducing small intestine injury in diabetic rats.
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PMID:Protective Effects of an Oxovanadium(IV) Complex with N2O2 Chelating Thiosemicarbazone on Small Intestine Injury of STZ-Diabetic Rats. 3281 91