Several cardiovascular risk factors (dyslipidaemia, hypertension, glucose intolerance, hypercoagulability, obesity, hyperinsulinaemia and low-grade inflammation) cluster in the insulin resistance syndrome. Treatment of these individual risk factors reduces cardiovascular complications. However, targeting the underlying pathophysiological mechanisms of the insulin resistance syndrome is a more r...

OBJECTIVE Thiazolidinediones and insulin are associated with a higher risk of fractures in type 2 diabetic patients. Incretin hormones increase bone density in experimental models, but the effect of dipeptidyl peptidase-4 (DPP-4) inhibitors on bone fractures has not been reported so far. RESEARCH DESIGN AND METHODS A meta-analysis was performed including all randomized clinical trials with a ...

BACKGROUND Patients with type 2 diabetes have a 40% increased risk of bladder cancer. Thiazolidinediones, especially pioglitazone, may increase the risk. We conducted a systematic review and meta-analysis to evaluate the risk of bladder cancer among adults with type 2 diabetes taking thiazolidinediones. METHODS We searched key biomedical databases (including MEDLINE, Embase and Scopus) and so...

Human carboxylesterase (CES) 1A is responsible for the biotransformation of angiotensin-converting enzyme (ACE) inhibitors such as imidapril and temocapril. Because antidiabetic or antihyperlipidemic drugs are often coadministered with ACE inhibitors in clinical pharmacotherapy, the inhibitory effect of these drugs on CES1A1 enzyme activity was investigated. In addition, the inhibitory effect o...

Betaine hydrochloride (BHC), as an ionic salt was found to be an efficient and recyclable catalyst for the one-pot synthesis of 4-thiazolidinediones. The methodology of study was achieved by one-pot condensation of aromatic aldehydes, aromatic amine and mercaptoacetic acid in the presence of betaine hydrochloride (BHC) at reflux temperature in ethanol as solvent. The efficiency of Betaine hydro...

The molecular mechanism by which hypolipidemic fibrates and antidiabetic thiazolidinediones exert their hypotriglyceridemic action are discussed. Increased activity of lipoprotein lipase (LPL), a key lipolytic enzyme, and decreased levels of apolipoprotein C-III (apo C-III) seem to explain the hypotriglyceridemic effects of compounds. Both fibrates and thiazolidinediones exert their action by a...

Thiazolidinediones, insulin-sensitizing agents, have been reported to increase glucose uptake along with the expression of glucose transporters in adipocytes and cardiomyocytes. Recently, we have further suggested that the translocation of GLUT4 is stimulated by thiazolidinediones in L6 myocytes. However, the direct effects of thiazolidinediones on translocation of glucose transporters have not...

The enzyme dipeptidyl peptidase-4 (DPP-4) prevents the inactivation of glucagon-like peptide-1 (GLP-1). Since GLP-1–based therapy is a promising novel treatment of type 2 diabetes, the strategy to inhibit the enzyme has been explored. Several DPP-4 inhibitors are in clinical development; these are orally active and increase levels of active GLP-1, which in turn increases insulin secretion and r...

Thiazolidinediones are used to treat type 2 diabetes mellitus because they decrease plasma glucose, insulin, triglyceride, and fatty acid levels. Thiazolidinediones are agonists for peroxisome proliferator-activated receptor gamma, a nuclear receptor that is highly expressed in fat tissue. We identify glyceroneogenesis as a target of thiazolidinediones in cultured adipocytes and fat tissues of ...

Type 2 diabetes is characterised by a gradual decline in glycaemic control and progression from oral glucose-lowering monotherapy to combination therapy and exogenous insulin therapy. Functional decline of the insulin-secreting beta-cells is largely responsible for the deterioration in glycaemic control. Preservation of beta-cell functionality, in addition to maintaining glycaemic control and r...