Study on Gluco-Regulatory Potential of Glimepiride Sulfonamide Using In silico, In Vitro and In Vivo Approaches

Abstract

Glimepiride sulfonamide (GS) is a drug intermediate to synthesize glimepiride (antidiabetic drug). We hypothesized that GS exerts gluco-regulatory effect because GS is comprised of the structural components of dipeptidyl peptidase-IV (DPP-IV) inhibitors sitagliptin and DPP-728and glimepiride (sulfonylurea based antidiabetic drug).We analyzed the drug-likeness and docking efficiency of GS with DPP-IV using in silico tools. Also DPP-IV inhibition assays were conducted in vitro. Gluco-regulatory potential and parameters of drug safety were evaluated on normal euglycemic and streptozotocin (STZ) induced diabetic rats. We observed strong drug-likeness and DPP-IV binding efficiency of GS. Similarly, profound DPP-IV inhibition was also observed in vitro. Studies on euglycemic and STZ induced diabetic rats revealed antidiabetic potential for GS without significant change in the studied toxicological parameters. Glimepiride sulfonamide has antidiabetic potential mainly through DPP-IV inhibition, but also through insulin stimulation and alpha-amylase inhibition.

Glucose Homeostatic and Pancreas Protective Potential of Tecomella Undulata Root Extract in Streptozotocin Induced Diabetic Rats .

“…Hyperglycemia and non-functional pancreatic β-cell are considered as a diabetic pathological condition from primary description [30,31]. Whereas there are several kinds of pharmacological approaches for …”

Improvements in HOMA indices and pancreatic endocrinal tissues in type 2-diabetic rats by DPP-4 inhibition and antioxidant potential of an ethanol fruit extract of Withania coagulans 

“…Basic parameters: The serum parameters measured by using standard methods included glucose [24], total protein [25], insulin [26], total cholesterol [27], HDL-cholesterol [28], triglyceride [29], SGOT [30], SGPT [30], urea [31], uric acid [32], and creatinine [33]. The lipid pro le (total cholesterol, HDL-cholesterol, LDL-cholesterol, Triglyceride and VLDL -cholesterol) was assessed following Friedewald's formula [34][35][36].…”