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
Keywords: Alanine amino transaminase, alpha-amylase, aspartate aminotransferase, diabetes, dipeptidyl peptidase-IV, insulin, lipid peroxidation, urea.
Current Pharmaceutical Design
Title:Study on Gluco-Regulatory Potential of Glimepiride Sulfonamide Using In silico, In Vitro and In Vivo Approaches
Volume: 20 Issue: 32
Author(s): Hamendra Singh Parmar, Mahesh Kumar Bhinchar, Muskan Bhatia, Nikita Chordia, Ishan Raval, Digvijay Singh Chauhan, E. Manivannan, Rameshwar Jatwa and Anil Kumar
Affiliation:
Keywords: Alanine amino transaminase, alpha-amylase, aspartate aminotransferase, diabetes, dipeptidyl peptidase-IV, insulin, lipid peroxidation, urea.
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
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Parmar Singh Hamendra, Bhinchar Kumar Mahesh, Bhatia Muskan, Chordia Nikita, Raval Ishan, Chauhan Singh Digvijay, Manivannan E., Jatwa Rameshwar and Kumar Anil, Study on Gluco-Regulatory Potential of Glimepiride Sulfonamide Using In silico, In Vitro and In Vivo Approaches, Current Pharmaceutical Design 2014; 20 (32) . https://dx.doi.org/10.2174/1381612820666140318114832
DOI https://dx.doi.org/10.2174/1381612820666140318114832 |
Print ISSN 1381-6128 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4286 |
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