DPP-IV inhibitory potential of naringin: an in silico, in vitro and in vivo study

Diabetes Res Clin Pract. 2012 Jul;97(1):105-11. doi: 10.1016/j.diabres.2012.02.011. Epub 2012 Mar 10.

Abstract

The incretin based therapies are an emerging class of antidiabetic drugs, with two categories: one is glucagone like peptide-1 (GLP-1) agonists and the other one is dipeptidyl peptidase (CD26; DPP-IV) inhibitors. However, in the DPP-IV inhibitors category only few compounds are commercially available and also have some undesirable effects. Therefore, in the present work we tried to explore a naturally occurring compound naringin for its potential DPP-IV inhibition and antidiabetic potential. It is noteworthy that this compound is abundantly present in orange peel and thus may provide cost effective treatment for diabetes, especially type 2 diabetes mellitus. In the present study, we have conducted virtual docking study and observed tight binding of naringin, as shown by higher negative values of H bond lengths, while in vitro DPP-IV inhibition assay has also shown better inhibition by naringin. In vivo study, in response to 10 days administration of 40 mg/kg of naringin twice daily to Wistar albino rats, inhibited the serum levels of DPP-IV activity, random glucose concentration with concomitant increase in insulin levels. All the comparisons were made with the standard commercially available drug sitagliptin.

MeSH terms

  • Animals
  • Blood Glucose / drug effects
  • Blood Glucose / metabolism
  • Computer Simulation
  • Diabetes Mellitus / drug therapy*
  • Diabetes Mellitus / enzymology
  • Diabetes Mellitus, Experimental / drug therapy*
  • Diabetes Mellitus, Experimental / enzymology
  • Dipeptidyl-Peptidase IV Inhibitors / administration & dosage
  • Dipeptidyl-Peptidase IV Inhibitors / pharmacology*
  • Drug Administration Schedule
  • Female
  • Flavanones / administration & dosage
  • Flavanones / pharmacology*
  • Glucagon-Like Peptide 1 / agonists
  • Humans
  • Hypoglycemic Agents / administration & dosage
  • Hypoglycemic Agents / pharmacology*
  • In Vitro Techniques
  • Insulin / metabolism
  • Lipid Peroxidation
  • Male
  • Pancreas / drug effects*
  • Pancreas / enzymology
  • Rats
  • Rats, Wistar

Substances

  • Blood Glucose
  • Dipeptidyl-Peptidase IV Inhibitors
  • Flavanones
  • Hypoglycemic Agents
  • Insulin
  • Glucagon-Like Peptide 1
  • naringin