Inhibitory effect of quercetin in the formation of advance glycation end products of human serum albumin: An in vitro and molecular interaction study

Int J Biol Macromol. 2015 Aug:79:336-43. doi: 10.1016/j.ijbiomac.2015.05.004. Epub 2015 May 14.

Abstract

Non-enzymatic glycation entails the reaction between the carbonyl group of a sugar with the amino group of a protein giving rise to Schiff base and Amadori products. The formation of advanced glycation end products (AGEs) leads to the generation of free radicals, which play an important role in the pathophysiology of ageing and diabetes. Bioavailable dietary antioxidants like quercetin (QC) are thought to inhibit AGEs formation. This study was aimed to investigate the effect of quercetin on AGE formation and features the glycation of human serum albumin (HSA) and its characterization by various spectroscopic techniques. The effect of quercetin, against the formation of AGEs was studied using a glycated human serum albumin product, haemoglobin-δ-gluconolactone, and aminoguanidine. The results were then corroborated with estimation of protein oxidation, lipid peroxidation and comet assay. On the basis of the experimental data, computational docking studies were then performed to understand the location of the site of quercetin binding and its best bound conformation with respect to human serum albumin. Through this study we have demonstrated the mechanism of formation of AGE and its inhibition by quercetin. We have also suggested that the supplementation with dietary antioxidants like quercetin might protect against free radical toxicity.

Keywords: AGEs; Comet assay; Lipid and protein oxidation; Molecular docking; Quercetin.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antioxidants / pharmacology*
  • Binding Sites
  • Gluconates / chemistry
  • Glycation End Products, Advanced / antagonists & inhibitors
  • Glycation End Products, Advanced / chemistry*
  • Glycation End Products, Advanced / pharmacology
  • Glycosylation
  • Guanidines / chemistry
  • Hemoglobins / chemistry*
  • Humans
  • Lactones / chemistry
  • Lipid Peroxidation / drug effects
  • Lymphocytes / chemistry
  • Lymphocytes / drug effects
  • Molecular Docking Simulation
  • Primary Cell Culture
  • Protein Binding
  • Quercetin / pharmacology*
  • Serum Albumin / chemistry*
  • Solutions

Substances

  • Antioxidants
  • Gluconates
  • Glycation End Products, Advanced
  • Guanidines
  • Hemoglobins
  • Lactones
  • Serum Albumin
  • Solutions
  • Quercetin
  • pimagedine
  • beta-glucono-1,5-lactone