Inhibition behaviours of some phenolic acids on rat kidney aldose reductase enzyme: an in vitro study

J Enzyme Inhib Med Chem. 2017 Dec;32(1):277-284. doi: 10.1080/14756366.2016.1250752.

Abstract

Aldose reductase (AR) inhibitors have vital importance in the treatment and prevention of diabetic complications. In this study, rat kidney AR was purified 19.34-fold with a yield of 3.49% and a specific activity of 0.88 U/mg using DE-52 Cellulose anion exchange chromatography, gel filtration chromatography and 2'5' ADP Sepharose-4B affinity chromatography, respectively. After purification, the in vitro inhibition effects of some phenolic acids (tannic acid, chlorogenic acid, sinapic acid, protocatechuic acid, 4-hydroxybenzoic acid, p-coumaric acid, ferulic acid, vanillic acid, syringic acid, α-resorcylic acid, 3-hydroxybenzoic acid and gallic acid) were investigated on purified enzyme. We determined IC50, Ki values and inhibition types of these phenolic acids. As a result, tannic and chlorogenic acid had a strong inhibition effect. On the other hand, gallic acid had a weak inhibition effect. In this study, all phenolic acids except for chlorogenic acid and p-coumaric acid showed non-competitive inhibition effects on rat kidney AR.

Keywords: Aldose reductase; diabetic complications; inhibition; phenolic acids.

MeSH terms

  • Aldehyde Reductase / antagonists & inhibitors*
  • Animals
  • Electrophoresis, Polyacrylamide Gel
  • Hydroxybenzoates / pharmacology*
  • In Vitro Techniques
  • Kidney / enzymology*
  • Rats

Substances

  • Hydroxybenzoates
  • Aldehyde Reductase
  • phenolic acid