In vitro and in silico Xanthine Oxidase Inhibitory Activity of Selected Phytochemicals Widely Present in Various Edible Plants

Comb Chem High Throughput Screen. 2020;23(9):917-930. doi: 10.2174/1386207323666200428075224.

Abstract

Aim and objective: The present study was designed to evaluate the xanthine oxidase (XO) inhibitory and antioxidant activities of 30 bioactive compounds present in edible food plants for the possible treatment of hyperuricemia.

Materials and methods: The XO inhibitory, SO and DPPH radical scavenging activities of selected dietary polyphenols were determined by using colorimetric assays. The molecular docking analysis was performed to evaluate the insight into inhibitory mode of action of bioactive compounds against XO.

Results: The results show that apigenin, galangin, kaempferol, quercetin, genistein and resveratrol potently inhibit XO enzyme among all tested compounds. Flavonoids exhibit higher, anthocyanins and hydroxycinnamic acids moderate, maslinic acid, ellagic acid, salicylic acid, [6]-gingerol and flavan-3-ols showed weak XO inhibitory activity. The results of molecular docking study revealed that these bioactive compounds bind with the active site of XO and occupy the active site which further prevents the entrance of substrate and results in the inhibition of XO.

Conclusion: Inhibition of XO gives a robust biochemical basis for management of hyperuricemia, gout and other associated diseases via controlling uric acid synthesis.

Keywords: Xanthine oxidase; antioxidant activities; bioactive compounds; gout; hyperuricemia; phytochemicals.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acids, Carbocyclic / chemistry
  • Antioxidants / chemistry*
  • Antioxidants / pharmacology
  • Drug Evaluation, Preclinical
  • Enzyme Inhibitors / chemistry*
  • Enzyme Inhibitors / pharmacology
  • Flavonoids / chemistry
  • Glycosides / chemistry
  • Gout / drug therapy*
  • Humans
  • Hyperuricemia / drug therapy*
  • In Vitro Techniques
  • Molecular Docking Simulation
  • Phenols / chemistry
  • Phytochemicals
  • Plant Extracts / chemistry*
  • Plant Extracts / pharmacology
  • Plants, Edible / chemistry*
  • Pyrans / chemistry
  • Structure-Activity Relationship
  • Superoxides / chemistry
  • Xanthine Oxidase / antagonists & inhibitors*

Substances

  • Acids, Carbocyclic
  • Antioxidants
  • Enzyme Inhibitors
  • Flavonoids
  • Glycosides
  • Phenols
  • Phytochemicals
  • Plant Extracts
  • Pyrans
  • Superoxides
  • Xanthine Oxidase