Bangladesh Journal of Pharmacology (Dec 2011)

Study of potential xanthine oxidase inhibitors: In silico and in vitro biological activity

  • Muthuswamy Umamaheswari,
  • Arumugam Madeswaran,
  • Kuppusamy Asokkumar,
  • Thirumalaisamy Sivashanmugam,
  • Varadharajan Subhadradevi,
  • Puliyath Jagannath

DOI
https://doi.org/10.3329/bjp.v6i2.9175
Journal volume & issue
Vol. 6, no. 2

Abstract

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In an attempt to develop potent anti gout agents, coumarin derivatives and polyphenolic compounds were selected for present study. The docking energy of 2-benzyl coumarin was found to be -7.50 kcal/mol which was less than that of the standard allopurinol (-4.47 kcal/mol). All the selected compounds were found to exhibit lower binding energy (-7.50 to -4.68 kcal/mol) than allopurinol. Docking results confirm that selected compounds showed greater inhibition of xanthine oxidase due to their active binding sites. In xanthine oxidase assay, IC50 value of 2-benzyl coumarin was found to be 26 ± 1.16 µg/mL, whereas that of allopurinol was 24 ± 0.28 µg/mL. All the compounds exhibited IC50 values ranging between 26 ± 1.16 to 58 ± 0.74 µg/mL. In enzyme kinetic studies, coumarin derivatives showed competitive and polyphenolic compounds showed non competitive type of enzyme inhibition. It can be concluded that coumarin derivatives could be a remedy for the treatment of gout and related inflammatory disorders.

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