Antioxidant, anti-inflammatory, and enzyme inhibitory activity of natural plant flavonoids and their synthesized derivatives

J Biochem Mol Toxicol. 2018 Jan;32(1). doi: 10.1002/jbt.22002. Epub 2017 Oct 3.

Abstract

The synthesized flavonoid derivatives were examined for their antioxidant, anti-inflammatory, xanthine oxidase (XO), urease inhibitory activity, and cytotoxicity. Except few, all the flavonoids under this study showed significant antioxidant activity (45.6%-85.5%, 32.6%-70.6%, and 24.9%-65.5% inhibition by DPPH, ferric reducing/antioxidant power, and oxygen radical absorption capacity assays) with promising TNF-α inhibitory activity (42%-73% at 10 μM) and IL-6 inhibitory activity (54%-81% at 10 μM) compared with that of control dexamethasone. The flavonoids luteolin, apigenin, diosmetin, chrysin, O3Ꞌ , O7 -dihexyl diosmetin, O4Ꞌ , O7 -dihexyl apigenin, and O7 -hexyl chrysin, showed an inhibition with IC50 values (4.5-8.1 μg/mL), more than allopurinol (8.5 μg/mL) at 5 μM against XO and showing more than 50% inhibition at a final concentration (5 mM) with an IC50 value of ranging from 4.8 to 7.2 (μg/mL) in comparison with the positive control thiourea (5.8 μg/mL) for urease inhibition. Thus, the flavonoid derivatives may be considered as potential antioxidant and antigout agents.

Keywords: antioxidant; flavonoids; inhibition; urease; xanthine oxidase.

Publication types

  • Comparative Study

MeSH terms

  • Animals
  • Anti-Inflammatory Agents, Non-Steroidal / chemistry
  • Anti-Inflammatory Agents, Non-Steroidal / pharmacology*
  • Antioxidants / chemistry
  • Antioxidants / pharmacology*
  • Cell Survival / drug effects
  • Drug Design*
  • Enzyme Inhibitors / chemistry
  • Enzyme Inhibitors / pharmacology*
  • Flavonoids / chemistry
  • Flavonoids / pharmacology*
  • Gout Suppressants / chemistry
  • Gout Suppressants / pharmacology
  • Humans
  • Inflammation Mediators / antagonists & inhibitors
  • Inflammation Mediators / metabolism
  • Kinetics
  • Lipopolysaccharides / toxicity
  • Milk Proteins / antagonists & inhibitors
  • Milk Proteins / metabolism
  • Molecular Structure
  • THP-1 Cells
  • Urease / antagonists & inhibitors
  • Urease / metabolism
  • Xanthine Oxidase / antagonists & inhibitors
  • Xanthine Oxidase / metabolism

Substances

  • Anti-Inflammatory Agents, Non-Steroidal
  • Antioxidants
  • Enzyme Inhibitors
  • Flavonoids
  • Gout Suppressants
  • Inflammation Mediators
  • Lipopolysaccharides
  • Milk Proteins
  • Xanthine Oxidase
  • Urease