Antioxidant and Anti-inflammatory Activities of N-((3,4-Dihydro-2H-benzo[h]chromene-2-yl)methyl)-4-methoxyaniline in LPS-Induced BV2 Microglial Cells

Biol Pharm Bull. 2015;38(12):1831-5. doi: 10.1248/bpb.b15-00473.


Microglial activation is known to cause inflammation resulting in neurotoxicity in several neurological diseases. N-((3,4-Dihydro-2H-benzo[h]chromene-2-yl)methyl)-4-methoxyaniline (BL-M), a chromene derivative, was originally synthesized with the perspective of inhibiting nuclear factor-kappa B (NF-κB), a key regulator of inflammation. The present study evaluated the antioxidant and anti-inflammatory potential of BL-M in lipopolysaccharide (LPS)-stimulated BV2 microglial cells. Our results demonstrated that BL-M significantly inhibited the formation of 1,1-diphenyl-2-picrylhydrazyl radicals, as well as lipid peroxidation in rat brain homogenate in a concentration-dependent manner. In addition, it suppressed the generation of intracellular reactive oxygen species, and the levels of pro-inflammatory mediators including nitric oxide, tumor necrosis factor-α, and interleukin-6 in LPS-induced BV2 cells. Western blotting analyses revealed the inhibition of inhibitor of kappa B alpha (IκBα) phosphorylation and NF-κB translocation by BL-M in LPS-activated cells. Therefore, our study highlights marked antioxidant and anti-inflammatory activities of BL-M, and suggests that this compound may have a beneficial impact on various neurodegenerative diseases associated with inflammation.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Aniline Compounds / pharmacology*
  • Animals
  • Anti-Inflammatory Agents / pharmacology*
  • Antioxidants / pharmacology*
  • Benzopyrans / pharmacology*
  • Biphenyl Compounds / metabolism
  • Cell Line
  • I-kappa B Proteins / metabolism
  • Inflammation / chemically induced
  • Inflammation / metabolism*
  • Inflammation Mediators / metabolism*
  • Lipid Peroxidation / drug effects*
  • Lipopolysaccharides
  • Microglia / drug effects*
  • Microglia / metabolism
  • NF-KappaB Inhibitor alpha
  • NF-kappa B / metabolism
  • Nitric Oxide / metabolism
  • Picrates / metabolism
  • Rats
  • Reactive Oxygen Species / metabolism
  • Tumor Necrosis Factor-alpha / metabolism


  • Aniline Compounds
  • Anti-Inflammatory Agents
  • Antioxidants
  • Benzopyrans
  • Biphenyl Compounds
  • I-kappa B Proteins
  • Inflammation Mediators
  • Lipopolysaccharides
  • N-((3,4-dihydro-2H-benzo(h)chromene-2-yl)methyl)-4-methoxyaniline
  • NF-kappa B
  • Nfkbia protein, rat
  • Picrates
  • Reactive Oxygen Species
  • Tumor Necrosis Factor-alpha
  • NF-KappaB Inhibitor alpha
  • Nitric Oxide
  • 4-anisidine
  • 1,1-diphenyl-2-picrylhydrazyl