title: 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.
abstract: 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.
authors.affiliation: College of Pharmacy, Dongguk University-Seoul.
authors.forename: Md
authors.initials: M
authors.lastname: Moniruzzaman
authors.forename: Gyeongjun
authors.initials: G
authors.lastname: Lee
authors.forename: Shambhunath
authors.initials: S
authors.lastname: Bose
authors.forename: Minho
authors.initials: M
authors.lastname: Choi
authors.forename: Jae-Kyung
authors.initials: JK
authors.lastname: Jung
authors.forename: Heesoon
authors.initials: H
authors.lastname: Lee
authors.forename: Jungsook
authors.initials: J
authors.lastname: Cho
mesh_terms: D000814:Aniline Compounds / Q000494:pharmacology*; D000818:Animals; D000893:Anti-Inflammatory Agents / Q000494:pharmacology*; D000975:Antioxidants / Q000494:pharmacology*; D001578:Benzopyrans / Q000494:pharmacology*; D001713:Biphenyl Compounds / Q000378:metabolism; D002460:Cell Line; D020672:I-kappa B Proteins / Q000378:metabolism; D007249:Inflammation / Q000139:chemically induced / Q000378:metabolism*; D018836:Inflammation Mediators / Q000378:metabolism*; D015227:Lipid Peroxidation / Q000187:drug effects*; D008070:Lipopolysaccharides; D017628:Microglia / Q000187:drug effects* / Q000378:metabolism; D000072000:NF-KappaB Inhibitor alpha; D016328:NF-kappa B / Q000378:metabolism; D009569:Nitric Oxide / Q000378:metabolism; D010851:Picrates / Q000378:metabolism; D051381:Rats; D017382:Reactive Oxygen Species / Q000378:metabolism; D014409:Tumor Necrosis Factor-alpha / Q000378:metabolism
chemical_list: D000814:Aniline Compounds; D000893:Anti-Inflammatory Agents; D000975:Antioxidants; D001578:Benzopyrans; D001713:Biphenyl Compounds; D020672:I-kappa B Proteins; D018836:Inflammation Mediators; D008070:Lipopolysaccharides; C000610768:N-((3,4-dihydro-2H-benzo(h)chromene-2-yl)methyl)-4-methoxyaniline; D016328:NF-kappa B; C000606206:Nfkbia protein, rat; D010851:Picrates; D017382:Reactive Oxygen Species; D014409:Tumor Necrosis Factor-alpha; D000072000:NF-KappaB Inhibitor alpha; D009569:Nitric Oxide; C013813:4-anisidine; C004931:1,1-diphenyl-2-picrylhydrazyl