When used as an alternative source of drugs to treat inflammation-associated diseases, phytochemicals with anti-inflammatory properties provide beneficial impacts. Galangin is one of the most naturally occurring flavonoids. Galangin has many biological activities, such as anti-inflammatory, antioxidant, antiproliferative, antimicrobial, anti-obesity, antidiabetic, and anti-genotoxic activities. We observed that galangin was well tolerated and positively impacted disease underlying inflammation for the renal, hepatic, central nervous system, cardiovascular, gastrointestinal system, skin, and respiratory disorders, as well as ulcerative colitis, acute pancreatitis, retinopathy, osteoarthritis, osteoporosis, and rheumatoid arthritis. Galangin anti-inflammatory effects are mediated mainly by suppressing p38 mitogen-activated protein kinases, nuclear factor-kappa B, and nod-like receptor protein 3 signals. These effects are confirmed and supported by molecular docking. Clinical translational research is required to accelerate the bench-to-bedside transfer and determine whether galangin can be utilised as a safe, natural source of pharmaceutical anti-inflammatory medication for humans.

A series of diaryl imidazole derivatives (5a-h) was designed as novel selective COX-2 anti-inflammatory drug candidates. The designed compounds were synthesised, and their structures were characterized by spectroscopic analysis. The anticipated anti-inflammatory activity for the synthesized compounds was assessed by in-vitro cyclooxygenases (COX-1/COX-2) inhibition assay. Most of tested compounds demonstrated moderate COX-2 inhibitory activity and selectivity (IC50 = 0.068 – 0.80 μm, SI = 7.5 - 175) in comparison to indomethacin (IC50 = 0.079 μm, SI = 12.5) and celecoxib (IC50 = 0.046 μm, SI = 315.22). Molecular modelling study of the synthesized compounds into the active site of COX-2 enzyme was performed to rationalize their preferred binding affinity; except for compound 5f, all compounds showed binding with amino acids at the selectivity pocket Additionally, In-silico simulation studies explored the drug drug-likeness parameters of the synthesized compounds, all synthesized compounds exhibited promising physicochemical parameters and pharmacokinetics according to the in-silico simulation results.