Aerial part extracts of Kitaibelia balansae Boiss. were examined for their phenolic contents, as well as anti-inflammatory activities. The chemical compositions of the extracts were analysed by spectrophotometric and chromatographic (HPLC/ MS/MS and HPLC-PDA) approaches. To measure anti-inflammatory activity, the effects of the extracts on nitric oxide (NO) and Tumour Necrosis Factor-α (TNF-α) levels were measured in lipopolysaccharide (LPS) treated murine macrophage cell line (RAW 264.7). The ethyl acetate fraction was found to be abundant in phenolic compounds (259.78 ± 15.07 mgGAE/ gextract). Rutin was identified as the major compound in all the extracts. The ethyl acetate fraction potentially inhibited NO and TNF-α production (37.26 µM and 1781.524 pg/mL, respectively, 6 h) in LPS induced cells.