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Rosa rugosa Thunb., is as a medicinal plant known for anti‐diabetic, and anti‐inflammatory activities. However, the specific active compounds responsible for the individual pharmacological effects of in R. rugosa extract (95% EtOH) remain unknown. Here, we hypothesized that terpenoid structure, the most abundant constituents in R. rugosa extract, are responsible for its anti‐inflammatory activity. We investigated the phytochemical substituents (compounds 1–13) and newly purified 11‐methoxy polisin A, and 13‐methoxy bisaborosaol F using NMR and ESI‐MS and to screened their effects on NO production in LPS‐induced macrophages. Rugosic acid A (RA) induced to ameliorate NO production, iNOS, and pro‐inflammatory cytokines associated with the NF‐κB. And, RA suppressed IL‐6 secretion and IL‐6‐mediated STAT3 activation in LPS‐mediated inflammation. In addition, RA was evaluated in LPS‐mediated acute lung injury (ALI) model similar to acute pneumonia. Our results suggested that RA was suppressed to translocate nuclear NF‐κB and IL‐6‐mediated STAT3 activation. Finally, RA led to amelioration of ALI by decreasing myeloperoxidase (MPO) and inhibiting phosphorylation of NF‐κB and STAT3. Our group originally found that R. rugosa extract had new methoxy compounds and RA may be alternative natural agent for acute pneumonia similar to severe acute respiratory syndrome by coronavirus.