AbstractOne new lactone (1) named Ardisicreolide C, together with three saponin compounds, Ardisiacrispin B (2), Ardisicrenoside A (3), Ardisiacrispin A (4) were isolated and identified from the leaves of Ardisia crenata Sims. The structures of 1–4 were elucidated by 1D, 2D‐NMR and HR‐MS spectra and together with the published data. In view of structures with lactone moieties showed good anti‐inflammatory activity, the anti‐inflammatory effects of Ardisicreolide C on LPS‐induced RAW264.7 cells were evaluated by enzyme linked immunosorbent assay (ELISA) method. As a result, Ardisicreolide C could reduce release of nitric oxide (NO), tumour necrosis factor α (TNF‐α), interleukin 1β (IL‐1β), interleukin 4 (IL‐4) and interleukin 10 (IL‐10) of the cell supernatant to exert anti‐inflammatory activity. This indicates that the leaves as non‐medicinal parts of Ardisia crenata Sims contain compounds with good anti‐inflammatory activity, which provides a new direction for the discovery of anti‐inflammatory drugs.