A new triterpenoid, 3β‐hydroxyurs‐12‐en‐28,20β‐olide (1), as well as thirteen known terpenoids (2–14) and three known phenylpropanoids (15–17), were isolated from the twigs and leaves of Abelia macrotera. Compounds 2, 5–17 were isolated for the first time from the Abelia genus. The structure of compound 1 was determined using the characteristic spectral data (HR‐ESI‐MS, UV, 1D and 2D‐NMR, and X‐ray single‐crystal diffraction. Furthermore, the inhibitory effects of all compounds on NO production in LPS‐induced RAW 264.7 cells were tested, and compound 15 showed obvious inhibitory effect, with IC50 values of 23.77±1.61 μM. Through target screening and molecular docking technology, it can be speculated that compound 15 may play an anti‐inflammatory role by combining with Cathepsin G & Chymase and HPG D.