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Two new germacranolides, carpelipine C (1) and carpelipine D (2), together with four known ones (3–6), were isolated from Carpesium lipskyi Winkl. flowers, a folk Tibetan herbal medicine with antipyretic‐analgesic and anti‐inflammatory effects. The chemical structures of new structure were illuminated by diversified spectroscopic and X‐ray crystallographic analyses. Compounds 1 and 3 dramatically suppressed the synthesis of NO and decreased pre‐inflammatory protein expression of iNOS and COX‐2 in LPS‐induced RAW264.7 cells. Furthermore, it was revealed that NF‐κB/MAPK signaling pathway were involved in the anti‐inflammatory process of 1 and 3, and their effects on reducing oxidative stress by activating Nrf2/HO‐1 pathway were also measured. This article indicated that the traditional use of C. lipskyi to treat inflammatory diseases has a certain rationality.

Seven new acyclic diterpenes, namely lipskynoids A–G (1–7), were isolated from the flowers of Carpesium lipskyi, a traditional Tibetan herbal medicine with anti‐inflammatory and antipyretic‐analgesic effects. These new compounds were elucidated by analysis of extensive spectroscopic data including ESI‐MS, 1D, 2D NMR, and DP4+ analyses. Biological assays showed that 1–7 display significant inhibitory effects against the NO production in LPS‐induced RAW264.7 cells with its IC50 values from 9.9 to 18.47 μM, however, no cytotoxicity effect was observed of these isolates against the growth of HePG2, PC3, DU145, and A549 cells.