| Summary: | <i>Ferula sinkiangensis</i> K. M. Shen (Apiaceae) is distributed in arid desert areas of Xinjiang, and its resin is a traditional Chinese medicine to treat gastrointestinal digestive diseases. To explore bioactive components from <i>F. sinkiangensis</i>, three new lignans and thirteen known components were isolated. The structural elucidation of the components was established utilizing spectroscopic analyses together with ECD calculations. Griess reaction results indicated new compounds <b>1</b> and <b>2</b> significantly decreased NO production in LPS-stimulated RAW 264.7 macrophages, and ELISA results indicated that they effectively attenuated LPS-induced inflammation by inhibiting TNF-α, IL-1β, and IL-6 expressions. The in silico approach confirmed that compound <b>1</b> docked into the receptors with strong binding energies of −5.84~−10.79 kcal/mol. In addition, compound <b>6</b> inhibited the proliferation of AGS gastric cancer cells with IC<sub>50</sub> values of 15.2 μM by suppressing the cell migration and invasion. This study disclosed that <i>F. sinkiangensis</i> might be a promising potential resource for bioactive components.
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