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<i>Nepeta bracteata</i> Benth. is used clinically to treat tracheal inflammation, coughs, asthma, colds, fevers, adverse urination, and other symptoms, along with functions in clearing heat and removing dampness. However, there have been few studies characterizing the material basis of its efficacy. Therefore, the aim of this study was to screen for compounds with anti-inflammatory activities in <i>N. bracteata</i> Benth. Using silica gel, ODS C18, and Sephadex LH-20 column chromatography, as well as semipreparative HPLC, 10 compounds were separated from <i>N. bracteata</i> Benth. extract, including four new diterpenoids (<b>1</b>–<b>4</b>), one amide alkaloid (<b>5</b>), and five known diterpenoids (<b>6</b>–<b>10</b>). The structures of all the isolates were elucidated by HR-ESI-MS, NMR, and CD analyses. Using lipopolysaccharide (LPS)-stimulated RAW 264.7 cells, we investigated the anti-inflammatory activities of compounds <b>1</b>–<b>10</b>. It is worth noting that all were able to inhibit nitric oxide (NO) production with IC₅₀ values < 50 μM and little effect on RAW 264.7 macrophage viability. Compounds <b>2</b> and <b>4</b> displayed remarkable inhibition with IC₅₀ values of 19.2 and 18.8 μM, respectively. Meanwhile, screening on HCT-8 cells demonstrated that compounds <b>2</b> and <b>4</b> also had moderate cytotoxic activities with IC₅₀ values of 36.3 and 41.4 μM, respectively, which is related to their anti-inflammatory effects.