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A new flavone glucoside, acacetin-7- O -(3″- O -acetyl-6″- O -malonyl)-β-d-glucopyranoside ( 1 ), two new phenolic glucosides, (3 R ,7 R )-tuberonic acid-12- O -[6'- O -( E )-feruloyl]-β-d-glucopyranoside ( 14 ) and salicylic acid-2- O -[6'- O -( E )-feruloyl]-β-d-glucopyranoside ( 15 ), and two new phenylpropanoid glucosides, chavicol-1- O -(6'- O -methylmalonyl)-β-d-glucopyranoside ( 17 ) and chavicol-1- O -(6'- O -acetyl)-β-d-glucopyranoside( 18 ), as well as 26 known compounds, 2 - 13 , 16 , and 19 - 31 , were isolated from the aerial parts of Agastache rugose . The structures of the new compounds were established by spectroscopic/spectrometric methods such as HRESIMS, NMR, and ECD. The anti-inflammatory effect of the isolated compounds was evaluated by measuring their inhibitory activities on prostaglandin E 2 (PGE 2 ) in lipopolysaccharide (LPS)-treated RAW 264.7 macrophages. New compounds 1 , 15 , 17 , and 18 inhibited LPS-induced PGE 2 production with IC 50 values of 16.8 ± 0.8, 33.9 ± 4.8, 14.3 ± 2.1, and 48.8 ± 4.4 μM, respectively. Compounds 5 , 7 , 9 - 11 , 13 , 19 , 20 , 22 , and 27 - 30 showed potent inhibitory activities with IC 50 values of 1.7-8.4 μM.