The anti-inflammatory (INF) compounds (1-15) were isolated from Agrimonia pilosa Ledeb. (APL) by activity-guided isolation technique. The isolated compounds (1-15) were identified as quercetin-7-O-rhanmoside (1), apigenin-7-O-glycoside (2), kaempferol-7-O-glycoside (3), apigenin-7-O-[6"-(butyl)-glycoside] (4), querceitn (5), kaempferol (6), apigenin (7), apigenin-7-O-[6"-(pentyl)-glycoside] (8), agrimonolide (9), agrimonolide-6-O-glucoside (10), desmethylagrimonolide (11), desmethylagrimonolide-6-O-glucoside (12), luteolin (13), vitexin (14) and isovitexin (15). Flavonoids, compound 2, 3, 11, and 14-15 have been found in APL for the first time. Furthermore, two novel flavone derivatives, compound 4 and 8, have been isolated inceptively in plant. In the no cytotoxicity concentration ranges of <TEX>$0-20{\mu}M$</TEX>, nitric oxide (NO) production level of 1-15 was estimated in LPS-treated Raw 264.7 macrophage cells. The flavone aglycones, 7 (apigenin, <TEX>$IC_{50}=3.69{\pm}0.34{\mu}M$</TEX>), 13 (luteolin, <TEX>$IC_{50}=4.62{\pm}0.43{\mu}M$</TEX>), 6 (kaempferol, <TEX>$IC_{50}=14.43{\pm}0.23{\mu}M$</TEX>) and 5 (quercetin, <TEX>$IC_{50}=19.50{\pm}1.71{\mu}M$</TEX>), exhibited excellent NO inhibitory (NOI) activity in dose-dependent manner. In the structure activity relationship (SAR) study of apigenin-derivatives (APD), apigenin; Api, apigenin-7-O-glucoside; Api-G, apignenin-7-O-[6"-(butyl)-glycoside]; Api-BG and apignenin-7-O-[6"-(pentyl)-glycoside]; Api-P, from APL on INF activity was investigated. The INF mediators level such as NO, INF-cytokines, NF-KB proteins, iNOS and COX-2 were sharply increased in Raw 264.7 cells by LPS. When pretreatment with APD in INF induced macrophages, NOI activity of Api was most effective than other APD with <TEX>$IC_{50}$</TEX> values of <TEX>$3.69{\pm}0.77{\mu}M$</TEX>. And the NOI activity was declined in the following order: Api-BG (<TEX>$IC_{50}=8.91{\pm}1.18{\mu}M$</TEX>), Api-PG (<TEX>$IC_{50}=13.52{\pm}0.85{\mu}M$</TEX>) and