Flavonoids are a class of natural products widely distributed in the plant kingdom. It has been reported that the major bioactive constituents of many medicinal herbs were flavonoids for their antioxidant, anti-inflammatory, and anti-carcinogenic activities [1]. Among them C-glycosylflavonoids also have various activities, such as antioxidant, antimolluscidal, antimicrobial, antinociceptive, antispasmodic, antihepatotoxic, anti-inflammatory, antidiabetic, antihypertensive, and others [2]. Luxemburgia octandra St. Hil (Ochnaceae) is a shrub or small tree distributed throughout the Brazilian Southeastern region. Ochnaceae is a large tropical family including 40 genera and 600 species with the greatest concentration in tropical South America [3]. In the course of our phytochemical and pharmacological investigations of Brazilian plants, we have studied species of both Ouratea and Luxemburgia genera, in which the presence of biflavonoids was observed [4][5][6][7], along with their antitumor activities [8][9][10].In the present study we investigated the anti-inflammatory activity of the flavonoids 2cc,3cc-dihydro-ochnaflavone (1), 7-O-methylorientin (2), orientin (3), orientin 2cc-O-glucoside (4), and catechin (5) using the mouse model of ear edema.The structures of the flavonoids 2cc,3cc-dihydro-ochnaflavone (1), 7-O-methylorientin (2), orientin (3), orientin 2cc-O-glucoside (4), and catechin (5) were identified by EI-MS, 1 H NMR, 13 C NMR, and comparison of those with literature data [11,12].Flavonoids 1-5 were tested in vivo for their ability to reduce the inflammatory response in the TPA-induced ear edema in mice (1.0 mg/ear). Compounds 2 and 3 showed activity in the ear topical test, inducing an edema inhibition over 50%, which was comparable to that of indomethacin at a dose of 0.5 mg/ear (Table 1). Compound 2 showed excellent anti-inflammatory activity and was relatively more effective than compounds 3 and 4 and indomethacin. However, these flavonoids 2-4 reduced the edematous response, with compound 2 the most active one. Note that the presence of the methoxy group may be responsible for the large increase in activity. Moreover, it increases the liposolubility and absorption, leading to more pronounced activity [13]. O O OH HO OH O O O OH OH 1 O OH HO OH OH OH O O OH R 1 O OH OH HOH 2 C HO OR 2 O HO 2 -4 2: R 1 = CH 3 , R 2 = H; 3: R 1 = R 2 = H 4: R 1 = H, R 2 = Glc 5