The methanolic extract from the root of Scutellaria baicalensis Georgi and its flavonoids, wogonin, baicalein, and baicalin were evaluated for anti-inflammatory action and the activatory effect on gingival fibroblasts. In LPS-induced production of IL-1 beta, three flavonoids at 1 microgram/ml expressed a significant (> 50%) inhibitory effect, similar to that of prednisolone. Moreover, the flavonoids inhibited IL-1 beta-induced synthesis of PGE2 and LTB4 considerably, although the effect of wogonin on LTB4 synthesis was marginal. In addition, three flavonoids exerted a moderate inhibition (33-36%) of collagenolytic activity, comparable to 40% inhibition by tetracycline. Meanwhile, the cellular activity of fibroblasts was augmented remarkably (40%) by baicalein (2) and slightly by baicalin (3) or wogonin (1). Consistent with the cellular activation, flavonoids enhanced the synthesis of both collagen and total protein in fibroblasts, in contrast to growth factors which increased only the synthesis of total protein. Although the effects of the methanolic extract resembled those of the flavonoids, the extract expressed a preferential effect on the synthesis of collagen and total protein.