Scutellaria barbataD. Don (Lamiaceae) (SB) is a perennial herb, which is natively distributed throughout Korea and southern China. This herb is known in traditional Chinese medicine as Ban-Zhi-Lian and in traditional Korean medicine as Banjiryun. SB has been used as an antiinflammatory and antitumor agent. The SB showed strong growth-inhibitory activity and cancer chemopreventive activity in assays representing three major stages of carcinogenesis. The SB was found to act as an antimutagen; it mediated antiinflammatory effects; inhibited cyclooxygenase and hydroperoxidase functions (antipromotion activity). In addition, SB inhibited the development of preneoplastic lesions in carcinogen-treated mouse mammary glands in culture and inhibited tumorigenesis in a mouse skin cancer model. On the other hand, an inhibitory effect of SB on the growth of gynecological cancer cell lines such as HeLa cell and human ovary cancer (HOC) was shown. When HOC cells were treated with SB, the expression of cyclooxygenase-2 was inhibited. These data suggest that SB merits investigation as a potential cancer chemopreventive agent in humans, especially in gynecological cancers.