The flavonoids extracted from dried roots of Scutellaria species have been used in traditional Eastern medicine for the treatment of several human ailments, including cancer and inflammation. Modern science proved that wogonin is one of the major bioactive agents responsible for the physiological activity of Baikal skullcap (Scutellaria baicalensis Georgi.), which has been regarded as a potent anticancer agent. In this mini review, anti-inflammatory, antioxidant and anticancer activity of wogonin are discussed. Besides, the bioavailability of wogonin and utilization of nanotechnology to improve the bioavailability of wogonin are also presented.