The Chinese herbal medicine, Xiao-Chai-Hu-Tang (XCHT), with Bupleurum radix as the main ingredient, is used for treating hepatitis. Although there are many varieties of Bupleurum in the herbal market, Bupleurum kaoi is the only indigenous species belonging to the Bupleurum genus plant in Taiwan which is commercially cultivated for making health-promoting products. The present study examined the hepatoprotective and antioxidative properties of XCHT formulated with commercially cultivated B. kaoi. The activities of aspartate aminotransferase (AST), alanine aminotransferase (ALT), superoxide dismutase (SOD), catalase, glutathione peroxidase (GPx), glutathione reductase (GRd) and glutathione-S-transferase (GST) as well as lipid peroxidation in rats treated with CCl4 were analyzed to evaluate the hepatoprotective property of XCHT. The results showed that the enzyme levels in the serum of rats treated with XCHT extract prior to receiving CCl4 were significantly lower (p < 0.05) than those in the rats that received CCl4 only. Malondialdehyde formation was also reduced when XCHT extract was given. In comparison with the extract of XCHT, the extract of B. kaoi showed similar hepatoprotective abilities. Since the levels of SOD, catalase, GPx, GRd and GST were compensation increased in CCl4 treatment, it was suggested that XCHT or B. kaoi markedly suppressed lipid peroxidation and reversed the activities of the antioxidant enzymes to the normal levels.