The hepatoprotective potential of antrosterol (ergostatrien-3β-ol, ST1) from Antrodia camphorata (AC) against carbon tetrachloride (CCl4)-induced liver damage was evaluated in preventive models in mice. Pretreatment with ST1 markedly prevented the elevation of aspartate aminotransferase (AST), alanine aminotransferase (ALT) and liver lipid peroxides in CCl4-treated mice. The activities of antioxidant enzymes [catalase (CAT), superoxide dismutase (SOD) and glutathione peroxidase (GPx)] were significantly increased after treatment with CCl4invivo. In addition, ST1 decreased the level of nitric oxide (NO) production and tumour necrosis factor-alpha (TNF-α) in CCl4-treated mice. In this study, these results pointed out that ST1 can inhibit lipid peroxidation, enhance the activities of antioxidant enzymes, decreases the TNF-α level, nitric oxide production and inducible nitric oxide synthase (iNOS), and cyclooxygenase-2 (COX-2) expressions. Therefore, it was speculated that ST1 protects mice from liver damage through their anti-inflammation capacity.