Glioma remains to threaten the human health, and development of new therapeutic drugs from herb source is very important. Podophyllotoxin and schisanhenol are two important herbal ingredients exerting therapeutic potential towards glioma. The recent study aims to determine the podophyllotoxin-schisanhenol interaction through evaluating the influence of podophyllotoxin-induced liver toxicity towards the metabolism of schisanhenol. Podophyllotoxin-induced liver toxicity was indicated by disturbed amino acids metabolism in the liver. The metabolic behavior of schisanhenol was compared in the liver microsomes from control mice and podophyllotoxin-treated mice. The K-m and V-max values were calculated to be 14.8 mu M and 4 nmol/min/mg protein for the metabolism of schisanhenol in the liver microsomes from control mice. The K-m and V-max values were calculated to be 12.5 mu M and 0.4 nmol/min/mg protein for the metabolism of schisanhenol in the liver microsomes from podophyllotoxin-treated mice. Based on the above data, podophyllotoxin-induced liver damage significantly decreased the metabolic elimination of schisanhenol, which guide the research and development of these two herbal ingredients to treat glioma.