AIM: To study the levels of 5-fluorouracail (5-FU) in plasma, liver and tumor in patients with hepatoceilular carcinoma after oral administration of 5’-deoxy-5-fluorouridine (5’-DFUR). METHODS: Thirty-nine patients with hepatoceilular carcinoma were treated with oral 5’-DFUR for more than 4 d before operation. The contents of 5-FU in plasma, liver and tumor were measured by high performance liquid chromatography (HPLC) and apoptosis of tumor cells was evaluated by in-situ TUNEL after resection of tumor. RESULTS: The concentrations of 5-FU were 1.1 μg/mL, 5.6, 5.9, and 10.5 μg/g in plasma, the liver tissue, the center of tumor and the periphery of tumor, respectively. 5-FU concentration was significantly higher in the periphery of tumor than that in the liver tissue and the center of tumor (10.5±1.6 μg/g vs 5.6±0.8 μg/g, t = 21.38, P<0.05; 10.5±1.6 μg/g vs 5.9±0.9 μg/g, t = 20.07, P<0.05). 5-FU level was significantly lower in plasma than that in the liver and the tumor (1.1±0.3 μg/mL vs 5.6±0.8 μg/g, t = 19.63, P<0.05; 1.1±0.3 μg/mL vs 10.5±1.6 μg/g, t= 41.01, P<0.05). Apoptosis of tumor cells was significantly increased after oral 5’-DFUR compared to the control group without 5-DFUR treatment. CONCLUSION: There is a higher concentration of 5-FU distributed in the tumor compared with liver tissue and apoptosis of tumor cells is increased following oral 5’-DFUR compared with the control group. The results indicate that 5’-DFUR is hopeful as neo-adjuvant chemotherapy to prevent recurrence after resection of hepatoceilular carcinoma. AIM: To study the levels of 5-fluorouracail (5-FU) in plasma, liver and tumor in patients with hepatoceilular carcinoma after oral administration of 5’-deoxy-5-fluorouridine patients with hepatoceilular carcinoma were treated with oral 5’-DFUR for more than 4 d before operation. The contents of 5-FU in plasma, liver and tumor were measured by high performance liquid chromatography (HPLC) and apoptosis of tumor cells were evaluated by in-situ TUNEL after resection of tumor. RESULTS: The concentrations of 5-FU were 1.1 μg / mL, 5.6, 5.9, and 10.5 μg / g in plasma, the liver tissue, the center of tumor and the periphery of tumor, respectively . 5-FU concentration was significantly higher in the periphery of tumor than that in the liver tissue and the center of tumor (10.5 ± 1.6 μg / g vs 5.6 ± 0.8 μg / g, t = 21.38, P <0.05; 10.5 ± 1.6 g / g vs. 5.9 ± 0.9 μg / g, t = 20.07, P <0.05) .5-FU level was significantly lower in plasma than that in the liver and the tumor (1.1 ± 0.3 μg / mL vs 5.6 ± 0.8 μg / g, t = 19.63, P <0.05; 1.1 ± 0.3 μg / mL vs. 10.5 ± 1.6 μg / g, t = 41.01, P <0.05) after oral 5’-DFUR compared to the control group without 5-DFUR treatment. CONCLUSION: There is a higher concentration of 5-FU distributed in the tumor compared with liver tissue and apoptosis of tumor cells increased following oral 5’-DFUR with the control group. The results indicate that 5’-DFUR is hopeful as neo-adjuvant chemotherapy to prevent recurrence after resection of hepatoceilular carcinoma.