N3-邻甲苯甲酰基氟尿嘧啶对肿瘤细胞生长的抑制作用

以MTT法测定N^3-邻甲苯甲酰基氟尿嘧啶（1）对低分化人胃腺癌细胞SGC7901、人上皮样胃腺癌细胞MKN-45的生长抑制作用。结果表明，1的细胞生长抑制作用有明显的浓度和时间依赖性。加入肝微粒体酶S-9，可显著提高1对肿瘤细胞生长抑制作用。分别以荷小鼠肉瘤S180和小鼠肝癌H22的小鼠为模型进行体内实验，以0．2、0．4和0.8mmol／kg灌胃给药12～15d，1次，d。结果表明，1对小鼠肉瘤S180和小鼠肝癌H22抑瘤率分别为42％、55％、60％和40％、64％、88％：阳性对照药卡培他滨（2．1mmol／kg）的抑瘤率分别为43％和45％。1剂量为0．2、0.4和0．8mmol／kg，连续给药3周，对分别移植SGC7901和MKN-45细胞裸鼠的抑瘤率为40％、63％、76％和41％、61％、82％。

Effect of Growth Inhibition on Tumour Cells Induced by N3-o-Toluyl-flulorouracil

MTT assay was used to measure the growth inhibition of N~3-o-toluyl-flulorouracil (1) to SGC7901 and MKN-45 cells in in vitro test. The results showed that the growth inhibition effect had significant concentration and time dependency. The inhibition effect could be significantly increased by adding liver microsomal enzymes (S-9 mixture). The inhibitive rate of different doses (0.2,0.4 and 0.8mmol/kg, qd for 12-15d) was investigated using tumor-bearing mice (S180 sarcoma and H22 hepatic carcinoma cells, respectively) as animal model. The results showed that inhibitive rate of 1 to S180 sarcoma and H22 hepatic carcinoma cells were 42 %, 55 %, 60 % and 40 %, 64 %, 88 %, respectively;the rate of contrast drug capecitabine (2.1mmol/kg) was 43 % and 45 %, respectively. The inhibitive rate of 1 to nude mice transplanted SGC7901 and MKN-45 cells was 40 %, 63 %, 76 % and 41 %, 61 %, 82 %, when the drug was administrated for 3 weeks at the doses of 0.2, 0.4 and 0.8mmol/kg, respectively.