瞄准:在人的胃的癌细胞线 SGC-7901 和 MKN-45 上评估 atofluding 衍生物 N (3 )-o-toluyl-fluorouracil (TFU ) 的生长抑制功效。方法:没有或与肝 microsomal 酶,由 TFU 的房间生长抑制被 MTT 和 clonogenic 试金测量。在裸体老鼠的癌症房间的异种皮移植被采用学习 TFU 在活体内的 anti-proliferative 效果。结果:TFU 禁止了 SGC-7901 和 MKN-45 细胞的生长。然而,房间生长上的 TFU 的禁止的效果不是重要的。抑制率面对肝 microsomal 酶被提高,变化在 SGC-7901 房间的 4.73%-48.57% 和在 MKN-45 房间的 9.0%-62.02% 。在活体内, TFU 在裸体老鼠推迟了 SGC-7901 和 MKN-45 细胞的生长。抑制率在 SGC-7901 房间是 40.49% , 63.24% ,和 75.98% 并且 40.76% , 61.41% ,和 82.07% 在 MKN-45 房间当口头的剂量分别地是 25, 50,和 100 mg/kg 时。TFU 治疗被老鼠很好通常在体重与不到 20% 减小容忍。结论:TFU 禁止人的胃的癌房间的生长。抑制率面对肝 microsomal 酶被增加。TFU 的功效可以与 5 氟尿嘧啶(5-FU ) 的支撑的版本被联系由酶调停了。
AIM: To evaluate the growth inhibition efficacy of atofluding derivative N3-o-toluyl-fluorouracil (TFU) on human gastric carcinoma cell lines SGC-7901 and MKN-45. METHODS: Cell growth inhibition by TFU was measured by MTT and clonogenic assays without or with liver microsomal enzymes. Xenografts of cancer cells in nude mice were employed to study the anti-proliferative effects of TFU in vivo. RESULTS: TFU inhibited the growth of SGC-7901 and MKN-45 cells. However, the inhibitory effects of TFU on cell growth were not significant. The inhibition rates were enhanced in the presence of liver microsomal enzymes, ranging 4.73%-48.57% in SGC-7901 cells and 9.0%-62.02% in MKN-45 cells. In v/vo, TFU delayed the growth of SGC-7901 and MKN-45 cells in nude mice. The inhibition rates were 40.49%, 63.24%, and 75.98% in SGC-7901 cells and 40.76%, 61.41%, and 82.07% in MKN-45 cells when the oral doses were 25, 50, and 100 mg/kg, respectively. TFU treatment was generally well tolerated by mice with less than 20% reduction in body weight. CONCLUSION: TFU inhibits the growth of human gastric carcinoma cells. The inhibition rates are increased in the presence of liver microsomal enzymes. The efficacy of TFU may be associated with the sustaining release of 5-fluorouracil (5-FU) mediated by the enzymes.