CAJ | 학술논문

目的：探讨N-异喹啉-3-羧酸-L-甘氨酸苄酯（ IQ-G-OBzl）对人食管癌细胞的体内外抑制作用。｀方法①体外实验：人食管癌细胞分为5-FU组、L-甘氨酸苄酯组、3-羧酸异喹啉组及IQ-G-OBzl组，分别采用相应药物干预；MTT法检测药物对细胞的IC50值；流式细胞仪检测细胞内活性氧（ ROS）水平。②体内实验：制作115只小鼠食管癌移植瘤模型，分为生理盐水组、IQ-G-OBzl组、L-甘氨酸苄酯组、3-羧酸异喹组及5-FU组，分别给予相应药物干预后计算抑瘤率。结果在体外实验中IQ-G-OBzl 组的IC50高于5-FU组，但低于L-甘氨酸苄酯组、3-羧酸异喹啉组（P＜0．05）；IQ-G-OBzl组细胞内ROS水平明显高于L-甘氨酸苄酯组、3-羧酸异喹组及生理盐水组（P＜0．05）。体内实验中IQ-G-OBzl组抑瘤率高于L-甘氨酸苄酯组及3-羧酸异喹组（P＜0．05）。结论 IQ-G-OBzl体内、外均有抗食管癌作用；其作用机制可能为升高细胞内ROS水平。
목적：탐토N-이규람-3-최산-L-감안산변지（ IQ-G-OBzl）대인식관암세포적체내외억제작용。｀방법①체외실험：인식관암세포분위5-FU조、L-감안산변지조、3-최산이규람조급IQ-G-OBzl조，분별채용상응약물간예；MTT법검측약물대세포적IC50치；류식세포의검측세포내활성양（ ROS）수평。②체내실험：제작115지소서식관암이식류모형，분위생리염수조、IQ-G-OBzl조、L-감안산변지조、3-최산이규조급5-FU조，분별급여상응약물간예후계산억류솔。결과재체외실험중IQ-G-OBzl 조적IC50고우5-FU조，단저우L-감안산변지조、3-최산이규람조（P＜0．05）；IQ-G-OBzl조세포내ROS수평명현고우L-감안산변지조、3-최산이규조급생리염수조（P＜0．05）。체내실험중IQ-G-OBzl조억류솔고우L-감안산변지조급3-최산이규조（P＜0．05）。결론 IQ-G-OBzl체내、외균유항식관암작용；기작용궤제가능위승고세포내ROS수평。
Objective To investigate antitumor ability of N-isoquinoline-3-carbonyl-L-Glycine-benzylester ( IQ-G-OB-zl)on the human esophageal carcinoma cells in vitro and in vivo .Methods ①In vitro test:there were four groups in vitro test and esophageal carcinoma cells were treated with 5-FU, (L-Gly-OBzl), IQ and IQ-G-OBzl, respectively;MTT assays were performed to assess the IC 50;Intracellular reactive oxygen species ( ROS) were detected by flow cytometry .②In vivo test:the model of esophageal carcinoma in 115 nude mice was established;there were five groups in vivo test ( NS, IQ-G-OBzl, L-G-OBzl, IQ and IQ-G-OBzl) and were treated with each compound respectively .then weight of tumor was meas-ured, the inhibition rate of tumor was calculated .Results In vitro test, the IC50 of IQ-G-OBzl group was higher than that of 5-FU group, but less than that of L-Gly-OBzl and IQ groups(P<0.05).In vivo test, the inhibition rate of IQ-G-OBzl group was higher than that of L-Gly-OBzl and IQ groups (all P<0.05);the ROS level of IQ-G-OBzl group was significant-ly higher than that of L-Gly-OBzl, IQ and NS groups(P<0.05).Conclusion IQ-G-OBzl has anti-esophageal carcinoma ability in vitro and vivo , and it has no obvious side effects , whose mechanism may be related to the increasing level of ROS.