IQ-G-OBzl对人食管癌细胞体内外抑制作用的研究  

Inhibitory effect of N-isoquinoline-3-carbonyl-L-Glycine-benzylester on human esophageal carcinoma cells in vitro and in vivo

作　　者：杨国栋[1] 张晓英[2] 冯志松[1] 任权[1] 江毅敏[1] 

机构地区：[1]川北医学院附属医院,四川南充637000 [2]川北医学院基础医学院

出　　处：《山东医药》2014年第10期17-20,共4页Shandong Medical Journal

基　　金：川北医学院科研发展重点项目(CBY13-A-ZP16)

摘　　要：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。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.

关 键 词：N-异喹啉-3-羧酸-L-甘氨酸苄酯 食管癌 活性氧 

分 类 号：R735.1[医药卫生—肿瘤]