【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。更多还原

【Abstract】 Objective To investigate antitumor ability of N-isoquinoline-3-carbonyl-L-Glycine-benzylester( IQ-G-OBzl) 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 IC50; 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-GOBzl,L-G-OBzl,IQ and IQ-G-OBzl) and were treated with each compound respectively. then weight of tumor was measured,the inhibition rate of tumor was calculated. Results In vitro test,the IC50of 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 significantly 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.更多还原