2,2,6,6-四甲基-3-烯哌啶氮氧自由基鱼藤酮肟酯体外抗肿瘤作用  

Anti-tumor activity of 2,2,6,6-tetramethy l-3-enepiperidine nitroxide rotenone proxetil in vitro

作　　者：陈晓[1] 侯文丹[2] 肖潇[2] 杨亚亚[2] 赵希琼[2] 侯翠兰[3] 刘映前[4] 张小郁[3] 李文广[2] 

机构地区：[1]兰州大学第二医院普外科,甘肃兰州730030 [2]兰州大学医学院基础医学院药理学研究所,甘肃兰州730000 [3]兰州大学医学院基础医学院生理研究所,甘肃兰州730000 [4]兰州大学医学院药学院,甘肃兰州730000

出　　处：《兰州大学学报（医学版）》2014年第4期63-70,共8页Journal of Lanzhou University（Medical Sciences）

基　　金：甘肃省科技厅项目(1208RJZA257)

摘　　要：目的 研究2,2,6,6-四甲基-3-烯哌啶氮氧自由基鱼藤酮肟酯（PNR）体外抗肿瘤作用.方法 用磺酰罗丹明B（SRB）法检测PNR对肿瘤细胞增殖能力的影响;用流式细胞术检测PNR对Tea8113细胞周期的影响;用Transwell迁移法观察PNR对Tca8113细胞迁移能力的影响;用4＇,6-二脒基-2-苯基吲哚（DAPI）荧光染色法观察Tca8113细胞凋亡形态.结果 PNR对Tca8113、A549、HepG 2、BCG 823和EJ等人癌细胞均有增殖抑制作用.PNR在0.8～ 12.8μg/mL剂量范围内浓度、时间依赖性地抑制A549、HepG 2和BCG 823细胞的生长.2～7 μg/mL明显抑制Tca8113和EJ细胞生长,量效关系明显,对Tca8113和EJ细胞抑制作用在24 h已达高峰.综合比较,PNR对Tca8113细胞的抑制作用最强.PNR还明显抑制Tca8113细胞的迁移活性,阻止Tca8113细胞于S期,减少G1期细胞比例,并能明显诱导Tca8113细胞凋亡.结论 PNR对多种肿瘤细胞的生长有明显抑制作用,对Tca8113细胞的作用最强,并能抑制其迁移,诱导其凋亡.Objective To investigate the anti-rumor activity of 2,2,6,6-tetramethy l-3-ene-piperidine nitroxide rotenone proxetil （PNR） in vitro.Methods The inhibition effect of PNR on proliferation of various cell lines was examined with the SRB assay.The migration of Tca8113 cells was evaluated by Transwell migration assay.Cell cycle was tested by FCM.The apoptosis morphology of Tca8113 cells was observed by DAPI staining method.Results PNR could significantly inhibit the proliferation of Tca8113,A549,HepG2,BCG823 and EJ cells in vitro.PNR 0.8-12.8 μg/mL inhibited the proliferation ofA549,HepG2 and BCG823 cells in a time-and-dose-dependent manner.While PNR 2-7 μg/mL inhibited the proliferation of Tca8113 and EJ only in a dose-dependent manner,and the inhibit effects reached the highest point in 24 h.The sensitivity of PNR was different among these five tumor cells and Tca8113 cell was the most sensitive.PNR could obviously inhibit Tca8113 cells migration,accumulate Tca8113 cells in the S phase and a parallel decrease in G1 phase after 24 h and 48 h of PNR treatment.Moreover,PNR could efficiently induce the apoptosis of Tca8113 cells.Conclusion PNR has anti-tumor activity on a variety of tumor cells.Tca8113 cell was most sensitive to it.It also can inhibit Tca8113 cell migration and induce Tca8113 cell apoptosis.

关 键 词：藤酮衍生物 抗肿瘤 细胞周期 细胞凋亡 细胞迁移 

分 类 号：R965.1[医药卫生—药理学]