呫吨酮并吡啶衍生物XP-15抗人肺癌A549细胞的作用  

Anticancer effect of Xanthono-pyridine derivative XP-15 on human lung carcinoma A549 cells

作　　者：车冠华 蒋君男 陈毅飞[1] 齐娜[1] 覃江克[2] 戴支凯[1] 

机构地区：[1]桂林医学院药理学教研室,广西桂林541004 [2]广西师范大学化学与药学学院 药用资源化学与药物分子工程国家重点实验室,广西桂林541004

出　　处：《现代肿瘤医学》2015年第3期289-293,共5页Journal of Modern Oncology

基　　金：国家自然科学基金资助项目(编号:21002015)

摘　　要：目的:观察9-(2-吗啡啉乙酰胺基)-7H-吡啶并(4,3-c)呫吨-7-酮(XP-5)抗人肺癌A549细胞的作用及可能的机制。方法:采用MTT法和细胞克隆实验观察XP-15对A549细胞增殖的抑制作用,应用PI/Hoechest33258染色和流式细胞术检测细胞凋亡,荧光分光光度计检测细胞内钙和线粒体膜电位。Real time PCR检测Bad和金属硫蛋白1A(metallothionein 1A,MT-1A)mRNA的表达。结果:XP-15能剂量依赖性地抑制A549细胞增殖,并能诱导细胞凋亡。与阴性对照组比,XP-15作用后,A549细胞的细胞内钙和线粒体膜电位均降低、MT-1A mRNA的表达上调,而Bad mRNA的表达无明显变化。结论:XP-15具有诱导A549细胞凋亡的作用,可能与其降低细胞内钙和线粒体膜电位有关。Objective ： To investigate the anticancer effect and potential mechanism of 2 - morpholino - N - [ 7 - oxo - 7H - chromeno（ 3,2 - h ） quinolin - 9 - yl] acetamide （ XP - 15 ） on human lung carcinoma cell line A549 in vitro. Methods：Call viability was measured by MTF assay and colony formation assay. PI/Hoechest33258 dying and flow cytometer were used for apoptosis analysis. Intercellular calcium concentration and mitoehondrial membrane po- tential were detected by spectrofluorophotometer. A549 cells treated with XP - 15 were collected for Bad and metallo- thionein 1A （ MT - 1 A） transcript analysis by real - time reverse transcriptase - polymerase chain reaction （ RT - PCR）. Results：XP- 15 inhibited cell proliferation of A549 cells in a dose- dependent manner and induced A549 cells apoptosis. After exposure to XP - 15, intercellular calcium and mitochondrial membrane potential were de- creased, MT - 1A mRNA up - regulated in A549 cells. However, there were no differences in mRNA levels of Bad between XP -15 group and control group. Conclusion：XP- 15 can induce apoptosis on A549 cells ,which might be associated with decrease of intercellular calcium and mitochondrial membrane potential.

关 键 词：9-(2-吗啡啉乙酰胺基)-7H-吡啶并(4 3-c)呫吨-7-酮 人肺癌细胞A549 凋亡 

分 类 号：R979.1[医药卫生—药品] R730.53[医药卫生—药学]