茚并吡啶类衍生物诱导HEp-2细胞凋亡  

Apoptosis induced by indeno[1,2-b]pyridines in laryngeal cancer HEp-2cells

作　　者：虞莹[1] 梁中琴[1] 朱永明[2] 

机构地区：[1]苏州大学医学部药学院药理系,苏州215123 [2]苏州大学医学部药学院药学系,苏州215123

出　　处：《中国新药杂志》2011年第19期1907-1910,1915,共5页Chinese Journal of New Drugs

基　　金：国家自然科学基金(30873052;81072656)

摘　　要：目的:探讨1-甲基-5-(4-二甲氨基苄烯)-5H-茚[1,2b]吡啶三氟甲磺酸盐(受试物)对人喉表皮样肿瘤细胞HEp-2的增殖抑制和凋亡诱导作用。方法:采用MTT法观察受试物对HEp-2增殖的抑制作用,Hoechst 33258荧光染色观察HEp-2细胞凋亡形态学变化,流式细胞仪PI单染法检测细胞周期及凋亡率,采用Western Blot分析检测促凋亡蛋白Bid的表达。结果:1-甲基-5-(4-二甲氨基苄烯)-5H-茚[1,2b]吡啶三氟甲磺酸盐可抑制HEp-2细胞的增殖,并呈时间和剂量依赖性;用受试物(4μmol.L-1)处理细胞(24和48 h),经Hoechst 33258荧光染色,可见细胞凋亡形态学改变;流式细胞仪检测显示,HEp-2细胞周期发生改变,凋亡率增加;Western Blot分析结果显示,受试物可使促凋亡蛋白Bid表达水平上升。结论:1-甲基-5-(4-二甲氨基苄烯)-5H-茚[1,2b]吡啶三氟甲磺酸盐可抑制HEp-2细胞增殖,诱导其凋亡。Objective： To investigate the inhibiting effect of 4-（ （Z）-（5H-1-methyl-indeno [ 1,2-b] pyri- dine-5-ylidene） methyl）-N,N-dimethylbezenamine trifluoromethylsulfonate on proliferation and its inducing effect of apoptosis in Human laryngeal epidermoid carcinoma HEp-2 cells. Methods： Inhibition of cell proliferation was determined by MTT assay. Hoechst 33258 fluorescent staining was used to observe the morphological changes of apoptosis. Cell cycle and apoptosis rate were analyzed by flow cytometry （FCM） after PI staining. The pro-apoptosis protein Bid expression was detected by Western Blot analysis. Results： 4-（ （Z）-（5H-l-methyl-indeno [ 1,2-b] pyridine-5-ylidene）methyl）-N,N-dimethylbezenamine trifluoromethylsulfonate significantly inhibited the growth of HEp-2 cells in a dose- and time-dependant manner. Hoechst staining showed the morphological changes of apopto- sis after treatment with the compound （4μmol·L^-1 ） time-dependently. Flow cytometry showed changes in cell cycle and an increase in apoptosis after treatment. Western Blot analysis indicated the increased expression of pro-apoptosis protein Bid. Conclusion ： 4- （ （Z） - （ 5H-1 -methyl-indeno [ 1,2-b ] pyridine-5-ylidene ） methyl） -N, N-dimethylbezenamine trifluoromethylsulfonate can significantly inhibit proliferation and induce apoptosis in HEp-2 cells.

关 键 词：1-甲基-5-(4-二甲氨基苄烯)-5H-茚[1 2b]吡啶三氟甲磺酸盐 HEP-2细胞 凋亡 

分 类 号：R979.1[医药卫生—药品]