CalothrixinB衍生物对白血病K562细胞的抑制作用及机制  

Inhibitory Effects and Mechanism of a Calothrixin B Derivative on Leukemia K562 Cells

作　　者：龙群 肖潇[1,2,3] 宋晶睿 饶青[2,3] 刘晟 何志旭 李艳梅[2,3] LONG Qun;XIAO Xiao;SONG Jingrui;RAO Qing;LIU Sheng;HE Zhixu;LI Yanmei(Department of Immunology&Stem Cell and Tissue Engineering Research Center,Guizhou Medical University,Guiyang 550004,Guizhou,China;State Key Laboratory for Functions and Applications of Medicinal Plants,Guizhou Medical University,Guiyang 550014,Guizhou,China;Key Laboratory of Chemistry for Natural Products of Guizhou Province and Chinese Academic of Sciences,Guiyang 550014,Guizhou,China)

机构地区：[1]贵州医科大学基础医学院免疫教研室&组织工程与干细胞实验中心,贵州贵阳550004 [2]贵州医科大学省部共建药用植物功效与利用国家重点实验室,贵州贵阳550014 [3]贵州省中国科学院天然产物化学重点实验室,贵州贵阳550014

出　　处：《贵州医科大学学报》2020年第5期497-504,共8页Journal of Guizhou Medical University

基　　金：国家自然科学基金项目(81872772、81960546、U1812403-4);贵州省科技计划项目[黔科合平人才(2019)5406、QKH20181409、QKH20192762、QKH20205008]。

摘　　要：目的:研究CalothrixinB衍生物L20对白血病K562细胞的抑制作用及其机制。方法:采用四唑盐(MTT)法检测化合物L20对K562细胞的抑制作用,使用流式细胞分析仪检测化合物L20对K562细胞凋亡及周期的影响,用DCFH-DA标记的荧光探针通过荧光显微镜观察活性氧(ROS)的改变,Western蛋白印迹检测相关蛋白的表达。结果:L20处理后的K562细胞增殖受到明显抑制,L20能够诱导K562细胞凋亡,并使其细胞周期阻滞在G 2/M期,L20还可以使ROS在K562细胞中堆积;在蛋白水平上L20能够下调p-ERK、BCL-2和p-CDC25C,上调BAX、p-CDK1及CDC25C,并激活Caspase家族。结论:L20具有通过MAPK通路诱导K562细胞凋亡及将细胞周期阻滞在G 2/M期的活性。Objective:To study the inhibitory effect and its mechanism of Calothrixin B derivative-a compound L20 on leukemia K562 cells.Methods:MTT assay was used to detect the growth inhibitory effect of compound L20 on K562 cells.Flow cytometry was used to compound L20-mediated apoptosis and cell cycle.Reactive oxygen species(ROS)was observed with a microscope.Western blot was used to detect protein expression levels.Results:Compound L20 significantly inhibited the proliferation of K562 cells,induced apoptosis and blocked the cell cycle in G 2/M phase.In addition,compound L20 led to ROS accumulation in K562 cells.Furthermore,compound L20 downregulated p-ERK,BCL-2 and p-CDC25C,upregulated BAX,p-CDK1 and CDC25C,and activated the Caspase family.Conclusion:Compound L20 induces the apoptosis of K562 cells through the MAPK pathway and blocks the cell cycle in G2/M phase.

关 键 词：白血病 Calothrixins B K562细胞 凋亡 G2/M期 MAPK通路 

分 类 号：R915[医药卫生—微生物与生化药学]