紫草素衍生物诱导肺癌细胞A549细胞周期阻滞及细胞凋亡

Shikonin Derivatives Induce Cell Cycle Arrest and Apoptosis of Lung Cancer Cell Line A549

以1,4-二甲氧基苯和马来酸酐为原料,合成5,8-二甲氧基萘-1,4-二酮,通过加成反应分别制备亚砜和氨基的2-取代萘醌类衍生物a和b,采用MTT实验检测两种化合物诱导肺癌细胞A549细胞周期阻滞及细胞活性,探讨二者的结构与活性关系,并阐述其导致细胞周期阻滞及细胞凋亡的具体作用机制。结果证明,化合物a通过激活抑癌基因P53及丝裂原活化蛋白激酶信号通路对A549细胞增殖有显著抑制作用,同时可以显著促进细胞凋亡;而化合物b并无显著作用。

New sulfinyl and amino naphthoquinone derivatives of 5,8-dimethoxy-naphthalene-1,4-dione which is synthesized by reaction of 1,4-dimethoxy benzene and maleic anhydride.These two derivatives a,b were examined by MTT assay to test the effects on the proliferation inhibition of A549 cells,and to clarify the structure-activity relationship and the molecular mechanism of their biological activities.The results showed that compound a could inhibit cell proliferation and promote cell apoptosis by activating p53 and mitogen activated protein kinases(MAPKs)signal pathway,while compound b had no effect on A549 cell proliferation.