靛玉红及其类似物抗肿瘤和神经保护作用的研究进展  

Research progress on effects of indirubin and its structurally similar compounds on anticancer and neuroprotection

作　　者：王英[1,2] 沙飞[1,2] 陈月华[1,2] 李铭源[1,2] 

机构地区：[1]中药质量研究国家重点实验室,澳门大学,澳门999078 [2]澳门大学中华医药研究院,澳门999078

出　　处：《中草药》2014年第16期2404-2411,共8页Chinese Traditional and Herbal Drugs

基　　金：澳门科学技术发展基金(078/2011/A3;045/2007/A3)

摘　　要：天然产物靛玉红广泛存在于中药大青叶、青黛、板蓝根中,历史上主要用于治疗白血病。现代药理学研究表明靛玉红是具代表性的细胞周期蛋白依赖性激酶(CDKs)和糖原合成酶激酶-3(GSK-3)抑制剂,对二者的抑制作用均是通过与ATP竞争性靶点结合。研究发现很多肿瘤和神经退行性疾病会伴随CDKs和GSK-3的异常磷酸化,靛玉红结构上的特点使其对肿瘤和神经退行性疾病具有双重药理活性。因此,靛玉红及其类似物对于同时治疗肿瘤和神经退行性疾病的新型药物开发表现出良好前景。Indirubin is the active ingredient in many Chinese materia medica and mainly used to treat leukemia. It has been founded as leading inhibitor of cyclin-dependent kinases （CDKs） and glycogen synthase kinase-3 （GSK-3） by competing with ATP binding sites. Increasing new findings pointed out that the unique chemical structure of indirubin could contribute to the polypharmacological activities particularly against cancer and neurodegeneration therapy while these diseases shared common molecular link on abnormal phosphorylation of CDKs and GSK-3. In this review, the underlying mechanisms of dual actions ofindirubin and its structurally similar compounds on therapy of cancer and neurodegenerative diseases are presented.

关 键 词：靛玉红 抗肿瘤 神经退行性疾病 细胞周期蛋白依赖性激酶 糖原合成酶激酶-3 

分 类 号：R285[医药卫生—中药学]