摘要
近年来,肿瘤细胞多药耐药导致临床治疗失败引起了广泛关注。研究发现P-糖蛋白(P-gp)的过度表达在肿瘤多药耐药中扮演了重要角色。P-gp能将化疗药物排出细胞外,降低化疗的成功率,使肿瘤细胞耐药。川芎嗪不仅可以通过抑制MDR1-mRNA的表达及降低Ca^(2+)浓度下调P-gp的表达、抑制ATP酶活性使P-gp失去功能、调节酶的活性、促进耐药细胞凋亡等逆转肿瘤细胞多药耐药,还能与其他药物协同逆转耐药,起到增效减毒的作用。本文对川芎嗪逆转肿瘤细胞多药耐药的机制进行综述,特别是P-gp介导机制,为川芎嗪应用于临床提供思路和借鉴。
In recent years,the failure of clinical treatment caused by multidrug resistance of tumor cells has attracted widespread attention.Studies have found that overexpression of P-glycoprotein(P-gp)plays an important role in tumor cells multidrug resistance.P-gp can expel chemotherapeutic drugs out of cells,reduce the success rate of chemotherapy,and make tumor cells resistant.Ligustrazine can not only down-regulate the expression of P-gp by inhibiting the expression of MDR1-mRNA and reduce the concentration of Ca^(2+),inhibit the activity of ATPase to make P-gp lose its function,but also reverse the tumor cells multidrug resistance by regulating the activity of the induced enzyme and promoting the apoptosis of drug-resistant cells.It can synergize with other drugs to reverse drug resistance and play a role in synergism and attenuation.the mechanism of ligustrazine in reversing multidrug resistance of tumor cells was reviewed in this article,especially the P-gp-mediated mechanism,to provide ideas and references for the clinical application of ligustrazine.
作者
孙亚棋
聂旭阳
高敬林
花丽
高笑男
冯章英
王明霞
SUN Ya-qi;NIE Xu-yang;GAO Jing-lin;HUA Li;GAO Xiao-nan;FENG Zhang-ying;WANG Ming-xia(Department of Clinical Pharmacology,The Fourth Hospital of Hebei Medical University,Shijazhuang 050035,China)
出处
《中国新药杂志》
CAS
CSCD
北大核心
2022年第16期1580-1583,共4页
Chinese Journal of New Drugs
基金
国家“重大新药创制”科技重大专项资助项目(2020ZX09201006)
河北省自然基金重点项目(H2021206432)
河北医学科学研究重点课题计划项目(20200105)。
关键词
川芎嗪
P-糖蛋白
多药耐药
肿瘤细胞
ligustrazine
P-glycoprotein
multidrug resistance
tumor cells
