异甘草素及其衍生物逆转多药耐药的机制  

MDR mechanism of isoliquiritigenin and derivatives

作　　者：景云荣[1,2,3] 马秋菊 陈阳 刘文丽 周微[2] 赵临襄 JING Yunrong;MA Qiuju;CHEN Yang;LIU Wenli;ZHOU Wei;ZHAO Linxiang(College of Life Science and Technology,Mudanjiang Normal University,Mudanjiang 157011,Heilongjiang,China;Jiangsu Tasly Diyi Pharmaceutical Co.,Ltd.,Huaian 223003,Jiangsu,China;School of Pharmaceutical Engineering,Shenyang Pharmaceutical University,Shenyang 110016,Liaoning,China)

机构地区：[1]牡丹江师范学院生命科学与技术学院,黑龙江牡丹江157011 [2]江苏天士力帝益药业有限公司,江苏淮安223003 [3]沈阳药科大学制药工程学院,辽宁沈阳110016

出　　处：《山东大学学报（理学版）》2023年第7期32-36,51,共6页Journal of Shandong University(Natural Science)

基　　金：黑龙江省自然科学基金资助项目(LH2020H078);黑龙江省教育厅基础科研业务项目(1451MSYYB002);牡丹江师范学院校级项目(QN2021001)。

摘　　要：对异甘草素衍生物ISL-1、ISL-2的结构进行表征,并检测了其多药耐药逆转活性,进一步利用P-gp高表达的犬肾细胞MDCK-MDR1模型,考察异甘草素及其衍生物与P-gp的相互作用。实验结果表明,异甘草素、ISL-1和ISL-2对乳腺癌耐药细胞株MDA435/LCC6 MDR具有不同程度的逆转作用,同时均是P-gp的弱底物,具有显著的抑制P-gp外排的作用,有望成为高效低毒的多药耐药逆转剂。The structures of isoliquiritigenin derivatives,ISL-1 and ISL-2,were characterized and evaluated for their MDR reversal activity in vitro.Canine kidney cell MDCK-MDR1 model with high expression of P-gp was used to investigate their interaction with P-gp.The experimental results showed that isoliquiritigenin,ISL-1 and ISL-2 exhibited MDR reversal activity on breast cancer MDR cell line MDA435/LCC6 MDR in different levers.They can significantly inhibit the efflux of P-gp,which are weak substrates of P-gp.It is expected to become MDR reversal agents with high efficiency and low toxicity.

关 键 词：异甘草素 衍生物 P糖蛋白 多药耐药 逆转剂 

分 类 号：R914.5[医药卫生—药物化学]