Coniferyl ferulate,isolated from Radix Angelicae sinensis,reverses multidrug resistance via strong inhibition of GST and down-regulation of P-glycoprotein

作     者：Chang Chen~1,Xinhua Lu~2,Zhiyong Yan~3,Shaojing Li~1 1 Institute of Chinese Materia Medica,China Academy of Chinese Medical Sciences,Beijing 100700, China 2 New Drug Research and Development Centre of North China Pharmaceutical Group Corporation, Hebei,050015,China 3 College of life science and engineering,Southwest Jiaotong University,Chengdu 610031,China 

会议名称：《中药与天然药高峰论坛暨第十二届全国中药和天然药物学术研讨会》

会议日期：2012年

学科分类：1008[医学-中药学(可授医学、理学学位)] 1006[医学-中西医结合] 100602[医学-中西医结合临床] 10[医学] 

关 键 词：coniferyl ferulate Radix Angelicae sinensis(Umbelliferae) multidrug resistance glutathione-S-transferase 

摘      要：P-glycoprotein(P-gp)and glutathione-S-transferase(GST)are key players in multidrug resistance(MDR).Inhibition of the expression of P-gp and/or GST has emerged as a promising therapeutic strategy for the reversal of *** ferulate(CF),isolated from Radix Angelicae sinensis(RAS),strongly inhibited human placental *** 50%inhibition concentration (IC50)was 0.3μM,which is greater than an known GST p1-1 inhibitor,ethacrynic acid(EA), using the established HTS *** analysis and computational docking were used to examine the mechanism of inhibition by *** and the expression of P-gp mRNA were evaluated in the MDR positive B-MD-C1(ADR+/+)cell line to investigate the MDR reversal effect of *** results demonstrated dual inhibition of both P-gp expression and GST activity by CF in a concentration-dependent ***,RAS may be a potential source of MDR reversing agents for pharmaceutical use.