文献类型：期刊文献

英文题名：Reversal effect of 2′,4′-dihydroxy-6′-methoxy-3′,5′-dimethylchalcone on multi-drug resistance in resistant human hepatocellular carcinoma cell line BEL-7402/5-FU

作者：Huang, Hai-ya[1];Niu, Jiang-long[1];Zhao, Li-ming[1];Lu, Yan-hua[1]

机构：[1]E China Univ Sci & Technol, State Key Lab Bioreactor Engn, Shanghai 200237, Peoples R China

年份：2011

卷号：18

期号：12

起止页码：1086

外文期刊名：PHYTOMEDICINE

收录：;WOS:【SCI-EXPANDED(收录号:WOS:000296304600010)】；

基金：This work was supported by the National Natural Science Foundation of China (No. 30870253), and partially supported by Shanghai Leading Academic Discipline Project (B505) and the National Special Fund for State Key Laboratory of Bioreactor Engineering (2060204).

语种：英文

外文关键词：DMC (chalcone derivative); Hepatocellular carcinoma; Multi-drug resistance; Modulator; MRP1

摘要：Multi drug resistance (MDR) is a major obstacle in the chemotherapeutic treatment of many human cancers. 2',4'-Dihydroxy-6'-methoxy-3',5'-dimethylchalcone (DMC), a chalcone, isolated from the buds of Cleistocalyx operculatus, has been shown to have antitumor effects on human carcinoma SMMC-7721 cells in vitro and in vivo. In this paper, we studied the reversal effect and the mechanism of DMC on human hepatocellular carcinoma drug-resistant cells BEL-7402/5-FU in vitro. Administration of DMC reversed the multi-drug resistance of human hepatocellular carcinoma BEL-7402/5-FU cells significantly. DMC enhanced the sensitivity of BEL-7402/5-FU cells to 5-fluorouracil (5-FU) and doxorubicin (DOX). Staining with Hoechst 33258 and flow cytometric analysis showed that DMC has apoptosis-inducing effect on BEL-7402/5-FU cells. It could also increase the concentration of 5-FU in the resistant multi-drug-resistant cells. We also observed that over-expression of the multi-drug resistance-associated protein (MRP1) and of the glutathione S-transferase pi (GST-pi) contributed to MDR in BEL-7402/5-FU cells. The mRNA expressions of MRP1 and GST-pi and the protein expression of MRP1 were decreased by DMC. These data demonstrated that DMC could effectively reverse MDR in BEL-7402/5-FU cells. (C) 2011 Elsevier GmbH. All rights reserved.