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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.

Abstract
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 π (GST-π) contributed to MDR in BEL-7402/5-FU cells. The mRNA expressions of MRP1 and GST-π 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.
AuthorsHai-ya Huang, Jiang-long Niu, Li-ming Zhao, Yan-hua Lu
JournalPhytomedicine : international journal of phytotherapy and phytopharmacology (Phytomedicine) Vol. 18 Issue 12 Pg. 1086-92 (Sep 15 2011) ISSN: 1618-095X [Electronic] Germany
PMID21596545 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
CopyrightCopyright © 2011 Elsevier GmbH. All rights reserved.
Chemical References
  • 2',4'-dihydroxy-6'-methoxy-3',5'-dimethylchalcone
  • Antimetabolites, Antineoplastic
  • Chalcones
  • Fluorouracil
Topics
  • Antimetabolites, Antineoplastic (analysis)
  • Carcinoma, Hepatocellular (drug therapy)
  • Cell Line, Tumor (drug effects)
  • Chalcones (pharmacology, therapeutic use)
  • Chromatography, High Pressure Liquid
  • Drug Evaluation, Preclinical
  • Drug Resistance, Neoplasm (drug effects)
  • Flow Cytometry
  • Fluorouracil (analysis)
  • Gene Expression Regulation, Neoplastic (drug effects)
  • Humans
  • Liver Neoplasms (drug therapy)

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