Synthesis and antimultidrug resistance evaluation of icariin and its derivatives

A series of icariin derivatives were synthesized. Their multidrug resistance (MDR) reversal activities were evaluated by MTT assay and the results indicated that the derivatives were the potent modulators of MDR. It was showed that the derivatives significantly increased the intracellular accumulati...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2009-08, Vol.19 (15), p.4237-4240
Main Authors: Liu, Dong-Fang, Li, Yan-Ping, Ou, Tian-Miao, Huang, Shi-Liang, Gu, Lian-Quan, Huang, Min, Huang, Zhi-Shu
Format: Article
Language:English
Subjects:
Antineoplastic agents
Antineoplastic Agents - chemical synthesis
Antineoplastic Agents - pharmacology
ATP-Binding Cassette, Sub-Family B, Member 1 - metabolism
Biological and medical sciences
Caco-2 Cells
Cell Line, Tumor
Chemistry, Pharmaceutical - methods
Drug Design
Drug Resistance, Multiple
Drug Resistance, Neoplasm
Flavonoids - chemical synthesis
Flavonoids - pharmacology
General aspects
Humans
Icariin derivatives
Inhibitory Concentration 50
Medical sciences
Models, Chemical
Multidrug resistance reversal activity
P-Glycoprotein inhibitors
Pharmacology. Drug treatments
Reverse Transcriptase Polymerase Chain Reaction
Synthesis
Tetrazolium Salts - pharmacology
Thiazoles - pharmacology
Time Factors
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Summary:A series of icariin derivatives were synthesized. Their multidrug resistance (MDR) reversal activities were evaluated by MTT assay and the results indicated that the derivatives were the potent modulators of MDR. It was showed that the derivatives significantly increased the intracellular accumulation of ADR in MCF-7/ADR cells compared with drug sensitive MCF-7 cells. The results of bi-directional assay and reverse transcription polymerase chain reaction (RT-PCR) assay showed that the derivatives had high inhibitory activity against P-gp efflux function and significantly down-regulated on the expression of P-gp.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2009.05.103