Abstract
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.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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ATP Binding Cassette Transporter, Subfamily B, Member 1 / metabolism
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Antineoplastic Agents / chemical synthesis*
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Antineoplastic Agents / pharmacology
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Caco-2 Cells
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Cell Line, Tumor
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Chemistry, Pharmaceutical / methods*
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Drug Design
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Drug Resistance, Multiple*
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Drug Resistance, Neoplasm*
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Flavonoids / chemical synthesis*
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Flavonoids / pharmacology
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Humans
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Inhibitory Concentration 50
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Models, Chemical
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Reverse Transcriptase Polymerase Chain Reaction
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Tetrazolium Salts / pharmacology
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Thiazoles / pharmacology
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Time Factors
Substances
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ATP Binding Cassette Transporter, Subfamily B, Member 1
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Antineoplastic Agents
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Flavonoids
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Tetrazolium Salts
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Thiazoles
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thiazolyl blue
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icariin