Abstract
Multidrug resistance (MDR) is a serious obstacle encountered in cancer treatment. In this study, we established an in vitro multiple drug resistant HepG2 cell line (HepG2/ADM), and characterized its MDR. This model was used to screen potential candidate chemosensitisers from over 200 purified naturally occurring compounds extracted from plants and animals. Cantharidin was found to have a significant reversal on MDR in our model. Further, our results showed that Cantharidin could significantly inhibit P-gp (P-glycoprotein) expression, mRNA transcription, as well as MDR1 promoter activity. These results suggest that Cantharidin is a novel and potent MDR reversal agent and may be a potential adjunctive agent for tumor chemotherapy.
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 / drug effects
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ATP Binding Cassette Transporter, Subfamily B, Member 1 / genetics*
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Cantharidin / pharmacology*
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Cantharidin / therapeutic use
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Carcinoma, Hepatocellular / drug therapy
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Carcinoma, Hepatocellular / genetics*
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Cell Line
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Cell Line, Tumor
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Cell Survival / drug effects
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Down-Regulation
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Drug Resistance, Multiple / drug effects*
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Enzyme Inhibitors / pharmacology
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Enzyme Inhibitors / therapeutic use
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Gene Expression Regulation, Neoplastic / drug effects
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Hepatocytes / cytology
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Hepatocytes / drug effects
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Humans
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Kidney
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Liver Neoplasms / drug therapy
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Liver Neoplasms / genetics*
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RNA, Messenger / genetics
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RNA, Neoplasm / genetics
Substances
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ATP Binding Cassette Transporter, Subfamily B, Member 1
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Enzyme Inhibitors
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RNA, Messenger
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RNA, Neoplasm
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Cantharidin