Abstract
Euphorbia factor L1 (EFL1) belongs to diterpenoids of genus Euphorbia. In this article, its reversal activity against ABCB1-mediated MDR in KBv200 and MCF-7/adr cells was reported. However, EFL1 did not alter the sensitivity of KB and MCF-7 cells to chemotherapeutic agents. Meanwhile, EFL1 significantly increased accumulation of doxorubicin and rhodamine 123 in KBv200 and MCF-7/adr cells, showing no significant influence on that of KB and MCF-7 cells. Furthermore, EFL1 could enhance the ATP hydrolysis activity of ABCB1 stimulated by verapamil. At the same time, EFL1 inhibited the efflux of ABCB1 in KBv200 and MCF-7/adr cells. In addition, EFL1 did not downregulate expression of ABCB1 in KBv200 and MCF-7/adr cells either in mRNA or protein level.
Copyright © 2011 Wiley-Liss, Inc.
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
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ATP Binding Cassette Transporter, Subfamily B, Member 1 / genetics
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ATP Binding Cassette Transporter, Subfamily B, Member 1 / metabolism*
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Adenosine Triphosphatases / metabolism
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Adenosine Triphosphate / metabolism
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Antibiotics, Antineoplastic / metabolism
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Antibiotics, Antineoplastic / pharmacokinetics
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Antibiotics, Antineoplastic / pharmacology
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Blotting, Western
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Cell Line, Tumor
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Cell Survival / drug effects
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Diterpenes / chemistry
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Diterpenes / metabolism
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Diterpenes / pharmacology*
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Dose-Response Relationship, Drug
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Down-Regulation
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Doxorubicin / metabolism
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Doxorubicin / pharmacokinetics
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Doxorubicin / pharmacology
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Drug Resistance, Multiple / drug effects*
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Drug Resistance, Neoplasm / drug effects*
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Euphorbia / chemistry*
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Flow Cytometry
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Humans
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Hydrolysis / drug effects
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Molecular Structure
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Phenylpropionates / chemistry
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Phenylpropionates / pharmacology*
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Plant Extracts / chemistry
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Plant Extracts / metabolism
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Plant Extracts / pharmacology
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Reverse Transcriptase Polymerase Chain Reaction
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Rhodamine 123 / metabolism
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Rhodamine 123 / pharmacokinetics
Substances
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ABCB1 protein, human
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ATP Binding Cassette Transporter, Subfamily B
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ATP Binding Cassette Transporter, Subfamily B, Member 1
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Antibiotics, Antineoplastic
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Diterpenes
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Phenylpropionates
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Plant Extracts
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euphorbia factor L1
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Rhodamine 123
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Doxorubicin
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Adenosine Triphosphate
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Adenosine Triphosphatases