Source:http://linkedlifedata.com/resource/pubmed/id/19051210
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
4
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pubmed:dateCreated |
2009-3-30
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pubmed:abstractText |
Five phenylbutenoid derivatives from the rhizomes of Zingiber cassumunar Roxb. (Zingiberaceae) were evaluated for their P-glycoprotein (P-gp) inhibitory effects in a P-gp over-expressing multidrug resistant (MDR) human breast cancer cell line, MCF-7/ADR. As a result, a phenylbutenoid dimer, (+/-)-trans-3-(3,4-dimethoxyphenyl)-4-[(E)-3,4-dimethoxystyryl]cyclohex-1-ene (1), exhibited highly potent P-gp inhibitory activity, decreasing the IC(50) value of daunomycin (DNM) to 4.31 +/- 0.40 microm in the cells (DNM IC(50) = 37.1 +/- 0.59 microm). The positive control, verapamil decreased the IC(50) value of DNM to 6.94 +/- 0.40 microm. Three phenylbutenoid monomers, 2-4 from this plant, also resulted in a significant decrease in the IC(50) values of DNM compared with the control. In particular, compound 1 markedly enhanced [(3)H]-DNM accumulation and significantly reduced [(3)H]-DNM efflux compared with the control, and this effect was more potent than that of verapamil, a well-known P-gp inhibitor. These results suggest that compound 1 of Z. cassumunar can be developed as a potent chemo-sensitizing agent that reverses P-gp-mediated MDR in human cancer chemotherapy.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Cyclohexenes,
http://linkedlifedata.com/resource/pubmed/chemical/Daunorubicin,
http://linkedlifedata.com/resource/pubmed/chemical/P-Glycoprotein,
http://linkedlifedata.com/resource/pubmed/chemical/Verapamil,
http://linkedlifedata.com/resource/pubmed/chemical/trans-3-(3,4-dimethoxyphenyl)-4-((E)...
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pubmed:status |
MEDLINE
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pubmed:month |
Apr
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pubmed:issn |
1099-1573
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pubmed:author | |
pubmed:copyrightInfo |
(c) 2008 John Wiley & Sons, Ltd.
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pubmed:issnType |
Electronic
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pubmed:volume |
23
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
472-6
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pubmed:meshHeading |
pubmed-meshheading:19051210-Cell Line, Tumor,
pubmed-meshheading:19051210-Cyclohexenes,
pubmed-meshheading:19051210-Daunorubicin,
pubmed-meshheading:19051210-Drug Resistance, Neoplasm,
pubmed-meshheading:19051210-Humans,
pubmed-meshheading:19051210-Inhibitory Concentration 50,
pubmed-meshheading:19051210-Molecular Structure,
pubmed-meshheading:19051210-P-Glycoprotein,
pubmed-meshheading:19051210-Rhizome,
pubmed-meshheading:19051210-Verapamil,
pubmed-meshheading:19051210-Zingiberaceae
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pubmed:year |
2009
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pubmed:articleTitle |
Potent modulation of P-glycoprotein activity by naturally occurring phenylbutenoids from Zingiber cassumunar.
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pubmed:affiliation |
College of Pharmacy, Center for Cell Signaling and Drug Discovery Research, Ewha Womans University, Seoul 120-750, Korea.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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