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Potent modulation of p-glycoprotein activity by naturally occurring phenylbutenoids from zingiber cassumunar

Title
Potent modulation of p-glycoprotein activity by naturally occurring phenylbutenoids from zingiber cassumunar
Authors
Chung S.Y.Han A.-R.Sung M.K.Jung H.J.Nam J.-W.Seo E.-K.Lee H.J.
Ewha Authors
서은경이화정한아름
SCOPUS Author ID
서은경scopus; 이화정scopus; 한아름scopusscopus
Issue Date
2009
Journal Title
Phytotherapy Research
ISSN
0951-418XJCR Link
Citation
vol. 23, no. 4, pp. 472 - 476
Indexed
SCI; SCIE; SCOPUS WOS scopus
Abstract
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, (+)-»ans-3-(3, 4-dimethoxyphenyl)- 4-[(E)-3,4-dimethoxystyryl]cyclohex-1-ene (1), exhibited highly potent P-gp inhibitory activity, decreasing the IC50 value of daunomycin (DNM) to 4.31 + 0.40 hm in the cells (DNM IC50 = 37.1 + 0.59 hm). The positive control, verapamil decreased the IC50 value of DNM to 6.94 + 0.40

Im. Three phenylbutenoid monomers, 24 from this plant, also resulted in a significant decrease in the IC50 values of DNM compared with the control. In particular, compound 1 markedly enhanced [ 3H]-DNM accumulation and significantly reduced [3H]-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. Copyright © 2008 John Wiley & Sons, Ltd.
DOI
10.1002/ptr.2650
Appears in Collections:
약학대학 > 약학과 > Journal papers
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