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Potent modulation of p-glycoprotein activity by naturally occurring phenylbutenoids from zingiber cassumunar
- Potent modulation of p-glycoprotein activity by naturally occurring phenylbutenoids from zingiber cassumunar
- Chung S.Y.; Han A.-R.; Sung M.K.; Jung H.J.; Nam J.-W.; Seo E.-K.; Lee H.J.
- Ewha Authors
- 서은경; 이화정; 한아름
- SCOPUS Author ID
- 서은경; 이화정; 한아름
- Issue Date
- Journal Title
- Phytotherapy Research
- Phytotherapy Research vol. 23, no. 4, pp. 472 - 476
- SCI; SCIE; SCOPUS
- Document Type
- 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.
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