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Tenacigenin B derivatives reverse P-glycoprotein-mediated multidrug resistance in HepG2/Dox cells

  作者 Hu, YJ; Shen, XL; Lu, HL; Zhang, YH; Huang, XA; Fu, LC; Fong, WF  
  选自 期刊  Journal of natural products;  卷期  2008年71-6;  页码  1049-1051  
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[摘要]Tenacissimoside A (1) and 11 alpha-O-benzoyl-12 beta-O-acetyltenacigenin B (2), two derivatives of tenacigenin B (3) from the plant Marsdenia tenacissima, reversed multidrug resistance in P-glycoprotein (Pgp)-overexpressing multidrug-resistant cancer cells. The sensitivity of HepG2/Dox cells to the antitumor drugs doxorubicin, vinblastine, puromycin, and paclitexel was increased by 18, 10, 11-, and 6-fold by 20 mu g/mL (or 25 mu M) of 1 and 16-, 53-, 16-, and 326-fold by 20 mu g/mL (or 39 mu M) of 2, respectively. A preliminary mechanistic study has suggested that I might modulate Pgp-mediated multidrug resistance through directly interacting with the Pgp substrate site.

 
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