Tenacigenin B Derivatives Reverse P-Glycoprotein-Mediated Multidrug Resistance inHepG2/Dox Cells

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• 作者：Ying-Jie Hu ; Xiao-Ling Shen ; Hong-Long Lu ; Yu-Hu Zhang ; Xin-An Huang ; Lin-Chun Fu ; Wang-Fun Fong
• 刊名：Journal of Natural Products
• 出版年：2008
• 出版时间：June 2008
• 年：2008
• 卷：71
• 期：6
• 页码：1049 - 1051
• 全文大小：88K
• 年卷期：v.71,no.6(June 2008)
• ISSN：1520-6025

文摘

Tenacissimoside A (1) and 11α-O-benzoyl-12β-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 μg/mL (or 25 µM) of 1 and 16-, 53-, 16-, and 326-fold by 20 μg/mL (or 39 µM) of 2, respectively. A preliminary mechanistic study has suggested that 1 might modulate Pgp-mediated multidrug resistance through directly interacting with the Pgp substrate site.