Potent P-glycoprotein inhibition of emodin derivative: synthesis and biological evaluation

作者：Wang Jianhong; Gan Ying; Li Shaobin; Luo Tianwei; Zhang Yahong; Zhao Jin^*

来源：Medicinal Chemistry Research, 2014, 23(4): 2106-2112.

DOI：10.1007/s00044-013-0805-z

• Emodin derivative
• Biological evaluation
• Cytotoxicity
• P-gp inhibitory activity

A new series of emodin derivatives was prepared and evaluated for their in vitro antiproliferative activity. Preliminary results revealed that these derivatives exhibited weak or negligible cytotoxicity at 10 mu M against various cancer cell lines (i.e., K562, HepG2, and HCT116 cell lines) as well as normal hepatic cells (QSG7701). Interestingly, the evaluation for P-glycoprotein (P-gp) modulation indicated that they possessed potent P-gp inhibitory activity. Among them, the effect of compound 6 on P-gp inhibition was even greater than that of Verapamil, the known P-gp modulator. Therefore, the natural emodin scaffold could be employed as safe and effective modulator of P-gp mediated drug resistance in cancer chemotherapy.

• 出版日期2014-4
• 单位河南大学