Antioxidant xanthone derivatives induce cell cycle arrest and apoptosis and enhance cell death induced by cisplatin in NTUB1 cells associated with ROS

作者：Cheng Jen Hao; Huang A Mei; Hour Tzyh Chyuan; Yang Shyh Chyun; Pu Yeong Shiau; Lin Chun Nan^*

来源：European Journal of Medicinal Chemistry, 2011, 46(4): 1222-1231.

DOI：10.1016/j.ejmech.2011.01.043

• Xanthone
• Antioxidation
• Cytotoxicity
• Reactive oxygen species

In an effort to develop novel antioxidant as anticancer agents, a series of xanthones were prepared. In vitro screening, the synthetic xanthones revealed significant inhibitory effects on xanthine oxidase and ABTS radical-cation scavenging activity. The selective compounds 2 and 8 induced an accumulation of NTUB1 cells in the G(1) phase arrest and cellular apoptosis by the increase of ROS level. The combination of cisplatin and 2 significantly enhanced the cell death in NTUB1 cells. Compounds 2 and 8 did not show cytotoxic activity in selected concentrations against SV-HUC1 cells. The present results suggested that antioxidants 2 and 8 may be used as anticancer agent for enhancing the therapeutic efficacy of anticancer agents and to reduce their side effect.

• 出版日期2011-4