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

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 G1 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.

Graphical abstractA series of xanthones have been synthesized and evaluated their antioxidant and cytotoxic activities. The enhancement of reactive oxygen species in NTUB1 cells was observed.Figure optionsDownload full-size imageDownload as PowerPoint slideResearch highlights► A series of xanthone derivatives were synthesized. ► Several synthetic xanthones identified as XO inhibitor and revealed ABTS·+ scavenging activity. ► 2 and 8 induced an accumulation of NTUB1 in the G1 phase arrest and apoptosis by the increase of ROS level. ► The combination of cisplatin and antioxidant 2 enhanced the cell death in NTUB1 cells.