Anti-tumor activity evaluation of novel chrysin-organotin compound in MCF-7 cells

作者：Xuan, Hong-zhuan^*; Zhang, Jun-hong; Wang, Yue-hua; Fu, Chong-luo; Zhang, Wei

来源：Bioorganic & Medicinal Chemistry Letters, 2016, 26(2): 570-574.

DOI：10.1016/j.bmcl.2015.11.072

• Chrysin
• Chrysin-organotin
• MCF-7 cells
• Apoptosis
• Autophagy

Chrysin (5,7-dihydroxylflavone, Chry) is a natural flavonoid extracted from plants and propolis. In this work, a novel chrysin-organotin (Chry-Sn) compound with enhanced anticancer activities was synthesized by the reaction of chrysin and triphenyltin chloride, and its potential anticancer effects against cancer cells were measured using various methods. Sulforhodamine B (SRB) results showed that chrysin and Chry-Sn had significant inhibition effects on the proliferation of MCF-7, A549 and HeLa human cancer cell lines in a dose-and time-dependent manner. These results suggested that Chry-Sn possessed enhanced anticancer effects. Hoechst 33258 staining and acridine orange staining results showed apoptosis and nuclei fragments significantly increased after being treated with chrysin and Chry-Sn respectively. Moreover, chrysin and Chry-Sn significantly increased ROS levels in MCF-7 cells. Western blot results showed that chrysin and Chry-Sn activated caspase 3 and induced autophagy by increasing LC3-II level. All results showed collectively that Chry-Sn could be a more promising drug than chrysin in anticancer treatment.

• 出版日期2016-1-15
• 单位聊城大学