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

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• 作者：Hong-zhuan Xuan^a ; ^&dagger ; ; ^{hongzhuanxuan@163.com" class="auth_mail" title="E-mail the corresponding author} ; Jun-hong Zhang^b ; ^&dagger ; ; Yue-hua Wang^a ; Chong-luo Fu^a ; Wei Zhang^a
• 关键词：Chrysin ; Chrysin&ndash ; organotin ; MCF-7 cells ; Apoptosis ; Autophagy
• 刊名：Bioorganic & Medicinal Chemistry Letters
• 出版年：2016
• 出版时间：15 January 2016
• 年：2016
• 卷：26
• 期：2
• 页码：570-574
• 全文大小：1750 K

文摘

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.