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

[Display omitted] 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 an...

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 2016-01, Vol.26 (2), p.570-574
Hauptverfasser: Xuan, Hong-zhuan, Zhang, Jun-hong, Wang, Yue-hua, Fu, Chong-luo, Zhang, Wei
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Sprache:eng
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Zusammenfassung:[Display omitted] 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.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2015.11.072