In this study, firstly, 1‐(7‐ethoxy‐1‐benzofuran‐2‐yl) ethanone and 1,1’‐(7‐ethoxy‐1‐benzofuran‐2,4‐diyl)diethanone were synthesized for the starting reagent purposes. The synthesized benzofuran‐chalcone salts were soluble in water at room temperature. Structural analysis of the synthesized compounds was characterized by elemental analysis, FT‐IR and NMR spectroscopy techniques. The anticancer activities of the compounds were determined by SRB viability assay in human lung cancer (A549, H1299) and breast cancer (MCF‐7, MDA‐MB‐231) cell lines. Findings for apoptosis were determined by flow cytometry analysis and the PARP‐ELISA method. The results of the in vitro SRB analysis of the compounds showed that some of the chalcone hybrids were very effective on both types of cancer in a dose and time‐dependent manner. Treatment of all cancer cell types with these hybrids resulted in a significant increase in the percentage of early and mainly late apoptotic cells, demonstrating their apoptosis‐inducing effects via the Caspase 3/7 Activity.
This article covers the anticancer activities and mechanisms of action of Cu(II) complexes of flavonoid‐derived quercetin and 1,10‐phenanthroline ligands. The antiproliferative activity of the complex and its ligands was evaluated by MTT, ATP, and SRB viability assays in human lung cancer cells (A549, H1299). Findings for apoptosis were determined by fluorescent staining, flow cytometry analysis, and the M30 antigen method. In addition, the mechanism of action of the complex was investigated by Annexin V staining, caspase 3/7 activity, ROS formation, and cell cycle analysis. The involvement of caspases, thus, apoptosis was confirmed by rescuing cell death by using a pan‐caspase inhibitor (Z‐VAD‐FMK). Again, increased ROS levels in the cell showed that death may occur by apoptosis. For this reason, the accuracy of ROS‐induced apoptosis in cells has been proven as a result of the application of N‐acetylcysteine (NAC), which is a ROS inhibitor. The efficacy of the complex was compared with Cisplatin and ligands. The results showed that the Cu(II) flavonoid complex is cytotoxic on lung cancer cells and may have the potential to act as an effective metal‐based anticancer drug with a lower IC50 over Cisplatin.
Angelica sylvestris and Delphinium staphisagria are medicinal and aromatic herbs with a long history in medicine and food industry. In this study, we have investigated anti-cancer activity of Angelica sylvestris and Delphinium staphisagria extracts on various cell lines of lung (A549), breast (MCF-7), colon (HT-29), and cervix (HeLa) origin. Also, cytotoxicity was tested on human healthy bronchial epithelial (BEAS-2B) cells. In vitro experiments showed that plant extracts suppressed cell growth and proliferation at low concentrations by reducing cell viability on cancer cells in a time and concentration-dependent manner. It was observed that Angelica sylvestris was more effective in HT-29 and HeLa cells and Delphinium staphisagria in A549 and MCF-7 cells by suppressing cell proliferation and increasing cell death. Cell death mode (apoptosis/necrosis) was investigated via fluorescent imaging, caspase-cleaved cytokeratin 18, activated caspase-3, and cleaved-PARP (poly (ADP-ribose) polymerase). In order to evaluate the cell death HIGHLIGHTS• Anticancer activities of ASE and DSE extracts were investigated.• Angelica sylvestris have anticancer potential on HT-29 and HeLa cells.• Delphinium staphisagria have anticancer potential on A549 and MCF-7 cells.• ASE and DSE extracts induce apoptosis on cancer cells.
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