7-Piperazine ethyl chrysin inhibits proliferation of lung cancer cells via induction of apoptosis

Di Li, Lifei Li, Lingzhan Wang, Jianguo Li, Bin Zhang
2019 Tropical Journal of Pharmaceutical Research  
Purpose: To investigate the effect of 7-piperazine ethyl chrysin (PEC) on A-427 and A-549 lung cancer cell lines. Methods: The cell lines were incubated with PEC at doses of 2, 4, 6, 8 and 10 µM for 24, 48 and 72 h, and their viabilities at each time interval were assessed using 3-(4,5-dimethylthiazol-2-yl)-2,5diphenyltetrazolium bromide (MTT) assay. Cell apoptosis was evaluated with annexin V fluorescein isothiocyanate/propidium iodide staining, while the expression of ERK1/2 protein was
more » ... 2 protein was determined using western blot. The involvement of ERK1/2 in the effect of PEC on viability and apoptosis was assessed by incubating the cells with PD98059 (an inhibitor of ERK1/2). Results: Exposure to PEC at doses ≥ 4 µM significantly reduced the viability of A-427 and A-549 cell lines in time-and concentration-dependent manners at 48 h (p < 0.02). The viability of A-427 and A-549 cells was reduced to 21 and 18 %, respectively, on treatment with 8 µM PEC for 48 h. Moreover, PEC treatment induced apoptosis in A-427 (59.67 %) and A-549 (61.37 %) cells after 48 h. Western blot data revealed that PEC also significantly inhibited phosphorylation of ERK1/2 in both cancer cell lines (p < 0.05). Incubation of A-427 and A-549 cells with PD98059 for 48 h also reduced their viability and induced their apoptosis (p < 0.05). Conclusion: These results indicate that PEC inhibits the viability of lung cancer cells via inhibition of ERK1/2 expression. Thus, PEC may be efective for the treatment of lung carcinoma but further studies are required to ascertain this. This is an Open Access article that uses a funding model which does not charge readers or their institutions for access and distributed under the terms of the Creative Commons Attribution License (http://creativecommons.org/licenses/by/4.0) and the Budapest
doi:10.4314/tjpr.v17i10.4 fatcat:5ta3d3seofb7zcc27yeyyw4eg4