Evaluation of anticancer properties of a new α-methylene-δ-lactone DL-249 on two cancer cell lines
2017
Pomorska, Dorota K. | Gach-Janczak, Katarzyna | Jakubowski, Rafał | Janecki, Tomasz | Szymański, Jacek | Janecka, Anna
The anticancer activity of a new synthetic α-methylene-δ-lactone DL-249 was reported in leukemia HL-60 and breast cancer MCF-7 cells and compared with the activity of a natural α-methylene-γ-lactone from Tanacetum parthenium, parthenolide. The chemical synthesis of DL-249 was performed using Horner-Wadsworth-Emmons methodology. The cytotoxic activity of the tested compounds was assessed by an MTT test. The ability to induce apoptosis was studied by flow cytometry. The expression levels of genes were determined by quantitative real-time PCR. DL-249 and parthenolide inhibited the growth of HL-60 and MCF-7 cells with IC₅₀ values below 10 μM. DL-249 was a stronger apoptosis inducer than parthenolide in both cell lines and both compounds produced a more pronounced effect on HL-60 than on MCF-7 cells. DL-249 and PTL significantly up-regulated expression of Bax, caspase-9, caspase-3 and p53 genes and decreased the level of Bcl-2 and Bcl-xl genes in both cancer cell lines. Additionally DL-249 caused cell cycle arrest in the subG0/G1phase. A new synthetic α-methylene-δ-lactone, DL-249 showed the anticancer activity on two cancer cell lines and seemed to be a better apoptosis inducer than parthenolide which makes this compound an attractive lead for further studies.
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