Chalcone Methoxy Derivatives Exhibit Antiproliferative and Proapoptotic Activity on Canine Lymphoma and Leukemia Cells
Aleksandra Pawlak , Marta Henklewska , Beatriz Hernandez Suarez , Mateusz Łużny , Ewa Kozłowska , Bożena Obmińska-Mrukowicz , Tomasz Janeczko
AbstractChalcones are interesting candidates for anti-cancer drugs due to the ease of their synthesis and their extensive biological activity. The study presents antitumor activity of newly synthesized chalcone analogues with a methoxy group on a panel of canine lymphoma and leukemia cell lines. The antiproliferative effect of the 2′-hydroxychalcone and its methoxylated derivatives was evaluated in MTT assay after 48 h of treatment in different concentrations. The proapoptotic activity was studied by cytometric analysis of cells stained with Annexin V/FITC and propidium iodide and by measure caspases 3/7 and 8 activation. The DNA damage was evaluated by Western blot analysis of phosphorylated histone H2AX. The new compounds had selective antiproliferative activity against the studied cell lines, the most effective were the 2′-hydroxy-2″,5″-dimethoxychalcone and 2′-hydroxy-4′,6′-dimethoxychalcone. 2′-Hydroxychalcone and the two most active derivatives induced apoptosis and caspases participation, but some percentage of necrotic cells was also observed. Comparing phosphatidylserine externalization after treatment with the different compounds it was noted that the addition of two methoxy groups increased the proapoptotic potential. The most active compounds triggered DNA damage even in the cell lines resistant to chalcone-induced apoptosis. The results confirmed that the analogues could have anticancer potential in the treatment of canine lymphoma or leukemia.
|Journal series||Molecules, ISSN 1420-3049, (N/A 100 pkt)|
|Publication size in sheets||0.7|
|Keywords in English||chalcones; apoptosis; DNA damage; anticancer activity; canine cancer cell lines|
|License||Journal (articles only); published final; ; with publication|
|Score||= 100.0, 28-04-2021, ArticleFromJournal|
|Publication indicators||= 3; = 2; : 2017 = 1.146; : 2018 = 3.06 (2) - 2018=3.38 (5)|
|Citation count*||5 (2021-05-16)|
* presented citation count is obtained through Internet information analysis and it is close to the number calculated by the Publish or Perish system.