Abstract：
:Parthenolide (PTL), a well-known sesquiterpene lactone of natural origin with α,β-unsaturated carbonyl structure, has proven to show promising anti-cancer properties. In this report, anti-proliferative potential of two synthetic methyleneisoxazolidin-5-ones, MZ-6 and MZ-14, with the same structural motif, has been investigated in human hepatoma HepG2 cells. The effects on apoptosis induction and DNA damage were evaluated. All compounds decreased the number of live cells and increased the number of late apoptotic cells. However, only MZ-14 was able to induce DNA damage. Both synthetic compounds increased intracellular reactive oxygen species (ROS) generation and mitochondrial membrane potential changes at the same level as PTL. Additionally, cell survival was analyzed after a combined treatment, in which HepG2 cells were preincubated for 24 h with MZ-6, MZ-14 or PTL and irradiated with different doses of X-rays. The inhibition of cell survival was assessed by the clonogenic assay. We have shown that the clone formation was strongly inhibited by the combined treatment. The synergistic effect was observed for all three compounds but MZ-6 was significantly more effective. It is interesting to note that in HepG2 cells MZ-6 was the least cytotoxic of the tested compounds, did not induce DNA damage and was less active than the others in the clonogenic cell survival assay. It seems advantages from the point of view of the further in vivo studies that the compound with the lowest cytotoxic activity showed the strongest sensitizing effect.
journal_name
Chem Biol Interactjournal_title
Chemico-biological interactionsauthors
Gach K,Grądzka I,Wasyk I,Męczyńska-Wielgosz S,Iwaneńko T,Szymański J,Koszuk J,Janecki T,Kruszewski M,Janecka Adoi
10.1016/j.cbi.2016.01.011subject
Has Abstractpub_date
2016-03-25 00:00:00pages
68-73eissn
0009-2797issn
1872-7786pii
S0009-2797(16)30011-4journal_volume
248pub_type
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