AI Article Synopsis
- Chalcones and their derivatives show potential as compounds with anti-cancer effects against leukemia, specifically targeting the K562 and Jurkat cell lines.
- The study tested three synthetic chalcones (F07, F09, and F10), which exhibited cytotoxicity with IC values between 1.03 and 31.66 µM and induced apoptosis through intrinsic and extrinsic pathways.
- Notably, these compounds did not harm healthy human blood cells or affect platelet function, indicating their potential as safe and effective candidates for new leukemia treatments.
Article Abstract
Chalcones and their derivatives have been described as promising compounds with antiproliferative activity against leukemic cells. This study aimed to investigate the cytotoxic effect of three synthetic chalcones derived from 1-naphthylacetophenone (F07, F09, and F10) in acute leukemia cell lines (K562 and Jurkat) and examine the mechanisms of cell death induced by these compounds. The three compounds were cytotoxic to K562 and Jurkat cells, with IC values ranging from 1.03 to 31.66 µM. Chalcones induced intrinsic and extrinsic apoptosis, resulting in activation of caspase-3 and DNA fragmentation. F07, F09, and F10 were not cytotoxic to human peripheral blood mononuclear cells, did not produce any significant hemolytic activity, and did not affect platelet aggregation after ADP stimulation. These results, combined with calculations of molecular properties, suggest that chalcones F07, F09, and F10 are promising molecules for the development of novel antileukemic drugs.
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| http://dx.doi.org/10.1016/j.bioorg.2021.105315 | DOI Listing |
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