Apoptotic effect of Naphthoquinone derivatives on HCT116 colon cancer cells

Naphthoquinone is found in the core structure of many natural compounds, most notably the K vitamins. Numerous molecules with the 1,4-naphthoquinone moiety are known to display distinct biological activities including anti-cancer, anti-inflammatory and anti-bacterial activities. Vitamin K2 and doxorubicin, which are used to treat bleeding and lymphoma respectively, belong to this class of chemicals. Although the exact mechanism of action of these molecules is still under investigation, it may include interactions with DNA, inhibition of topoisomerase II, and production of ROS, all of which contribute individually or in combination to DNA damage and cell death. Based on our previous study, 3 novel naphthoquinone derivatives were synthesized and their anti-proliferative activity against HCT116 colon cancer cells was assessed using FACS and Caspase assays. Using this analysis, we found that the production of ROS by naphthoquinones played a critical role in the induction of apoptosis, since pre-treatment of the cells with antioxidant NAC decreased the cytotoxicity level of these compounds.