Abstract

BackgroundThe role of Diphenyldifluoroketone (EF24), a synthetic analogue of curcumin with noteworthy antitumor potential, remains unclear in non-small cell lung cancer (NSCLC). Herein, the inhibitory effect of EF24 on NSCLC and its mechanism were studied.MethodsCytotoxicity was measured by MTT assay, colony formation assay and xenograft model. Cell apoptosis and reactive oxygen species (ROS) level were quantified by flow cytometer. Protein level was detected by western blot assay. Mitochondria and autophagosomes were observed using transmission electron microscope and confocal microscopy.ResultsIn-vitro, EF24 significantly induced proliferation inhibition, apoptosis, mitochondrial fission and autophagy of NSCLC cell lines. These cytotoxic effects were significantly attenuated by two reactive oxygen species (ROS) scavengers, indicating its anti-cancer effects largely depend on ROS accumulation. In-vivo, EF24 inhibited tumor growth in a dose-dependent manner. Moreover, no pathological changes of heart, lung, spleen, kidney and liver of mice were observed. Collectively, EF24 induced ROS accumulation, in turn activates cell apoptosis, and then exerts its cytotoxicity on NSCLC cells.ConclusionsThe results showed that EF24 exerted cytotoxicity against NSCLC via ROS accumulation. Thus, EF24 might serve as a potential anti-cancer agent for the treatment of NSCLC.

Highlights

  • Non-small cell lung cancer (NSCLC) is considered to be the leading type of cancers worldwide, accounting for about 80% of lung cancer cases, and its global morbidity and mortality have been showing a significant upward trend [1]

  • Our findings indicated that EF24 might exert an effective anti-cancer effect by increasing intracellular reactive oxygen species (ROS), which provides a prospect for clinical non-small cell lung cancer (NSCLC) treatment

  • EF24 inhibits the growth and colony formation of NSCLC cells in‐vitro To verify the cytotoxic potency of EF24 against NSCLC, we first determined the effects of EF24 on cell proliferation in four NSCLC cell lines (A549, SPC-A1, H460 and H520)

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Summary

Introduction

Non-small cell lung cancer (NSCLC) is considered to be the leading type of cancers worldwide, accounting for about 80% of lung cancer cases, and its global morbidity and mortality have been showing a significant upward trend [1]. This is closely related to the negative impact of environmental and dietary factors, as well as the. The role of Diphenyldifluoroketone (EF24), a synthetic analogue of curcumin with noteworthy antitumor potential, remains unclear in non-small cell lung cancer (NSCLC). The inhibitory effect of EF24 on NSCLC and its mechanism were studied

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