Abstract

Background:Cancer is a significant health problem around the world and one of the leading causes of human death. The need for novel, selective and non-toxic anti-cancer agents is still urging. Aim of the work: to investigate the anti-proliferative and pro-apoptotic effects of the synthesized ciprofloxacin 3,4,5 tri-methoxy chalcone hybrid (CCH) on the HepG2 hepatocellular carcinoma and MCF7 breast carcinoma cell lines. Materials and Methods:HepG2 and MCF7cell lines were treated with CCH. Cell viability and cell cycle analysis were performed. Protein and mRNA expression levels of P53, COX-2 and TNF-α were analyzed by western blotting and RT-PCR respectively. Results:CCH caused concentration and time-dependent reduction in the viability of human HepG2 and MCF7 cells, pre-G1 apoptosis and cell cycle arrest at G2/M stage, significantly higher P53 and TNF-α mRNA and protein expression levels but significantly lower COX2 mRNA and protein expression levels. Conclusion:CCH showed obvious anti-proliferative and apoptosis-inducing activities in both cell lines.

Highlights

  • Being one of the most urging health problems worldwide, Cancer is still one of the most difficult medical challenges (Abd El-Baky et al, 2020; Avendan and Menéndez, 2008)

  • Protein and mRNA expression levels of P53, COX-2 and TNF-α were analyzed by western blotting and Reverse transcriptase-polymerase chain reaction (RT-PCR) respectively

  • When MCF7 and HepG2 cell lines were treated with IC50 (54 ug/ml and 22ug/ml) of chalcone hybrid (CCH) respectively for 24h, we found a substantial amount of cells arrested during the G2/M phase

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Summary

Introduction

Being one of the most urging health problems worldwide, Cancer is still one of the most difficult medical challenges (Abd El-Baky et al, 2020; Avendan and Menéndez, 2008). It was shown to induce cell cycle arrest, break DNA double‐strands, and trigger apoptosis of cancer cells (Smart et al, 2008). At high concentrations (usually 200-300 μg/ml), ciprofloxacin can cause apoptosis of bladder carcinoma cells and may lead to the arrest of the cell cycle at the S/ G2 stage (Aranha et al, 2000). Aim of the work: to investigate the anti-proliferative and pro-apoptotic effects of the synthesized ciprofloxacin 3,4,5 tri-methoxy chalcone hybrid (CCH) on the HepG2 hepatocellular carcinoma and MCF7 breast carcinoma cell lines. Results: CCH caused concentration and time-dependent reduction in the viability of human HepG2 and MCF7 cells, pre-G1 apoptosis and cell cycle arrest at G2/M stage, significantly higher P53 and TNF-α mRNA and protein expression levels but significantly lower COX2 mRNA and protein expression levels. Conclusion: CCH showed obvious anti-proliferative and apoptosis-inducing activities in both cell lines

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