Department of Biochemistry, Faculty of Pharmacy, Deraya University, Minia, Egypt.
Department of Biochemistry, Faculty of Pharmacy, Minia University, Minia, Egypt.
Anticancer Res. 2020 May;40(5):2739-2749. doi: 10.21873/anticanres.14245.
BACKGROUND/AIM: Ciprofloxacin has been used as an antibiotic in the clinic for decades. Recently, ciprofloxacin and its derivatives have shown promising anti-proliferative and cytotoxic activities against several malignant cells. The aim of this study was to investigate the effect of a new derivative of ciprofloxacin on colorectal cancer (HCT116) and non-small lung carcinoma (A549) cells.
Cell viability was detected by the MTT assay. Flow cytometry was used to examine the cell cycle and apoptosis. Expression of bax, bcl2, p53 and p21 was investigated by qRT-PCR and western blotting.
Ciprofloxacin-derivative had an anti-proliferative effect on both cell lines in a concentration-dependent manner and caused cell cycle arrest at the G/M phase and apoptosis. p53 and Bax proteins were overexpressed, while p21 and bcl2 gene expression was decreased after treatment with the ciprofloxacin derivative.
This new ciprofloxacin derivative can be potentially used for the treatment of colorectal cancer and non-small lung carcinoma.
背景/目的：环丙沙星作为一种抗生素在临床上已经使用了几十年。最近，环丙沙星及其衍生物对几种恶性细胞表现出有前景的抗增殖和细胞毒性作用。本研究旨在探讨一种新型环丙沙星衍生物对结直肠癌（HCT116）和非小细胞肺癌（A549）细胞的影响。
用 MTT 法检测细胞活力。用流式细胞术检测细胞周期和凋亡。用 qRT-PCR 和 Western blot 检测 bax、bcl2、p53 和 p21 的表达。
环丙沙星衍生物对两种细胞系均具有浓度依赖性的增殖抑制作用，并导致细胞周期阻滞在 G/M 期和凋亡。p53 和 Bax 蛋白表达上调，而 p21 和 bcl2 基因表达下调。
这种新型环丙沙星衍生物可能可用于治疗结直肠癌和非小细胞肺癌。
