氟喹诺酮类抗生素包括盖氏沙星的衍生物。最近，这些物质被推崇用于癌症治疗。在本研究中，我们检查了一种新型合成的盖氏沙星衍生物在人髓性白血病细胞株KG1-a中的细胞毒性和诱导凋亡潜力。这种盖氏沙星衍生物，7-(4-(2-(苯基氧基)-2-氧乙基)-哌嗪-1-基)-1-环丙基-6-氟-4-氧-1,4-二氢喹啉-3-羧酸（4-BHPCP），在IC50为25µM的浓度下，表现出活性药物的特性。通过荧光染料Hoechst 33,258染色和Annexin V/PI双染实验，对4-BHPCP的凋亡活性进行了形态学评估。实时定量PCR被用来评估一些与凋亡相关基因的表达水平的变化，包括Bcl-2、Bax和Survivin（qRT-PCR）。qRT-PCR分析结果表明，4-BHPCP通过时间依赖性地下调Survivin和Bcl-2，上调Bax以及增加Bax/Bcl-2基因的转录，促进了KG1-a细胞系中的凋亡。这些结果暗示着这种新型化合物可能是治疗急性髓系白血病的有前途的选择。© 2023. 作者与斯普林格自然集团（Springer Nature）下属斯普林格科学与商业媒体有限责任公司（Springer Science+Business Media, LLC）有独家许可。

The fluoroquinolone class of antibiotics includes derivatives of the drug ciprofloxacin. These substances have recently been advocated for the treatment of cancer. In the current study, we examined the cytotoxicity and apoptosis-inducing potential of a novel synthetic ciprofloxacin derivative in the human myeloid leukemia KG1-a cell line. With an IC50 of 25µM, this ciprofloxacin derivative, 7-(4-(2-(benzhydryloxy)-2-oxoethyl) piperazin-1-yl)-1-cyclopropyl-6-fluoro-4-oxo-1,4 dihydroquinoline-3- carboxylic acid (4-BHPCP), was an active drug. Through Hoechst 33,258 staining and Annexin V/PI double staining experiments, the apoptotic activity of the 4-BHPCP was assessed morphologically. Real-time quantitative PCR was used to assess changes in the expression level of certain apoptosis-related genes, including Bcl-2, Bax, and Survivin (qRT PCR). The results of the qRT PCR analysis demonstrated that 4-BHPCP promotes apoptosis in the KG1-a cell line by down-regulating Survivin and Bcl2, up-regulating Bax, and increasing the Bax/Bcl2 transcripts in a time-dependent manner. These results imply that this novel chemical may be a promising therapy option for acute myeloid leukemia.© 2023. The Author(s), under exclusive licence to Springer Science+Business Media, LLC, part of Springer Nature.