Furoquinolone and its derivatives exhibit antimicrobial, anti-allergic, anti-inflammatory and anticancer properties. The present study investigated the anti-tumor activity of synthesized intermediates of furoquinolone in human promyelocytic leukemia HL-60 cells. The biological effects of the active compound ethyl 2-anilino-4-oxo-4,5-dihydrofuran-3-carboxylate (compound 131) were examined in HL-60 cells. The following properties were analyzed: Cell survival, cell cycle profile, caspase-3 activity, Bax and Bcl-2 expression, the amount of intracellular Ca2+, the number of reactive oxygen species (ROS) and the mitochondrial membrane potential. Compound 131 (50% cytotoxic concentration, 23.5 µM) significantly reduced the proliferation of HL-60 cells and was revealed to induce apoptosis in HL-60 cells in a concentration-dependent manner. Moreover, this was associated with the activation of caspase-3, upregulation of Bax, an increase in intracellular Ca2+ and ROS production, and a decrease in mitochondrial membrane potential and Bcl-2 expression levels. Compound 131, a novel 4,5-dihydrofuran-3-carboxylate, induced apoptosis in HL-60 cells via the increase of intracellular Ca2+ and ROS to alter the mitochondrial membrane potential and the protein level of Bax and Bcl-2, as well as activating caspase-3. The results of the current study indicate that compound 131 may represent a promising compound for the development of anti-leukemia therapeutics.

中文翻译：

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2-苯胺基-4-氧代-4，5-二氢呋喃-3-羧酸乙酯显示出抗增殖活性，并诱导早幼粒细胞白血病HL-60细胞凋亡。

呋喃喹诺酮及其衍生物具有抗菌，抗过敏，抗炎和抗癌的特性。本研究研究了呋喃喹诺酮的合成中间体在人早幼粒细胞白血病HL-60细胞中的抗肿瘤活性。在HL-60细胞中检查了活性化合物2-苯胺基-4-氧代-4，5-二氢呋喃-3-羧酸乙酯（化合物131）的生物效应。分析了以下特性：细胞存活，细胞周期概况，caspase-3活性，Bax和Bcl-2表达，细胞内Ca2 +的量，活性氧（ROS）的数量和线粒体膜电位。化合物131（50％的细胞毒性浓度，23.5 µM）显着降低了HL-60细胞的增殖，并显示出以浓度依赖的方式诱导HL-60细胞凋亡。而且，这与caspase-3的激活，Bax的上调，细胞内Ca2 +和ROS产生的增加以及线粒体膜电位和Bcl-2表达水平的降低有关。化合物131，一种新型的4,5-二氢呋喃-3-羧酸盐，通过增加细胞内Ca2 +和ROS改变线粒体膜电位以及Bax和Bcl-2的蛋白水平，诱导HL-60细胞凋亡。激活caspase-3。当前研究的结果表明，化合物131可能代表抗白血病治疗药物开发的有前途的化合物。5-二氢呋喃-3-羧酸盐通过细胞内Ca2 +和ROS的增加诱导HL-60细胞凋亡，从而改变线粒体膜电位和Bax和Bcl-2的蛋白水平，并激活caspase-3。当前研究的结果表明，化合物131可能代表抗白血病治疗药物开发的有前途的化合物。5-二氢呋喃-3-羧酸盐通过细胞内Ca2 +和ROS的增加诱导HL-60细胞凋亡，从而改变线粒体膜电位和Bax和Bcl-2的蛋白水平，并激活caspase-3。当前研究的结果表明，化合物131可能代表抗白血病治疗药物开发的有前途的化合物。