Department of Public Health, Dietetics and Lifestyle Disorders, Faculty of Medicine, University of Information Technology and Management in Rzeszow, Sucharskiego 2, 35-225 Rzeszow, Poland.
Department of Public Health, Dietetics and Lifestyle Disorders, Faculty of Medicine, University of Information Technology and Management in Rzeszow, Sucharskiego 2, 35-225 Rzeszow, Poland.
Chem Biol Interact. 2017 Jan 25;262:46-56. doi: 10.1016/j.cbi.2016.12.008. Epub 2016 Dec 11.
4-Thiazolidinones are a known class of prospective drug-like molecules, especially in the design of new anticancer agents. Two of the most prominent subtypes of these compounds are 5-ene-2-amino(amino)-4-thiazolidinones and thiopyrano[2,3-d]thiazoles. The latter are considered to be cyclic mimetics of biologically active 5-ene-4-thiazolidinones with similar pharmacological profiles. Therefore, the aim of this study was to evaluate the impact of 4-thiazolidinone-based compounds on cytotoxicity, the apoptotic process, and metabolism in the human squamous carcinoma (SCC-15) cell line. The SCC-15 cells were cultured in phenol red-free DMEM/F12 medium supplemented with 10% FBS, hydrocortisone, and exposed to rising concentrations (1 nM-100 μM) of the studied compounds for 6, 24 and 48 h. Afterwards, reactive oxygen species (ROS) formation, cell viability, caspase-3 activity, and cell metabolism were measured. The obtained results showed that all of the studied compounds in a wide range of concentrations (1 nM-100 μM) increased DCF fluorescence which suggests a stimulation of ROS production. Nevertheless, these new compounds showed cytotoxic and proapoptotic properties only at high (10-100 μM) concentrations. Our studies are the first to be carried out on these compounds and require further investigation to clarify the mechanism of action of their anticancer potential.
4-噻唑烷酮是一类已知的潜在药物样分子，特别是在设计新型抗癌药物方面。这些化合物中最突出的两个亚类是 5-烯-2-氨基（氨基）-4-噻唑烷酮和噻吩并[2,3-d]噻唑。后者被认为是具有相似药理学特征的生物活性 5-烯-4-噻唑烷酮的环状类似物。因此，本研究的目的是评估基于 4-噻唑烷酮的化合物对人鳞状细胞癌（SCC-15）细胞系的细胞毒性、细胞凋亡过程和代谢的影响。将 SCC-15 细胞在无酚红 DMEM/F12 培养基中培养，该培养基中添加 10% FBS、氢化可的松，并使细胞暴露于研究化合物的上升浓度（1 nM-100 μM）下 6、24 和 48 h。然后，测量活性氧（ROS）形成、细胞活力、caspase-3 活性和细胞代谢。获得的结果表明，在所研究的化合物的宽浓度范围内（1 nM-100 μM），所有化合物均增加了 DCF 荧光，这表明 ROS 生成受到刺激。然而，这些新化合物仅在高浓度（10-100 μM）下表现出细胞毒性和促凋亡特性。我们的研究是首次针对这些化合物进行的，需要进一步研究以阐明其抗癌潜力的作用机制。
