Marinova Petya, Blazheva Denica, Slavchev Aleksandar, Genova-Kalou Petia
Department of General and Inorganic Chemistry with Methodology of Chemistry Education, Faculty of Chemistry, University of Plovdiv, "Tzar Assen" str. 24, 4000 Plovdiv, Bulgaria.
Department of Microbiology and Biotechnology, University of Food Technologies, 26 Maritza Blvd., 4002 Plovdiv, Bulgaria.
BioTech (Basel). 2025 Jul 1;14(3):53. doi: 10.3390/biotech14030053.
This study investigates the cytotoxic properties of metal complexes incorporating thio-uracil derivatives, specifically 2,4-dithiouracil and 6-propyl-2-thiouracil. The research focuses on the cytotoxic effects of Cu(II) and Pd(II) complexes with 6-propyl-2-thiouracil, as well as mixed-ligand transition metal Cu(II) and Au(III) complexes of 2,4-dithiouracil with 2-thiouracil and uracil. Cytotoxic activity was assessed against human cervical carcinoma cells (HeLa) and normal kidney cells from the African green monkey. The results demonstrated that incorporating Cu(II) and Au(III) into the compound structures significantly enhanced their cytotoxic effects. Notably, all tested complexes exhibited a stronger inhibitory effect on cancer cell proliferation compared to normal cells, with the palladium(II) complex of 6-propyl-2-thiouracil showing the lowest CD value against the tumor cell line (0.00064 mM), which were 149 times lower than that of the ligand (0.0955 mM). These findings suggest that thio-uracil-based metal complexes, particularly those containing palladium (II) and gold(III), hold significant potential for further development as anticancer agents.
本研究调查了含有硫代尿嘧啶衍生物（特别是2,4-二硫代尿嘧啶和6-丙基-2-硫代尿嘧啶）的金属配合物的细胞毒性特性。该研究聚焦于铜（II）和钯（II）与6-丙基-2-硫代尿嘧啶形成的配合物的细胞毒性作用，以及2,4-二硫代尿嘧啶与2-硫代尿嘧啶和尿嘧啶形成的混合配体过渡金属铜（II）和金（III）配合物的细胞毒性作用。针对人宫颈癌细胞（HeLa）和非洲绿猴的正常肾细胞评估了细胞毒性活性。结果表明，将铜（II）和金（III）纳入化合物结构显著增强了它们的细胞毒性作用。值得注意的是，与正常细胞相比，所有测试的配合物对癌细胞增殖均表现出更强的抑制作用，6-丙基-2-硫代尿嘧啶的钯（II）配合物对肿瘤细胞系的最低半数致死浓度（CD值）为0.00064 mM，比配体的（0.0955 mM）低149倍。这些发现表明，基于硫代尿嘧啶的金属配合物，特别是那些含有钯（II）和金（III）的配合物，作为抗癌剂具有巨大的进一步开发潜力。
