Abás Elisa, Aguirre-Ramírez Diego, Laguna Mariano, Grasa Laura
Departamento de Química Inorgánica, Instituto de Síntesis Química y Catálisis Homogénea, Universidad de Zaragoza-CSIC, Plaza S. Francisco s/n, 50009 Zaragoza, Spain.
Departamento de Farmacología, Fisiología y Medicina Legal y Forense, Facultad de Veterinaria, Universidad de Zaragoza, Miguel Servet, 177, 50013 Zaragoza, Spain.
Biomedicines. 2021 Nov 26;9(12):1775. doi: 10.3390/biomedicines9121775.
New dithiocarbamate cycloaurated complexes have been synthesized and their physicochemical and in vitro antitumor properties have been evaluated. All the performed studies highlighted good transport through the blood and biodistribution, according to the balance between the properties of hydrophilicity/lipophilicity and the binding of moderate strength to the BSA protein. Furthermore, none of the complexes exhibited reduction or decomposition reactions, presenting excellent physiological stability. The in vitro cytotoxic effect was evaluated on human colon cancer cell line Caco-2/TC7, and the complexes showed great antiproliferative activity and excellent selectivity, as much less effect was detected on normal Caco-2/TC7 cells. Most of the complexes exhibit antiproliferative activity that was better than or similar to auranofin, and at least nine times better than that of cisplatin. Its action mechanism is still under discussion since no evidence of cell cycle arrest was found, but an antioxidant role was shown for some of the selective complexes. All complexes were also tested as antimicrobial drugs, exhibiting good activity towards and . bacteria and and fungi.
新型二硫代氨基甲酸盐环金属化金配合物已被合成，并对其理化性质和体外抗肿瘤特性进行了评估。所有开展的研究都表明，根据亲水性/亲脂性特性之间的平衡以及与牛血清白蛋白（BSA）蛋白的中等强度结合，这些配合物在血液中的转运和生物分布良好。此外，没有一种配合物表现出还原或分解反应，具有出色的生理稳定性。在人结肠癌细胞系Caco-2/TC7上评估了体外细胞毒性作用，这些配合物表现出很强的抗增殖活性和出色的选择性，因为在正常Caco-2/TC7细胞上检测到的作用要小得多。大多数配合物表现出的抗增殖活性优于或类似于金诺芬，且至少比顺铂强九倍。由于未发现细胞周期停滞的证据，其作用机制仍在讨论中，但一些选择性配合物显示出抗氧化作用。所有配合物还作为抗菌药物进行了测试，对某些细菌和真菌表现出良好的活性。
