In this work, we present a recently developed ruthenium complex that shows anticancer activity in gallbladder cancer cells. After the synthesis of the new ruthenium complexes, the antiproliferative, cytotoxicity, and apoptosis activities were evaluated in vitro by the triple assay ApoTox-Glo. Then, the transcription levels of genes related to apoptosis were evaluated by real-time PCR (q-PCR). The ruthenium complex, called Ru-UCN3, inhibits the proliferation of gallbladder cancer cells G-415 by means of apoptosis, which was demonstrated by the overexpression of the pro-apoptotic genes Puma, Diablo, and Caspasa-9 together with the repression of the anti-apoptotic genes Bcl-xL and Bcl-2. In addition, we found strong caspase 3/7 activity in the cells at 24 h of the Ru-UCN3 exposure, which was evaluated by the triple ApoTox-Glo assay. The new ruthenium complexes evaluated had an inhibitory effect on G-415 cells. We think that Ru-UCN3 could be a promising anticancer agent, which should be explored with more in vitro and in vivo assays and probably with the chemical modulation of this molecule.
在这项工作中,我们介绍了一种新近开发的
钌复合物,它在胆囊癌细胞中显示出抗癌活性。在合成了新的
钌复合物后,我们采用 ApoTox-Glo 三重检测法对其体外抗增殖活性、细胞毒性和细胞凋亡活性进行了评估。然后,通过实时 PCR(q-PCR)评估了与细胞凋亡相关的
基因转录
水平。
钌复合物(Ru-UCN3)通过细胞凋亡抑制了胆囊癌细胞 G-415 的增殖,表现为促凋亡
基因 Puma、Diablo 和 Caspasa-9 的过度表达以及抗凋亡
基因 Bcl-xL 和 Bcl-2 的抑制。此外,我们还发现,在暴露于 Ru-UCN3 24 h 时,细胞中的 caspase 3/7 活性很强。所评估的新
钌复合物对 G-415 细胞具有抑制作用。我们认为,Ru-UCN3 可能是一种很有前途的抗癌剂,应该通过更多的体外和体内试验以及可能对该分子进行的
化学修饰来进行探索。