Dipartimento di Scienza e Tecnologia del Farmaco, University of Turin, Via P. Giuria 9, 10125 Torino, Italy.
Dipartimento di Chimica, University of Turin, Via P. Giuria 7, 10125 Torino, Italy.
Molecules. 2021 Sep 12;26(18):5534. doi: 10.3390/molecules26185534.
Vanadium has a good therapeutic potential, as several biological effects, but few side effects, have been demonstrated. Evidence suggests that vanadium compounds could represent a new class of non-platinum, metal antitumor agents. In the present study, we aimed to characterize the antiproliferative activities of fluorescent vanadyl complexes with acetylacetonate derivates bearing asymmetric substitutions on the β-dicarbonyl moiety on different cell lines. The effects of fluorescent vanadyl complexes on proliferation and cell cycle modulation in different cell lines were detected by ATP content using the CellTiter-Glo Luminescent Assay and flow cytometry, respectively. Western blotting was performed to assess the modulation of mitogen-activated protein kinases (MAPKs) and relevant proteins. Confocal microscopy revealed that complexes were mainly localized in the cytoplasm, with a diffuse distribution, as in podocyte or a more aggregate conformation, as in the other cell lines. The effects of complexes on cell cycle were studied by cytofluorimetry and Western blot analysis, suggesting that the inhibition of proliferation could be correlated with a block in the G2/M phase of cell cycle and an increase in cdc2 phosphorylation. Complexes modulated mitogen-activated protein kinases (MAPKs) activation in a cell-dependent manner, but MAPK modulation can only partly explain the antiproliferative activity of these complexes. All together our results demonstrate that antiproliferative effects mediated by these compounds are cell type-dependent and involve the cdc2 and MAPKs pathway.
钒具有良好的治疗潜力,因为已经证明了它具有多种生物学效应,而副作用较少。有证据表明,钒化合物可能代表一类新型的非铂类金属抗肿瘤药物。在本研究中,我们旨在研究具有不对称取代基的β-二酮部分的荧光氧钒配合物对不同细胞系的增殖抑制活性。通过使用 CellTiter-Glo 发光测定法和流式细胞术分别检测荧光氧钒配合物对不同细胞系中增殖和细胞周期调节的影响。通过 Western blot 评估有丝分裂原激活的蛋白激酶(MAPKs)和相关蛋白的调节。共聚焦显微镜显示,复合物主要定位于细胞质中,分布弥散,如足细胞,或在其他细胞系中呈更聚集的构象。通过细胞流式术和 Western blot 分析研究复合物对细胞周期的影响,表明增殖抑制可能与细胞周期 G2/M 期阻滞和 cdc2 磷酸化增加有关。复合物以细胞依赖性方式调节有丝分裂原激活的蛋白激酶(MAPKs)的激活,但 MAPK 调节只能部分解释这些复合物的增殖抑制活性。总之,我们的研究结果表明,这些化合物介导的增殖抑制作用依赖于细胞类型,并涉及 cdc2 和 MAPKs 途径。