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Synthesis, immunomodulation and cytotoxic effects of vanadium (IV) complexes

机译:钒(IV)配合物的合成,免疫调节和细胞毒性作用

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Vanadium is known to exhibit several bioactivities and shows potential as a pharmaceutical drug. The current studies were conducted with the goal of synthesizing a new generation of oxovanadium(IV) complexes, investigating their effects on cancer cell proliferation and their immunomodulatory properties, and predicting possible structure activity relationships. The elucidation of the structures of the synthesized complexes was achieved using elemental analysis, conductivity measurements, magnetic property measurements, and IR and electronic spectroscopies. These studies suggest that the synthesized complexes have a binuclear structure. All of the complexes were evaluated on different cancer cell lines, including HeLa, PC-3, and C33A, and on the normal 3T3 fibroblast cells. Some of the compounds exhibited prominent inhibitory activities on the cervical cancer cell lines and the prostate cancer PC-3 cells. The immunomodulatory activity of the vanadium compounds was evaluated on human phagocytes for ROS (reactive oxygen species) production using luminol- and lucigenin-based chemiluminescence assays. No potent effect was exerted by the majority of the tested compounds on whole blood oxidative burst activity. A study of human T-cells proliferation in vitro on vanadium complexes was also conducted. The majority of the compounds were observed to exhibit potent inhibitory effects. The superoxide, nitric oxide and DPPH (2,2-diphenyl-1- picrylhydrazyl) radical scavenging properties were also determined.
机译:钒具有多种生物活性,并显示出作为药物的潜力。进行当前的研究的目的是合成新一代的氧钒(IV)复合物,研究其对癌细胞增殖的影响及其免疫调节特性,并预测可能的结构活性关系。使用元素分析,电导率测量,磁性能测量以及IR和电子光谱学对合成复合物的结构进行了阐明。这些研究表明合成的复合物具有双核结构。在不同的癌细胞系(包括HeLa,PC-3和C33A)以及正常的3T3成纤维细胞上评估了所有复合物。一些化合物对子宫颈癌细胞系和前列腺癌PC-3细胞表现出显着的抑制活性。使用基于鲁米诺和光泽精的化学发光分析评估了钒化合物对人吞噬细胞产生ROS(活性氧)的免疫调节活性。大多数测试化合物对全血氧化爆发活性没有发挥有效作用。还进行了人类T细胞在钒配合物上的体外增殖研究。观察到大多数化合物表现出有效的抑制作用。还测定了超氧化物,一氧化氮和DPPH(2,2-二苯基-1-甲基肼基)的自由基清除性能。

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