Department of Chemistry, University of Isfahan, Isfahan, 81746-73441, Iran.
Department of Chemistry, University of Isfahan, Isfahan, 81746-73441, Iran.
Eur J Med Chem. 2017 Jul 28;135:230-240. doi: 10.1016/j.ejmech.2017.04.053. Epub 2017 Apr 22.
The reaction of a racemic mixture of Schiff base tridentate ligand with vanadium(V) affords homochiral vanadium complex, (VO(R-L))O and (VO(S-L))O due to ligand "self-recognition" process. The formation of homochiral vanadium complex was confirmed by H NMR, C NMR and X-ray diffraction. The HSA- and DNA-binding of the resultant complex is assessed by absorption, fluorescence and circular dichroism (CD) spectroscopy methods. Based on the results, the HSA- and DNA-binding constant, K, were found to be 8.0 × 10 and 1.9 × 10 M, respectively. Interestingly, in vitro cytotoxicity assay revealed the potent anticancer activity of this complex on two prevalent cancer cell lines of MCF-7 (IC50 value of 14 μM) and HeLa (IC50 value of 36 μM), with considerably low toxicity on normal human fibroblast cells. The maximum cell mortality of 12.3% obtained after 48 h incubation of fibroblast cells with 100 μM of the complex. Additionally, the specific DNA- and HSA-binding was also shown using molecular docking method. The synthesized complex displayed high potential for biomedical applications especially for development of novel and efficient anticancer agents.
外消旋席夫碱三齿配体与钒(V)的反应由于配体的“自我识别”过程而得到手性均一的钒配合物(VO(R-L))O 和 (VO(S-L))O。手性钒配合物的形成通过 1H NMR、13C NMR 和 X 射线衍射得到证实。通过吸收、荧光和圆二色性 (CD) 光谱法评估所得配合物与 HSA 和 DNA 的结合。根据结果，发现 HSA 和 DNA 的结合常数 K 分别为 8.0×10 和 1.9×10 M。有趣的是，体外细胞毒性试验表明该配合物对两种常见的癌细胞系 MCF-7（IC50 值为 14 μM）和 HeLa（IC50 值为 36 μM）具有很强的抗癌活性，对正常人类成纤维细胞的毒性相当低。在用 100 μM 配合物孵育 48 小时后，成纤维细胞的最大细胞死亡率为 12.3%。此外，还使用分子对接方法显示了与 DNA 和 HSA 的特异性结合。该合成的配合物具有很高的生物医学应用潜力，特别是用于开发新型有效的抗癌药物。
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