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Water-Soluble Dioxidovanadium(V) Complexes of Aroylhydrazones: DNA/BSA Interactions, Hydrophobicity, and Cell-Selective Anticancer Potential
Inorganic Chemistry ( IF 4.3 ) Pub Date : 2021-10-01 , DOI: 10.1021/acs.inorgchem.1c01899 Gurunath Sahu 1 , Atanu Banerjee 1 , Rajib Samanta 1 , Monalisa Mohanty 1 , Sudhir Lima 1 , Edward R T Tiekink 2 , Rupam Dinda 1
Inorganic Chemistry ( IF 4.3 ) Pub Date : 2021-10-01 , DOI: 10.1021/acs.inorgchem.1c01899 Gurunath Sahu 1 , Atanu Banerjee 1 , Rajib Samanta 1 , Monalisa Mohanty 1 , Sudhir Lima 1 , Edward R T Tiekink 2 , Rupam Dinda 1
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Five new anionic aqueous dioxidovanadium(V) complexes, [{VO2L1,2}A(H2O)n]α (1–5), with the aroylhydrazone ligands pyridine-4-carboxylic acid (3-ethoxy-2-hydroxybenzylidene)hydrazide (H2L1) and furan-2-carboxylic acid (3-ethoxy-2-hydroxybenzylidene)hydrazide (H2L2) incorporating different alkali metals (A = Na+, K+, Cs+) as countercation were synthesized and characterized by various physicochemical techniques. The solution-phase stabilities of 1–5 were determined by time-dependent NMR and UV–vis, and also the octanol/water partition coefficients were obtained by spectroscopic techniques. X-ray crystallography of 2–4 confirmed the presence of vanadium(V) centers coordinated by two cis-oxido-O atoms and the O, N, and O atoms of a dianionic tridentate ligand. To evaluate the biological behavior, all complexes were screened for their DNA/protein binding propensity through spectroscopic experiments. Finally, a cytotoxicity study of 1–5 was performed against colon (HT-29), breast (MCF-7), and cervical (HeLa) cancer cell lines and a noncancerous NIH-3T3 cell line. The cytotoxicity was cell-selective, being more active against HT-29 than against other cells. In addition, the role of hydrophobicity in the cytotoxicity was explained in that an optimal hydrophobicity is essential for high cytotoxicity. Moreover, the results of wound-healing assays indicated antimigration in case of HT-29 cells. Remarkably, 1 with an IC50 value of 5.42 ± 0.15 μM showed greater activity in comparison to cisplatin against the HT-29 cell line.
中文翻译：
芳酰腙的水溶性二氧化钒 (V) 配合物：DNA/BSA 相互作用、疏水性和细胞选择性抗癌潜力
五种新的阴离子水性二氧化钒 (V) 配合物 [{VO 2 L 1,2 }A(H 2 O) n ] α ( 1 – 5 )，与芳酰腙配体 pyridine-4-carboxy acid (3-ethoxy-2 -羟基亚苄基）酰肼（H 2 L 1）和呋喃-2-羧酸（3-乙氧基-2-羟基亚苄基）酰肼（H 2 L 2）结合不同的碱金属（A = Na +，K +，Cs +）作为抗阳离子通过各种物理化学技术合成和表征。溶液相稳定性1 –5通过时间依赖性NMR和UV-vis确定，并且辛醇/水分配系数通过光谱技术获得。2-4的X 射线晶体学证实了钒 (V) 中心的存在，该中心由两个顺式- 氧化 -O 原子和双阴离子三齿配体的 O、N 和 O 原子配位。为了评估生物学行为，通过光谱实验筛选了所有复合物的 DNA/蛋白质结合倾向。最后，细胞毒性研究1 – 5对结肠 (HT-29)、乳腺癌 (MCF-7) 和宫颈 (HeLa) 癌细胞系和非癌性 NIH-3T3 细胞系进行了研究。细胞毒性是细胞选择性的，对 HT-29 的活性高于对其他细胞的活性。此外，疏水性在细胞毒性中的作用被解释为最佳疏水性对于高细胞毒性至关重要。此外，伤口愈合试验的结果表明 HT-29 细胞具有抗迁移作用。值得注意的是，与顺铂相比，IC 50值为 5.42 ± 0.15 μM 的1对 HT-29 细胞系表现出更大的活性。
更新日期：2021-10-18
中文翻译：
芳酰腙的水溶性二氧化钒 (V) 配合物：DNA/BSA 相互作用、疏水性和细胞选择性抗癌潜力
五种新的阴离子水性二氧化钒 (V) 配合物 [{VO 2 L 1,2 }A(H 2 O) n ] α ( 1 – 5 )，与芳酰腙配体 pyridine-4-carboxy acid (3-ethoxy-2 -羟基亚苄基）酰肼（H 2 L 1）和呋喃-2-羧酸（3-乙氧基-2-羟基亚苄基）酰肼（H 2 L 2）结合不同的碱金属（A = Na +，K +，Cs +）作为抗阳离子通过各种物理化学技术合成和表征。溶液相稳定性1 –5通过时间依赖性NMR和UV-vis确定，并且辛醇/水分配系数通过光谱技术获得。2-4的X 射线晶体学证实了钒 (V) 中心的存在，该中心由两个顺式- 氧化 -O 原子和双阴离子三齿配体的 O、N 和 O 原子配位。为了评估生物学行为，通过光谱实验筛选了所有复合物的 DNA/蛋白质结合倾向。最后，细胞毒性研究1 – 5对结肠 (HT-29)、乳腺癌 (MCF-7) 和宫颈 (HeLa) 癌细胞系和非癌性 NIH-3T3 细胞系进行了研究。细胞毒性是细胞选择性的，对 HT-29 的活性高于对其他细胞的活性。此外，疏水性在细胞毒性中的作用被解释为最佳疏水性对于高细胞毒性至关重要。此外，伤口愈合试验的结果表明 HT-29 细胞具有抗迁移作用。值得注意的是，与顺铂相比，IC 50值为 5.42 ± 0.15 μM 的1对 HT-29 细胞系表现出更大的活性。
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