This investigation focuses on the synthesis and characterization of three new, water‐soluble palladium complexes, with potential to overcome the drawbacks of platinum‐based anti‐cancer drugs. The complexes contain small N‐heterocyclic carbene (NHC) ligands, having groups that impart water solubility. The anti‐cancer effects of these complexes were evaluated in two different cancer cell lines, namely,HeLa, a cervical cancer cell line and A549,adenocarcinoma human alveolar basal epithelial cell line. Cytotoxicity of the complexes was compared with cisplatin, an established platinum‐based anti‐cancer moiety, using the MTT assay (MTT is 3‐(4,5‐dimethylthiazol‐2‐yl)‐2,5‐diphenyltetrazolium bromide). Aqueous solutions of the synthesized complexes demonstrated significant cytotoxicity in both the cell lines. The synthesized metal complexes resulted in a stronger, cytotoxic effect in A549 cells (lung cancer cells), as compared to cisplatin. Furthermore, interaction of these palladium compounds with DNA was studied using gel electrophoresis and spectrometry methods. The result suggested that the complexes interacted with DNA via intercalation. Interaction with BSA (Bovine Serum Albumin) was investigated using UV–Vis spectroscopy suggesting positive interaction of palladium complex with BSA proteins. Furthermore, fluorescence studies revealed quenching of protein fluorescence thus, indicating dynamic quenching mechanism with the number of association sites being calculated as ∼1.

中文翻译：

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新型水溶性N-杂环碳-钯配合物有望成为抗肿瘤药物：研究DNA和蛋白质的相互作用

这项研究的重点是三种新型水溶性钯配合物的合成和表征，有可能克服基于铂的抗癌药物的缺点。配合物包含小的N杂环卡宾（NHC）配体，具有赋予水溶性的基团。在两种不同的癌细胞系HeLa（子宫颈癌细胞系）和A549（腺癌人肺泡基底膜上皮细胞系）中评估了这些复合物的抗癌作用。使用MTT分析法（MTT为3-（4,5-二甲基噻唑-2-基）-2-溴5-二苯基四唑鎓），将复合物的细胞毒性与已建立的铂基抗癌部分顺铂进行了比较。合成复合物的水溶液在两种细胞系中均显示出明显的细胞毒性。与顺铂相比，合成的金属配合物在A549细胞（肺癌细胞）中产生了更强的细胞毒性作用。此外，使用凝胶电泳和光谱法研究了这些钯化合物与DNA的相互作用。结果表明复合物通过嵌入与DNA相互作用。与牛血清白蛋白（牛血清白蛋白）的相互作用已通过紫外-可见光谱研究，表明钯复合物与牛血清白蛋白之间存在正相互作用。此外，荧光研究揭示了蛋白质荧光的淬灭，因此表明了动态淬灭机理，缔合位点的数量被计算为〜1。使用凝胶电泳和光谱法研究了这些钯化合物与DNA的相互作用。结果表明，复合物通过嵌入与DNA相互作用。与牛血清白蛋白（BSA）的相互作用已通过UV-Vis光谱进行了研究，表明钯复合物与牛血清白蛋白（BSA）具有正相互作用。此外，荧光研究揭示了蛋白质荧光的淬灭，因此表明了动态淬灭机理，缔合位点的数量被计算为〜1。使用凝胶电泳和光谱法研究了这些钯化合物与DNA的相互作用。结果表明复合物通过嵌入与DNA相互作用。与牛血清白蛋白（牛血清白蛋白）的相互作用已通过紫外-可见光谱研究，表明钯复合物与牛血清白蛋白之间存在正相互作用。此外，荧光研究揭示了蛋白质荧光的淬灭，因此表明了动态淬灭机理，缔合位点的数量被计算为〜1。