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(ɳ- 柠檬烯)双氯芬酸钌配合物作为抗癌化疗药物的评价:与生物分子的相互作用,细胞毒性测定。

Evaluation of (ɳ-cymene) ruthenium diclofenac complex as anticancer chemotherapeutic agent: interaction with biomolecules, cytotoxicity assays.

机构信息

a Department of Chemistry, College of Sciences, King Saud University , Riyadh , KSA.

b Surfactant Research Chair , King Saud University , Riyadh , KSA.

出版信息

J Biomol Struct Dyn. 2019 Sep;37(15):3905-3913. doi: 10.1080/07391102.2018.1528180. Epub 2018 Dec 24.

DOI:10.1080/07391102.2018.1528180
PMID:30257617
Abstract

The designing of metal-based anticancer therapeutic agents can be optimized in a better and rapid way if the ligands utilized have standalone properties. Therefore, even when the organometallic/coordination complex (i.e., metallodrug) gets dissociated in extreme conditions, the ligand can endorse its biological properties. Herein, we have synthesized and characterized ɳ--cymene ruthenium diclofenac complex. Furthermore, the ruthenium complex interactions with human serum albumin (HSA) and ct-DNA have been studied using various spectroscopic studies viz., UV, fluorescence, and circular dichroism and exhibited a significant binding propensity. Furthermore, cytotoxicity assays were carried out against human breast cancer "MCF-7" cell line. The ɳ--cymene ruthenium diclofenac complex registered significant cytotoxicity with an IC value of ∼25.0 µM which is comparable to the standard drugs. The ɳ--cymene ruthenium diclofenac complex was able to decrease the MCF-7 cell proliferation and induced significant levels of apoptosis with relatively low toxicity.

摘要

如果所利用的配体具有独立的性质,那么金属基抗癌治疗剂的设计可以以更好和更快的方式得到优化。因此,即使在极端条件下,有机金属/配位化合物(即金属药物)发生解离,配体也可以维持其生物学性质。在此,我们合成并表征了ɳ--柠檬烯二氯芬酸钌配合物。此外,还使用各种光谱研究(如紫外、荧光和圆二色性)研究了钌配合物与人血清白蛋白(HSA)和 ct-DNA 的相互作用,显示出显著的结合倾向。此外,还对人乳腺癌“MCF-7”细胞系进行了细胞毒性测定。ɳ--柠檬烯二氯芬酸钌配合物具有显著的细胞毒性,IC 值约为 25.0 μM,与标准药物相当。ɳ--柠檬烯二氯芬酸钌配合物能够降低 MCF-7 细胞的增殖,并诱导显著水平的细胞凋亡,同时具有相对较低的毒性。

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