首页> 外文期刊>Journal of biological inorganic chemistry: JBIC: a publication of the Society of Biological Inorganic Chemistry >Organometallic rhenium tricarbonyl-enrofloxacin and -levofloxacin complexes: synthesis, albumin-binding, DNA-interaction and cell viability studies
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Organometallic rhenium tricarbonyl-enrofloxacin and -levofloxacin complexes: synthesis, albumin-binding, DNA-interaction and cell viability studies

机译:有机金属铼三羰基苯甲酸盐和-levofloxacin复合物:合成,白蛋白结合,DNA相互作用和细胞活力研究

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摘要

Organometallic rhenium complexes have recently been considered in the development of novel antitumor agents due to their suitable properties. A series of rhenium(I) tricarbonyl complexes was synthesized with the quinolone antimicrobial agents enrofloxacin (Herx) and levofloxacin (Hlfx) and solvent (e.g., methanol), imidazole (im) or pyridine (py) as co-ligands. The complexes were characterized by spectroscopic methods. The interaction of the rhenium complexes with bovine serum albumin was investigated by fluorescence emission spectroscopy and the corresponding binding constants were determined. The binding of the rhenium complexes to calf-thymus DNA was monitored by UV-Vis spectroscopy, viscosity measurements and competitive studies with ethidium bromide. These studies indicated that intercalation is the most possible mode of action and the corresponding DNA-binding constants of the complexes were calculated. The cytotoxicity of the Re-complexes against human K-562 erythroleukemia cells was found to be moderate to high. These preliminary results are promising and warrant the design of new Re-complexes with improved properties in future studies.
机译:由于其合适的性质,最近在新型抗肿瘤剂的发育中被考虑了有机金属金属铼络合物。用喹诺酮抗微生物剂富含氧氟沙星(Herx)和左氧氟沙星(HLFX),溶剂(例如,甲醇),咪唑(IM)或吡啶(Py)用溶剂(例如,甲醇),吡啶(Py)作为共配体,合成一系列铼(I)三羰基络合物。通过光谱方法表征复合物。通过荧光发射光谱研究与牛血清白蛋白的铼络合物的相互作用,并测定相应的结合常数。通过UV-Vis光谱,粘度测量和溴化乙锭的竞争性研究监测铼络合物对小牛胸腺DNA的结合。这些研究表明,嵌入是最可能的作用方式,并计算复合物的相应DNA结合常数。发现对人K-562赤粒血症细胞的重复合物的细胞毒性是中等的。这些初步结果是有前途的,并提供新的重组设计,以改善未来的研究。

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