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含异烟肼衍生希夫碱的双核铋(III)配合物的设计、合成与生物评价。

Design, synthesis, and biological evaluation of dinuclear bismuth(III) complexes with Isoniazid-derived Schiff bases.

机构信息

Hunan Provincial Key Laboratory of Xiangnan Rare-Precious Metals Compounds and Applications, School of Chemistry and Environmental Science, Xiangnan University, Chenzhou 423000, Hunan Province, China.

Hunan Provincial Key Laboratory of Xiangnan Rare-Precious Metals Compounds and Applications, School of Chemistry and Environmental Science, Xiangnan University, Chenzhou 423000, Hunan Province, China.

出版信息

J Inorg Biochem. 2022 Oct;235:111931. doi: 10.1016/j.jinorgbio.2022.111931. Epub 2022 Jul 16.

DOI:10.1016/j.jinorgbio.2022.111931
PMID:35868066
Abstract

Four dinuclear bismuth(III) Schiff-base complexes bearing Schiff-base ligands have been synthesized and structurally characterized by single-crystal X-ray diffraction, elemental analysis, and spectral techniques (FT-IR, NMR and MS). The analytical data reveal the bismuth(III) complexes possess 1:1 metal-ligand ratios. In vitro biological studies have revealed that bismuth(III) complexes displayed much higher antibacterial and antitumor activities than their parent ligands, which involves two gram-negative (S. aureus, B. subtili) and two gram-positive (E. coli, P. aeruginosa) bacteria, and human gastric cancer SNU-16 cells. The power-time curves of S. pombe exposed to tested compounds were detected by bio-microcalorimetry. Some thermokinetic parameters (k, Pt and Q) were derived based on the metabolic power-time curves, and their quantitative relationships with the concentrations (c) were further discussed.

摘要

已经合成了四个双核铋(III)席夫碱配合物,这些配合物带有席夫碱配体,并通过单晶 X 射线衍射、元素分析和光谱技术(FT-IR、NMR 和 MS)进行了结构表征。分析数据表明,铋(III)配合物具有 1:1 的金属-配体比例。体外生物研究表明,铋(III)配合物的抗菌和抗肿瘤活性明显高于其母体配体,涉及两种革兰氏阴性(金黄色葡萄球菌、枯草芽孢杆菌)和两种革兰氏阳性(大肠杆菌、铜绿假单胞菌)细菌以及人胃癌 SNU-16 细胞。通过生物微量热法检测了暴露于测试化合物的 S. pombe 的功率-时间曲线。根据代谢功率-时间曲线得出了一些热动力学参数(k、Pt 和 Q),并进一步讨论了它们与浓度(c)的定量关系。

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