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基于 4,5-二氢-1H-吡唑-1-基部分的 Os(IV) 配合物的荧光、DNA 相互作用和细胞毒性研究:合成、表征和生物学评价。

Fluorescence, DNA Interaction and Cytotoxicity Studies of 4,5-Dihydro-1H-Pyrazol-1-Yl Moiety Based Os(IV) Compounds: Synthesis, Characterization and Biological Evaluation.

机构信息

Department of Chemistry, Sardar Patel University, Vallabh Vidyanagar, Gujarat, 388 120, India.

Cell Biology Laboratory, Indian Institute of Advanced Research, Koba, Gandhinagar, Gujarat, 382421, India.

出版信息

J Fluoresc. 2021 Mar;31(2):349-362. doi: 10.1007/s10895-020-02657-1. Epub 2021 Jan 3.

Abstract

Osmium(IV) pyrazole compounds and ligands were synthesized and well characterised. Ligands were characterized by heteronuclear NMR spectroscopy (H & C), elemental analysis, IR spectroscopy and liquid crystal mass spectroscopy. Os(IV) complexes were characterized by ESI-MS, ICP-OES, IR spectroscopy, conductance measurements, magnetic measurements and electronic spectroscopy. Binding of compounds with HS-DNA were evaluated using viscosity measurements, absorption titration, fluorescence quenching, and molecular docking, which show effective intercalation mode exhibited by compounds. Binding constant of Os(IV) complexes are found to be 8.1 to 9.2 × 10 M. Bacteriostatic and cytotoxic activities were carried out to evaluate MIC, LC, and IC. The compounds have been undergone bacteriostatic screening using three sets of Gram and two sets of Gram bacteria. MIC of complexes are found to be 72.5-100 μM, whereas that of ligands fall at about 122.5-150 μM.. LC count of ligands fall in the range of 16.22-17.28 μg/mL whereas that of complexes of Os(IV) fall in the range of 4.87-5.87 μg/mL. IC of osmium compounds were evaluated using HCT-116 cell line. All the Os(IV) compounds show moderate IC.

摘要

合成并充分表征了锇(IV)吡唑配合物和配体。通过异核 NMR 光谱 (H 和 C)、元素分析、IR 光谱和液晶质谱对配体进行了表征。通过 ESI-MS、ICP-OES、IR 光谱、电导率测量、磁性测量和电子光谱对 Os(IV)配合物进行了表征。使用粘度测量、吸收滴定、荧光猝灭和分子对接评估了化合物与 HS-DNA 的结合,结果表明化合物表现出有效的嵌入模式。Os(IV)配合物的结合常数发现为 8.1 至 9.2×10 M。进行了抑菌和细胞毒性活性评估以确定 MIC、LC 和 IC。使用三组革兰氏阳性菌和两组革兰氏阴性菌对化合物进行了抑菌筛选。复合物的 MIC 发现为 72.5-100 μM,而配体的 MIC 约为 122.5-150 μM。配体的 LC 计数范围为 16.22-17.28 μg/mL,而 Os(IV)配合物的 LC 计数范围为 4.87-5.87 μg/mL。使用 HCT-116 细胞系评估了锇化合物的 IC。所有 Os(IV)化合物均表现出中等的 IC。

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