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Fluorescence, DNA Interaction and Cytotoxicity Studies of 4,5-Dihydro-1H-Pyrazol-1-Yl Moiety Based Os(IV) Compounds: Synthesis, Characterization and Biological Evaluation
Journal of Fluorescence ( IF 2.7 ) Pub Date : 2021-01-03 , DOI: 10.1007/s10895-020-02657-1
Bharat H Pursuwani 1 , Bhupesh S Bhatt 1 , Foram U Vaidya 2 , Chandramani Pathak 2 , Mohan N Patel 1
Affiliation  

Osmium(IV) pyrazole compounds and ligands were synthesized and well characterised. Ligands were characterized by heteronuclear NMR spectroscopy (1H & 13C), 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 × 104 M−1. Bacteriostatic and cytotoxic activities were carried out to evaluate MIC, LC50, and IC50. The compounds have been undergone bacteriostatic screening using three sets of Gram+ve and two sets of Gram-ve bacteria. MIC of complexes are found to be 72.5–100 μM, whereas that of ligands fall at about 122.5–150 μM.. LC50 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. IC50 of osmium compounds were evaluated using HCT-116 cell line. All the Os(IV) compounds show moderate IC50.



中文翻译:

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

合成并充分表征了锇 (IV) 吡唑化合物和配体。通过异核NMR光谱( 1 H & 13 C)、元素分析、IR光谱和液晶质谱表征配体。Os(IV) 配合物通过 ESI-MS、ICP-OES、红外光谱、电导测量、磁性测量和电子光谱进行表征。使用粘度测量、吸收滴定、荧光猝灭和分子对接来评估化合物与 HS-DNA 的结合,这表明化合物表现出有效的嵌入模式。发现Os(IV) 复合物的结合常数为8.1 至9.2 × 10 4  M -1。进行抑菌和细胞毒活性以评估 MIC、LC50,和IC 50。这些化合物均经过使用三套革兰氏菌的筛选+已经和两套革兰氏-ve细菌。发现复合物的 MIC 为 72.5-100 μM,而配体的 MIC 约为 122.5-150 μM。LC 50配体的计数范围为 16.22-17.28 μg/mL,而 Os(IV) 的复合物的 MIC落在 4.87–5.87 μg/mL 的范围内。使用HCT-116细胞系评估锇化合物的IC 50。所有的Os(IV)化合物都显示出中等的IC 50

更新日期:2021-01-04
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