含苯并噻唑O,N,S供体螯配体钯配合物:体外细胞毒性、与CT-DNA和BSA蛋白相互作用的研究

IF 1.7 4区 化学 Q3 Chemistry
RAHUL NASKAR, PARAMITA GHOSH, SUBRATA MANDAL, SUBRATA JANA, NABENDU MURMU, TAPAN KUMAR MONDAL
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引用次数: 0

摘要

合成了一种新的钯(II)配合物[Pd(LSEt)Cl] (C1)与基于苯并噻唑的ONS供体钳形配体(HLSEt) (HLSEt = 2-(苯并噻唑-2-基)-6-((2-(乙基噻唑)苯基)亚氨基)甲基)苯酚)。研究了C1与CT DNA的相互作用,发现其结合常数为4.0×105 M−1。用荧光猝灭法测定了溴化乙啶(EB)从EB- ctdna络合物中被C1取代的能力,得到了Stern-Volmer猝灭常数(Ksv)为4.3×105 M−1。同样,用紫外可见和荧光方法研究了C1与BSA蛋白的相互作用。测定表观关联常数(Ka)和Ksv (Ka = 2.8×104 M−1,Ksv = 5.5×104 M−1)。采用MTT法测定复合物[Pd(LSEt)Cl] (C1)对人胃癌细胞株(AGS)的体外细胞毒性。C1对AGS的半数最大抑制浓度(IC50)(9.55±1.23µM)低于顺铂(23.13±1.03µM)。在此基础上,合成了新的钯(II)配合物[Pd(LSEt)Cl] (C1)与苯并噻唑基ONS供体钳形配体(HLSEt)配合物,并用多种光谱技术对其进行了表征。用紫外可见和荧光法研究了C1与CT DNA和BSA蛋白的相互作用。采用MTT法评价该复合物对人胃癌细胞株的体外细胞毒性。钯(II)配合物对AGS癌细胞的半最大抑制浓度(IC50)为9.55±1.23µM,低于顺铂(23.13±1.03µM)。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

Palladium(II) complex bearing benzothiazole based O,N,S donor pincer ligand: Study of in-vitro cytotoxicity, interaction with CT-DNA and BSA protein

Palladium(II) complex bearing benzothiazole based O,N,S donor pincer ligand: Study of in-vitro cytotoxicity, interaction with CT-DNA and BSA protein

A new palladium(II) complex, [Pd(LSEt)Cl] (C1) with benzothiazole based ONS donor pincer ligand (HLSEt) was synthesized (where, HLSEt = 2-(benzothiazol-2-yl)-6-(((2-(ethylthio)phenyl)imino)methyl)phenol). Interaction of C1 with CT DNA was investigated, and its binding constant was found to be 4.0×105 M−1. The proficiency of ethidium bromide (EB) displacement from its EB-CTDNA complex by C1 was performed by the fluorescence quenching method, and Stern-Volmer quenching constant (Ksv) was found to be 4.3×105 M−1. Similarly, the interaction of C1 with BSA protein was investigated by UV-Vis and fluorescence methods. The apparent association constant (Ka) and Ksv were determined (Ka = 2.8×104 M−1 and Ksv = 5.5×104 M−1). In vitro cytotoxicity of the complex, [Pd(LSEt)Cl] (C1), towards human gastric cancer cell lines (AGS) was assessed by the MTT assay method. The half maximal inhibitory concentration (IC50) of C1 (9.55 ± 1.23 µM) towards AGS cancer lines was found to be lower than cisplatin (23.13 ± 1.03 µM).

Graphical abstract

Herein, new palladium(II) complex, [Pd(LSEt)Cl] (C1) with benzothiazole-based ONS donor pincer ligand (HLSEt) was synthesized and characterized by several spectroscopic techniques. Interaction of C1 with CT DNA and BSA protein was investigated by UV-Vis and fluorescence methods. In vitro cytotoxicity of the complex toward human gastric cancer cell lines (AGS) was evaluated by the MTT assay method. The half maximal inhibitory concentration (IC50) of the palladium(II) complex (9.55±1.23 µM) was found to be less compared to cisplatin (23.13±1.03 µM) towards AGS cancer lines.

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来源期刊
Journal of Chemical Sciences
Journal of Chemical Sciences Chemistry-General Chemistry
CiteScore
2.90
自引率
5.90%
发文量
107
审稿时长
12 months
期刊介绍: Journal of Chemical Sciences is a monthly journal published by the Indian Academy of Sciences. It formed part of the original Proceedings of the Indian Academy of Sciences – Part A, started by the Nobel Laureate Prof C V Raman in 1934, that was split in 1978 into three separate journals. It was renamed as Journal of Chemical Sciences in 2004. The journal publishes original research articles and rapid communications, covering all areas of chemical sciences. A significant feature of the journal is its special issues, brought out from time to time, devoted to conference symposia/proceedings in frontier areas of the subject, held not only in India but also in other countries.
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