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Bipyrazole Based Novel Bimetallic µ-oxo Bridged Au(III) Complexes as Potent DNA Interacalative, Genotoxic, Anticancer, Antibacterial and Cytotoxic Agents
Journal of Inorganic and Organometallic Polymers and Materials ( IF 4 ) Pub Date : 2020-06-06 , DOI: 10.1007/s10904-020-01618-2
Darshana N. Kanthecha , Bhupesh S. Bhatt , Mohan N. Patel , Dilip B. Raval , Vasudev R. Thakkar , Foram U. Vaidya , Chandramani Pathak

Six bipyrazole based Au(III) complexes were synthesized and characterized by 1H-NMR, 13C (APT) NMR, FT-IR, Mass spectrometry, elemental analysis and conductance measurement. The analysis show that complexes are ionic in nature and bimetallic with oxygen atom as bridging ligand. The DNA binding ability of compounds were checked as change in absorption band in UV-Vis spectra of HS-DNA and change in relative viscosity of DNA in presence of compounds. The results support intercalation mode of binding with good affinity of compounds toward DNA as evaluated by estimation of binding constant values. The molecular docking study also supports the experimental data. The anticancer activity of complexes were evaluated against A549 (Lung adenocarcinoma) cell line by MTT assay in terms of IC50 value. The cell viability assay showed significant potency of complexes as staining of death cells with trypan blue dye. The genotoxicity of compounds were checked by smearing observed in DNA of S. pombe cell under the influence of complexes. The compounds showed significant cytotoxicity against brine shrimp.



中文翻译:

基于联吡唑的新型双金属µ-氧代桥联Au(III)络合物作为有效的DNA相互作用剂,遗传毒性,抗癌剂,抗菌剂和细胞毒剂

合成了六种基于联吡唑的Au(III)配合物,并通过1 H-NMR,13 C(APT)NMR,FT-IR,质谱,元素分析和电导率测量进行了表征。分析表明,该络合物本质上是离子性的,并且以氧原子作为桥联配体是双金属的。检查化合物的DNA结合能力,作为HS-DNA的UV-Vis光谱中吸收带的变化和存在化合物时DNA的相对粘度的变化。结果支持了结合的插入模式,通过对结合常数值的评估可以评估化合物对DNA的亲和力。分子对接研究也支持实验数据。通过ICT的MTT分析评估了复合物对A549(肺腺癌)细胞系的抗癌活性。50值。细胞存活力测定显示,用锥虫蓝染料对死亡细胞染色后,复合物具有显着的效力。通过在复合物的作用下在粟酒裂殖酵母细胞的DNA中观察到的涂片检查来检查化合物的遗传毒性。这些化合物对盐水虾显示出明显的细胞毒性。

更新日期:2020-06-06
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