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Efficient interrupting skills of amino acid metallointercalators with DNA at physiological pH: Evaluation of biological assays

机译:生理pH下DNA的氨基酸金属脉络器的高效中断技巧:生物学测定评价

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摘要

The 4-aminoantipyrine derivatives (-NO_2, -OCH_3) and their mixed-ligand complexes with amino acids have been synthesized and investigated for their binding with CT DNA using UV-visible spectroscopy, cyclic voltammetry, and viscosity measurements under physiological conditions of pH (stomach 4.7; blood 7.4). The results from all techniques i.e. binding constant (K_b), and free energy change (?G) were in good agreement and inferred spontaneous compound-DNA complexes formation via intercalation. Among all the compounds 1 and 4 showed comparatively greater binding at pH 7.4 as evident from its greater K_b values. All the complexes exhibit oxidative cleavage of supercoiled (SC) pBR322 plasmid DNA in the presence of H_2O_2 as an activator. It is remarkable that at 25 μM concentration 1 and 4 completely degrade SC DNA into undetectable minor fragments and thus they act as efficient chemical nucleases. Among the new complexes, complexes 1 and 4 have highest potential against all the microorganisms tested. The results of the above biological experiments also reveal that the choice of different metal ions has little influence on the DNA binding, DNA cleavage and antimicrobial assay.
机译:已经合成了4-氨基丙氨酸衍生物(-NO_2,-OCH_3)和它们的混合配体配合物,并研究了使用UV可见光谱,循环伏安法和pH的生理条件下与CT DNA的结合与CT DNA的结合(胃4.7;血7.4)。来自所有技术的结果,即结合常数(K_B)和自由能变化(Δg)是良好的一致性,并通过插层推断出自发化合物-DNA复合物形成。在所有化合物1和4中,在pH7.4中显示比其更大的K_B值的明显更大。所有复合物在H_2O_2作为活化剂的情况下表现出超硅酸锆(SC)PBR322质粒DNA的氧化切割。值得注意的是,在25μm浓度的1和4中完全降解了Sc DNA到未定例的轻微碎片,因此它们充当高效的化学核酸酶。在新的复合物中,复合物1和4对测试所有微生物的潜力最高。上述生物实验的结果还揭示了不同金属离子的选择对DNA结合,DNA裂解和抗微生物测定几乎没有影响。

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