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首页> 外文期刊>Physical chemistry chemical physics: PCCP >Bioactive supra decorated thiazolidine-4-carboxylic acid derivatives attenuate cellular oxidative stress by enhancing catalase activity
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Bioactive supra decorated thiazolidine-4-carboxylic acid derivatives attenuate cellular oxidative stress by enhancing catalase activity

机译：生物活性超装饰噻唑烷-4-羧酸衍生物通过增强过氧化氢酶活性来衰减细胞氧化应激

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摘要

A pharmacophoric motif decorated with supramolecular functionalities (TZT) was designed for potential interaction with biological targets. Main insights of this work include the correlation of supra functionalities of TZT with its binding ability to proteins leading to the modulation of their structure and bioactivity as a promising perspective in the field of cellular protection from oxidative stress. To investigate the role of TZT in obliterating oxidative stress at a molecular level, its binding propensity with bovine serum albumin (BSA) and bovine liver catalase (BLC) was characterized using various biophysical methods. The binding constants of TZT with BSA (K-b = 2.09 x 10(5) M-1) and BLC (K-b = 2.349 x 10(5) M-1) indicate its considerable interaction with these proteins. TZT efficiently triggers favourable structural changes in BLC, thereby enhancing its enzyme activity in a dose dependent manner. The enzyme kinetics parameters of TZT binding to BLC were quantified using the Michaelis-Menten model. Both in silico and experimental results suggest that an increased substrate availability could be the reason for enhanced BLC activity. Furthermore, physiological relevance of this interaction was demonstrated by investigating the ability of TZT to attenuate oxidative stress. Treatment with TZT was found to mitigate the inhibition of A549 cell proliferation in the presence of high concentrations of vitamin C. This finding was confirmed at a molecular level by PARP cleavage status, demonstrating that TZT inhibits apoptotic cell death induced by oxidative stress.
机译：设计了一种用超分子官能团（TZT）装饰的药物术基术，专为与生物靶标而互动。本作作品的主要见解包括TZT的同上函数与其结合蛋白质的结合能力，导致其结构和生物活性的调节，作为氧化应激的细胞保护领域的有希望的视角。为了研究TZT在分子水平抑制氧化应激的作用，其用各种生物物理方法表征其与牛血清白蛋白（BSA）和牛肝脏过氧化氢酶（BLC）的结合倾向。具有BSA的TZT的结合常数（K-B = 2.09×10（5）m-1）和BLC（K-B = 2.349×10（5）M-1）表示其与这些蛋白质相当大的相互作用。 TZT有效地触发了BLC中有利的结构变化，从而以剂量依赖性方式提高其酶活性。使用Michaelis-Menten模型量化TZT与BLC结合的酶动力学参数。在硅和实验结果中既表明，增加的基材可用性可能是增强BLC活性的原因。此外，通过研究TZT衰减氧化应激的能力，证明了这种相互作用的生理相关性。发现用TZT治疗减轻A549细胞增殖在高浓度的维生素C中的抑制。该发现在PARP切割状态下在分子水平确认，证明TZT抑制氧化应激诱导的凋亡细胞死亡。

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