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首页> 外文期刊>Journal of enzyme inhibition and medicinal chemistry. >The biological effects of vanadyl curcumin and vanadyl diacetylcurcumin complexes: the effect on structure, function and oxidative stability of the peroxidase enzyme, antibacterial activity and cytotoxic effect
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The biological effects of vanadyl curcumin and vanadyl diacetylcurcumin complexes: the effect on structure, function and oxidative stability of the peroxidase enzyme, antibacterial activity and cytotoxic effect

机译:钒基姜黄素和钒酰二乙酰尿蛋白复合物的生物学作用:过氧化物酶的结构,功能和氧化稳定性,抗菌活性和细胞毒性作用

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摘要

Curcumin has multiple pharmacological effects, but it has poor stability. Complexation of curcumin with metals improves its stability. Here, the effects of vanadyl curcumin and vanadyl diacetylcurcumin on the function and structure of horseradish peroxidase enzyme were evaluated by spectroscopic techniques. Cytotoxic effect of the complexes was also assessed on MCF-7 breast cancer, bladder and LNCaP prostate carcinoma cell line. The results showed that the complexes improve catalytic activity of HRP, and also increase its tolerance against the oxidative condition. The result also indicated that the affinity of HRP for hydrogen peroxide substrate decreases, while the affinity increases for phenol substrate. Circular dichroism and fluorescence spectroscopies showed that compactness of the enzyme structure around the catalytic heme group and the distance between the heme group and tryptophan residue decreases after the binding. The antibacterial and cytotoxic results indicated that the complexes have anticancer potential, but they have no considerable antibacterial activity.
机译:姜黄素具有多种药理作用,但稳定性较差。姜黄素与金属络合可提高其稳定性。在这里,通过光谱技术评估了钒基姜黄素和钒基二乙酰胆红素对辣根过氧化物酶功能和结构的影响。对MCF-7乳腺癌、膀胱癌和LNCaP前列腺癌细胞系也评估了复合物的细胞毒性作用。结果表明,配合物提高了HRP的催化活性,并增强了其对氧化条件的耐受性。结果还表明,HRP对过氧化氢底物的亲和力降低,而对苯酚底物的亲和力增加。圆二色谱和荧光光谱表明,结合后,催化血红素基团周围的酶结构紧凑,血红素基团与色氨酸残基之间的距离减小。抗菌和细胞毒性实验结果表明,该复合物具有抗癌潜力,但没有明显的抗菌活性。

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