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Development of novel pyrazole-1,2,4-triazole derivatives as tyrosinase inhibitors: Design, preparation, mechanism of action and anti-browning application
Food Chemistry ( IF 8.5 ) Pub Date : 2024-08-02 , DOI: 10.1016/j.foodchem.2024.140722 Jinfeng Zhang , Wei Yang , Min He , Zhiyun Peng , Guangcheng Wang
Food Chemistry ( IF 8.5 ) Pub Date : 2024-08-02 , DOI: 10.1016/j.foodchem.2024.140722 Jinfeng Zhang , Wei Yang , Min He , Zhiyun Peng , Guangcheng Wang
Tyrosinase (Polyphenol oxidase), a key enzyme in enzymatic browning, is an attractive target for developing new anti-browning agents in the food industry. In this work, twenty pyrazole-1,2,4-triazole derivatives ( were synthesized and tested in vitro, most of compounds showed potent anti-tyrosinase activity. Of these, (IC = 1.02 ± 0.08 μM) was found to be 14 folds stronger than kojic acid (IC = 14.74 ± 1.23 μM) and behaved as a mixed type inhibitor. Besides, the disappeared peak of dopaquinone in the HPLC assay intuitively validated the inhibitory effect of . Copper ions chelating, fluorescence quenching and molecular docking assays showed that coordination with copper is the key to play a role. Furthermore, exhibited excellent anti-browning ability for the Tratt, the non-enzymatic browning experiment showed that could prevent browning in non-enzymatic ways. It is suggested that these derivatives could serve as the leading compounds to find more efficient anti-browning agents in the future.
中文翻译:
新型吡唑-1,2,4-三唑衍生物作为酪氨酸酶抑制剂的开发:设计、制备、作用机制和抗褐变应用
酪氨酸酶(多酚氧化酶)是酶促褐变的关键酶,是食品工业中开发新型抗褐变剂的一个有吸引力的目标。在这项工作中,合成了二十种吡唑-1,2,4-三唑衍生物(并进行了体外测试,大多数化合物表现出有效的抗酪氨酸酶活性。其中,(IC = 1.02 ± 0.08 μM)被发现是 14 倍比曲酸强(IC = 14.74 ± 1.23 μM),并且表现为混合型抑制剂。此外,HPLC 测定中多巴醌的消失峰直观地验证了铜离子螯合、荧光猝灭和分子对接测定的抑制效果。与铜的配位是发挥作用的关键,此外,Tratt表现出优异的抗褐变能力,非酶促褐变实验表明,这些衍生物可以作为非酶促褐变的抑制剂。领先化合物在未来寻找更有效的抗褐变剂。
更新日期:2024-08-02
中文翻译:
![](https://scdn.x-mol.com/jcss/images/paperTranslation.png)
新型吡唑-1,2,4-三唑衍生物作为酪氨酸酶抑制剂的开发:设计、制备、作用机制和抗褐变应用
酪氨酸酶(多酚氧化酶)是酶促褐变的关键酶,是食品工业中开发新型抗褐变剂的一个有吸引力的目标。在这项工作中,合成了二十种吡唑-1,2,4-三唑衍生物(并进行了体外测试,大多数化合物表现出有效的抗酪氨酸酶活性。其中,(IC = 1.02 ± 0.08 μM)被发现是 14 倍比曲酸强(IC = 14.74 ± 1.23 μM),并且表现为混合型抑制剂。此外,HPLC 测定中多巴醌的消失峰直观地验证了铜离子螯合、荧光猝灭和分子对接测定的抑制效果。与铜的配位是发挥作用的关键,此外,Tratt表现出优异的抗褐变能力,非酶促褐变实验表明,这些衍生物可以作为非酶促褐变的抑制剂。领先化合物在未来寻找更有效的抗褐变剂。