Farmacognosia, Facultad de Ciencias Bioquímicas y Farmacéuticas, Universidad Nacional de Rosario and Consejo Nacional de Investigaciones Científicas y Técnicas (CONICET), Suipacha 531, 2000 Rosario, Argentina.
Instituto de Biología Molecular y Celular de Rosario (IBR-CONICET), Facultad de Ciencias Bioquímicas y Farmacéuticas, Universidad Nacional de Rosario, Argentina.
Food Chem. 2021 Mar 30;341(Pt 1):128232. doi: 10.1016/j.foodchem.2020.128232. Epub 2020 Sep 28.
The inhibition of enzymatic browning is an attractive target to elevate the quality of foods. The objective of this work is to describe a novel platform for the discovery of tyrosinase inhibitors, based on (a) one-pot preparation of a library of thiosemicarbazide compounds, (b) biological evaluation using tyrosinase TLC bioautography, (c) inhibitor identification via mass spectrometry coupled to bioautography. During these proof-of-concept experiments, the approach led to the straightforward identification of a new thiosemicarbazone with improved tyrosinase inhibition properties and fresh-cut apple slices antibrowning effect when compared to kojic acid. In conclusion, the platform represents an interesting strategy for the discovery of this type of inhibitors.
抑制酶促褐变是提高食品质量的一个有吸引力的目标。本工作的目的是描述一种基于（a）一锅法制备硫代卡巴肼化合物文库，（b）使用酪氨酸酶 TLC 生物自显影进行生物评价，（c）通过与生物自显影相结合的质谱法鉴定抑制剂的新型酪氨酸酶抑制剂发现平台。在这些概念验证实验中，该方法直接鉴定出一种新型的硫代卡巴腙，与曲酸相比，它具有更好的酪氨酸酶抑制性能和鲜切苹果片的防褐变效果。总之，该平台代表了发现此类抑制剂的一种有趣策略。
