Tang Lilin, Zhang Wenpeng, Zhao Haiyan, Chen Zilin
Key Laboratory of Combinatorial Biosynthesis and Drug Discovery, Ministry of Education, and School of Pharmaceutical Sciences, Wuhan University, Wuhan, China.
State Key Laboratory of Transducer Technology, Chinese Academy of Sciences, Beijing, China.
J Sep Sci. 2015 Aug;38(16):2887-92. doi: 10.1002/jssc.201500371. Epub 2015 Jul 14.
A capillary-electrophoresis-based method for the screening of tyrosinase inhibitors in traditional Chinese medicines was developed. The method integrated electrophoretically mediated microanalysis with sandwich mode injection, partial filling, and rapid polarity switching techniques, and carried out on-column enzyme reaction and the separation of substrate and product. The conditions were optimized including the background electrolyte, mixing voltage, and the incubation time. Finally, the screening of nine standard natural compounds of traditional Chinese medicines was carried out. The inhibitors can be directly identified from the reduced peak area of the product compared to that obtained without any inhibitor. Chlorogenic acid (100 μM) showed inhibitory activity with the inhibitory percentage of 19.8%, while the other compounds showed no inhibitory activity. This method has great application potential in drug discovery from traditional Chinese medicines.
建立了一种基于毛细管电泳的中药酪氨酸酶抑制剂筛选方法。该方法将电泳介导的微分析与夹心模式进样、部分填充和快速极性切换技术相结合，进行柱上酶反应以及底物和产物的分离。对背景电解质、混合电压和孵育时间等条件进行了优化。最后，对9种中药标准天然化合物进行了筛选。与未添加任何抑制剂时相比，可通过产物峰面积的减小直接鉴定出抑制剂。绿原酸（100 μM）表现出抑制活性，抑制率为19.8%，而其他化合物未表现出抑制活性。该方法在中药药物发现方面具有巨大的应用潜力。
