Kojic acid-amino acid conjugates as tyrosinase inhibitors
Kojic acid-amino acid conjugates as tyrosinase inhibitors
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DOI：
10.1016/j.bmcl.2009.08.041
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发表时间：
2009-10-01
影响因子：
2.7
通讯作者：
Lee, Yoon-Sik
中科院分区：
文献类型：
--
作者：
Noh, Jin-Mi;Kwak, Seon-Yeong;Lee, Yoon-Sik
曲酸（KA）是一种已知的酪氨酸酶抑制剂，但其抑制活性和稳定性不足。我们用氨基酸修饰KA并筛选其酪氨酸酶抑制活性。其中，曲酸-苯丙氨酸酰胺（KA-F-NH 2）表现出最强的抑制活性，在50 ℃下可保持3个月以上，并通过动力学分析确定为非竞争性抑制剂。它还表现出多巴色素还原活性。我们还提出了一个新的酪氨酸酶抑制机制的基础上的对接模拟数据。(C)2009爱思唯尔有限公司保留所有权利。
Kojic acid (KA), a well known tyrosinase inhibitor, has insufficient inhibitory activity and stability. We modified KA with amino acids and screened their tyrosinase inhibitory activity. Among them, kojic acid-phenylalanine amide (KA-F-NH2) showed the strongest inhibitory activity, which was maintained for over 3 months at 50 degrees C, and acted as a noncompetitive inhibitor as determined by kinetic analysis. It also exhibited dopachrome reducing activity. We also propose a new tyrosinase inhibition mechanism based on the docking simulation data. (C) 2009 Elsevier Ltd. All rights reserved.