期刊
FOOD CHEMISTRY
卷 362, 期 -, 页码 -出版社
ELSEVIER SCI LTD
DOI: 10.1016/j.foodchem.2021.130241
关键词
Kojic acid; Heterocycle; Tyrosinase inhibitors; Antibrowning agents
资金
- One Thousand Talents Program of Guizhou Province [[2019]4]
- Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Guizhou University [KY[2019]037]
The study identified 4d as a potent tyrosinase inhibitor with copper-chelating ability, low cytotoxicity, and significant antibrowning effects. These compounds may serve as lead molecules for developing novel tyrosinase inhibitors and antibrowning agents.
Tyrosinase plays an important role in melanin biosynthesis and enzymatic browning of fresh-cut fruit and vegetables. To discover potent tyrosinase inhibitors and antibrowning agents, a series of novel kojic acid derivatives containing bioactive heterocycle moiety (4a-4l) were designed and synthesized. Thereinto, 4d displayed the most potent tyrosinase inhibitory activity with IC50 of 3.23 +/- 0.26 mu M and behaved as a competitive inhibitor with a Ki of 1.96 mu M, compared to kojic acid (IC50 = 32.23 +/- 2.01 mu M). Besides, copper-chelating assay, fluorescence spectrum quenching experiment, ANS-binding fluorescence quenching analysis, and molecular modeling studies indicated that 4d may inhibit tyrosinase activity by chelating with copper ions in the active site of tyrosinase. Furthermore, 4d exhibited low cytotoxic activity and significant antibrowning effects. This study suggests that these compounds may serve as lead molecules for developing novel tyrosinase inhibitors and antibrowning agents.
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