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<p>Tyrosinase is the key rate limiting enzyme that controls melanin production. A series of novel kojic acid-cinnamic acid hybrids (<b>JP1</b>~<b>26</b>) were synthesized as tyrosinase inhibitors. All compounds displayed potential anti-tyrosinase activity with IC<sub>50</sub> values of 0.51~1.53 µM, ~ 10–30 folds stronger than control kojic acid. Among them, the strongest inhibitor <b>JP5</b> inhibited tyrosinase in a mixed-type. Fluorescence quenching, 3D fluorescence, and CD spectra revealed the binding characteristic of <b>JP5</b> with tyrosinase. Molecular docking displayed their binding detail with catalytic site residues. In addition, <b>JP5</b> also could inhibit intracellular tyrosinase activity, thence, inhibiting melanin production in B16 cells. Therefore, kojic acid-cinnamic acid hybrids could service as potential tyrosinase inhibitors.</p>

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Synthesis and biological evaluation of novel Kojic acid-cinnamic acid hybrids as tyrosinase inhibitors

  • 期刊论文

  • 发表日期：

    2026年3月1日

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  • Yaxin Wen,
  • Qingqing Yu,
  • Fang Yang,
  • Jianping Li,
  • Ming Lang,
  • Jia-Lei Yan,
  • Xuetao Xu

摘要

Tyrosinase is the key rate limiting enzyme that controls melanin production. A series of novel kojic acid-cinnamic acid hybrids (JP1~26) were synthesized as tyrosinase inhibitors. All compounds displayed potential anti-tyrosinase activity with IC50 values of 0.51~1.53 µM, ~ 10–30 folds stronger than control kojic acid. Among them, the strongest inhibitor JP5 inhibited tyrosinase in a mixed-type. Fluorescence quenching, 3D fluorescence, and CD spectra revealed the binding characteristic of JP5 with tyrosinase. Molecular docking displayed their binding detail with catalytic site residues. In addition, JP5 also could inhibit intracellular tyrosinase activity, thence, inhibiting melanin production in B16 cells. Therefore, kojic acid-cinnamic acid hybrids could service as potential tyrosinase inhibitors.