Academic Journal

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

Λεπτομέρειες βιβλιογραφικής εγγραφής
Τίτλος: Synthesis and biological evaluation of novel Kojic acid-cinnamic acid hybrids as tyrosinase inhibitors.
Συγγραφείς: Wen Y; School of Pharmacy and Food Engineering & Guangdong Provincial Key Laboratory of Large Animal Models for Biomedicine & International Healthcare Innovation Institute (Jiangmen), Wuyi University, Jiangmen, 529020, China., Yu Q; School of Pharmacy and Food Engineering & Guangdong Provincial Key Laboratory of Large Animal Models for Biomedicine & International Healthcare Innovation Institute (Jiangmen), Wuyi University, Jiangmen, 529020, China., Yang F; Jiangmen Customs Technology Center, Jiangmen, 529020, China., Li J; School of Pharmacy and Food Engineering & Guangdong Provincial Key Laboratory of Large Animal Models for Biomedicine & International Healthcare Innovation Institute (Jiangmen), Wuyi University, Jiangmen, 529020, China., Lang M; School of Pharmacy and Food Engineering & Guangdong Provincial Key Laboratory of Large Animal Models for Biomedicine & International Healthcare Innovation Institute (Jiangmen), Wuyi University, Jiangmen, 529020, China. langm2019@163.com., Yan JL; School of Pharmacy and Food Engineering & Guangdong Provincial Key Laboratory of Large Animal Models for Biomedicine & International Healthcare Innovation Institute (Jiangmen), Wuyi University, Jiangmen, 529020, China. yanjialei@wyu.edu.cn., Xu X; School of Pharmacy and Food Engineering & Guangdong Provincial Key Laboratory of Large Animal Models for Biomedicine & International Healthcare Innovation Institute (Jiangmen), Wuyi University, Jiangmen, 529020, China. wyuchemxxt@126.com.
Πηγή: Molecular diversity [Mol Divers] 2026 Oct; Vol. 30 (5), pp. 7235-7246. Date of Electronic Publication: 2026 Mar 01.
Τύπος έκδοσης: Journal Article
Γλώσσα: English
Στοιχεία περιοδικού: Publisher: ESCOM Science Publishers Country of Publication: Netherlands NLM ID: 9516534 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1573-501X (Electronic) Linking ISSN: 13811991 NLM ISO Abbreviation: Mol Divers Subsets: MEDLINE
Imprint Name(s): Original Publication: Leiden, The Netherlands : ESCOM Science Publishers, c1995-
Ιατρικοί όροι (MeSH): Pyrones*/chemistry , Pyrones*/pharmacology , Pyrones*/chemical synthesis , Monophenol Monooxygenase*/antagonists & inhibitors , Monophenol Monooxygenase*/chemistry , Monophenol Monooxygenase*/metabolism , Cinnamates*/chemistry , Cinnamates*/pharmacology , Cinnamates*/chemical synthesis , Enzyme Inhibitors*/pharmacology , Enzyme Inhibitors*/chemical synthesis , Enzyme Inhibitors*/chemistry, Melanins/biosynthesis ; Molecular Docking Simulation ; Animals ; Mice
Περίληψη: 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.
(© 2026. The Author(s), under exclusive licence to Springer Nature Switzerland AG.)
Competing Interests: Declarations. Conflict of interest: The authors declare no competing interests.
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Grant Information: 2021B1212040016 Science and Technology Planning Project of Guangdong Province
Contributed Indexing: Keywords: Cinnamic acid; Kojic acid; Tyrosinase inhibitors
Substance Nomenclature: 0 (Pyrones)
6K23F1TT52 (kojic acid)
EC 1.14.18.1 (Monophenol Monooxygenase)
0 (Cinnamates)
0 (Enzyme Inhibitors)
140-10-3 (cinnamic acid)
0 (Melanins)
Entry Date(s): Date Created: 20260301 Date Completed: 20261006 Latest Revision: 20261008
Update Code: 20261008
DOI: 10.1007/s11030-026-11487-5
PMID: 41764693
Βάση Δεδομένων: MEDLINE
Περιγραφή
ISSN:1573-501X
DOI:10.1007/s11030-026-11487-5