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Arbutin: mechanism of its depigmenting action in human melanocyte culture
Abstract
Arbutin, a naturally occurring beta-D-glucopyranoside of hydroquinone, is effective in the topical treatment of various cutaneous hyperpigmentations characterized by hyperactive melanocyte function. We examined the mechanism of its depigmenting action in human melanocyte cultures. Arbutin inhibited the tyrosinase activity of cultured human melanocytes at noncytotoxic concentrations. It did not affect the expression of tyrosinase mRNA. Melanin production was inhibited significantly by arbutin, as determined by measuring eumelanin radicals with an electron spin resonance spectrometer. The study of the kinetics and mechanism for inhibition of tyrosinase confirms the reversibility of arbutin as a competitive inhibitor of this enzyme. The utilization of L-tyrosine or L-dopa as the substrate suggests a mechanism involving competition with arbutin for the L-tyrosine binding site at the active site of tyrosinase. These results suggest that the depigmenting mechanism of arbutin in humans involves inhibition of melanosomal tyrosinase activity, rather than suppression of the expression and synthesis of tyrosinase.
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“and can reduce pigment darkening by inhibiting tyrosinase (122).”
From Photoprotection: a Review of the Current and Future Technologies (2010) · cites this paper as [122]
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Metadata
- Authors
- Maeda, K., & Fukuda, M.
- Affiliations
- Shiseido Group (Japan) (JP)
- ORCID
- Fukuda, M
- Venue
- The Journal of Pharmacology and Experimental Therapeutics
- Publisher
- Elsevier BV
- Published
- 1996-02
- Volume
- 276
- Issue
- 2
- Pages
- 765-769
- ISSN
- 0022-3565 (ISSN-L)
- OpenAlex
- W1905363600
- Cited by
- 533
- References
- 0
- Citations by year
- 2026: 12 · 2025: 13 · 2024: 14 · 2023: 14 · 2022: 16 · 2021: 24 · 2020: 24 · 2019: 24 · 2018: 22 · 2017: 28 · 2016: 23 · 2015: 22 · 2014: 24 · 2013: 21 · 2012: 30
- FWCI
- 1.31
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Journal of Pharmacology and Experimental Therapeutics (publishedVersion)
- PubMed (publishedVersion)
- PubMed
- Topics
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Cell Biology › melanin and skin pigmentation
- Health Sciences › Medicine › Dermatology › Dermatologic Treatments and Research
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Melanoma and MAPK Pathways
- Keywords
- arbutin, depigmenting agents, melanocytes, tyrosinase inhibition, melanogenesis, competitive inhibition, eumelanin, hyperpigmentation, tyrosine, L-DOPA, melanosomes
- MeSH terms
- Arbutin, Basidiomycota, Cell Survival, Cells, Cultured, Humans, Melanins, Melanocytes, Pigmentation, Monophenol Monooxygenase
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