Cited by 544melanin and skin pigmentationDermatologic Treatments and ResearchMelanoma and MAPK Pathways

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Arbutin: mechanism of its depigmenting action in human melanocyte culture

Maeda, K, Fukuda, M·1996·The Journal of Pharmacology and Experimental Therapeutics

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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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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)
DOI: 10.1016/s0022-3565(25)12357-4
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
Licence: www.elsevier.com/tdm/userlicense/1.0/ (tdm)
www.elsevier.com/legal/tdmrep-license (tdm)
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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Arbutin: mechanism of its depigmenting action in human melanocyte culture

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