Background and objective
The biosafety of hydroquinone and its derivatives as skin whitening agent remains controversial. Here, we investigated the effects of hydroquinone, arbutin, and deoxyarbutin (d-arb) on melanogenesis and antioxidation using cultured melan-a melanocytes in the presence or absence of ultraviolet A (UVA)-induced oxidative stress and determined whether d-arb enables to be an alterative to hydroquinone and arbutin for skin whitening use.
d-arb was synthesized in this study by removing all hydroxyl groups from the glucose side-chain of arbutin. Tyrosinase activity was measured by 14C-tyrosine incorporation, the intracellular reactive oxygen species (ROS) level was monitored by H2DCFDA fluorescence labeling, and the cell viability was determined by MTT assay in murine melan-a melanocytes treated with hydroquinone, arbutin and deoxyarbutin in the presence or absence of UVA-induced oxidative stress.
The cytotoxicity of hydroquinone and arbutin except for d-arb was increased while the cells exposed to a nontoxic dose (3 J/cm2) of UVA irradiation. Suppressed ROS generation was noted by the treatment of d-arb to compare with arbutin and hydroquinone. All three compounds had a similar inhibition on tyrosinase activity in dose-dependent manners with two- to three-fold decreases over the untreated control. There was no change in expression of tyrosinase protein in cells treated with arbutin or hydroquinone, but a decreased protein expression of tyrosinase was seen in deoxyarbutin-treated cells.
Deoxyarbutin exerts potent tyrosinase inhibition, lessened cytotoxicity, and certain antioxidation potential, may serve as an effective and safe alternative to hydroquinone for use in skin whitening.
Abbreviations:d-Arb (deoxyarbutin), ROS (reactive oxygen species), 8mop (8-methoxypsoralen), MTT (methyl thiazole tetrazolium), H2DCFDA (2′,7′-dichlorodihydrofluorescein diacetate), PMA (phorbol 12-myristate 13-acetate), D-PBS (Dulbecco's phosphate buffered saline), UVA (ultraviolet A)
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Published online: July 12, 2010
Accepted: June 1, 2009
Received in revised form: May 12, 2009
Received: January 28, 2009
© 2009 Japanese Society for Investigative Dermatology. Published by Elsevier Inc. All rights reserved.