Effects of hydroquinone and its glucoside derivatives on melanogenesis and antioxidation: Biosafety as skin whitening agents.
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.


METHODS
d-arb was synthesized in this study by removing all hydroxyl groups from the glucose side-chain of arbutin. Tyrosinase activity was measured by (14)C-tyrosine incorporation, the intracellular reactive oxygen species (ROS) level was monitored by H(2)DCFDA 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.


RESULTS
The cytotoxicity of hydroquinone and arbutin except for d-arb was increased while the cells exposed to a nontoxic dose (3J/cm(2)) 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.


CONCLUSIONS
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.
Hu
Zhi-Ming
ZM
Department of Dermatology, Renmin Hospital of Wuhan University, China.
Zhou
Qiong
Q
Lei
Tie-Chi
TC
Ding
Shen-Feng
SF
Xu
Shi-Zheng
SZ
D000818:Animals; D000975:Antioxidants / Q000494:pharmacology; D001104:Arbutin / Q000031:analogs & derivatives / Q000494:pharmacology; D002460:Cell Line; D006873:Hydroquinones / Q000494:pharmacology*; D008543:Melanins / Q000096:biosynthesis*; D008544:Melanocytes / Q000187:drug effects* / Q000378:metabolism / Q000528:radiation effects; D051379:Mice; D008810:Mice, Inbred C57BL; D014442:Monophenol Monooxygenase / Q000037:antagonists & inhibitors / Q000378:metabolism; D018384:Oxidative Stress / Q000187:drug effects* / Q000502:physiology; D017382:Reactive Oxygen Species / Q000037:antagonists & inhibitors / Q000378:metabolism*; D012880:Skin Pigmentation / Q000187:drug effects* / Q000502:physiology; D014466:Ultraviolet Rays / Q000009:adverse effects
D000975:Antioxidants; D006873:Hydroquinones; D008543:Melanins; D017382:Reactive Oxygen Species; D001104:Arbutin; D014442:Monophenol Monooxygenase; C504954:deoxyarbutin; C031927:hydroquinone